Derivatives amidocarbonyl acid, pharmaceutical composition and a method of reducing blood glucose

 

(57) Abstract:

The invention relates to new compounds of formula I, where R1- H, alkyl, aryl, R2- alkyl, R3- H, halogen, the nitro-group, R4- H, alkyl, Z is alkyl, W is alkyl, alkoxy, substituted aryl, substituted heteroaryl, where the heteroatoms may be O, N, S, and substituted amino group and substituted oxygraph, X - substituted aryl or substituted heteroaryl, where the heteroatoms may be O, N, S. the compounds of formula I possess hypoglycemic activity and therefore can be used as drugs intended to reduce the level of glucose in the blood. 3 C. and 35 C.p. f-crystals, 156 table.

The technical field

The invention relates to a derivative amidocarbonyl acid, or their pharmacologically acceptable salts, or their pharmacologically acceptable esters. These compounds have a remarkable effect on lowering blood glucose, lowering lipid, improve insulin resistance, reduce inflammatory diseases, immune regulation, inhibition aldoses reductase, inhibition of 5-lipoxygenase, suppression of lipid peroxidation, aktivirovannogo PPAR (advance is worn to the composition, containing the above derivative amidocarbonyl acid, their pharmacologically acceptable salts or their pharmaceutically acceptable esters as active ingredient used in the treatment or prevention of the following diseases. These diseases include diseases caused primarily by insulin resistance such as diabetes, hyperlipemia, obesity, weakened glucose tolerance (IGT), impaired glucose tolerance non-IGT (NGT), hypertension, fatty liver, diabetic complications (e.g. retinopathy, nephropathy, neurosis, cataracts, coronary disease, and the like), arteriosclerosis, diabetes gestational diabetes (GDM), polycystic ovary syndrome (PCOS) and cell damage caused by atherosclerosis (for example brain damage caused by apoplexy and the like); inflammatory disease type epiphyseal osteomyelitis, pain, pyrexia, rheumatoid arthritis, inflammatory enteritis, acne, sunburn, psoriasis, eczema, allergic diseases, asthma, gastrointestinal ulcers, cancer, cachexia, autoimmune diseases and pancreatitis; osteoporosis; cataract; and the like.

The present invention relates to the use of these soedineniya or prevention of these diseases by introducing a pharmacologically effective amount of such compounds warm-blooded animals.

Background of the invention

Although commonly used insulin and connections sulfonylureas, such as tolbutamide and glipizide, as therapeutic agents for diabetes mellitus and hyperglycemia, were recently presented carboxylic acid derivatives for use as therapeutic agents with insulin independent diabetes. These compounds are described, for example, in the following publications:

(1-1) the international patent publication WO 91/19702 (Japanese PCT application (Kokai) N. Hei 5-507920);

(1-2) international patent publication WO 94/29285;

(1-3) international patent publication WO 94/29302;

(1-4) the international patent publication WO 95/03288; and

(1-5) the international patent publication WO 96/04260.

However, the compounds described above are different from the compounds of the present invention, described below, so that the first connection does not have the structural characteristics of the compounds described herein which contain amide bond in the side chain carboxylic acid derivative.

Compounds having amide linkages in the side chains are described, for example, in the following publications:

(2-1) Japanese patent application (Kokai) N. Hei 6-172339;

(2-2) international patent publications which differ from the compounds according to this invention, described below, so that the first connection on the end of the molecules have thiazolidine and the like groups.

Although derivatives of carboxylic acids having amide bond in the side chain, as described, for example, in the following publications:

(3-1) Japanese patent application (Kokai) N. Hei 5-155828; and

(3-2) Japanese patent application (Kokai) N. Hei 5-279353,

the compound (3-1) and the compound (3-2) differ from the compounds according to the present invention, the pharmacological activity and chemical structure. The compound (3-1) has an effect on the inhibition of aggregation, and in the molecule of the compound (3-1) have amino or similar group in positions 2-5 carboxylic acids and heterocyclic group or the like at the end of the side chain. The compound (3-2) has inhibitory activity against damage to the ischemic tissue and is a derivative of acetic acid.

Description of the invention

The authors of the present invention conducted intensive research derived amidocarbonyl acids and their pharmaceutically acceptable salts and esters, which have a strong effect on lowering blood glucose, lowering lipid, improve insulin resistance, ass is Ximenez, suppression of lipid peroxidation, activation of PPAR (activating receptor peroxisomal proliferation) and weakening osteoporosis and established the present invention.

In more detail, the present invention relates to new derivatives amidocarbonyl acid, their pharmacologically acceptable salts and pharmaceutically acceptable esters, which can be used as therapeutic or prophylactic agents for diseases caused, mainly, insulin resistance, such as diabetes, hyperlipemia, obesity, weakened glucose tolerance (IGT), impaired glucose tolerance non-IGT (NGT), hypertension, fatty liver, diabetic complications (e.g. retinopathy, nephropathy, neurosis, cataracts, coronary artery disease, and the like), arteriosclerosis, diabetes gestational diabetes (GDM), polycystic ovary syndrome (PCOS) and cell damage caused by atherosclerosis (e.g., brain damage caused by apoplexy and the like); inflammatory diseases of type epiphyseal osteomyelitis, pain, pyrexia, rheumatoid arthritis, inflammatory enteritis, acne, sunburn, psoriasis, eczema, allergic zabolevaniya, juvenile rheumatoid arthritis, Sjogren syndrome, progressive systemic sclerosis, mixed connective tissue disease, dermatomyositis, Hashimoto's disease, primary myxoma, thyrotoxicosis, perniciosa anemia, ulcerative colitis, autoimmune atrophic gastritis, idiopathic Addison disease, male sterility syndrome?, acute progressive glomerulonephritis, myasthenia gravis, polymyositis, common bladderwort, gallbladder pemphigoid, sympathetic ophthalmia, multiple sclerosis, autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura, rheumatic fever, lupus hepatitis, primary biliary cirrhosis, a disease Baccheta, CREST syndrome, and the like), and pancreatitis; osteoporosis and cataracts.

Further, the invention relates to medicinal products containing as active component new derivatives amidocarbonyl acid, their pharmacologically acceptable salts or their pharmaceutically acceptable esters.

The invention relates to a derived amidocarbonyl acid of the formula (I):

< / BR>
its pharmacologically acceptable salts or its pharmaceutically acceptable ether.

In the formula

R1predki aracelio group, comprising from 7 to 12 carbon atoms;

R2is a straight or branched alkylenes group containing from 1 to 6 carbon atoms;

R3represents (i) hydrogen atom, (ii) straight or branched alkyl group comprising from 1 to 6 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (v) halogen atom, (vi) a nitro-group, (vii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (viii) aryl group containing from 6 to 10 carbon atoms which may have from 1 to 5 substituents described below, (ix) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (x) a hydroxyl group, or (xi) straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms;

R4represents a hydrogen atom or a straight or branched alkyl group comprising from 1 to 6 carbon atoms;

Z is a straight or once svetlanna alkyl group, comprising from 1 to 6 carbon atoms, (ii) hydroxyl group, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (v) aryl group containing from 6 to 10 carbon atoms which may have from 1 to 5 substituents described below, (vi) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described hereinafter, on the aryl group, (vii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (viii) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (x) arkitip, comprising from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (xi) aryloxyalkyl group, aryl group which contains 6 to 10 carbon atoms which may have from 1 to 5 substituents described hereinafter, and alkalines 5-10-membered heteroaryl group, containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xiii) mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xiv) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (XIV) mono - or decillions 5-10 membered saturated heterocyclic group, containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xvi) amino group, (xvii) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xviii) a straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xix) N-alkyl-N-killingray, including straight or branched alkyl group containing from 1 to 4 carbon atoms, and aryl group containing from 6 to 10 carbon atoms which may have from 1 to 5 substituents , (XX) killingray comprising from 6 to 10 carbon atoms, which may contain the in carbon which may contain from 1 to 5 substituents described later on the aryl group or (xxii) arachidonoylethanolamine, including aracelio group containing from 7 to 12 carbon atoms which may have from 1 to 5 substituents described later on the aryl group;

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described hereinafter, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described hereinafter, when W represents (1) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (2) hydroxyl group, (3) straight or branched CNS group containing from 1 to 4 carbon atoms, (4) a straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (5) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described below (6) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described below for aryl group is the R next on the aryl group, (8) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (9) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (10) arkitip comprising from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, (11) aryloxyalkyl group, in which the aryl group is an aryl group comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described below, and the alkyl group is straight or branched alkyl group comprising from 1 to 4 carbon atoms, (12) mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (13) a mono - or decillions 5-10-membered heteroepitaxial group containing from 1 to 4 heteroatoms, selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (14) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising uruppu, containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or

X represents an aryl group containing from 6 to 10 carbon atoms which may have from 1 to 3 substituents described hereinafter, when W represents (1) an amino group, (2) a straight or branched monoalkylamines, in which the alkyl group contains from 1 to 4 carbon atoms, (3) a straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (4) N-alkyl-N-killingray, includes straight or branched alkyl group containing from 1 to 4 carbon atoms, and aryl group containing from 6 to 10 carbon atoms which may have from 1 to 5 substituents, and (5) killingray comprising from 6 to 10 carbon atoms which may have from 1 to 5 substituents described later on the aryl group, (6) aralkylamines comprising from 7 to 12 carbon atoms which may have from 1 to 5 substituents described later on the aryl group or (7) arachidonoylethanolamine, including aracelio the group consisting of from 7 to 12 carbon atoms which may have from 1 to 5 slasticarnu from the group includes (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxylgroups, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 carbon atoms, (v) straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, (vi) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vii) a straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (viii) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described below, (x) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (xi) straight or branched alkylsulfonyl comprising from 1 to 4 carbon atoms, (xii) halogen atom, (xiii) nitro-group, (xiv) cyano, (xv) amino groups, (xvi) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xvii) straight or branched alkoxycarbonylmethyl, to the th group has from 7 to 12 carbon atoms, (xix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (xx) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group, (xxi) aryl group containing from 6 to 10 carbon atoms and which may contain from 1 to 3 substituents , which may be the same or different, described later, (xxii) alloctype, containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group, (xxiii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group, (xxiv) arylsulfonyl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group, (xxv) arylsulfonamides comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (xxvi) a mono - or dicyclo oxygen, the nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below, (xxvii) a mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below, (xxviii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below, (xxix) mono - or decillions 5-10-membered heteroarylboronic group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below (xxx) mono - or decillions 5-10-membered heteroatomcontaining containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents , described later, heteroaryl group (the nitrogen atom of the amino group may be substituted by straight or branched chain alkyl groups containing from 1 to 6 carbon atoms) and (xxxi) mono - or dizik the dust, including an oxygen atom, nitrogen atom and sulfur atom.

The above Deputy represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) a straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (viii) straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, (ix) halogen atom, (x) nitro-group, (xi) cyano, (xii) carboxyl group, (xiii) amino groups, (xiv) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xv) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xvi) straight or branched aminoalkyl group containing from 1 to Li branched alkyl group, comprising from 1 to 4 carbon atoms, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xviii) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl groups, which may be the same or different and each has from 1 to 4 carbon atoms, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xix) straight or branched alkoxycarbonylmethyl, in which the alkoxy group has from 1 to 4 carbon atoms or (xx) arachidonoylethanolamine in which kalkilya group has from 7 to 12 carbon atoms; and

Y represents a single bond, an oxygen atom, a sulfur atom or a group of the formula: >N-R5(where R5represents a hydrogen atom, a straight or branched alkyl group comprising from 1 to 6 carbon atoms, a straight or branched aliphatic acyl group containing from 1 to 8 carbon atoms or an aromatic acyl group containing from 7 to 11 carbon atoms).

In the case when R1, R3, R4, R5or W represent a straight or branched alkyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, penttila, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1 - methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1 - dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2 - dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl or 1,2,2-trimethylpropyl; preferably each R1, R3, R4and R5is a straight or branched alkyl group containing from 1 to 4 carbon atoms, and W is a straight or branched alkyl group comprising from 2 to 6 carbon atoms; more preferably, each R1, R3, R4and R5is a group of methyl, ethyl, propyl, isopropyl, butyl or isobutyl, and W represents a group of ethyl, propyl, isopropyl, butyl, isobutyl or pentile. Even more preferably, each R1and R5represents an alkyl group containing one or two carbon atom (particularly, a methyl group), R3represents a methyl group, ethyl or isopropyl (particularly, a methyl group or isopropyl)"), and W represents a group of propyl, butyl or pentile (in particular group, propyl or butyl).

In the case when R1represents aracelio group containing from 7 to 12 carbon atoms, kalkilya group is a group in which a straight or branched alkyl group comprising from 1 to 4 carbon atoms is substituted by an aryl group and includes, for example, a benzyl group, Venetia, 3-phenylpropyl, 4-phenylbutyl, 5-phenylpentane, 6-phenylhexane, 1-naphthylmethyl or 2-naphthylmethyl preferred group of benzyl, Venetia or 3-phenylpropyl, a more preferred group of 3-phenylpropyl.

In the case when R2or Z represents a straight or branched alkylenes group containing from 1 to 6 carbon atoms, Allenova group includes, for example, a group of methylene, ethylene, mutilation, ethylethylene, 1,1 - dimethylethylene, 1,2-dimethylethylene, trimethylene, 1 - methyltrienolone, 1-ethyltryptamine, 2-methyltryptamine, 1,1-dimethyltrimethylene, tetramethylene, pentamethylene or hexamethylene, preferred R2representing a straight or branched alkylenes group containing from 2 to 5 carbon atoms, more site the MOU carbon even more preferred R2representing a group of ethylene, trimethylene or mutilation, more preferred R2representing a group of ethylene. Preferably, Z is a straight or branched alkylenes group containing from 1 to 4 carbon atoms (for example, methylene, ethylene, mutilation, ethylethylene, trimethylene, 1 - methyltrienolone or 2-methyltryptamine), more preferred Allenova group having one or two carbon atoms, even more preferred group is methylene.

In the case when R3or W represents a straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, alkoxygroup includes, for example, a methoxy group, ethoxy, propoxy, isopropoxy, butoxy, sec-butoxy, tert-butoxy or isobutoxy; preferred R3representing alkoxygroup, including from 1 to 3 carbon atoms (in particular, methoxy group, ethoxy or isopropoxy); more preferred alkoxygroup, including one or two carbon atom (in particular, methoxy group). Preferably W is alkoxygroup, including from 1 to 3 carbon atoms, more preferred ethoxypropan.

In the case when R3represents a halogen atom, the halogen atom includes fluorine atom, chlorine atom, bromine atom or iodine atom; preferred fluorine atom, a chlorine atom or a bromine atom; more preferred fluorine atom or a chlorine atom.

In the case when R3or W represents a straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, dialkylamino includes, for example, a dimethylamino group, diethylamino, dipropylamino, diisopropylamino, dibutylamino, N-methyl-N-ethylamino or N-ethyl-N-isopropylamino; preferred group, dimethylamino or diethylamino; more preferred g is 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described below unsubstituted aryl group includes, for example, a phenyl group or naphthyl, preferably phenyl group. The substituted aryl group includes, for example, a group of methylphenyl, ethylphenyl, propylphenyl, isopropylphenyl, triptoreline, hydroxyphenyl, acetylphenyl, methoxyphenyl, methylendioxyphenyl, benzyloxyphenyl, methylthiophenyl, methansulfonate, ftoheia, dipthera, chlorphenyl, dichlorophenyl, nitrophenyl, (dimethylamino)phenyl, benzylphenol, biphenylyl, phenoxyphenyl, phenylthiophene, phenylsulfonyl (phenylcarbonylamino)phenyl, pyridylethenyl, pyridinemethanol, pyridylmethyl (pyridylsulfonyl)phenyl, matildaville, triternate, hydroxynaphthyl, methoxyethyl, ptomaphila, chloronaphthyl or pyridylmethyl; preferred aryl group, containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described below; a more preferred group of methylphenyl, ethylphenyl, isopropylphenyl, methoxyphenyl, methylthiophenyl or chlorphenyl.

In the case when R3or W represents aracelio group containing from 7 to 12 carbon atoms represent a group in which a straight or branched alkyl group comprising from 1 to 4 carbon atoms, substituted by the above aryl group and includes, for example, a benzyl group, Venetia, 3-phenylpropyl, 4-phenylbutyl, 5-phenylpentane, 6-phenylhexane, naphthylmethyl, methylbenzyl, cryptomelane, methoxybenzyl, methylenedioxybenzyl, methylthiomethyl, methysulfonylmethane, tormentil, Chlorobenzyl, 2-(were) ethyl, 2-(methoxyphenyl)ethyl, 3-were)propyl, 3-(methoxyphenyl)propyl, 4-(were)butyl or 4-(methoxyphenyl)butyl; a preferred R3that represents a benzyl group or Venetia; more preferred group is benzyl. Preferred W representing aracelio group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group; more preferred kalkilya group including from 7 to 10 carbon atoms (for example, benzyl group, Venetia, 3-phenylpropyl or 4-phenylbutyl); most preferred group of 3-phenylpropyl or 4-phenylbutyl (in particular, group 3-phenylpropyl).

In the case when R3is a straight or branched aliphatic acyl group include, propionyl, butyryl, isobutyryl, pentanoyl or pivaloyl, the preferred group is formyl, acetyl or pivaloyl; the most preferred group is formyl or acetyl.

In the case when W is alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, the unsubstituted alloctype includes, for example, a group of phenoxy or naphthyloxy; preferred fenoxaprop.

Substituted alloctype includes, for example, a group of methylphenoxy, ethylenoxy, propylenoxide, isopropylphenoxy, tert-butylphenoxy, triptoreline, methoxyphenoxy, ethoxyphenoxy, isopropoxyphenoxy, triftormetilfosfinov, methylthiophene, ethylthiophene, cyanogenetic, formylphenoxy, fervency, divergence, triterpenols, Pantothenate, chlorphenoxy, dichlorphenoxy, trichlorophenoxy, viridifrons, biphenyloxy, methysulfonylmethane, methylnaphthalene, ethylnaphthalene, papillations, isopropylnaphthalene, tert-butylnaphthalene, triftormetilfosfinov, methoxynaphthalene, ethoxynaphthalene, isopropoxyphenoxy, tripterocalyx, petitionplease, editionphilology, chloronaphthalene, dichloronaphthalene, trichlorophenoxy, pyridylmethylene, biphenyloxy or methysulfonylmethane; preferred alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group; more preferred fenoxaprop, which may contain from 1 to 3 substituents described later, on the phenyl group (in particular fenoxaprop, which may have one Deputy , described later, on the phenyl group); more preferred methylphenoxy, ethylenoxy, isopropylphenoxy, tert-butylphenoxy, triptoreline, methoxyphenoxy, ethoxyphenoxy, triftormetilfosfinov, cyanogenetic, formylphenoxy, fervency, divergence, triterpenols, Pantothenate, chlorphenoxy, dichlorphenoxy, trichlorophenoxy, pyridylamine or methansulfonate; even more preferred group of methylphenoxy, ethylenoxy, isopropylphenoxy, tert-butylphenoxy, triptoreline, methoxyphenoxy, ethoxyphenoxy, triftormetilfosfinov, cyanogenetic, formylphenoxy, fervency, divergence, triterpenols, Pantothenate, chlorphenoxy, dichlorphenoxy, trichlorophenoxy or methansulfonate; in particular, ormeloxifene, 3 fervency, 4-fervency or 4 chlorphenoxy.

In the case when W is killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, the unsubstituted aristocrata includes, for example, a group of phenylthio or naphthylthio; preferred phenylthiourea. Substituted aristocrata includes, for example, a group of methylphenylthio, atinfinity, propylphenyl, isopropylphenyl, methoxyphenyl, ethoxyphenyl, methylthiophenyl, ethylthiophene, biginelli, 4-methanesulfonamido, methylnaphthalene, eternality, populartity, isopropylnaphthalene, methoxynaphthalene, ethoxynaphthalene, petitionary, editionafter or 4 methanesulfonamido; preferred aristocrata comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described below; more preferred phenylthiourea, which may contain from 1 to 3 substituents described later, on the phenyl group; most preferred group methylphenylthio, isopropylphenyl or methoxybenzylthio.

In the case when W is aralkylated comprising from 7 to 12 atoms oscilloscope is a group, in which straight or branched alkyloxy comprising from 1 to 4 carbon atoms, substituted by the above aryl group and includes, for example, benzyloxy group, penetrate, 3 phenylpropoxy, 4-phenylbutyrate, 1 naphthalenyloxy or 2 - naphthalenyloxy; preferred arancelaria comprising from 7 to 10 carbon atoms; more preferred group is benzyloxy or penetrate (in particular, a benzyloxy group). Substituted arancelaria includes, for example, a group of methylbenzylamine, methoxybenzyloxy, 2-(were)ethoxy, 2- (methoxyphenyl)ethoxy, 3-(were)propoxy, 3- (methoxyphenyl)propoxy, 4-(were)butoxy or 4-(methoxyphenyl)butoxy; preferred arancelaria comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group; more preferred group of methylbenzylamine or 2-(were)ethoxy.

In the case when W is arkitip comprising from 7 to 12 carbon atoms in the aryl group, which may contain from 1 to 5 substituents described below, the unsubstituted kalkiliya is a group in which a straight or branched allylthiourea, VK is benzylthio, penetito, 3 phenylpropyl, 4-phenylbutyl, 1 naphthylmethyl or 2-naphthylmethyl; preferred group benzylthio or penetito; more preferred menzilcioglu. Substituted kalkiliya includes, for example, a group of metavarsity, methoxybenzylthio, 2-(were)ethylthio, 2-(methoxyphenyl)ethylthio, 3-(were)propylthio, 3-(methoxyphenyl)propylthio, 4-(were)butylthio or 4-(methoxyphenyl)butylthio; preferred kalkiliya comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group; more preferred group of methylbenzyl or 2-(were) ethylthio.

In the case when W is aryloxyalkyl the group in which the aryl group is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, aryloxyalkyl group includes, for example, a group of phenoxymethyl, 2-phenoxyethyl, 3-phenoxypropane, 4-phenoxybutyl, naphthylacetyl, 2-naphthylacetyl, 3-naphthylenediamine or 4-naphthyloxy, containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms; more preferred aryloxyalkyl group in which the aryl group has from 6 to 10 carbon atoms, and the alkyl group is straight or branched and has from 1 to 4 carbon atoms; even more preferred group of phenoxymethyl, 2-phenoxyethyl, 3-phenoxypropane or 4-phenoxybutyl; and the most preferred group 2-phenoxyethyl or 3-phenoxypropane (in particular, group 2 - phenoxyethyl).

In the case when W is a mono - or decillions 5-10-membered heteroaryl group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, the heteroaryl group includes, for example, a group of furil, teinila, pyrrolyl, azepine, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazole, 1,2,3-oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, chinoline or benzoxazolyl; preferred group pyrrolyl, imidazolyl, furyl which is a mono - or decillions 5-10-membered heteroepitaxy, containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, heteroanalogues includes, for example, a group of forelocks, titilate, pyrrolidone, azaindole, pyrazolinone, imidazolinone, oxazolidone, isoxazolidine, thiazolidine, isothiazolinone, 1,2,3-oxadiazolyl, triazolinone, tetrazolate, thiadiazolidine, pyranyloxy, pyridyloxy, pyridazinone, pyrimidinone, pyrazinone or benzoxazolinone; preferred group forelocks, titilate, pyrrolidone, imidazolidine, thiazolidine or pyridyloxy; more preferred pyridyloxy.

In the case when W is a mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, heteroanalogues includes, for example, a group of furylthio, tianity, Peralillo, againinto, personilty, imidazolidine, oxazolidine, isoxazolidine, thiazolino, isothiazoline, 1,2,3 - oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pirinelli, pyridylthio, Mirilashvili, pyrimidinyl, personalty or benzoxazolyl; predpochtitelnei preferred group benzoxazolyl.

In the case when W is a mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, a saturated heterocyclic group includes, for example, a group of morpholinyl, thiomorpholine, pyrrolidine, pyrroline, imidazolidine, imidazoline, pyrazolidine, pyrazoline, piperidine or piperazinil; preferred group of morpholinyl, thiomorpholine, pyrrolidine, imidazoline, piperidine or piperazinil.

In the case when W is a straight or branched monoalkylamines, in which the alkyl group contains from 1 to 4 carbon atoms, monoalkylamines includes, for example, the group methylamino, ethylamino, propylamino, isopropylamino, butylamino, sec-butylamino, tert-butylamino or isobutylamino; preferred straight or branched monoalkylamines, including from 1 to 3 carbon atoms; more preferred Propylamine.

In the case when W is an N-alkyl-N-killingray, including straight or branched alkyl group containing from 1 to 4 carbon atoms, and aryl gilna group unsubstituted N-alkyl-N-killingray includes, for example, the group of methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl or tert-butyl; a preferred group of methyl, ethyl, propyl, isopropyl, butyl or isobutyl; more preferred methyl group or ethyl. The aryl group includes, for example, a phenyl group or naphthyl; the preferred phenyl group. Specific examples of unsubstituted N-alkyl-N-killingray include, for example, the group of N-methyl-N-phenylamino, N-ethyl-N-phenylamino, N-propyl-N-phenylamino, N-isopropyl-N-phenylamino, N-butyl-N-phenylamino, N-isobutyl-N-phenylamino or N-methyl-N-naphthylamine; preferred group of N-methyl-N-phenylamino or N-ethyl-N-phenylamino; a more preferred group of N-ethyl-N-phenylamino. Substituted N-alkyl-N-killingray includes, for example, the group of N-methyl-N-(were)amino, N - ethyl-N-(were)amino, N-methyl-N-(methoxyphenyl)amino or N-ethyl-N-(methoxyphenyl)amino; preferred N-methyl-N-(were)amino group or N-ethyl-N-(were) amino group.

In the case when W is killingray comprising from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, the unsubstituted killingray includes, for example, a group FeNi the measures group (were)amino, (ethylphenyl)amino, (propylphenyl)amino, (isopropylphenyl)amino, (methoxyphenyl)amino, (ethoxyphenyl)amino, (methylthiophenyl)-amino, (ethylthiophene)amino, biphenylamine or (methanesulfonyl)amino; preferred (were)amino group, (isopropylphenyl)amino group or (methoxyphenyl)amino group.

In the case when W is aralkylamines comprising from 7 to 12 carbon atoms in aranceles group in which the aryl group may contain from 1 to 5 substituents described below, the unsubstituted aralkylamines is a group in which a straight or branched alkylamino comprising from 1 to 4 carbon atoms, substituted by the above aryl group and includes, for example, a group of benzylamine, phenethylamine, (3-phenylpropyl)amino, (4-phenylbutyl)amino, (1-naphthylmethyl)amino or (2-naphthylmethyl)amino; preferred benzylamino or phenethylamine; more preferred benzylaminopurine. Substituted aralkylamines includes, for example, a group (methylbenzyl)amino, (methoxybenzyl)amino, [2-(were)-ethyl] amino, [2- (methoxyphenyl)ethyl] amino, [3-(were)-propyl] amino, [3-(methoxyphenyl)propyl]amino, [4-(metalfan the Tyl] amino group.

In the case when W is arachidonoylethanolamine containing aracelio group containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents described later on the aryl group, the group includes, for example, benzyloxycarbonyloxy group.

In the case when W is an amino group, a straight or branched monoalkylamines, in which the alkyl group contains from 1 to 4 carbon atoms, straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, N-alkyl-N-killingray containing a straight or branched alkyl group containing from 1 to 4 carbon atoms and aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents described hereinafter, killingray, containing from 6 to 10 carbon atoms in the aryl group, which may contain from 1 to 5 substituents described hereinafter, or aralkylamines comprising from 7 to 12 carbon atoms in aranceles group in which the aryl group may contain from 1 to 5 substituents described hereinafter, preferably W represents: aminogroup is; the nternet or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms; N-alkyl-N-killingray containing a straight or branched alkyl group containing from 1 to 4 carbon atoms, and aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents ; or killingray comprising from 6 to 10 carbon atoms in the aryl group, which may contain from 1 to 5 substituents described below.

In the case when R5is a straight or branched aliphatic acyl group containing from 1 to 8 carbon atoms, or an aromatic acyl group containing from 7 to 11 carbon atoms, acyl group includes, for example, a group of formyl, acetyl, propionyl, butyryl, pentanoyl, hexanoyl, heptanoate, benzoyl or p-toluoyl; preferred straight or branched aliphatic acyl group comprising from 1 to 8 carbon atoms; more preferred straight or branched aliphatic acyl group containing from 2 to 5 carbon atoms; the preferred acetyl group.

In the case when X made the th , described below unsubstituted aryl group includes, for example, a phenyl group or naphthyl, preferably phenyl group.

When X represents an aryl group which is substituted by from 1 to 3 substituents described hereinafter, the preferred number of substituents is one or two, more preferred one.

When X represents a mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below, unsubstituted heteroaryl group includes a monocyclic system or decillions system. If dziklicska system at least one ring represents a heterocyclic group. If dziklicska system two rings are condensed, when the one ring is a heterocycle, and the other is carbocycle, or both rings are heterocycles. The heterocycle is a 5 - or 6 - membered ring and contains from 1 to 4 heteroatoms selected from the group comprising a nitrogen atom, an oxygen atom and a sulfur atom. Carbocycle is Soi heteroaryl group, and disilicate system is called a condensed heteroaryl group. When the ring contains four heteroatoms, all four heteroatoms are preferably nitrogen atoms and the number of heteroatoms selected from the group comprising an oxygen atom and a sulfur atom, is equal to zero. When the ring contains three heteroatoms, preferably three, two or one heteroatom is nitrogen atoms, and one or two heteroatoms selected from the group comprising an oxygen atom and a sulfur atom. When the ring contains two heteroatoms, preferably one to two, one or zero was heteroatoms nitrogen atoms and zero, one or two heteroatoms, such as selected from the group comprising an oxygen atom and a sulfur atom. In the case when X is a heteroaryl group, a substituted from 1 to 3 substituents described hereinafter, the number of substituents is preferably one or two, more preferably one.

Unsubstituted monocyclic heteroaryl group includes, for example, a group pyrrolyl, such as group 2-pyrrolyl or 3-pyrrolyl; a group of furil, such as group 2-furil or 3-furil; group tanila, such as group 2-tanila or 3-tanila; group pyridyl, so Azolla; group pyrazolyl, such as group 3-pyrazolyl or 4-pyrazolyl; group oxazolyl, such as group 2-oxazolyl, 4-oxazolyl or 5-oxazolyl; group isoxazolyl, such as group 3-isoxazolyl, 4-isoxazolyl or 5-isoxazolyl; group thiazolyl, such as group 2-thiazolyl, 4-thiazolyl or 5-thiazolyl; group isothiazoline, such as group 3-isothiazole, 4-isothiazole or 5-isothiazole; group triazolyl, such as group 1,2,3-triazole-4-yl or 1,2,4-triazole-3-yl; a group thiadiazolyl, such as a group of 1,3,4-thiadiazole-2-yl; a group oxadiazolyl, such as group 1,3,4 - oxadiazol-2-yl; a group tetrazolyl, such as group 5-tetrazolyl; group pyridazinyl, such as group 3-pyridazinyl or 4-pyridazinyl; group pyrimidinyl, such as group 2-pyrimidinyl, 4-pyrimidinyl or 5-pyrimidinyl; group pyrazinyl; group oxazinyl, such as the group of 1,4-oxazin-2-yl or 1,4-oxazin-3-yl; and group teinila, such as the group of 1,4-thiazin-2-yl or 1,4-thiazin-3-yl; unsubstituted condensed heteroaryl group includes, for example, indolenine group, such as group indol-2-yl, indol-3-yl, indol-4-yl, indol-5-yl, indol-6-yl or indol-7-yl; indazolinone group, such as group indazol - 2-yl, and benzofuran-2-yl, benzofuran-3-yl, benzofuran-4-yl, benzofuran-5-yl, benzofuran-6-yl or benzofuran-7-yl; a group of benzothiophene, such as group benzothiophen-2-yl, benzothiophen-3-yl, benzothiophen-4-yl, benzothiophen-5-yl, benzothiophen-6-yl or benzothiophen-7-yl; a group benzimidazolyl, such as the group of benzimidazole-2-yl, benzimidazole-4-yl, benzimidazole-5-yl, the benzimidazole-6-yl or benzimidazole-7-yl; a group benzoxazolyl, such as group benzoxazol-2-yl, benzoxazol-4-yl, benzoxazol-5-yl, benzoxazol-6-yl or benzoxazol-7-yl; a group benzothiazolyl, such as a group, benzothiazol-2-yl, benzothiazol-4-yl, benzothiazol-5-yl, benzothiazol-6-yl or benzothiazol-7-yl; a group chinoline, such as group 2-chinoline, 3-chinoline, 4-chinoline, 5-chinoline, 6-chinoline, 7-ginalisa or 8-ginalisa; group izochinolina, such as group 1-izochinolina, 3-izochinolina, 4-izochinolina or 8-izochinolina; group benzoxazine, such as the group of 1,4-benzoxazin-2-yl or 1,4-benzoxazin-3-yl; a group of benzothiazine, such as the group of 1,4-benzothiazin-2-yl or 1,4-benzothiazin-3-yl; a group pyrrolo[2,3-b] pyridyl, such as group pyrrolo[2,3-b]pyrid-2-yl or pyrrolo[2,3-b]pyrid-3-yl; a group furo[2,3-b] pyridyl, such as group furo[2,3-b]pyrid-2-yl or furo[2,3-b]pyrid-is inila, such as a group of 1,8-naphthylidine-2-yl, 1,8-naphthylidine-3-yl, 1,5-naphthylidine-2-yl and 1.5-naphthylidine-3-yl; a group of imidazopyridine, such as band imidazo[4,5-b]pyrid-2-yl or imidazo[4,5-b]pyrid-5-yl; a group of oxazolopyridine, such as group oxazolo[4,5-b]pyrid-2-yl or oxazolo[5,4-b]pyrid-2-yl; and a group of triazolopyridine, such as group thiazolo[4,5-b]pyrid-2-yl or thiazolo [4,5-c]pyrid-2-yl.

Monocyclic heteroaryl group is preferably a 5 - or 6-membered ring group containing 1 to 3 heteroatoms selected from the group comprising a nitrogen atom, an oxygen atom and a sulfur atom, and includes the above as an example, the group pyrrolyl, a group of furil, group teenie, group pyridyl, a group of imidazolyl, group pyrazolyl, group oxazolyl, group isoxazolyl, group thiazolyl, group triazolyl, group thiadiazolyl, group oxadiazolyl, group pyridazinyl, group pyrimidinyl or group of pyrazinyl. Kondensirovannie heteroaryl group is preferably a condensed ring group of the benzene ring with a 5 - or 6-membered monocyclic heteroaryl group containing 1 to 3 heteroatoms, selected from the group vkluchila, group benzofuranyl, group benzothiophene, group benzimidazolyl, group benzoxazolyl, group benzothiazolyl, group chinoline or group izochinolina; more preferably a group of imidazolyl, group oxazolyl, group pyridyl, a group of indolyl, group chinoline or group izochinolina; even more preferably a group of pyridyl, a group of indolyl, group chinoline or group izochinolina; and most preferably a group of pyridyl, group chinoline or group izochinolina; in particular, the most preferred group of pyridyl.

When the above group, X represents an aryl group containing from 6 to 10 carbon atoms, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, aryl group and heteroaryl group can contain from 1 to 3 substituents as described above.

When the Deputy is a straight or branched alkyl group comprising from 1 to 6 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, straight or branched allylthiourea comprising from 1 to 4, the group may be the same or different and each has from 1 to 4 carbon atoms, these groups may include groups such as described above in the definition of R3. However, when the Deputy is a straight or branched alkyl group comprising from 1 to 6 carbon atoms, the alkyl group preferably includes a group of methyl, ethyl, propyl, isopropyl, butyl or tert - butyl, more preferred methyl group, isopropyl or tert-butyl.

When the Deputy is arachidonoylethanolamine in which kalkilya group has from 7 to 12 carbon atoms, the group includes, for example, benzyloxycarbonylamino.

When the Deputy is a straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, halogenated alkyl group includes, for example, a group of chlormethyl, methyl bromide, formatie, yodmetilat, diformate, trifloromethyl, pentaborate, 2,2,2-triptoreline, 2,2,2-trichloroethyl or trichloromethyl; preferred group of formatie, including from 1 to 3 fluorine atoms; more preferred group of trifloromethyl.

When the Deputy is a straight or branched, Alifu formyloxy, acetoxy, propionyloxy, butyryloxy, graylox, methacrylate or crotonville; preferred group alkanoyloxy comprising from 1 to 4 carbon atoms; more preferred group of alkanoyloxy, including one or two carbon atoms, the most preferred acetoxygroup.

When the Deputy is a straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, a halogenated alkoxygroup includes, for example, chloromethoxy, bromoethoxy, formatosi, admetox, deformedarse, triptoreline, pentaborate, 2,2,2-triptoreline, 2,2,2-trichloroethane, trichloromethane or 2,2,3,3-tetrafluoropropoxy; preferred straight or branched halogenated alkoxygroup, including from 1 to 3 carbon atoms; more preferred methoxy group, comprising from 1 to 3 fluorine atom or 2,2,3,3 - tetrafluoropropoxy; most preferred group triptoreline or 2,2,3,3-tetrafluoropropoxy (in particular, 2,2, 3,3-tetrafluoropropoxy).

When the Deputy is a straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, acyl group includes SEB is as straight or branched aliphatic acyl group, comprising 2 or 3 carbon atoms; more preferred acetyl group.

When the Deputy is a straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, alkylenedioxy includes, for example, a group of methylendioxy, Ethylenedioxy, trimethylenediamine, tetramethoxy or Propylenediamine; preferred group methylendioxy or Ethylenedioxy; more preferred methylendioxy.

When the Deputy is aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described hereinafter, arancelaria includes, for example, benzyloxy group, penetrate, 3 phenylpropoxy, 4-phenylbutane, 1 aftermatket or 2-aftermatket; preferred unsubstituted group aralkylated comprising from 7 to 12 carbon atoms (for example, benzyloxy group, 2-penetrate, 1 aftermatket or 2-aftermatket); more preferred benzyloxy.

When the Deputy is a straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, alkylsulfonyl group includes, for example, gr who were radioactive, second-butanesulfonyl or tert-butanesulfonyl preferred group methanesulfonyl, acanalonia or isopropanolamine; particularly preferred alkylsulfonyl group comprising one or two carbon atom (in particular methanesulfonyl group).

When the Deputy is a straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, monoalkylamines includes, for example, the group methylamino, ethylamino, propylamino, isopropylamino, butylamino, isobutylamino, sec-butylamino or tert-butylamino; preferred group methylamino, ethylamino, isopropylamino or tert-butylamino; more preferred methylaminopropyl.

When the Deputy is a straight or branched alkoxycarbonyl in which alkoxygroup has from 1 to 4 carbon atoms, alkoxycarbonylmethyl includes, for example, a group of methoxycarbonylamino, ethoxycarbonyl or tertbutoxycarbonyl; preferred tertbutoxycarbonyl.

When the Deputy is aracelio group containing from 7 to 12 atoms pleae in itself, for example, a benzyl group, Venetia, 3-phenylpropyl, 4 - phenylbutyl, 5-phenylpentane, 6-phenylhexane, 1 aftermatket or 2-aftermatket; preferred benzyl group, which may contain from 1 to 3 substituents described later, on the phenyl group; more preferred group is benzyl.

When the Deputy is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents , which may be the same or different, as described hereinafter, the aryl group includes, for example, the group of phenyl, naphthyl, methylphenyl, (trifluoromethyl) phenyl, hydroxyphenyl, methoxyphenyl, ethoxyphenyl (triptoreline) phenyl, methylenedioxyphenyl, (hydroxymethyl) phenyl, ftoheia, chlorphenyl, bromanil, nitrophenyl, formylphenyl, cyanophenyl, carboxyphenyl, AMINOPHENYL, (dimethylamino) phenyl, (aminomethyl) phenyl, (2-amino-ethyl)phenyl, [(N, N - dimethylamino)methyl]phenyl, (tert-butoxycarbonylamino) phenyl, (benzyloxycarbonylamino) phenyl or 4-hydroxy-3,5-dimetilfenil; preferred phenyl group, which may contain from 1 to 3 substituents described below (in particular, the group of phenyl, methylphenyl, (trifluoromethyl)phenyl, hydroxy who Anila, nitrophenyl, formylphenyl, cyanophenyl, carboxyphenyl, dimethylaminophenyl, aminomethylphenol, (N, N-dimethylaminomethyl) phenyl or 4-hydroxy-3,5-dimetilfenil); more preferred group of phenyl, methylphenyl, (trifluoromethyl)phenyl, hydroxyphenyl, methoxyphenyl (triptoreline) phenyl, methylenedioxyphenyl, (hydroxymethyl)phenyl, ftoheia, chlorphenyl, nitrophenyl, formylphenyl, cyanophenyl, carboxyphenyl, (dimethylamino)phenyl, (aminomethyl)phenyl, (N,N-dimethylaminomethyl)phenyl or 4-hydroxy-3,5-acid; the most preferred group of phenyl, (trifluoromethyl)phenyl, methoxyphenyl, (hydroxymethyl)phenyl, (triptoreline)phenyl, ftoheia, chlorphenyl, nitrophenyl, formylphenyl, carboxyphenyl, dimethylaminophenyl, (N,N - dimethylaminomethyl)phenyl or 4-hydroxy-3,5-dimetilfenil; in particular, the most preferred group of phenyl, (triptoreline)phenyl, methoxyphenyl, ftoheia, chlorphenyl, formylphenyl, carboxyphenyl or (dimethylamino)phenyl.

When the Deputy is alloctype comprising from 6 to 10 carbon atoms in the aryl group, which may contain from 1 to 3 substituents described hereinafter, alloctype includes, for example, g is Hinoki, bromophenoxy or methylenedioxyphenoxy; preferred fenoxaprop, which may contain from 1 to 3 substituents described below (in particular fenoxaprop).

When the Deputy is killigrew comprising from 6 to 10 carbon atoms in the aryl group, which may contain from 1 to 3 substituents described hereinafter, aristocrata includes, for example, a group of phenylthio, methylphenylthio, (trifluoromethyl)phenylthio, methoxybenzylthio, ethoxyphenyl, chlorophenylthio, pampanito, methylenedioxyphenyl or naphthylthio; preferred phenylthiourea, which may contain from 1 to 3 substituents described below (in particular phenylthiourea).

When the Deputy is arylsulfonyl group containing from 6 to 10 carbon atoms in the aryl group, which may contain from 1 to 3 substituents described hereinafter, arylsulfonyl group includes, for example, a group phenylsulfonyl, methylphenylsulfonyl, (trifluoromethyl) phenylsulfonyl, methoxy - phenylsulfonyl, ethoxybenzonitrile, chlorophenylsulfonyl, brompheniramine, methylenedioxyphenylacetone or naphthylmethyl; preferred phenylsulfonyl is arylsulfonamides, containing from 6 to 10 carbon atoms in the aryl group, which may contain from 1 to 3 substituents described below (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), an alkyl group substituent on the nitrogen atom has several meanings defined above. Arylsulfonamides includes, for example, (phenylsulfonyl) amino group, (methylphenylsulfonyl)amino group, (triftormetilfullerenov) amino group, (methoxybenzenesulfonyl) amino group, (ethoxyphenylacetic) -amino group, chlorophenylsulfonyl, Bromphenol-sulfonylamino, methylenedioxyphenethylamine, N-methyl - phenylcarbonylamino, (naphthylmethyl) -amino or N - methyl-naphtylcontaining; preferred (phenylsulfonyl) amino group which may contain from 1 to 3 substituents described hereinafter, phenyl group, or N-methyl-phenylcarbonylamino (in particular, phenylcarbonylamino or N-methyl-phenylcarbonylamino).

When the Deputy is a mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the data next unsubstituted heteroaryl group includes, for example, a group of furil, teinila, oxazolyl, isoxazolyl, thiazolyl, imidazolyl, chinoline, izochinolina, indolyl or pyridyl; preferred group of imidazolyl, chinoline or pyridyl; particularly preferred group of pyridyl. Group containing a Deputy, includes a group of methylpyridyl, (trifluoromethyl)pyridyl, hydroxypyridine, methoxypyridine, ethoxypyridine (triptoreline)pyridyl, (hydroxymethyl)pyridyl, perperidis, chloropyridine, bromperidol, nitropyridine, formylpyridine, cyanopyridyl, carboxypropyl, aminopyridine, (dimethylamino)pyridyl, (aminomethyl)pyridyl, (2-amino-ethyl)pyridyl, (N,N-dimethylaminomethyl)pyridyl, (tert-butoxycarbonylamino)pyridyl or (benzyloxycarbonylamino)pyridyl; preferred group of pyridyl, which may contain from 1 to 3 substituents , described below (for example, a group of methylpyridyl, (trifluoromethyl)pyridyl, hydroxypyridine, methoxypyridine (triptoreline)pyridyl, perperidis, chloropyridine, nitropyridine, formylpyridine, cyanopyridyl, carboxypropyl, aminopyridine, dimethylaminopyridine or (N, N-dimethylaminomethyl)pyridyl) or imidazolidine group (Tau is erode, in particular the group of N-methylimidazole); more preferred group (trifluoromethyl)pyridyl, methoxypyridine, perperidis, chloropyridine, nitropyridine, cyanopyridyl, aminopyridine or dimethylaminopyridine.

When the Deputy is a mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described hereinafter, heteroanalogues includes, for example, a group of forelocks, titilate, oxazolidone, isoxazolidine, thiazolidine, imidazolidine, hinomisaki, athinaiki, intolerance or pyridyloxy; preferred pyridyloxy, which can contain up to 3 substituents described below; in particular preferred pyridyloxy.

When the Deputy is a mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituent described later, heteroanalogues includes, for example, a group of furylthio, titillatio; preferred pyridylthio, which may contain from 1 to 3 substituents described below; in particular preferred pyridylthio.

When the Deputy is a mono - or decillions 5-10-membered heteroarylboronic group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituent described later, heteroarylboronic group includes, for example, a group fenilalanina, thienylmethyl, oxazolidinone, isoxazolidinone, triazolylmethyl, imidazolylalkyl, chinaillon, ethynodiolthinyl, indolylmethane or pyridylsulfonyl; preferred group pyridylsulfonyl, which may contain from 1 to 3 substituents described hereinafter; in particular preferred group pyridylsulfonyl.

When the Deputy is a mono - or decillions 5-10-membered, heteroarylboronic-group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below, heteroaryl groups (and the s carbon), heteroatomcontaining includes, for example, a group of fenilalanina, teilzunehmen, oxytrichloride, isoxazolecarboxylic, thiazolecarboxamide, imidazolidinylideneamino, N-methyl-imidazolidinylideneamino, chinaincorporated, ethynodiolthinyl, indolealkylamine, pyridinesulfonamide or N - methylenebismethacrylamide; preferred pyridinesulfonamide, which may contain from 1 to 3 substituents described hereinafter, peredelnoj group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms); particularly preferred group of pyridinesulfonamide or N - methyl-pyridinesulfonamide.

When the Deputy is a mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, a saturated heterocyclic group includes, for example, a group of morpholinyl, thiomorpholine, pyrrolidine, pyrroline, imidazolidine, imidazoline, pyrazolidine, pyrazoline, piperidine or piperazinil; PR is the group of piperidine).

When the Deputy is a straight or branched alkyl group comprising from 1 to 6 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, halogen atom, or a straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, these groups may include the same groups as those described above in the definition of R3.

When the Deputy is a straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, a straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, a straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, straight or branched monoalkylamines, in which the alkyl group contains from 1 to 4 carbon atoms, straight or branched alkoxycarbonyl in which alkoxygroup contains from 1 to 4 carbon atoms, or arachidonoylethanolamine in which kalkilya the group has from the case, when the Deputy is a straight or branched chain hydroxyalkyl groups containing from 1 to 4 carbon atoms, hydroxyalkyl group includes, for example, a group of hydroxymethyl, 2-hydroxyethyl, 3-hydroxypropyl or 4-hydroxybutyl preferred hydroxymethylene group.

When the Deputy is a straight or branched aminoalkyl group containing from 1 to 4 carbon atoms, aminoalkyl group includes, for example, a group of aminomethyl, 2-aminoethyl, 3-aminopropyl or 4-aminobutyl; preferred group aminomethyl or aminoethyl; more preferred aminomethyl group.

When the Deputy is monoalkylammonium group, in which monoalkylamines has one straight or branched alkyl group containing from 1 to 4 carbon atoms, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, monoalkylammonium group includes, for example, the group of N-methylaminomethyl, N-ethylaminomethyl, N - methylaminomethyl, N-ethylaminomethyl, N-methylaminopropyl or N-methylaminomethyl; preferred dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, dialkylaminoalkyl group includes, for example, the group of N,N-dimethylaminomethyl, N,N-diethylaminomethyl, N,N-dimethylaminoethyl, N,N-diethylaminoethyl, N, N-dimethylaminopropyl or N-dimethylaminomethyl; preferred group of N, N-dimethylaminoethyl or N,N-dimethylaminoethyl; more preferred group of N,N-dimethylaminomethyl.

Therefore, in the case when X is a substituted or unsubstituted aryl group containing from 6 to 10 carbon atoms, or saturated or unsaturated mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, and specific examples of these groups preferably include phenyl group, 1-naphthyl, 2-naphthyl, m-tolila, p-tolila, 3-ethylphenyl, 4-ethylphenyl, 3-isopropylphenyl, 4-isopropylphenyl, 3-tert-butylphenyl, 4-tert-butylphenyl, 4-chloromethylene, 4-brometea the 4-trichlorodiphenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-acetoxyphenyl, 4-acetoxyphenyl, 5-acetoxy-2-hydroxy-3,4,6-trimetilfenil, 3-methoxyphenyl, 4-methoxyphenyl, 3-ethoxyphenyl, 4-ethoxyphenyl, 3-isopropoxyphenyl, 4-isopropoxyphenyl, 3,4-methylenedioxyphenyl, benzyloxyphenyl, penetrometer, 1-naphthylmethyl, 3-methylthiophenyl, 4-methylthiophenyl, 3-ethylthiophene, 4-ethylthiophene, 3-isopropylphenyl, 4-isopropylphenyl, 3-methanesulfonyl, 4-methanesulfonyl-phenyl, 3-ethanolgasoline, 4-ethanolgasoline, 3-isopropylphenyl, 4-isopropylphenyl, 3-ftoheia, 4-ftoheia, 3-chlorphenyl, 4-chlorphenyl, 3-bromophenyl, 4-bromophenyl, 4-nitrophenyl, 4-AMINOPHENYL, 3-methylaminophenol, 4-ethylaminoethanol, 3-propylaniline, 4-butylaminoethyl, 3-dimethylaminophenyl, 4-diethylaminophenyl, 3-dipropylamine, 4-dibutylaminoethanol, 3-benzoylphenyl, 4-benzoylphenyl, 3-fenetylline, 4-(1-naphthylmethyl)phenyl, 3-biphenylyl, 4-biphenylyl, 3-(4-were)phenyl, 4-(4-were)phenyl, 3-(4-ethylphenyl)phenyl, 3-(4-triptoreline)phenyl, 4-(4-triptoreline)phenyl, 4-(2-hydroxyphenyl)phenyl, 4-(3-hydroxyphenyl)phenyl, 4-(4-hydroxyphenyl)phenyl, 4-(4-hydroxy-3, 5dimethylphenyl)phenyl, 3-(4-methoxyphenyl)phenyl, 4-(2-methoxyphenyl, 3-(2,5-acid)phenyl, 4-(2, 5-acid)phenyl, 4-(3-hydroxymethylene)phenyl, 4-(4-hydroxymethylene)phenyl, 4-(3-forfinal)phenyl, 4 -(4-forfinal)phenyl, 4-(3-chlorophenyl)phenyl, 4-(4-chlorophenyl)phenyl, 4-(3-bromophenyl)phenyl, 4-(4-bromophenyl)phenyl, 3-(3, 4-methylenedioxyphenyl)phenyl, 4-(3, 4-methylenedioxyphenyl)phenyl, 4-(2-formylphenyl)phenyl, 4-(3-formylphenyl)phenyl, 4-(4-formylphenyl)phenyl, 4-(3-carboxyphenyl) phenyl, 4-(4-carboxyphenyl)phenyl, 4-(3-N, N-dimethylaminomethylphenol)phenyl, 4-(4-N, N-dimethylaminomethylphenol) phenyl, 3-benzoylphenyl, 4-benzoylphenyl, 3-phenoxyphenyl, 4-phenoxyphenyl, 3-phenylthiophene, 4-phenylthiophene, 3-phenylsulfanyl, 4-phenylsulfonyl, 3-(phenylcarbonylamino)phenyl, 4-(phenylcarbonylamino)phenyl, 3-(N-methylphenylsulfonyl)-phenyl, 4-(N-methylphenylsulfonyl)phenyl, 3-(imidazol-1-yl)phenyl, 4-(imidazol-1-yl)phenyl, 3-(1-Mei-4-yl)phenyl, 4-(1-Mei-4-yl)phenyl, 3-(2-furyl)phenyl, 4-(2-furyl)phenyl, 3-(2-thienyl)phenyl, 4-(2-thienyl)phenyl, 3-(3 - thienyl)phenyl, 4-(3-thienyl)phenyl, 3-(2-pyridyl)phenyl, 4-(2-pyridyl)phenyl, 4-(2-triptorelin-5-yl)phenyl, 4-(2 - methoxypyridine-5-yl)phenyl, 4-(2-nitropyridine-5-yl)phenyl, 4-(2-N, N-dimethylaminopyridine-5-yl)phenyl, 3-(3-pyridyl)-phenyl, 4-(3-pyridyl)phenyl, 3-(4-perio)phenyl, 4-(4-pyridylthio)phenyl, 3-(2-pyridylsulfonyl)phenyl, 4-(2-pyridylsulfonyl)phenyl, 3-(3-pyridylsulfonyl)phenyl, 4-(3-pyridylsulfonyl)phenyl, 3-(2-pyridylsulfonyl)phenyl, 3-(N-methyl-2-pyridylsulfonyl)phenyl, 4-(2-pyridylsulfonyl)phenyl, 4-(M-methyl-2-pyridinesulfonamide)-phenyl, 3-(3-pyridylsulfonyl)phenyl, 3-(N-methyl-3-pyridylsulfonyl)phenyl, 4-(3-pyridylsulfonyl)-phenyl, 4-(N-methyl-3-pyridylsulfonyl)phenyl, 3-(oxazol-2-yl) phenyl, 4- (oxazol-2-yl) phenyl, 3-(oxazol-4-yl)phenyl, 4-(oxazol-4-yl)phenyl, 3-(oxazol-5-yl) phenyl, 4-(oxazol-5-yl)phenyl, 3-(thiazol-2-yl)phenyl, 4-(thiazol-2-yl)phenyl, 3-(thiazol-4-yl)phenyl, 4-(thiazol-4-yl)phenyl, 3-(thiazol-5-yl)phenyl, 4-(thiazol-5-yl)phenyl, 4-(piperidine-1-yl)phenyl, 1-methyl-2-pyrrolyl, 1-phenyl-2-pyrrolyl, 1-benzyl-2-pyrrolyl, 5-methyl-2-furil, 5-phenyl-2-furil, 5-methyl-2-tanila, 5-phenyl-2-tanila, 5-methyl-3-tanila, 5-phenyl-3-tanila, 1-methyl-3-pyrazolyl, 1-phenyl-3-pyrazolyl, 3-imidazolyl, 1-methyl-2-imidazolyl, 1-phenyl-2-imidazolyl, 1-methyl-4-imidazolyl, 1-phenyl-4-imidazolyl, 1-methyl-2-phenyl-4-imidazolyl, 1,5-dimethyl-2-phenyl-4-imidazolyl, 1,4-dimethyl-2-phenyl-5-imidazolyl, 4-oxazolyl, 5-oxazolyl, 2-methyl-4-oxazolyl, 2 - phenyl-4-oxazolyl, 2-methyl-5-oxazolyl, 2-phenyl-5-oxazole-thiazolyl, 2-methyl-5-thiazolyl, 2-phenyl-5-thiazolyl, 4-methyl-2-phenyl-5-thiazolyl, 5-methyl-2-phenyl-4-thiazolyl, 1-methyl-3-pyrazolyl, 1-phenyl-3-pyrazolyl, 3-methyl-5-isoxazolyl, 3-phenyl-5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 3-methyl-5-pyridyl, 3-ethyl-5-pyridyl, 3-phenyl-5-pyridyl, 2-methyl-5-pyridyl, 2-ethyl-5-pyridyl, 2-phenyl-5-pyridyl, 2-(4-methoxyphenyl)-5-pyridyl, 2-(4-forfinal)-5-pyridyl, 2-hydroxy-5-pyridyl, 2-methoxy-5-pyridyl, 2-ethoxy-5-pyridyl, 2 - isopropoxy-5-pyridyl, 2-(2,2,3,3-tetrafluoropropoxy)-5-pyridyl, 2-benzyloxy-5-pyridyl, 2-methylthio-5-pyridyl, 2-ethylthio-5-pyridyl, 2-isopropylthio-5-pyridyl, 2-methanesulfonyl-5-pyridyl, 2-econsultancy-5-pyridyl, 2-isopropylphenyl-5-pyridyl, 2-benzyl-5-pyridyl, 2-phenoxy-5-pyridyl, 2-phenylthio-5-pyridyl, 2-phenylsulfonyl-5-pyridyl, 2-phenylcarbonylamino-5-pyridyl, 2-(N-methyl-phenylcarbonylamino)-5-pyridyl, 3-methyl-6-pyridyl, 3-phenyl-6-pyridyl, 2-methyl-6-pyridyl, 2-phenyl-6-pyridyl, 2-methyl-4-pyrimidinyl, 2-phenyl-4-pyrimidinyl, 2-methoxy-4-pyrimidinyl, 2-ethoxy-4-pyrimidinyl, 2-isopropoxy-4-pyrimidinyl, 2-methylthio-4-pyrimidinyl, 2 ethylthio-4-pyrimidinyl, 2-isopropylthio-4-pyrimidinyl, 2-phenylthio-4-pyrimidinyl, 2-methanesulfonyl-4-pyrimidinyl, 2-econsultancy-4-pyrimidinyl, 2-ia, 2-methoxy-5-pyrimidinyl, 2 - ethoxy-5-pyrimidinyl, 2-isopropoxy-5-pyrimidinyl, 2-methylthio-5-pyrimidinyl, 2-ethylthio-5-pyrimidinyl, 2-isopropylthio-5-pyrimidinyl, 2-phenylthio-5-pyrimidinyl, 2-methanesulfonyl-5-pyrimidinyl, 2-econsultancy-5-pyrimidinyl, 2-isopropylphenyl-5-pyrimidinyl, 2-phenylsulfonyl-5-pyrimidinyl, 2-indolyl, 3-indolyl, 1-methyl-2-indolyl, 1-methyl-3-indolyl, 2-benzimidazolyl, 1-methyl-2-benzimidazolyl, 2-benzoxazolyl, 2-benzothiazolyl, 2-chinoline, 3-chinoline, 4-chinoline, 1-izochinolina, 3-izochinolina, 4-izochinolina or 8 - izochinolina; preferred group of phenyl, 1-naphthyl, 2-naphthyl, m-tolila, p-tolila, 3-ethylphenyl, 4-ethylphenyl, 3-isopropylphenyl, 4-isopropylphenyl, 4-trifloromethyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 4-hydroxy-3,5-dimetilfenil, 3-acetoxyphenyl, 4-acetoxyphenyl, 5-acetoxy-2-hydroxy-3,4,6-trimetilfenil, 3 - methoxyphenyl, 4-methoxyphenyl, 3-ethoxyphenyl, 4-ethoxyphenyl, 3 - isopropoxyphenyl, 4-isopropoxyphenyl, 3,4-methylene-dioxyphenyl, benzyloxyphenyl, 3-methylthiophenyl, 4-methylthiophenyl, 3-ethylthiophene, 4-ethylthiophene, 3-methanesulfonyl, 4-methanesulfonamide, 3-ethanolgasoline, 4 - ethanolgasoline, 3-ftoheia, 4-ftoheia, 3-chlorphenyl, 4 - chlorophenylsulfonyl)phenyl, 3-(4-ethylphenyl)phenyl, 3-(4-triptoreline)phenyl, 4-(4-triptoreline)phenyl, 4-(2-hydroxyphenyl) phenyl, 4-(3-hydroxyphenyl)phenyl, 4-(4-hydroxyphenyl)phenyl, 4-(4-hydroxy - 3, 5-dimetilfenil)phenyl, 3-(4-methoxyphenyl)phenyl, 4-(2 - methoxyphenyl)phenyl, 4-(3-methoxyphenyl)phenyl, 4-(4 - methoxyphenyl)phenyl, 3-(2,4-acid) phenyl, 4-(2, 4 - acid)phenyl, 3-(2,5-acid)phenyl, 4-(2,5 - acid)phenyl, 4-(3-hydroxymethylene)phenyl, 4-(4 - hydroxymethylene)phenyl, 4-(3-forfinal)phenyl, 4-(4-forfinal)phenyl, 4-(3-chlorophenyl)phenyl, 4-(4-chlorophenyl)phenyl, 3-(3,4-methylenedioxyphenyl)phenyl, 4-(3, 4-methylenedioxyphenyl) phenyl, 2-formylphenyl, 3-formylphenyl, 4-formylphenyl, 3-carboxyphenyl, 4-carboxyla, 3-N,N-dimethylaminomethylphenol, 4-N, N-dimethylaminomethylphenol, 3-phenoxyphenyl, 4-phenoxyphenyl, 3-phenylthiophene, 4-phenylthiophene, 3-phenyl of sulfanilamide, 4-phenylsulfanyl-phenyl, 3-(phenylcarbonylamino)phenyl, 4-(phenylcarbonylamino) phenyl, 3-(N-methylphenylsulfonyl)phenyl, 4-(N-methylphenylsulfonyl)phenyl, 3-(2-pyridyl)phenyl, 4-(2-pyridyl)phenyl, 4-(2-triptorelin-5-yl)phenyl, 4-(2-methoxypyridine-5-yl)phenyl, 4-(2-nitropyridine-5-yl)phenyl, 4-(2-N,N-dimethylaminopyridine-5-yl)phenyl, 3-(3-pyridyl)phenyl, 4-(3-pyridyl)phenyl, 3 is editio)phenyl, 3-(2-pyridylsulfonyl)phenyl, 4-(2-pyridylsulfonyl)phenyl, 3-(3-pyridylsulfonyl)phenyl, 4-(C-pyridylsulfonyl)phenyl, 3-(2-pyridylsulfonyl)phenyl, 3-(N-methyl-2-pyridylsulfonyl)phenyl, 4-(2-pyridyl-sulfonylamino)phenyl, 4-(N-methyl-2-pyridinesulfonamide)-phenyl, 3-(3-pyridylsulfonyl)phenyl, 3-N-methyl-3-pyridylsulfonyl) phenyl, 4-(3-pyridylsulfonyl)-phenyl, 4-(N-methyl-3-pyridylsulfonyl) phenyl, 4-(1-piperidinyl) phenyl, 3-imidazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 3-methyl-5 - pyridyl, 3-ethyl-5-pyridyl, 3-phenyl-5-pyridyl, 2-methyl-5-pyridyl, 2-ethyl-5-pyridyl, 2-phenyl-5-pyridyl, 2-hydroxy-5-pyridyl, 2-methoxy-5-pyridyl, 2-ethoxy-5-pyridyl, 2-isopropoxy-5-pyridyl, 2-(2,2,3,3-tetrafluoropropoxy)-5-pyridyl, 2-benzyloxy-5-pyridyl, 2-methylthio-5-pyridyl, 2 - ethylthio-5-pyridyl, 2-isopropylthio-5-pyridyl, 2-methanesulfonyl-5-pyridyl, 2-econsultancy-5-pyridyl, 2-isopropylphenyl-5-pyridyl, 2-benzyl-5-pyridyl, 2-phenoxy-5-pyridyl, 2-phenylthio-5-pyridyl, 2-phenylsulfonyl-5-pyridyl, 2-phenylcarbonylamino-5 - pyridyl, 2-(N-methylphenylsulfonyl)-5-pyridyl, 2-(4-methoxyphenyl)-5-pyridyl, 2-(4-forfinal)-5-pyridyl, 3-methyl-6-pyridyl, 3-phenyl-6-pyridyl, 2-methyl-6-pyridyl, 2-phenyl-6-pyridyl, 2-chinoline, 3-chinoline,m-tolila, p-tolila, 3-hydroxyphenyl, 4-hydroxyphenyl, 4-hydroxy-3,5-dimetilfenil, 3-acetoxyphenyl, 4-acetoxyphenyl, 5-acetoxy-2-hydroxy-3,4,6-trimetilfenil, 3-chlorphenyl, 4-chlorphenyl, 3-benzoylphenyl, 4-benzoylphenyl, 3-biphenylyl, 4-biphenylyl, 4-(4-triptoreline)phenyl, 4-(2-hydroxyphenyl)phenyl, 4-(3-hydroxyphenyl)phenyl, 4-(4-hydroxyphenyl)phenyl, 4-(2-methoxyphenyl)phenyl, 4-(3-methoxyphenyl)phenyl, 4-(4-methoxyphenyl)phenyl, 4-(4-hydroxy-3, 5dimethylphenyl)phenyl, 4-(4-forfinal)phenyl, 4-(4-chlorophenyl)phenyl, 4-(2-formylphenyl)phenyl, 4-(3-formylphenyl)phenyl, 4-(4-formylphenyl)phenyl, 4-(3-carboxyphenyl)phenyl, 4-(4-carboxyphenyl)phenyl, 4-(3-hydroxymethylene)phenyl, 4-(4-hydroxymethylene)phenyl, 4-(3-N, N-dimethylaminomethylphenol)phenyl, 4-(4-N, N-dimethylaminomethylphenol)phenyl, 3-phenoxyphenyl, 4-phenoxyphenyl, 3-phenylthiophene, 4-phenylthiophene, 3-phenylsulfanyl, 4-phenylsulfonyl, 3-(phenylcarbonylamino)phenyl, 4-(phenylcarbonylamino)phenyl, 3-(N-methylphenylsulfonyl)phenyl, 4-(N-were-sulfonylamino)phenyl, 3-(2-pyridyl) phenyl, 4-(2-pyridyl)phenyl, 4-(3-triptorelin-6-yl)phenyl, 4-(3-methoxypyridine-6-yl)phenyl, 4-(3-nitropyridine-6-yl)phenyl, 4-(3-N,N-dimethylaminopyridine-6-yl)phenyl, 3-(3-pyridyl)phenyl, 4-(3-pyridyl)phenyl, 3-(4-Piloto)phenyl, 3-(2-pyridylsulfonyl)phenyl, 4-(2-pyridylsulfonyl)phenyl, 3-(3-pyridylsulfonyl)phenyl, 4-(3-pyridylsulfonyl)phenyl, 3-(2-pyridylsulfonyl)phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-methoxy-5-pyridyl, 2-ethoxy-5-pyridyl, 2-isopropoxy-5-pyridyl, 2-(2,2,3,3-tetrafluoropropoxy)-5-pyridyl, 2-benzyloxy-5-pyridyl, 2-methylthio-5-pyridyl, 2-ethylthio-5-pyridyl, 2-methanesulfonyl-5-pyridyl, 2-econsultancy-5-pyridyl, 2-benzyl-5-pyridyl, 2-phenyl-5-pyridyl, 2-(4-methoxyphenyl)-5-pyridyl, 2-(4-forfinal)-5-pyridyl, 3-phenyl-5-pyridyl, 2-phenyl-6-pyridyl, 3-phenyl-6-pyridyl, 2-phenoxy-5-pyridyl, 2-phenylthio-5-pyridyl, 2-phenylsulfonyl-5-pyridyl, 2-phenylcarbonylamino-5-pyridyl, 2-(N-methylphenylsulfonyl-amino)-5-pyridyl, 2-methyl-5-pyridyl, 3-chinoline, 3-methyl-5-pyridyl, 3-ginalisa or 3-indolyl; the most preferred group is phenyl, p-tolila, 4-ftoheia, 4-benzylphenol, 4-biphenylyl, 4-(4-triptoreline) phenyl, 4-(2-hydroxyphenyl)phenyl, 4-(3-hydroxyphenyl)phenyl, 4- (4-hydroxyphenyl)phenyl, 4-(2-methoxyphenyl)phenyl, 4-(3 - methoxyphenyl)phenyl, 4-(4-methoxyphenyl)phenyl, 4-(4-hydroxy - 3, 5dimethylphenyl)phenyl, 4-(4-forfinal)phenyl, 4-(4-chlorophenyl)phenyl, 4-(2-formylphenyl)phenyl, 4-(3-formylphenyl)phenyl, 4-(4-formylphenyl)phenyl, 4-(3-carboxyphenyl)phenyl, shall fenil)-phenyl, 4-(4-N, N - dimethylaminomethylphenol)phenyl, 4-phenoxyphenyl, 4-phenylthiophene, 4-phenylsulfonyl, 4-(phenylcarbonylamino)phenyl, 4-(2-pyridyl)phenyl, 4-(3 - triptorelin-6-yl) phenyl, 4-(3-methoxypyridine-6-yl) phenyl, 4-(3-nitropyridine-6-yl)phenyl, 4-(3-N,N - dimethylaminopyridine-6-yl)phenyl, 4-(3-pyridyl)phenyl, 4-(4 - pyridyl)phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-methoxy-5-pyridyl, 2-ethoxy-5-pyridyl, 2-isopropoxy-5-pyridyl, 2-(2,2,3,3-tetrafluoropropoxy)-5-pyridyl, 2-benzyloxy-5-pyridyl, 2-methylthio-5-pyridyl, 2-ethylthio-5-pyridyl, 2-methanesulfonyl-5-pyridyl, 2-econsultancy-5-pyridyl, 2-benzyl-5-Perilla, 2-phenyl-5-pyridyl, 3-phenyl-5-pyridyl, 3-phenyl-6-pyridyl, 2-(4-methoxyphenyl)-5-pyridyl, 2-(4-forfinal)-5-pyridyl, 2-phenyl-6-pyridyl, 2-phenoxy-5-pyridyl, 2-phenylthio-5-pyridyl, 2-phenylsulfonyl-5-pyridyl, 2 phenylcarbonylamino-5-pyridyl, 2-(N-methylphenylsulfonyl-amino)-5-pyridyl, 2-methyl-5-pyridyl or 3-methyl-5-pyridyl.

When Y represents a group of the formula: >N-R5(where R5represents a hydrogen atom, a straight or branched alkyl group comprising from 1 to 6 carbon atoms (the alkyl group has the same values as described above in the definition of R3or a straight or Razvitie in itself, for example, a group of alkanol comprising from 1 to 8 carbon atoms, and a group of alkanol comprising from 3 to 8 atoms

carbon or aromatic acyl group containing from 7 to 11 carbon atoms), a group of the formula: >N-R5includes, for example, an imino group, methylamino, ethylimino, propylimino, isopropylamino, butylamino, isobutylamino, sec-butylamino, tert-butylamino, pentylamine, 1 methylbutylamine, 2-methylbutylamine, 3 methylbutylamine, 1,1-dimethylpropylene, 1,2-dimethylpropylene, 2,2-dimethylpropylene, 1 ethylpropylamine, hexylamino, 1 methylpentylamino, 2-methylpentylamino, 3 methylpentylamino, 4-methylpentylamino, 1,1-dimethylbutylamino, 1,2-dimethylbutylamino, 1,3-dimethylbutylamino, 2,2-dimethylbutylamino, 2,3-dimethylbutylamino, 3,3-dimethylbutylamino, 1 ethylbutylamine, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, acetylimino, propionamido, Butylimino, pentanediamine, hexanamine, leptanillinae, actinolite, benzoylamino or p-toluylene;

preferred aminogroup, straight or branched alkylamino comprising from 1 to 4 carbon atoms or acetylimino;

the most preferred aminogroup, methylaminopropyl, ethylimino or acetylen bratvany in acid additive salts of the acids according to conventional methods in the case when there is a core group. Such salts include salts of halogen acids such as hydrofluoric acid, hydrochloric acid, Hydrobromic acid and uudistoodetena acid; inorganic salts such as nitrate, perchlorate, sulfate and phosphate; salts of lower alkanesulphonic acids, such as methanesulfonate acid, triftormetilfullerenov acid and econsultancy acid; salts arylsulfonic acid, such as benzolsulfonat acid and p-toluensulfonate acid; salts of amino acids such as glutamic acid and aspartic acid; and salts of carboxylic acids, such as acetic acid, fumaric acid, tartaric acid, oxalic acid, maleic acid, malic acid, succinic acid, benzoic acid, mandelic acid, ascorbic acid, lactic acid, gluconic acid and citric acid; preferred salts of halogen acids.

Moreover, derivatives amidocarbonyl acid of the formula (I) can be converted to metal salts in accordance with conventional methods, as they have a carboxyl group. Such salts include salts of alkali metals such as lithium, sodium and potassium; Solh metals.

Derivatives metocarbamol acid of the formula (I) according to the present invention can be converted into pharmacologically acceptable ester according to conventional methods. Pharmacologically acceptable ester derivative amidocarbonyl acid (I), in particular, not limited to the use for medical purposes and pharmacologically acceptable compared amidocarbonyl acid of the formula (I).

Esters derived amidocarbonyl acid of the formula (I) according to the present invention include straight or branched alkyl group comprising from 1 to 6 carbon atoms; aracelio group containing from 7 to 19 carbon atoms; a straight or branched alkyl groups comprising from 1 to 5 carbon atoms, which is substituted by a straight or branched alkanoyloxy comprising from 1 to 6 carbon atoms; a straight or branched alkyl group comprising from 1 to 5 carbon atoms, which is substituted by a straight or branched allyloxycarbonyl comprising from 1 to 6 carbon atoms; straight or branched alkyl group comprising from 1 to 5 carbon atoms, which is substituted by cycloalkylcarbonyl comprising from 5 to 7 carbon atoms; a straight or branched who Lucaya from 5 to 7 carbon atoms; straight or branched alkyl group comprising from 1 to 5 carbon atoms, which is substituted by arylcarboxylic comprising from 6 to 10 carbon atoms; a straight or branched alkyl group comprising from 1 to 5 carbon atoms, which is substituted by aryloxypropanolamine comprising from 6 to 10 carbon atoms; or 2-oxo-1,3-dioxolan-4-ylmethylene group containing a straight or branched alkyl group comprising from 1 to 6 carbon atoms as a substituent at 5-position.

Straight or branched alkyl group comprising from 1 to 4 carbon atoms, and straight or branched alkyl group comprising from 1 to 6 carbon atoms, and includes methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, penttila, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1 - methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2 - dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl or 1,2,2-trimethylpropyl; preferred straight or branched alkyl group, Lee isobutyl; the most preferred methyl group or ethyl.

Kalkilya group comprising from 7 to 19 carbon atoms include benzyl group, Venetia, 3-phenylpropyl, 4-phenylbutyl, 1-naphthylmethyl, 2-naphthylmethyl or diphenylmethyl; preferred group is benzyl.

Cycloalkyl group comprising from 5 to 7 carbon atoms, includes a group of cyclopentyl, cyclohexyl or cycloheptyl; preferred group is cyclohexyl.

Aryl group comprising from 6 to 10 carbon atoms includes a phenyl group or naphthyl; preferred phenyl group.

Specific examples of preferred essential residues include methyl group, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, benzyl, acetoxymethyl, 1-(acetoxy)ethyl, propionylacetate, 1-(propionyloxy)ethyl, butyrylacetate, 1-(butyryloxy)ethyl, isobutyrylacetate, 1-(isobutyryloxy)ethyl, malariaclimate, 1-(valeriote)ethyl, isovalerylglycine, 1- (isovalerianic)ethyl, pivaloyloxymethyl, 1-(pivaloyloxy) ethyl, methoxycarbonylmethyl, 1-(methoxycarbonylamino)ethyl, ethoxycarbonylmethyl, 1-(ethoxycarbonyl)ethyl, propoxycarbonyl, 1-(is roximately, 1-(butoxycarbonylamino)ethyl, msobuttoniconandcaption, 1-(isobutoxyethene)ethyl, tert-butoxycarbonylmethyl, 1-(tert-butoxycarbonylamino) ethyl, cyclopentanecarboxylate, 1-(cyclopentanecarbonyl) ethyl, cyclohexanecarboxylate, 1-(cyclohexanecarbonyl)ethyl, cyclopentanecarboxylate, 1-(cyclopentanecarbonyl)ethyl, cyclohexyloxycarbonyloxy, 1-(cyclohexyloxycarbonyloxy)ethyl, benzoyloxymethyl, 1-(benzoyloxy)ethyl, phenoxycarbonylamino, 1-(phenoxycarbonylamino) or ethyl 5-methyl-2-oxo-1,3-dioxolan-4-ylmethyl.

In some cases, derivatives amidocarbonyl acid of formula (1), their pharmacologically acceptable salts or their pharmaceutically acceptable esters have different isomers. For example, an optical isomer is formed due to the asymmetric carbon in-position carboxylic acid. In the formula (1) all stereoisomers formed because of these asymmetric carbon atoms, and equivalent and non-equivalent mixtures of these isomers are shown as a single equation. Therefore, the present invention includes all of these isomers and mixtures of these isomers.

Moreover, according to the present invention, in the event that it is acceptable esters form a solvate (e.g., hydrates), the present invention includes all of these solvate.

In addition, the present invention includes all compounds that are converted in vivo and converted into derivatives amidocarbonyl acid of the formula (I) or its salt, for example the so-called prodrugs, such as amide derivatives.

Derivatives amidocarbonyl acid of the formula (I) preferably include:

(1) derivative amidocarbonyl acid, where R represents a hydrogen atom, a straight or branched alkyl group containing from 1 to 4 carbon atoms, or aracelio group containing from 7 to 9 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(2) derivative amidocarbonyl acid, where R1represents a hydrogen atom or a straight or branched alkyl group containing from 1 to 4 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(3) derivative amidocarbonyl acid, where R1represents a hydrogen atom or an alkyl group containing one or two carbon atoms, and their pharmacologically acceptable salt or their pharmacologically and, their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(5) derivative amidocarbonyl acid, where R2is a straight or branched alkylenes group containing from 2 to 5 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

6) derivative amidocarbonyl acid, where R2is a straight or branched alkylenes group containing from 2 to 4 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(7) derivative amidocarbonyl acid, where R2represents an ethylene group, trimethylene group or melatoninbuy group, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(8) derivative amidocarbonyl acid, where R2represents an ethylene group, a pharmacologically acceptable salt or their pharmacologically acceptable esters;

(9) derivative amidocarbonyl acid, where R3represents a hydrogen atom, a straight or branched alkyl group containing from 1 to 4 carbon atoms, alkoxygroup containing one or two carbon atoms, alkit is or branched aliphatic acyl group, comprising from 1 to 5 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(10) derivative amidocarbonyl acid, where R3represents a hydrogen atom, a halogen atom or a nitro-group, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(11) derivative amidocarbonyl acid, where R3represents a hydrogen atom, pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(12) derivative amidocarbonyl acid, where R4represents a hydrogen atom or a straight or branched alkyl group containing from 1 to 4 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters,

(13) derivative amidocarbonyl acid, where R4represents a hydrogen atom or an alkyl group containing one or two carbon atoms, and their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(14) derivative amidocarbonyl acid, where R4represents a hydrogen atom or methyl group, and their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(15) derived the and or their pharmacologically acceptable esters;

(16) derivative amidocarbonyl acid, where R4represents a methyl group, a pharmacologically acceptable salt or their pharmacologically acceptable esters;

(17) derivative amidocarbonyl acid, where Z is a straight or branched alkylenes group containing from 1 to 4 carbon atoms, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(18) derived amidocarbonyl acid, where Z is alkylenes group containing one or two carbon atoms, and their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(19) derivative amidocarbonyl acid, where Z represents a methylene group, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(20) derivatives amidocarbonyl acid, where W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) hydroxyl group, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (v) aryl group containing from 6 to 10 carbon atoms, which may sa, which may contain from 1 to 3 substituents1described later on the aryl group, (vii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (viii) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 1described later on the aryl group, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (x) arkitip comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xi) aryloxyalkyl the group in which the aryl group is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xii) mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xiii) mono - or decillions 5-10-Yes, the nitrogen atom and sulfur atom, (xiv) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (xv) a mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy1represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 carbon atoms, (v) straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, (vi) straight or branched alkoxygroup, comprising from 1 to 4 carbon atoms, (vii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (viii) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may put up with from 1 to 4 carbon atoms, (xi) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (xii) halogen atom, (xiii) nitro-group, (xiv) cyano, (xv) amino groups, (xvi) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xvii) straight or branched alkoxycarbonyl in which alkoxygroup has from 1 to 4 carbon atoms, (xviii) arachidonoylethanolamine in which kalkilya group has from 7 to 12 carbon atoms, (xix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xx) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xxi) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1that may be the same or different, described later, (xxii) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xxiii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xxv) arylsulfonamides comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group containing from 1 to carbon atoms), (xxvi) a mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described below, (xxvii) a mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described below, (xxviii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described below, (xxix) mono - or decillions, 5-10-membered heteroarylboronic group containing from 1 to 4 heteroatoms, selected and is SUP> described below (xxx) mono - or decillions 5-10-membered heteroatomcontaining containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described hereinafter, heteroaryl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms) and (xxxi) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy1represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) straight or branched hydroxyl) cyano, (xii) carboxyl group, (xiii) amino groups, (xiv) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xv) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xvi) straight or branched aminoalkyl group containing from 1 to 4 carbon atoms, (xvii) monoalkylammonium group, in which monoalkylamines - group contains one straight or branched alkyl group, comprising from 1 to 4 carbon atoms, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xviii) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xix) straight or branched alkoxycarbonyl in which alkoxygroup has from 1 to 4 carbon atoms or (xx) arachidonoylethanolamine, in which the aryl group has from 6 to 10 and their pharmacologically acceptable esters;

(21) derivative amidocarbonyl acid, in which W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) hydroxyl group, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched chain alkylthiols comprising from 1 to 4 carbon atoms, (v) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described below, (vi) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (vii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (viii) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 2described later on the aryl group, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents2described hereinafter, on the aryl group, (x) arkitip comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents2described hereinafter, allcause from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xii) mono - or decillions 5-10-membered, heteroaromatic-group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (xiii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy2represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 carbon atoms, (v) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vii) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (viii) straight or razwell is the Rupp, (xii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xiii) aryl groups containing from 6 to 10 carbon atoms, which may be the same or different and have from 1 to 3 substituents2described later, (xiv) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (xv) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (xvi) mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents2described below, (xvii) a mono - or decillions 5-10 - membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents2described below, (xviii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group, who were then, and (xix) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy 2represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (v) halogen atom, (vi) a nitro-group, (vii) formyl group, (viii) carboxyl group, (ix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms or (x) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms,

Borovoy acid, where W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iii) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents 3described later on the aryl group, (iv) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3described later on the aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3described later on the aryl group, (vi) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3described later on the aryl group, (vii) aryloxyalkyl the group in which the aryl group is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (viii) mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms, selected is killigrew, containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy3represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (vii) halogen atom, (viii) cyano and (ix) pyridyloxy group

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(23) derivatives amidocarbonyl acid, where W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iii) fenoxaprop, which may contain from 1 to 3 substituents4described later, on petitely 4described later, on the phenyl group, (v) Uralkaliy group containing 7 to 10 carbon atoms, (vi) aralkylated comprising from 7 to 10 carbon atoms, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms, and the alkyl group is a straight or branched group and contains from 1 to 4 carbon atoms, (viii) mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy4represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to b carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched allylthiourea containing about what Ohm carbon, (vii) halogen atom, (viii) cyano or (ix) pyridyloxy group

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(24) derivative amidocarbonyl acid, where W represents fenoxaprop, which may contain one Deputy5as described below, on fenilnoe group,

here Deputy5represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched allylthiourea containing one or two carbon atoms, (vi) straight or branched alkylsulfonyl group containing one or two carbon atoms, (vii) halogen atom, (viii) cyano or (ix) pyridyloxy group

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(25) derivative amidocarbonyl acid, where W represents fenoxaprop, which is the focus of a group, selected from the group including the group of methyl, ethyl, isopropyl, tert - butyl, trifloromethyl, methoxy, triptoreline and a fluorine atom, a chlorine atom,

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(26) derivative amidocarbonyl acid, where W is a group of phenoxy, methylphenoxy, ethylenoxy, isopropylphenoxy, tert-butylphenoxy, triptoreline, methoxyphenoxy, triftormetilfosfinov, fervency or chlorphenoxy, their pharmaceutically acceptable salts or their pharmaceutically acceptable esters,

(27) derivative amidocarbonyl acid, where X is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents7described below, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents7described below

here Deputy7represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenerator the aliphatic alloctype, comprising from 1 to 5 carbon atoms, (v) straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, (vi) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (viii) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3described below, (x) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (xi) straight or branched alkylsulfonyl comprising from 1 to 4 carbon atoms, (xii) halogen atom, (xiii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xiv) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3as described below, (xv) phenyl group, which may contain from 1 to 3 substituents 3as described below, (xvi) fenoxaprop, which may contain from 1 to 3 substituents3as described below, (xvii) panitierre heaven can contain from 1 to 3 substituents3as described below, (xix); phenylcarbonylamino, which may contain from 1 to 3 substituents3as described below, on the phenyl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (XX) follow group, (XXI) thienyl group, (xxii) oxazolidinyl group, (xxiii) isoxazolyl group, (xxiv) thiazolidine group, (xxv) pyridyloxy group, which may contain from 1 to 3 substituents3as described below, (xxvi) pyridyloxy, which may contain from 1 to 3 substituents 3as described below, (xxvii) pyridylthio, which may contain from 1 to 3 substituents3as described below, (xxviii) pyridylsulfonyl group, which may contain from 1 to 3 substituents3as described below, (xxix) imidazolidinyl group (the nitrogen atom in the ring may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (xxx) pyridinesulfonamide, which may contain from 1 to 3 substituents3described below, peredelnoj group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms) and (xxxi) mono - or dicklicious an oxygen atom, the nitrogen atom and sulfur atom,

here Deputy3represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) the nitrogroup, (x) formyl group, (xi) cyano, (xii) carboxyl group, (xiii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms and (xiv) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or razvetvlenno Ekologicheskie acceptable esters;

(28) derivative amidocarbonyl acid, where X is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents8described below, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents8described below

here Deputy8represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 carbon atoms, (v) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vii) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) straight or branched dialkylamino, in which each alkyl group may be one which is up to 3 substituents4as described below, (xi) fenoxaprop, which may contain from 1 to 3 substituents 4as described below, (xii) phenylthiourea, which may contain from 1 to 3 substituents4as described below, (xiii) follow group, (xiv) thienyl group, (xv) oxazolidinyl group, (xvi) isoxazolyl group, (xvii) thiazolidine group, (xviii) pyridyloxy group, which may contain from 1 to 3 substituents4as described below, (xix) imidazolidinyl group (the nitrogen atom in the ring may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms) and (xx) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy4represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 d is a, (vii) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) the nitrogroup, (x) formyl group, (xi) cyano, (xii) carboxyl group, (xiii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms and (xiv) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms,

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(29) derivative amidocarbonyl acid, where X is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents9described below, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents9described below

the estuaries straight or branched alkoxygroup, comprising from 1 to 4 carbon atoms, (iii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (v) phenyl group, which may contain from 1 to 3 substituents5as described below, (vi) fenoxaprop, which may contain from 1 to 3 substituents5as described below, (vii) pyridyloxy group, which may contain from 1 to 3 substituents 5described below and (viii) W mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy5represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group comprising from 1 to or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms and (xi) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms,

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(30) derivative amidocarbonyl acid, where X is a group of phenyl, naphthyl, imidazolyl, oxazolyl, pyridyl, indolyl, chinoline or izochinolina, which may contain from 1 to 3 substituents 10described below;

here Deputy10represents a group selected from the group including (i) hydroxyl group, (ii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched dialkylamino, which may be the same or different and in which each alkyl group has from 1 to 4 at the oxygraph, which may contain from 1 to 3 substituents6as described below, (vii) pyridyloxy group, which may contain from 1 to 3 substituents 6described below and (viii) a 5-10 membered saturated heterocyclic group with one ring or two rings containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy6represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, which may be the same or different and in which each of the alkyl groups has from 1 to 4 carbon atoms, and (xi) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising nd a straight or branched alkyl group, comprising from 1 to 4 carbon atoms,

their pharmaceutically acceptable salts or their pharmaceutically acceptable esters;

(31) derivatives amidocarbonyl acid, where X represents a phenyl group, indolyl, pyridyl or chinoline, which may contain from 1 to 3 substituents11described below;

here Deputy11represents a group selected from the group including (i) hydroxyl group, (ii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (v) phenyl group, which may contain from 1 to 3 substituents7as described below, (vi) fenoxaprop, which may contain from 1 to 3 substituents7as described below, (vii) pyridyloxy group, which may contain from 1 to 3 substituents 7described below, and (viii) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, the atom is(i) straight or branched alkyl group, comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms and (xi) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms,

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(32) derivative amidocarbonyl acid, where X represents a phenyl group which may have one Deputy12described below

here Deputy12is a group, vappu, the phenyl group (the phenyl group may be substituted by 1 to 3 substituents, which may be the same or different, include the group of methyl, ethyl, trifloromethyl, hydroxyl, methoxy, ethoxy, isopropoxy, triptoreline, methylendioxy and hydroxymethyl, fluorine atoms, chlorine atoms, the nitro-group, formyl group, cyano, carboxyl, dimethylamino, diethylamino and N,N-dimethylaminomethyl), phenoxy, phenylthio, phenylsulfonyl, phenylcarbonylamino, N-methylphenylsulfonyl and pyridyl (Peregrina group may be substituted by methyl group, ethyl, trifloromethyl, methoxy, ethoxy, isopropoxy or triptoreline, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl), pyridyloxy, pyridylthio, pyridylsulfonyl and piperidyl,

or

X represents pyridyloxy group which may contain one Deputy13described below

here Deputy13represents a group selected from the group comprising methyl group, isopropyl, methoxy, ethoxy, isopropoxy, 2,2,3,3-tetrafluoropropoxy and benzyloxy, allylthiourea containing one or two carbon atoms, alkylsulfonyl group containing one or two carbon atoms, bisetose, ethoxy or isopropoxy, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl), group phenoxy, phenylthio, phenylsulfonyl, phenylcarbonylamino and N-methylphenylethylamine,

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(33) derivative amidocarbonyl acid, where X represents a phenyl group which may contain one Deputy 12described below

here Deputy12represents a group selected from the group comprising methyl, isopropyl and hydroxyl group, a fluorine atom, a chlorine atom, group diethylamino and benzyl, phenyl group (the phenyl group may be substituted by 1 to 3 substituents, which may be the same or different, include the group of methyl, ethyl, trifloromethyl, hydroxyl, methoxy, ethoxy, isopropoxy, triptoreline, methylendioxy and hydroxymethyl, fluorine atoms, chlorine atoms, the nitro-group, formyl group, cyano, carboxyl, dimethylamino, diethylamino and N,N-dimethylaminomethyl), group phenoxy, phenylthio, phenylsulfonyl, phenylcarbonylamino and N-methylphenylethylamine, pyridyloxy group (Peregrina group may be substituted by a methyl group is the group dimethylaminopropoxy or diethylaminopropyl), group pyridyloxy, pyridylthio, pyridylsulfonyl and piperidyl,

their pharmacologically acceptable salt or their pharmacologically acceptable esters;

(34) derivatives amidocarbonyl acid, in which X represents pyridyloxy group which may contain one Deputy13described below

here Deputy13represents a group selected from the group comprising methyl group, isopropyl, methoxy, ethoxy, isopropoxy, 2,2,3,3-tetrafluoropropoxy and benzyloxy, allylthiourea containing one or two carbon atoms, alkylsulfonyl group containing one or two carbon atoms, benzyl group, phenyl group (the phenyl group may be substituted by methyl group, ethyl, trifloromethyl, methoxy, ethoxy or isopropoxy, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl), group phenoxy, phenylthio, phenylsulfonyl, phenylcarbonylamino and N-methylphenylethylamine,

their pharmacologically acceptable salts and pharmaceutically acceptable esters;

(35) derivative amidocarbonyl acid, where X is a 2,2,3,3 tetrafluoropyridine group or is ethoxy or isopropoxy, fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl), their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(36) derivative amidocarbonyl acid, where X is biphenylyl group (each phenyl group may be substituted by one Deputy, who may be the same or different, includes a methyl group, trifloromethyl, hydroxyl, methoxy or hydroxymethyl, a fluorine atom, a chlorine atom or a formyl group, carboxyl, nitro, dimethylamino or N,N-dimethylaminomethyl), pyridylamino group (Peregrina group may be substituted by one Deputy group includes methyl, ethyl, trifloromethyl, methoxy, ethoxy, isopropoxy or triptoreline, a fluorine atom, a chlorine atom or nitro, dimethylaminopropyl or diethylaminopropyl) or phenylpyridine group (the phenyl group may be substituted by one Deputy group includes methyl, ethyl, trifloromethyl, methoxy, ethoxy or isopropoxy, a fluorine atom, a chlorine atom, a nitro-group or dimethylaminopropyl), their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(37) derivatives amidocarbonyl acid, where X represents guidancematerials)phenyl, (forfinal)phenyl, (chlorophenyl)phenyl, (formylphenyl)phenyl, (carboxyphenyl)phenyl, (nitrophenyl)phenyl, (dimethylaminophenyl)phenyl or (N, N-dimethylaminomethylphenol)phenyl, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(38) derivative amidocarbonyl acid, where X is a group biphenylyl, (were)phenyl, (triptoreline)phenyl, (methoxyphenyl)phenyl, (forfinal)phenyl or (chlorophenyl)phenyl, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(39) derivatives amidocarbonyl acid, where X is a group biphenylyl, (forfinal)phenyl or (chlorophenyl) phenyl, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(40) derivative amidocarbonyl acid, where X is a group of pyridylethenyl (Peregrina group may contain one group of methyl, ethyl, trifloromethyl, methoxy, ethoxy or isopropoxy, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropyl or diethylaminopropyl), their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(41) derived amidocarbonyl acid, where X is a group of pyridylethenyl, (IU the Oli or their pharmacologically acceptable esters;

(42) derivative amidocarbonyl acid, where X is phenylpyridine group (the phenyl group may contain one group of methyl, ethyl, methoxy, ethoxy or isopropoxy, a fluorine atom, a chlorine atom or dimethylaminopropyl), their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(43) derivative amidocarbonyl acid, where X is a group of phenylpyridine, (methoxyphenyl)pyridyl or (forfinal)pyridyl, their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(44) derivatives amidocarbonyl acid, where Y represents a single bond, an oxygen atom, a sulfur atom or a group of the formula: >N-R5(where R5represents a hydrogen atom, a straight or branched alkyl group containing one or two carbon atoms, or straight or branched aliphatic acyl group containing from 2 to 5 carbon atoms), their pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(45) derivative amidocarbonyl acid, where Y represents a single bond or an oxygen atom, pharmacologically acceptable salts or their pharmaceutically acceptable esters;

(46) derivatives and farmacologicas acceptable esters.

Moreover, compounds in which R1selected from (1) to(4), R2selected from (5)- (8), R3selected from (9)-(11), R4selected from (12)-(16), Z is selected from (17)-(19), W is selected from (20)-(26), X is selected from (27)-(43) and Y is selected from (44)- (46) in combination with each other are preferred.

For example, phenylalkylamines acid of formula (1) includes:

(47) derived amidocarbonyl acid, where

R1represents a hydrogen atom, a straight or branched alkyl group containing from 1 to 4 carbon atoms, or aracelio group containing from 7 to 9 carbon atoms;

R2is a straight or branched alkylenes group containing from 2 to 4 carbon atoms;

R3represents a hydrogen atom, a straight or branched alkyl group containing from 1 to 4 carbon atoms, alkoxygroup, including one or two carbon atoms, allylthiourea, including one or two carbon atoms, a halogen atom, a nitro-group, a hydroxyl group or a straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms;

R4represents a hydrogen atom or a straight or branched alkyl group containing from 1 to 4 atoms is of Pereda;

W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) hydroxyl group, (iii) straight or branched alkoxygroup, lucaus from 1 to 4 carbon atoms, (iv) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (v) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents 1described below, (vi) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents 1described later on the aryl group, (vii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (viii) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 1described later on the aryl group, (x) arkitip comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xi) aryloxyalkyl group in which to reap from 1 to 3 substituents1described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xii) mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xiii) mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xiv) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (xv) a mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

Here Deputy1represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 a, (vi) a straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (viii) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1described below, (x) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (xi) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (xii) halogen atom, (xiii) nitro-group, (xiv) cyano, (xv) amino groups, (xvi) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xvii) straight or branched alkoxycarbonyl in which alkoxygroup has from 1 to 4 carbon atoms, (xviii) arachidonoylethanolamine in which kalkilya group has from 7 to 12 carbon atoms, (xix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xx) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain the Ohm carbon, which may contain from 1 to 3 substituents1that may be the same or different, described later, (xxii) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xxiii) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xxiv) arylsulfonyl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group, (xxv) arylsulfonamides comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1described later on the aryl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (xxvi) a mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described below, (xxvii) a mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the gr is described later, (xxviii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described below, (xxix) mono - or decillions 5-10-membered heteroarylboronic group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described below (xxx) mono - or decillions 5-10-membered heteroatomcontaining containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1described hereinafter, heteroaryl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms) and (xxxi) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy1represents a group selected from the group comprising (i) a straight or branched alkyl gruppuso from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) the nitrogroup, (x) formyl group, (xi) cyano, (xii) carboxyl group, (xiii) amino groups, (xiv) straight or branched monoalkylamines, in which the alkyl group has from 1 to 4 carbon atoms, (xv) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xvi) straight or branched aminoalkyl group containing from 1 to 4 carbon atoms, (xvii) monoalkylammonium group, in which monoalkylamines contains one straight or branched alkyl group containing from 1 to 4 carbon atoms, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xxviii) dialkylaminoalkyl group, in which dialkylamino be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xix) straight or branched alkoxycarbonyl in which alkoxygroup is a straight or branched alkoxygroup comprising from 1 to 4 carbon atoms and (xx) arachidonoylethanolamine, in which the aryl group contains from 6 to 10 carbon atoms and the alkyl group contains from 1 to 4 carbon atoms;

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents7described below, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents7described below

here Deputy7represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (vi) straight or branched aliphatic alloctype, vklyucheno carbon (vi) a straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (viii) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3described below, (x) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (xi) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (xii) halogen atom, (xiii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (xiv) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3described later, (xv) phenyl group, which may contain from 1 to 3 substituents3described later, (xvi) fenoxaprop, which may contain from 1 to 3 substituents 3described below, (xvii) phenylthiourea, which may contain from 1 to 3 substituents3described below, V (xviii) phenylsulfonyl group which may soora may contain from 1 to 3 substituents3described later, on the phenyl group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (xx) follow group, (xxi) thienyl group, (xxii) oxazolidinyl group, (xxiii) isoxazolyl group, (xxiv) thiazolidine group, (xxv) pyridyloxy group, which may contain from 1 to 3 substituents3described later, (xxvi) pyridyloxy, which may contain from 1 to 3 substituents 3described below, (xxvii) pyridylthio, which may contain from 1 to 3 substituents3described below, (xxviii) pyridylsulfonyl group, which may contain from 1 to 3 substituents3described below, (xxix) imidazolidinyl group (the nitrogen atom in the ring may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (xxx) pyridinesulfonamide, which may contain from 1 to 3 substituents3described hereinafter, peredelnoj group (the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms) and (xxxi) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms, selected the Oh group, selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) a straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) the nitrogroup, (x) formyl group, (xi) cyano, (xii) carboxyl group, (xiii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms and (xiv) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms; and

Y represents with ielemia esters;

(48) derivatives amidocarbonyl acid, where

R1represents a hydrogen atom, a straight or branched alkyl group containing from 1 to 4 carbon atoms, or aracelio group containing from 7 to 9 carbon atoms;

R2is a straight or branched alkylenes group containing from 2 to 4 carbon atoms;

R3represents a hydrogen atom, a halogen atom or a nitro-group;

R4represents a hydrogen atom or a straight

or branched alkyl group containing from 1 to 4 carbon atoms;

Z represents a methylene group;

W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) hydroxyl group, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (v) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described below, (vi) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (vii) aricioglu is e, on the aryl group, (viii) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 2described later on the aryl group, (ix) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (x) arkitip comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (xi) aryloxyalkyl the group in which the aryl group is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (xii) mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (xiii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy2represents a group selected from the group, svetlanna halogenated alkyl group, comprising from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 carbon atoms, (v) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vii) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (viii) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (ix) halogen atom, (x) nitro-group, (xi) cyano, (xii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 atoms

carbon, (xiii) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2that may be the same or different, described later, (xiv) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (xv) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2described later on the aryl group, (xvi) mono with an oxygen atom, the nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents2described below, (xvii) a mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents2described below, (xviii) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents2described below, and (xix) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy2represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (v) ATO is luminograph, in which each alkyl group may be the same or different, and (x) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms;

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents8described below, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents8described below

here Deputy 8represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched aliphatic alloctype comprising from 1 to 5 carbon atoms, (v) straight or razvitiyu, comprising from 1 to 4 carbon atoms, (vii) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each has from 1 to 4 carbon atoms, (x) phenyl group, which may contain from 1 to 3 substituents4described later, (xi) fenoxaprop, which may contain from 1 to 3 substituents 4described later, (xii) phenylthiourea, which may contain from 1 to 3 substituents4described later, (xiii) follow group, (xiv) thienyl group, (xv) oxazolidinyl group, (xvi) isoxazolyl group, (xvii) thiazolidine group, (xviii) pyridyloxy group, which may contain from 1 to 3 substituents4described below, (xix) imidazolidinyl group (the nitrogen atom in the ring may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms) and (xx) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy4is a group selected from the group vklyuchennoi halogenated alkyl group, comprising from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (viii) halogen atom, (ix) the nitrogroup, (x) formyl group, (xi) the cyano, (xii) carboxyl group, (xiii) straight or branched dialkylamino, in which each alkyl group may be the same or different and contain from 1 to 4 carbon atoms and (xiv) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms; and

Y represents an oxygen atom,

their pharmacologically acceptable salts and pharmaceutically acceptable esters;

(49) derived amidocarbonyl acid, where

R1is the ilen group, comprising from 7 to 9 carbon atoms;

R2is a straight or branched alkylenes group containing from 2 to 4 carbon atoms;

R3represents a hydrogen atom, a halogen atom or a nitro-group;

R4represents a hydrogen atom or a straight or branched alkyl group containing from 1 to 4 carbon atoms;

Z represents a methylene group;

W represents (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iii) alloctype comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3described later on the aryl group, (iv) killigrew comprising from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3described later on the aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 3described later on the aryl group, (vi) aralkylated comprising from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3described later on the aryl group, (vii) allow carbon which may contain from 1 to 3 substituents3described below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (viii) mono - or decillions 5-10-membered heteroepitaxy comprising from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy3represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (vii) halogen atom, (viii) cyano and (ix) pyridyloxy g is from 1 to 3 substituents9described below, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents9described below

here Deputy9represents a group selected from the group comprising (i) a hydroxyl group, a straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iii) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched dialkylamino, in which each alkyl group may be the same or different and contain from 1 to 4 carbon atoms, (v) phenyl group, which may contain from 1 to 3 substituents5as described below, (vi) fenoxaprop, which may contain from 1 to 3 substituents5as described below, (vii) pyridyloxy group, which may contain from 1 to 3 substituents 5described below and (viii) mono - or decillions 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom,

here Deputy5the imagine 1 to 6 carbon atoms, (ii) a straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group comprising from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and contain from 1 to 4 carbon atoms and (xi) dialkylaminoalkyl group, in which dialkylamino has two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms; and

Y represents an oxygen atom,

their pharmacologically acceptable salts or pharmaceutically acceptable esters;

(50) derived amidocarbonyl acid, in which

R1represents a hydrogen atom;

R2represents an ethylene group;

R3represents a hydrogen atom;

R5as described below, on the phenyl group;

here Deputy 5represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup comprising from 1 to 4 carbon atoms, (v) straight or branched allylthiourea, including one or two carbon atoms, (vi) straight or branched alkylsulfonyl group containing one or two carbon atoms, (viii) cyano and (ix) pyridyloxy group;

X represents a phenyl group which may contain one Deputy12described below

here Deputy12represents a group selected from the group comprising methyl, isopropyl and hydroxyl, fluorine atom, chlorine atom, group diethylamino and benzyl, phenyl group (the phenyl group may be substituted by 1 to 3 substituents, which may be the same or different, includes a group of maimela, a fluorine atom, a chlorine atom and a nitro-group, formyl group, cyano, carboxyl, dimethylamino, diethylamino and N,N-dimethylaminomethyl), group phenoxy, phenylthio, phenylsulfonyl, phenylcarbonylamino and N - methylphenylethylamine, pyridyloxy group (Peregrina group may be substituted by methyl group, ethyl, trifloromethyl, methoxy, ethoxy, isopropoxy or triptoreline, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl), group pyridyloxy, pyridylthio, pyridylsulfonyl and piperidyl,

or

X represents pyridyloxy group which may contain one Deputy 13described below

Here Deputy13represents a group selected from the group comprising methyl, isopropyl, methoxy, ethoxy, isopropoxy, 2,2,3,3-tetrafluoropropoxy and benzyloxy, aricioglu containing one or two carbon atoms, alkylsulfonyl group containing one or two carbon atoms, benzyl group, phenyl group (the phenyl group may be substituted by methyl group, ethyl, trifloromethyl, methoxy, ethoxy or isopropoxy, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl), group phenoxy, phenyl which the oxygen,

their pharmacologically acceptable salt or their pharmacologically acceptable esters; and

(51) derivative amidocarbonyl acid, where

R1represents a hydrogen atom;

R2represents an ethylene group;

R3represents a hydrogen atom;

R4represents a hydrogen atom;

Z represents a methylene group;

W represents fenoxaprop, which may contain one Deputy6as described below, on the phenyl group,

here Deputy6represents a group selected from the group comprising methyl, ethyl, isopropyl, tert-butyl, trifluoromethyl, methoxy, triptoreline, and fluorine atoms and chlorine;

X represents biphenylyl group (the substituents on each phenyl group may be the same or different and one of them may be substituted by a methyl group, trifloromethyl, hydroxyl, methoxy or hydroxymethyl, a fluorine atom, a chlorine atom or a formyl group, carboxyl, nitrogroup, dimethylaminopropoxy or N,N-dimethylaminomethylene group), pyridylamino group (Peregrina group may be substituted by one Deputy, selected from the group of methyl, ethyl, trifloromethyl, diethylaminopropyl) or phenyl group (the phenyl group may be substituted by one Deputy, selected from the group of methyl, ethyl, trifloromethyl, methoxy, ethoxy, isopropoxy, fluorine atom, chlorine atom and nitro group, and dimethylaminopropyl); and

Y represents an oxygen atom,

their pharmacologically acceptable salts and their pharmaceutically acceptable esters.

Moreover, it is preferable compound containing the following:

(52) derivative amidocarbonyl acid, where

R1represents a hydrogen atom or a straight or branched alkyl group comprising from 1 to 6 carbon atoms;

R2is a straight or branched alkylenes group containing from 1 to 6 carbon atoms;

R3represents (i) hydrogen atom, (ii) straight or branched alkyl group comprising from 1 to 6 carbon atoms, (iii) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (iv) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (v) halogen atom, (vi) a nitro-group, (vii) straight or branched dialkylamino, in which each alkyl group may be the same or different and contain from 1 to 4 carbon atoms, (viii) aryl group containing from 6 to 10 atoms ug is from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents described later on the aryl group;

R4represents a hydrogen atom or a straight or branched alkyl group comprising from 1 to 6 carbon atoms;

Z is a straight or branched alkylenes group containing from 1 to 4 carbon atoms;

W represents a group of ethyl, propyl, butyl, penttila, methoxy, ethoxy, propoxy, isopropoxy, methylthio, ethylthio, propylthio, isopropylthio, phenoxy, 4-methylphenoxy, 4-ethylenoxy, 4-isopropylphenoxy, 4-methoxyphenoxy, 4-chlorophenoxy, phenylthio, benzyl, Venetia, 3-phenylpropyl or 4-phenylbutyl;

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents described hereinafter, or mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents described below

here the Deputy represents a group selected from the group comprising (i) a straight or branched alkyl group comprising from 1 to 6 carbon atoms, (ii) straight or branched halogenides the aliphatic alloctype, comprising from 1 to 5 carbon atoms, (v) straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, (vi) straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, (vii) aralkylated comprising from 7 to 12 carbon atoms, (viii) straight or branched allylthiourea comprising from 1 to 4 carbon atoms, (ix) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (x) halogen atom, (xi) a nitro-group, (xii) straight or branched dialkylamino, in which each alkyl group may be the same or different having 1 to 4 carbon atoms, (xiii) Uralkaliy group containing from 7 to 12 carbon atoms, (XIV) aryl group containing from 6 to 10 carbon atoms (the aryl group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms, straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, a halogen atom or a straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms), (xv) alloctype comprising from 6 to 10 carbon atoms (ariline is a straight or branched halogenated alkyl group, comprising from 1 to 4 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, a halogen atom or a straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms), (xvi) killigrew comprising from 6 to 10 carbon atoms (the aryl group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms, straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, a halogen atom or a straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms), (xvii) arylsulfonyl group containing from 6 to 10 carbon atoms (the aryl group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms, straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, a halogen atom or a straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms), (xviii) arylsulfonamides, containing from 6 to 10 atoms of atomov carbon straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, straight or branched alkoxygroup comprising from 1 to 4 carbon atoms, a halogen atom or a straight or branched alkylenedioxy comprising from 1 to 4 carbon atoms, and the nitrogen atom of the amino group may be substituted by straight or branched alkyl group comprising from 1 to 6 carbon atoms), (xix) mono - or decillions 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xx) mono - or decillions 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xxi) mono - or decillions 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (xxii) mono - or decillions 5-10-membered heteroarylboronic group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom and (xxiii) mono - or decillions 5-10-membered heteroatomcontaining containing from 1 to 4 heteroatoms selected from g is a branched alkyl group, comprising from 1 to 6 carbon atoms); and

Y represents a single bond, an oxygen atom, a sulfur atom or a group of the formula >N-R5(where R5represents a hydrogen atom, a straight or branched alkyl group comprising from 1 to 6 carbon atoms, a straight or branched aliphatic acyl group containing from 1 to 8 carbon atoms, or an aromatic acyl group containing from 7 to 11 carbon atoms),

their pharmacologically acceptable salts or their pharmaceutically acceptable esters.

Illustrative compounds amidocarbonyl acid of formula I, their pharmacologically acceptable salts or their pharmaceutically acceptable esters of the present invention are illustrated in tables 1-155.

In this case, the tables 1-155 the following abbreviations are used.

Ex.No.Comp: number of illustrative compounds AC: acetyl, Bu: butyl, tBu: tert-butyl, Bimid: benzimidazolyl, Boxa: benzoxazolyl, Bthiz: benzothiazolyl, Bz: benzyl, Dea: diethylamine, Dma: dimethylamino, Dmam: dimethylaminomethyl, Et: ethyl. Fur: furyl. Hex: hexyl, Imid: imidazolyl, Ind: indolyl, Isox: isoxazolyl, MdO: methylendioxy, Me: methyl. Mor: morpholino, Np: naphthyl, Oxa: oxazolyl. Pen: pencil, Ph: phenyl, Pip: piperidinyl, PPr: 3-phenylpro the sludge, iQuin: ethanolic, Tfp: 2,2,3,3-tetrafluoropropyl, Thi: thienyl, Thiz: thiazolyl, di: di, tri: three, penta: Penta.

It should be noted that the compounds of table 1-145 have the following formula (Ia) and compounds of tables 146-155 have the following formula (Ib).

< / BR>
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Derivatives amidocarbonyl acid of the formula (I) according to the present invention, their pharmaceutically acceptable salts or their pharmaceutically acceptable esters can easily be obtained in accordance with the following method A (see diagram at the end of the description).

Method AND

Stage A1

In stage A1 obtain the connection formula (III) by acylation of compounds of formula (II).

This reaction, which reaction obtain the amide bond, is widely known in the chemistry of organic syntheses and usually preferably carried out in the presence of a solvent.

The solvent used here is not particularly limited, while it has no adverse effect, and includes, for example, inert solvents, preferably halogenated hydrocarbons such as dichloromethane and chloroform; esters such as ethyl acetate; ethers, such as tetrahydrofuran and dioxane; and amides, such as N,N-dimethylacetamide and N, N-dimethylformamide.

Alternatively, this reaction is completed by reacting the carboxylic acid used in this reaction, or a salt thereof with a lower alkyl ether of Harborview acid, such as ethylchloride and isobutylparaben, in the presence of a tertiary amine such as triethylamine and N - methylmorpholine, with a mixture of carboxylic acid anhydride, or by reacting the carboxylic acid used in this reaction, or a salt thereof, with N-hydroxysuccinimide, N - hydroxybenzotriazole or p-NITROPHENOL in the presence of carbodiimides, such as N,N-dicyclohexylcarbodiimide, to obtain the corresponding activated ester, and then by condensation of these compounds with amines.

obanno not limited to, while this has no adverse effect on the reaction and includes, for example, inert solvents, preferably halogenated hydrocarbons such as dichloromethane and chloroform; simple, such as tetrahydrofuran and dioxane; and aromatic hydrocarbons such as benzene and toluene.

As a further alternative, the connection is produced by interaction of the acid used in this reaction, or a salt thereof, with a halogenation agent, preferably pentachloride phosphorus, oxalylamino or thionyl chloride, to obtain the corresponding gelegenheid and then by the interaction of gelegenheid with amines as described above.

The reaction is usually carried out preferably in the presence of a solvent. The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes, for example, inert solvents, preferably halogenated hydrocarbons such as dichloromethane; ethers, such as tetrahydrofuran and dioxane; and aromatic hydrocarbons such as benzene and toluene.

The reaction is carried out at a temperature of from -20oC to 100oC, site from reagent the reaction temperature and solvent, it is usually from 30 minutes to 24 hours, preferably from 1 hour to 16 hours.

Stage A2

In stage A2 gain derived phenylalkylamines acid of the formula (I) and this stage is carried out by removal of the ether the residue from the compounds of formula (III).

This stage ends by hydrolysis with base in the presence of a solvent.

In the present reaction solvent used is not particularly limited, while it has no adverse effect on the reaction, and preferably includes, for example, ethers such as diethyl ether, tetrahydrofuran and dioxane; alcohols, such as methanol, ethanol and methoxyethanol; water; or a mixture of these solvents.

The base used in the reaction include, for example, hydroxides of alkali metals such as lithium hydroxide, sodium hydroxide and potassium hydroxide; and carbonates of alkali metals such as lithium carbonate, sodium carbonate and potassium carbonate; the preferred hydroxides of alkali metals.

The reaction temperature varies depending on the solvent and the base, but is 0oC to 140oC, preferably between 10oorites, the base and the reaction temperature, it is usually from 10 minutes to 24 hours, preferably from 30 minutes to 16 hours.

Alternatively, when the ester residue is a group, tert-butyl, group diphenylmethyl or group p-methoxybenzyl, this stage is carried out by reacting the ester with an organic acid such as formic acid, acetic acid, triperoxonane acid, methanesulfonate acid, benzolsulfonat acid, p-toluensulfonate acid and triftormetilfullerenov acid or with a mineral acid, such as hydrochloric acid and sulfuric acid, preferably triperoxonane acid or hydrochloric acid in the presence or absence of solvent.

When this reaction is used, the solvent, the solvent is not particularly limited, while it has no adverse effect on the reaction, and includes, for example, hydrocarbons, such as benzene, toluene, xylene, hexane and heptane; halogenoalkane hydrocarbons, such as chloroform, methylene chloride and carbon tetrachloride; ethers, such as diethyl ether, tetrahydrofuran and dioxane; alcohols such as methanol and ethanol; amides, such is and ethyl acetate; water; or a mixture of these solvents; preferred esters.

Although the reaction temperature varies depending on the acid used, it ranges from -10oC to 120oC, preferably from 0oC to 100oC.

Although the reaction time varies depending on the acid used and the reaction temperature, it is usually from 10 minutes to 24 hours, preferably from 30 minutes to 16 hours.

As an additional alternative, this stage ends by conducting catalytic reactions gidrogenizirovanii the compounds of formula (III) in the case where the ester residue is aracelio group such as a benzyl group or a group of diphenylmethyl. The catalyst used here includes, for example, palladium on carbon, palladium on charcoal, platinum oxide and platinum black, the preferred palladium on carbon.

The reaction is usually carried out preferably in the presence of a solvent. The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes, for example, hydrocarbons, such as benzene, toluene, xylene, Gex, the such as diethyl ether, tetrahydrofuran and dioxane; alcohols, such as methanol, ethanol and isopropanol; amides, such as N,N-dimethylformamide, N,N-dimethylacetamide and triamide of hexamethylphosphoric; carboxylic acids such as formic acid and acetic acid; or a mixture of these solvents; the preferred alcohols.

The reaction temperature is from 10oC to 140oC, preferably from 20oC to 120oC.

The reaction time varies depending on the reagent, reaction temperature and solvent, and is usually from 30 minutes to 3 days, preferably from 1 hour to 24 hours.

As another alternative, in the case when W1is a primary or secondary amino group protected by a conventional protective groups such as tert-butoxycarbonyl, after completion of the reaction remove the protection can be carried out in accordance with known methods, for example by reacting a protected amino compounds with acid, such as hydrochloric acid, at room temperature for from 30 minutes to 2 hours.

In the formula (II) method A, the compound (IIa) in which R1contains a hydrogen atom, can be policenew stage B1 in the method To obtain the compound of formula (VI) and the compound obtained by the interaction of the compounds of formula (IV) with the compound of the formula (V).

In the case when U is a hydroxyl group, the reaction is carried out in accordance with conventional Mitsunobu reaction [O. Mitsunobu, Synthesis, page 1, (1981)].

The reaction is usually carried out by reacting the azo compounds with phosphine in the presence of a solvent. As the azo compounds of reagent use C1-C4alkylsalicylate, such as diethylazodicarboxylate, and azodicarboxamide, such as 1,1'-(azodicarbon)dipiperidino. As phosphines use triarylphosphine, such as triphenylphosphine, and three(C1-C4alkyl)phosphines, such as tributylphosphine.

The reaction is usually carried out preferably in the presence of a solvent. The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes, for example, hydrocarbons, such as benzene, toluene, xylene, hexane and heptane; halogenated hydrocarbons such as chloroform, methylene chloride, carbon tetrachloride and 1,2-dichloroethane; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N - dimethylformamide, N,N-dimethylacetamide and triamide of hexamethylphosphoric; or a mixture of these solvents; the preferred hydrocarbons, halogen 20oC to 80oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 1 hour to 3 days, preferably from 5 hours to 2 days.

When U represents a halogen atom or a group of the formula-O-SO2-R6(where R6has the same meaning as defined above), the reaction is carried out in an inert solvent in the presence of a base.

The basis used here preferably includes carbonates of alkali metals such as sodium carbonate and potassium carbonate; hydrides of alkali metals, such as sodium hydride, potassium hydride and lithium hydride; alkoxides of alkali metals such as sodium methoxide, ethoxide sodium tert-piperonyl potassium and lithium methoxide; alkali lithium such as butyl lithium and methyl lithium; lithium amides such as diethylamid lithium, diisopropylamide lithium bis(trimethylsilyl)amide Letitia; bicarbonates of alkali metals such as sodium bicarbonate and potassium bicarbonate; and tertiary organic amines such as 1,5-diazabicyclo[4.3.0]non-5-ene, 1,8-diazabicyclo[5.4.0]undec-7-ene and N, N-diisopropylethylamine; more preferred carbonates of alkaline metal is th here especially not limited, as it has no adverse effect on this reaction, and includes hydrocarbons, such as benzene and toluene; ethers such as tetrahydrofuran and dioxane; alcohols, such as methanol, ethanol and tert-butanol; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and N-methylpyrrolidone; ketones, such as acetone and 2-butanone; NITRILES, such as acetonitrile; sulfoxidov, such as dimethyl sulfoxide; or a mixture thereof; the preferred esters, amides, ketones or sulfoxidov.

When this reaction is carried out in the presence of a catalyst phase transfer, such as iodide of benzyltriethylammonium and tetrabutylammonium iodide, hydroxides of alkali metals such as sodium hydroxide and potassium hydroxide, are used as the base, and the reaction is carried out in a solvent, which contains a two-layer system of water and a halogenated hydrocarbon such as methylene chloride and chloroform.

The reaction temperature is from -10oC to 120oC, preferably between 10oC to 100oC.

Although the reaction time varies depending on the reagent and reaction temperature, it is usually on the giving of the formula (VII) and it is conducted by removing hydroxyamino group, such as the group 2-tetrahydropyranyl, from compounds of formula (VI).

This reaction is carried out by the same method as the method of removing protection from acid, described in stage A2 method A.

Stage B3

In stage B3 obtain the connection formula (VIII) and it is conducted by converting the hydroxyl group of the compounds of formula (VII) halogen atom, or a group of the formula-O-SO2-R6(where R6has the same meaning as defined above).

Halogenoalkane carried out by reacting compound (VII) with a halogen acid, such as hydrochloric acid and bromatologia acid; guidami organic acids, such as thionyl chloride, thienylboronic, trichloride phosphorus, tribromide phosphorus, pentachloride phosphorus oxychloride and phosphorus; the reagent Vilsmaier, such as N,N-dimethylmorpholine and N, N-DIMETHYLPROPANE; or halogenated reagents containing phosphorus compounds such as triphenylphosphine and carbon tetrachloride or tetrabromide carbon, and dichlorophenylphosphine and debromination, in an inert solvent or without solvent.

The solvent used here is not particularly limited, until it has come, toluene, xylene, hexane and heptane; halogenated hydrocarbons such as chloroform, methylene chloride, carbon tetrachloride and 1,2-dichloroethane; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and hexamethylphosphoric triamide; or a mixture thereof; the preferred hydrocarbons, halogenated hydrocarbons or ethers.

The reaction temperature is from -50oC to 150oC, preferably from 0oC to 80oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 30 minutes to 3 days, preferably from 1 hour to 24 hours.

The sulfating reaction is conducted by reacting compound (VII) with a reagent of formula R6-SO2-U2or (R6-SO2)2(where R6has the same meaning as defined above, and U2represents a halogen atom (preferably chlorine atom) in an inert solvent in the presence of a base.

The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes, for example, hloroform, methylene chloride, carbon tetrachloride and 1,2-dichloroethane; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and hexamethylphosphoric triamide; nitrogen-containing aromatic compounds such as pyridine and kallidin; or mixtures thereof; preferred halogenated hydrocarbons or nitrogen-containing aromatic compounds.

The basis used here, includes the carbonates of alkali metals such as sodium carbonate and potassium carbonate; bicarbonates of alkali metals such as sodium bicarbonate and potassium bicarbonate; and tertiary organic amines, such as N-dimethylmorpholine, N,N-diisopropylethylamine 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene; preferred tertiary organic amines.

The reaction temperature is from -70oC to 100oC, preferably from 0oC to 80oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 30 minutes to 48 hours, preferably from 1 hour to 16 hours.

Stage B4

In stage B4 obtain compound of formula (IX) and spend pkotory defined above) of the compounds of formula (VIII) of the azide group.

This reaction is performed by reacting metal azide such as sodium azide, or an organic azide, such as tetrabutylammonium azide, in an inert solvent.

The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes, for example, hydrocarbons, such as benzene, toluene, xylene, hexane and heptane; halogenated hydrocarbons such as chloroform, methylene chloride, carbon tetrachloride and 1,2-dichloroethane; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N - dimethylformamide, N,N-dimethylacetamide and hexamethylphosphoric triamide; or a mixture thereof; the preferred esters or amides.

The reaction temperature is from 0oC to 150oC, preferably from 20oC to 100oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 1 hour to 3 days, preferably from 1 hour to 24 hours.

Stage B5

In stage B5 obtain compound of formula (IIa) and it is conducted by converting the azide group of the compounds of formula (IX) amino group.

The Population Raney, catalysis of Lindlar and the like as a catalyst or restore using triphenylphosphine, and the like in an inert solvent.

The solvent used here is not particularly limited, while it has no adverse effect on this reaction and includes, for example, hydrocarbons, such as benzene, toluene, xylene, hexane and heptane; alcohols such as methanol and ethanol; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and hexamethylphosphoric triamide; or a mixture thereof; the preferred alcohols or ethers.

The reaction temperature is from 0oC to 150oC, preferably from 20oC to 100oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 1 hour to 3 days, preferably from 1 hour to 24 hours.

Method

Stage C1

In stage C1 receives the connection formulas (XI) and it is conducted by reacting the compounds of formula (X) with the compound of the formula (V).

This stage is conducted by the same method described in stage B1 method Century.

Cadinene formula (XI).

When the protective group R7or R8represents a group which can be removed by catalytic reduction, such as kalkilya group and aracelikarsaalyna group, or a group that can be removed using an acid, such as triticina group and tert-butoxycarbonyl group, the reaction of removing the protective group is carried out by the same method described in stage A2 in method A.

When the protective group R7or R8represents an aliphatic acyl group such as formyl and the TRIFLUOROACETYL protective group is removed in basic terms.

The basis used here, includes the hydroxides of alkali metals such as sodium hydroxide, potassium hydroxide and lithium hydroxide; and carbonates of alkali metals such as sodium carbonate and potassium carbonate; the preferred hydroxides of alkali metals.

This reaction is preferably carried out in an inert solvent, for example alcohols, such as methanol and ethanol; water; ethers such as tetrahydrofuran and dioxane; and mixtures; more preferred alcohols.

The reaction temperature is from 0oC to 100oC, site is Ty from reagent the reaction temperature and solvent, it is usually from 30 minutes to 24 hours, preferably from 1 hour to 16 hours.

In the case when R7together with R8represents aminosidine group and it is falorni group, the protective group can be removed by treatment with hydrazine or primary amines.

The hydrazines used here include, for example, hydrazine, methylhydrazine and phenyl, the preferred hydrazine. The primary amines used here include methylamine, ethylamine, Propylamine, butylamine, isobutylamine, pentylamine and hexylamine, preferred Propylamine or butylamine.

This reaction is carried out in an inert solvent, for example alcohols, such as methanol and ethanol; ethers such as tetrahydrofuran and dioxane; halogenated hydrocarbons such as methylene chloride and chloroform; and preferably used mixtures thereof. The use of alcohols is preferred.

The reaction temperature is from 0oC to 100oC, preferably between 10oC to 80oC.

Although the reaction time varies depending on the reagent, the reaction temperature is ormula (II) method And connection in which R1represents an alkyl group or aracelio group can also be obtained in accordance with method D or method that is

Method D (see diagram at the end of the description)

Stage D1

In stage D1 receive compound of formula (IIb) and it is conducted by reacting the compounds of formula (VIII) with an amine of formula (XII).

This reaction is carried out in an inert solvent in the presence or absence of a base.

The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes, for example, hydrocarbons, such as benzene, toluene, xylene, hexane and heptane; alcohols such as methanol and ethanol; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and triamide of hexamethylphosphoric; or mixtures thereof; preferred esters or amides.

The basis used here, includes the carbonates of alkali metals such as sodium carbonate and potassium carbonate; bicarbonates of alkali metals such as sodium bicarbonate and potassium bicarbonate; and tertiary organic amines, such as triethylamine, T-methylmorpholine, N,N - Diisopropylamine is whether tertiary organic amines.

The reaction temperature is from 0oC to 150oC, preferably from 20oC to 100oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 1 hour to 3 days, preferably 1 hour to 24 hours.

Method E (see diagram at the end of the description)

Stage E1

In stage E1 receive the compound of formula (IIb) and it is conducted by reacting the compounds of formula (IIa) with a carbonyl compound of the formula (XIII).

This reaction is carried out in an inert solvent under reducing conditions, using a metal hydride, such as Bergerac sodium and cyanoborohydride sodium, or under conditions of catalytic reduction using palladium on carbon or Nickel of Renee as a catalyst.

The solvent used here is not particularly limited, while it has no adverse effect on this reaction, and includes hydrocarbons, such as benzene, toluene, xylene, hexane and heptane; alcohols such as methanol and ethanol; ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and triamide Gex is from 0oC to 150oC, preferably from 20oC to 100oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 1 hour to 3 days, preferably 1 hour to 24 hours.

In the formula (III) method A, the compound (IIIa) in which W represents alloctype, heterokaryosis, aricioglu or heterogroup can also be obtained in accordance with the method of F.

Method F (see diagram at the end of the description)

The F1 stage

In stage F1 method F receive the connection formulas (IIIa) and a compound obtained by interaction of the compounds of formula (XIV) with the compound of the formula (XV).

This stage is conducted by the same method described in stage B1 method Century.

In the formula (XI) method With the compound (XIa) in which W represents alloctype, heteroaryl group, aricioglu or heterogroup can be obtained in accordance with the method of G.

Method G (see diagram at the end of the description)

Stage G1

In the G1 phase of the method of G receive the compound of formula (XIa) and the connection is produced by the interaction of the compounds of formula (XVI) with the compound of the formula (XV).

Method H (see diagram at the end of the description)

Stage H1

In stage H1 method H obtain the connection formula (XIX) and the connection is produced by the interaction of the compounds of formula (XVII) with the compound of the formula (XVIII).

This reaction is performed by reacting compounds in an inert solvent in the presence of a base.

The basis used here preferably includes hydrides of alkali metals, such as sodium hydride, potassium hydride and lithium hydride; alkoxides of alkali metals such as sodium methoxide, ethoxide sodium tert-piperonyl potassium and lithium methoxide; alkali lithium such as butyl lithium and methyl lithium; lithium amides such as diethylamid lithium, diisopropylamide lithium bis(trimethylsilyl)amide lithium; or tertiary organic amines, such as 1, 5-diazabicyclo[4.3.0] non-5-ene and 1,8 - diazabicyclo[5.4.0]undec-7-ene; more preferred hydrides of alkali metals, alkoxides of alkali metals or lithium amides.

The inert solvent used herein is not particularly limited, while it has no adverse effect on this reaction, and s, such as methanol, ethanol and tert-butanol; amides such as N,N - dimethylformamide, N,N-dimethylacetamide and N-methylpyrrolidone; ketones, such as acetone and 2-butanone; NITRILES, such as acetonitrile; sulfoxidov, such as dimethyl sulfoxide; and mixtures thereof; preferred ethers, amides, ketones or sulfoxidov.

When this reaction is carried out in the presence of a catalyst phase transfer, such as iodide of benzyltriethylammonium and tetrabutylammonium iodide, the reaction is carried out in a solvent, which contains a two-layer system of water and a halogenated hydrocarbon such as methylene chloride and chloroform, using hydroxides of alkali metals such as sodium hydroxide and potassium hydroxide as the base.

The reaction temperature is from -10oC to 120oC, preferably between 10oC to 100oC.

Although the reaction time varies depending on the reagent and reaction temperature, it is usually from 30 minutes to 48 hours, preferably 1 hour to 16 hours.

Stage H2

In stage H2 gain derived phenylalkylamines acid of the formula (Ia) and it is conducted by removing residual ether proizvodila in this stage is completed by using the same method, described in stage A2 method A.

Stage decarboxylation ends by heating the derivative of malonic acid, obtained by the removal of essential residues of the compounds of formula (XIX) in the presence of a solvent.

The solvent used here is not particularly limited, while it has no adverse effect on this reaction and includes, for example, hydrocarbons, such as benzene, toluene, xylene and heptane; halogenated hydrocarbons such as chloroform and carbon tetrachloride; ethers, such as tetrahydrofuran and dioxane; alcohols, such as ethanol, propanol, methoxyethanol and ethylene glycol; amides such as N,N-dimethylformamide, N,N-dimethylacetamide and triamide of hexamethylphosphoric; and mixtures thereof; hydrocarbons or alcohols.

The reaction temperature is from 60oC to 180oC, preferably from 80oC to 150oC.

Although the reaction time varies depending on the reagent, reaction temperature and solvent, it is usually from 30 minutes to 2 days, preferably verse 1 hour to 24 hours.

In the formula (I) of the method And the compound (Ib) in which W represents alkylamino, dialkylamino is at the end of the description)

Stage I1

In stage I1 obtain the connection formula (IIIc) and it is carried out by alkylation or aralkylamines the compounds of formula (IIIb).

This reaction is carried out by the same method described in stage B1 of the method In the case when alkylhalogenide, aralkylated, alkylsulfonate or aralkylamines used as alkylating reagents.

When the alkylation is reducing and it is done with the use of carbonyl compounds, it is done by the same method described in stage E1 of the method that is

Stage I2

In stage 12 receives the compound of formula (Ib) and is carried out by removal of the ether the residue of the compounds of formula (IIIc).

This stage is conducted by the same method described in stage A2 method A.

The desired compound obtained in each of the stages described above can be purified, if necessary, by conventional methods such as column chromatography, recrystallization and presidenial after the reaction. For example, the reaction mixture respectively neutralized to the reaction mixture, the solvent for the extraction and the solvent is distilled off from the extract. The precipitate obtained in this Abramova connection.

Derivatives amidocarbonyl acid of formula I, their pharmacologically acceptable salts or their pharmaceutically acceptable esters have excellent results in reducing glucose, lipid-lowering, improved resistance to insulin, reduce inflammatory diseases, immune regulation, inhibition aldoses reductase, inhibition of 5-lipoxygenase, suppression of lipid peroxidation, activation of PPAR (activating receptor peroxisomal proliferation) and weakening osteoporosis and are useful as preventive and/or therapeutic agent (particularly a therapeutic agent for diabetes, hyperlipemia, obesity, reduced glucose tolerance, insulin resistance not-IGT, hypertension, fatty liver, diabetic complications (such as retinopathy, nephropathy, neurosis, cataracts, coronary disease, and the like), arteriosclerosis, diabetes, pregnancy, polycystic ovary syndrome, damage to cells in atherosclerosis and ischemic heart disease (for example brain damage caused by apoplexy); inflammatory diseases, such as epiphyseal osteomyelitis, pain, hyperthermia, rheumatic and the gastrointestinal ulcers, cancer, cachexia, autoimmune diseases and pancreatitis; osteoporosis; cataracts, things like that.

Derivatives amidocarbonyl acid of the formula (I) of the present invention, their pharmaceutically acceptable salts and esters administered in various forms. Introduction, in particular, is not limited and is determined depending on various kinds of forms of pharmaceutical compositions, age, sex and other conditions, the extent of disease of the patient, and the like. For example, the compound may be administered orally in the case of tablets, pills, powders, granules, syrups, solutions, suspensions, emulsions, granules and capsules. Meanwhile, in the case of injections, it is injected, single or in mixture with use of a solution adjuvant, such as glucose, amino acid, like that. Moreover, if necessary, it can be a single given intramuscularly, intracutaneously, subcutaneously or intraperitoneally. In the case of suppositories, it is introduced intrarectal. Oral administration is preferred. Various types of these pharmaceutical compositions can be obtained using known adjuvants used in known pharmaceutical formulations, such as excipients, binding ventureone substance agents, in accordance with conventional methods.

When this component is molded in the form of tablets, can be widely used media, well-known specialists in this field, including excipients, such as lactose, sucrose, sodium chloride, glucose, urea, starch, calcium carbonate, kaolin, crystalline cellulose and silicic acid; binders such as water, ethanol, propanol, single syrup, glucose solution, gelatin solution, carboxymethylcellulose, shellac, methylcellulose, potassium phosphate and polyvinylpyrrolidone; disintegrators such as dry starch, sodium alginate, agarose powder, powder of laminaran, sodium bicarbonate, calcium carbonate, the ether polyoxyethylenesorbitan aliphatic acid, sodium lauryl sulfate, monoglyceride of stearic acid, starch and lactose; agents that prevent disintegration, such as sucrose, stearic acid, cocoa butter and refined oil; agents that accelerate the absorption, such as Quaternary ammonium base and sodium lauryl sulfate; humectants such as glycerin and starch; adsorbents such as starch, lactose, kaolin, bentonite and colloidal silicic acid; and lubricants such as oceanclimate in the form of tablets, which is applied a covering film, for example a tablet covered with sugar, tablet coated with gelatin, small bowel tablet tablet film-coated, two-layer or multilayer tablet tablet.

When the present compound is formed in the form of pills, can be widely used media, well-known experts in this field and includes, for example, excipients such as glucose, lactose, starch, cacao butter, refined vegetable oil, kaolin and talc; binding agents, such as powder Arabian gum, powder tragakant, gelatin and ethanol; and disintegrators such as laminarinases agar. When the present compound is formed in the form of suppositories, can be widely used media, well-known experts in this field and includes, for example, polyethylene glycol, cacao butter, higher alcohols, esters of higher alcohols, gelatin and semi-synthetic glycerides.

When the present compound is formed as an injection, it is preferable that the solvent and suspendresume agents were sterile and isotonic with blood. When the present compound is formed in the form of solutions, emulsions and suspensions, can be used in all media, from outside the cell isostearoyl alcohol, polioksidony isostearoyl alcohol and polyoxyethylenesorbitan ester of aliphatic acid. By the way, in this case, the pharmaceutical compositions may contain a sufficient amount of NaCl, glucose, or glycerin to get isoosmotic solution. Further, these can also be added to conventional agents that enhance the solubilization, buffer and sedatives.

Moreover, if necessary, it may contain dyes, preservatives, flavoring agents, sweeteners and other pharmaceutical substances.

The amount of active ingredient contained in the abovementioned pharmaceutical preparations, in particular, is not limited and respectively selected from a wide range, and preferably, the content typically ranged from 1 to 70 mass% in all the compositions, more preferably from 1 to 30 mass%.

Although the dose may vary depending on symptoms, age, body weight, route of administration and pharmaceutical form of the drug, it is usually administered in amounts of 0.001 mg (preferably from 0.01 mg, more preferably 0.1 mg) as a lower limit and 2000 mg, preferably 200 mg, more preferably 20 mg) as an upper limit, the following examples reference examples, examples, experiments, and examples of the preparation are given hereinafter to illustrate the present invention and in no way limit the invention.

All of these1H-NMR spectra were determined in the indicated solvent, and chemical shifts are given in units of chemical shift relative to the internal standard tetramethylsilane (TMS), constants megatonnage interaction are given in Hertz (Hz).

(Example 1)

Ethyl 2-ethoxy-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 1-35)

Hydrazinehydrate (80%, 0,125 ml) was added to a solution of ethyl 2-ethoxy-3-[4-(2-fallimentare) phenyl] propionate (760 mg), which is the product of reference example 1, in methanol (5 ml) and the mixture was left to stand at room temperature for 1.5 hours. At the end of this time the reaction mixture was concentrated. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was dried over anhydrous sodium sulfate and concentrated by evaporation in vacuum to obtain derivatives.

Separately added carbonyldiimidazole (400 mg) to a suspension of 4-pyridine-2-eventing acid (400 mg) in Beso knogo solution. To this clear solution was added a solution of amine derivatives obtained as described above, in dichloromethane (5 ml) and the mixture was stirred at room temperature for 30 minutes. To the reaction mixture were added 4-pyridine-2-eventing acid (200 mg) and carbonyldiimidazole (170 mg). The mixture is then left to stand overnight, the reaction mixture was concentrated by evaporation in a vacuum. The residue was distributed between ethyl acetate and water and the layers were separated. The organic layer was dried over anhydrous magnesium sulfate and evaporated under reduced pressure. The residue was purified by chromatography on a column of silica gel using dichloromethane/methanol = 20/1 as eluent to obtain the connection specified in the header (135 mg) in the form of resin.

1H-NMR (270 MHz, CDCl3): ppm 1,08-of 1.29 (6H, m), 2,95 (2H, d, J=6.5 Hz), the 3.35 (1H, quintuplet, J= 7,0 Hz), 3,60 (1H, quintuplet, J=7,0 Hz), 3,83-4,30 (7H, m), 6,72 (1H, t, J=4.5 Hz), 6,86 (1H, t, J=8.5 Hz), 7,17 (2H, d, J=8.5 Hz), 7,25-7,40 (1H, m), 7,72 shed 8.01 (4H, m), 8,07 (2H, d, J=8.5 Hz), 8,70-8,80 (1H, m).

(Example 2)

Sodium 2-ethoxy-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy]phenyl]propionate (illustrative compound N 1-35)

To a solution of ethyl 2-ethoxy-3-[4-[2-(4-pyridine-2 - albenzaalbenza)ethoxy] phenyl] propionate (135 mg), which is p is at room temperature for 2 hours. At the end of this time the methanol was evaporated under reduced pressure and to the residue was added an aqueous solution of hydrochloric acid (1 N., of 0.55 ml) and ethyl acetate. An ethyl acetate layer was separated and dried over anhydrous magnesium sulfate and then concentrated under reduced pressure to give the desired compound (121 mg) in the form of resin.

An aqueous solution of 1 n sodium hydroxide (0,28 ml) was added to a solution of the desired product in methanol (3 ml) and the mixture was concentrated in vacuo to obtain the connection specified in the header (128 mg) as an amorphous solid product.

1H-NMR (270 MHz, deuterated dimethyl sulfoxide): 1,00 ppm (3H, t, J= 7,0 Hz) to 2.66 (2H, DD, J-9,0, of 14.0 Hz), is 2.88 (2H, DD, J=3,5, of 14.0 Hz), 3,42-3,70 (5H, m), 4,05 is 4.13 (1H, m), 6,83 (2H, d, J=8.5 Hz), 7,14 (2H, d, J= 8.5 Hz), 7,32-41 (1H, m), the 7.85-of 8.09 (4H, m), 8,17 (2H, d, J=8.5 Hz), 8,69 (1H, d, J=4.0 Hz), 8,80 (1H, t, J=5,5 Hz).

(Example 3)

Ethyl 2-(3-phenylpropyl)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl]propionate(ethyl ester of illustrative compounds N 9-35)

In the same way as described in example 1, the reaction was carried out using ethyl 2-(3-phenylpropyl)-3-[4-(2- fallimentare) phenyl] propionate (1.50 g), which is the product of reference example 2,4-pyridine-2-eventing acid (285 mg) and carbonadium the malls.1H-NMR (270 MHz, CDCl3): to 1.14 ppm (3H, t, J=7.0 Hz), 1,47-of 1.73 (4H, m), 2,50-2,70 (4H, m), 2,80 of 2.92 (1H, m) to 3.89 (2H, dt, J=5.0 and 5.0 Hz), Android 4.04 (2H, q, J= 7.0 Hz), is 4.15 (2H, t, J=5.0 Hz), to 6.67 (1H, t, J=5.0 Hz), at 6.84 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,10-7,20 (3H, m), 7,20-7,31 (3H, m), 7,73-7,79 (2H, m), of 7.90 (2H, d, J=8.5 Hz), 8,08 (2H, d, J-8.5 Hz), 8,71 (1H, d, J=5.0 Hz).

(Example 4)

2-(3-phenylpropyl)-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionic acid (illustrative compound N 9-35)

In the same way as described in example 2, ethyl 2-(3-phenylpropyl)-3-[4-[2-(4-pyridine - 2-albenzaalbenza)ethoxy]-phenyl]propionate (767 mg), which is the product of example 3 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 2.86 ml) and the reaction mixture was processed. The residue was led from a mixture of diisopropyl ether and ethyl acetate to obtain the connection specified in the header, (361 mg) as colorless crystals. So pl. 114-116oC.1H-NMR (270 MHz, CDCl3): ppm 1,50-1,79 (4H, m), 2.57 m is 2.75 (4H, m), 2,80-to 2.94 (1H, m), 3,85 (2H, q, J=5.5 Hz), 4,13-4,20 (2H, m), 6,69 (1H, t, J=5.5 Hz), 6,83 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,10-7,20 (3H, m), 7,22-to 7.32 (3H, m), 7,70-to 7.84 (4H, m), of 7.97 (2H, d, J=8.5 Hz), 8,67-8,71 (1H, m).

(Example 5)

Ethyl 2-(2-phenoxyethyl)-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 138-2)

Ka is stirred at room temperature for 30 minutes to obtain a transparent solution. To this solution was added a solution of ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(2-phenoxyethyl)propionate (476 mg), which is the product of reference example 3, in methylene chloride (5 ml) and the mixture was stirred at room temperature for 30 minutes and left overnight. At the end of this time the reaction mixture was concentrated and the residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated and dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel using dichloromethane/ethyl acetate = 1/1 as eluent, to obtain the compound indicated in heading (374 mg) in the form of resin.

1H-NMR (270 MHz, CDCl3): to 1.14 ppm (3H, t, J=7.0 Hz), 1,90-of 2.21 (2H, m), was 2.76-3,10 (3H, m), a 3.87-4,19 (8H, m), 6,65-6,69 (1H, m), PC 6.82-6.89 in (4H, m), 6,93 (1H, t, J= 7.5 Hz), 7,12 (2H, d, J=8.5 Hz), 7.23 percent-to 7.32 (3H, m), 7,76-7,83 (2H, m), of 7.90 (2H, d, J=8.5 Hz), of 8.09 (2H, d, J=8.5 Hz), 8,72 is 8.75 (1H, m).

(Example 6)

2-(2-Phenoxyethyl)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl] propionic acid (illustrative compound N 138-2)

An aqueous solution of potassium hydroxide (85%, of 0.13 g) was added to a solution of ethyl 2-(2-phenoxyethyl)-3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy] phenyl] propionate (350 mg) in ethanol (8 ml). CME is the making. To the residue was added an aqueous solution of hydrochloric acid (1 N., 2.0 ml) and ethyl acetate. An ethyl acetate layer was separated and dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to get the connection specified in the header (260 mg) as a foam mass.1H-NMR (270 MHz, CDCl3): ppm 1,93-2,22 (2H, m), 2,78-to 3.02 (3H, m), 3,86 (2H, dt, J=5.0 and 5.5 Hz), 4,00-4,08 (2H, m), 4,16-is 4.21 (2H, m), 6,65-6,69 (1H, m), 6,82-6,97 (5H, m), 7,12 (2H, d, J=8.5 Hz), 7,22-7,34 (3H, m), 7,72-a 7.85 (4H, m), of 7.97 (2H, d, J=8.5 Hz), 8,68-8,71 (1H, m).

An aqueous solution of sodium hydroxide (1 N., 0.51 ml) was added to a solution of the foam mass in ethanol (3 ml). The mixture was concentrated to obtain a solid product, which was washed with diethyl ether to obtain the connection specified in the header, (203 mg) as an amorphous solid product.

(Example 7)

Ethyl 2-phenoxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]-phenyl]propionate (ethyl ester of illustrative compounds N 6-35)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate (660 mg), which is the product of reference example 4, 4-pyridine-2-eventing acid (428 mg) and carbonyldiimidazole (418 mg) and the reaction mixture was treated with obtaining the connection specified in the header is), the 3.89 (2H, dt, J=5.0 and 5.5 Hz), 4,13-4,22 (4H, m), 4,74 (1H, DD, J= 5,5, 7,0 Hz), 6,63-6,69 (1H, m), at 6.84 (2H, d, J=9.0 Hz), 6.87 in (2H, d, J= 9.0 Hz), 6,94 (1H, t, J=7.5 Hz), 7,20-7,30 (5H, m), 7,75-7,80 (2H, m), of 7.90 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 8)

2 Phenoxy-3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy] -phenyl] propionic acid (illustrative compound No. 6-35)

In the same way as described in example 6, ethyl 2-phenoxy-3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy]phenyl]-propionate (327 mg), which is the product of example 7 were subjected to contact with an aqueous solution of potassium hydroxide (85%, 200 mg) and the reaction mixture was treated with obtaining the connection specified in the header (280 mg) as colorless crystals. So pl. 149-151oC.1H-NMR (270 MHz, CDCl3): ppm is 3.21 (2H, d, J=7,0 Hz), a 3.87 (2H, dt, J=5.0 and 5.5 Hz), 4,14-4,18 (2H, m), to 4.73 (1H, t, J=7.0 Hz), 6,84-6,94 (6H, m), 7,19-7,31 (5H, m), 7,75-7,80 (2H, m), 7,88 (2H, d, J=8.5 Hz), with 8.05 (2H, d, J=8,5 Hz), 8,71 (1H, d, J=4.5 Hz).

(Example 9)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridine-2 - albenzaalbenza) ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 7-35)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy) phenyl]-2-(4-isopropylphenoxy)propionate (13,52 g), which is the product of reference example 5,4-the current was led from diisopropyl ether to obtain compound, specified in the header (scored 8.38 g) as colorless crystals. So pl. 77-79oC.1H-NMR (270 MHz, CDCl3): ppm 1,14-1,25 (9H, m), 2,72-2,90 (1H, m), 3,12-3,19 (2H, m) to 3.89 (2H, dt, J=5.0 and 5.5 Hz), 4,11-4,22 (4H, m), 4,69 (1H, DD, J=5,5, 7.5 Hz), of 6.65 (1H, user.t) of 6.75 (2H, d, J= 8.5 Hz), 6,86 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,20-7,31 (3H, m), 7,76-7,81 (2H, m), 7,88 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,69 is 8.75 (1H, m).

(Example 10)

2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl]propionic acid (illustrative compound N 7-35)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate (scored 8.38 g), which is the product of example 9 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 30,32 ml) and the reaction mixture was treated with obtaining the connection specified in the header (of 7.95 g) in the form of a white powder. 1H-NMR (270 MHz, CDCl3): to 1.16 ppm (6H, d, J=7,0 Hz), 2,70-is 2.88 (1H, m), 3,19 (2H, d, J=6.0 Hz), 3,80-to 3.89 (2H, m), 4,11-4,18 (2H, m), of 4.77 (1H, t, J=6.0 Hz), 6,77-to 6.88 (5H, m), 7,07 (2H, d, J=8.5 Hz), 7,21 (2H, d, J= 8.5 Hz), 7,25-to 7.35 (1H, m), of 7.70 (1H, d, J=8.5 Hz), 7,75-7,86 (3H, m), 7,89 (2H, d, J=8.5 Hz), 8,70-8,77 (1H, m).

(Example 11)

Ethyl 2-butyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]-phenyl]propionate (ethyl ester of illustrative compounds N 4-35)

The reaction was carried out which is the product of reference example 6, 4-pyridine-2-eventing acid (996 mg) and carbonyldiimidazole (810 mg) and the reaction mixture was treated with obtaining the connection specified in the header (1.04 g) as a white powder. So pl. 112-115oC.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=6.5 Hz), of 1.16 (3H, t, J=7.0 Hz), of 1.20 to 1.37 (4H, m), 1,39 by 1.68 (2H, m), 2,35-2,63 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), with 3.89 (2H, t, J=5.0 Hz), 4,06 (2H, KB, J=7,0 Hz) to 4.15 (2H, t, J=5.0 Hz), 6,66 (1H, user.C) at 6.84 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,21-7,31 (1H, m), to 7.77-7,79 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 12)

2-butyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] -phenyl] propionic acid (illustrative compound N 4-35)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (0,92 g), which is the product of example 11 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.80 ml) and the reaction mixture was treated with obtaining the connection specified in the header (1.06 g) as a white powder. So pl. 137-139oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), 1,21-of 1.42 (4H, m), 1,45 is 1.70 (2H, m), 2.57 m) is 2.80 (1H, m), 2,70 (1H, DD, J=5.0 and 13.5 Hz), 2,87 (1H, DD, J=9,0, 13.5 Hz), 3,86 (2H, t, J=5.0 Hz), 4,17 (2H, t, J= 5.0 Hz), 6,77 (1H, user.C) 6,83 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7.23 percent-7,38 (1H, m), 7,72 to 7.75 (2H, m), 7,79 (2H, d, J=benzoylamine)ethoxy]phenyl]propionate(ethyl ester of illustrative compounds N 37-3)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-methyl-2-(3-phenylpropyl)propionate (796 mg), which is the product of reference example 7,4-pyridine-2-eventing acid (438 mg) and carbonyldiimidazole (428 mg) and the reaction mixture was treated with obtaining the connection specified in the header (285 mg) as a colourless oil.

1H-NMR (270 MHz, CDCl3): of 1.05 ppm (3H, s) of 1.24 (3H, t, J=7.0 Hz), 1,38 and 1.80 (4H, m), 2,56-to 2.65 (3H, m) to 2.94 (1H, d, J=13,0 Hz) to 3.89 (2H, dt, J=5.0 And 5.5 G), 4,07-4,18 (4H, m), of 6.65 (1H, user.C) to 6.80 (2H, d, J=8.5 Hz), of 6.99 (2H, d, J=8.5 Hz), 7,14-7,30 (6H, m), 7,75-7,79 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 14)

Sodium 2-methyl-2-(3-phenylpropyl)-3-[4-[2-(4- pyridine-2-yl-benzoylamine)ethoxy]phenyl]propionate (illustrative compound N 37-3)

In the same way as described in example 6, ethyl 2-methyl-2-(3-phenylpropyl)-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate (0,131 mg), which is the product of example 13 were subjected to contact with an aqueous solution of potassium hydroxide (85%, 0.24 g) and the reaction mixture was treated with. The residue was subjected to chromatography on a column of silica gel using dichloromethane/methanol = 20/1 as eluent to give the desired compound. Water Rastogi product. The solid product washed with diisopropyl ether to obtain the connection specified in the header (177 mg) as a white powder. So pl. 108-111oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm of 1.01 (3H, s), 1,15-of 1.85 (4H, m), 2,55-2,78 (3H, m), 3,03 (1H, d, J=13,0 Hz), 3,71-3,93 (2H, m), 4,13-to 4.38 (2H, m), 6,97 (2H, d, J=8.5 Hz), 7,21-of 7.69 (8H, m), 8,08-8,45 (6H, m), 8,86-8,98 (1H, m), which is 9.09 is 9.15 (1H, m).

(Example 15)

Ethyl 2-methyl-2-phenoxy-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 33-3)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-methyl-2-phenoxypropionate (760 mg), which is the product of reference example 8, 4-pyridine-2-eventing acid (460 mg) and carbonyldiimidazole (440 mg) and the reaction mixture was treated with obtaining the connection specified in the header (930 mg) in the form of syrup.

1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J=7.0 Hz), of 1.40 (3H, s), 3,11 (1H, d, J=14,0 Hz), 3,29 (1H, d, J=14,0 Hz) to 3.89 (2H, dt, J=5.0 and 5.5 Hz), 4,10-of 4.25 (2H, m), 4,18 (2H, q, J=7.0 Hz), of 6.71 (1H, user.C) 6,75-6,86 (4H, m), 6,97 (1H, t, J=7.0 Hz), 7,13-7,33 (5H, m), 7,74-to 7.84 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,71 (1H, d, J=5.0 Hz).

(Example 16)

2-Methyl-2-phenoxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionic acid (iridin-2-albenzaalbenza)ethoxy] -phenyl]propionate (930 mg), which is the product of example 15 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.60 ml) at 70oC and the reaction mixture was treated with obtaining the connection specified in the header (545 mg) as a white powder. So pl. 76-79oC.1H-NMR (270 MHz, CDCl3): of 1.44 ppm (3H, s) and 3.15 (1H, d, J=14,0 Hz), or 3.28 (1H, d, J=14,0 Hz), a 3.87 (2H, t, J=5.0 Hz), of 4.16 (2H, t, J= 5.0 Hz), to 6.75 (1H, user.C) at 6.84 (2H, d, J=8.5 Hz), 6,92 (2H, d, J=8.5 Hz), 6,97 (1H, t, J=7.0 Hz), 7,15-7,34 (5H, m), 7,70-7,88 (4H, m), of 7.97 (2H, d, J=8.5 Hz), 8,73 (1H, d, J=4.0 Hz).

(Example 17)

Ethyl 2-(4-isopropylphenoxy)-2-methyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 34-3)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(4-isopropylphenoxy)-2-methylpropionate (510 mg), which is the product of reference example 9, 4-pyridine-2 - eventing acid (279 mg) and carbonyldiimidazole (272 mg) and the reaction mixture was treated with obtaining the connection specified in the header (487 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (6H, d, J=7,0 Hz) of 1.23 (3H, t, J=7,0 Hz) to 1.37 (3H, s), and 2.83 (1H, septet, J=7.0 Hz), 3,10 (1H, d, J= 13.5 Hz), 3,26 (1H, d, J=13.5 Hz), 3,90 (2H, dt, J=5.0 and 5.0 Hz), 4,17 (2H, t, J= 5.0 Hz), is 4.21 (2H, kV, J=7,0 Hz), 6,69 (1H, user.t, J=5.0 Hz), , ,71-8,73 (1H, m).

(Example 18)

2-(4-Isopropylphenoxy)-2-methyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionic acid (illustrative compound N 34-3)

In the same way as described in example 6, ethyl 2-(4-isopropylphenoxy)-2-methyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (486 mg), which is the product of example 17 was subjected to contact with an aqueous solution of potassium hydroxide (85%, 0.17 g) and the reaction mixture was processed. The residue is washed with diisopropyl ether to obtain the connection specified in the header (335 mg) as a white powder. So pl. 141-143oC.

1H-NMR (270 MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz), USD 1.43 (3H, s) 2,84 (1H, septet, J-7.0 Hz) and 3.15 (1H, d, J=14,0 Hz) at 3.25 (1H, d, J=14,0 Hz), 3,83-3,93 (2H, m), 4,17 (2H, t, J=5.0 Hz), 6,70 (1H, user.t, J=6.0 Hz), 6,85 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J-8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7,27-7,33 (1H, m), 7,72-7,80 (2H, m), 7,83 (2H, d, J=8.5 Hz), 8,00 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 19)

Ethyl 2-butyl-2-methyl-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 30-3)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2 - aminoethoxy) phenyl]-2-butyl-2-methylpropionate (2,42 g), which is the product silo the Vali with the connection, specified in the header, (970 mg) as a white powder.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7,0 Hz) of 1.06 (3H, s), 1,12-of 1.46 (8H, m), 1.60-to or 1.77 (1H, m), 2.63 in (1H, d, J=13.5 Hz), 2,97 (1H, d, J= 13.5 Hz), 3,86-3,93 (2H, m), 4,07-4,18 (4H, m), of 6.68 (1H, user.t, J=5.0 Hz), PC 6.82 (2H, d, J= 8.5 Hz), 7,03 (2H, d, J=8.5 Hz), 7.24 to 7,31 (1H, m), 7,76-7,80 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,71-8,73 (1H, m).

(Example 20)

2-Butyl-2-methyl-3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy] -phenyl] propionic acid (illustrative compound N 30-3)

In the same way as described in example 6, ethyl 2-butyl-2-methyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] -phenyl]propionate (350 mg), which is the product of example 19 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and aqueous solution of potassium hydroxide (85%, 0.1 g) and the reaction mixture was processed. The residue was subjected to chromatography on a column of silica gel using dichloromethane/methanol = 19/1 as eluent, to obtain the solid product, which was washed with a mixture of diisopropyl ether and hexane to obtain the connection specified in the header (133 mg) as a white powder. So pl. of 105.5 - 107,5oC.1H-NMR (270 MHz, CDCl3): ppm of 0.91 (3H, t, J=7,0 Hz) of 1.09 (3H, s), of 1.20 to 1.48 (5H, m), 1,66-of 1.78 (1H, m) of 2.64 (1H, d, J 13.5 Hz), 3,00 (1H, d, J=13.5 Hz), 3,83-3,93 (2H, m), 4.09 to 4,18 (2H, m), 6,79-6,83 (1H,P> (Example 21)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-butylphosphonate (ethyl ether illustrative compounds N 4-15)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (666 mg), which is the product of reference example 6, biphenyl-4-carboxylic acid (450 mg) and carbonyldiimidazole (442 mg) and the reaction mixture was treated with obtaining the connection specified in the header (705 mg) as a yellow powder. So pl. 89-90oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J= 7.0 Hz), 1,22-of 1.32 (4H, m), 1,40 was 1.69 (2H, m), 2,53-2,63 (1H, m), 2,69 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J for 8.5, 13.5 Hz), with 3.89 (2H, q, J 5.0 Hz), 4,07 (2H, q, J=7,0 Hz) to 4.15 (2H, t, J=5.0 Hz), 6,63 (1H, t, J=5.0 Hz), 6,85 (2H, d, J= 8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,37 is 7.50 (3H, m), 7,60-to 7.68 (4H, m), 7,86 (2H, d, J=8,5 Hz).

(Example 22)

3-[4-[2-(Biphenyl-4-carbylamine)ethoxy] phenyl] -2-butyl-propionic acid (illustrative compound N 4-15)

In the same way as described in example 2, ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-butylphosphonate (450 mg), which is the product of example 21 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.00 ml) and the reaction mixture was treated with obtaining the connection specified in 43 (4H, m), 1,46-of 1.73 (2H, m), 2,58-of 2.66 (1H, m), of 2.72 (1H, DD, J=6,5, and 13.5 Hz), 2,89 (IH, DD, J=8,5, and 13.5 Hz), a 3.87 (2H, q, J=5.0 Hz), of 4.13 (2H, t, J= 5.0 Hz), of 6.71 (1H, t, J=5.0 Hz), at 6.84 (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,35-7,49 (3H, m), 7,58-of 7.70 (4H, m), a 7.85 (2H, d, J=8,5 Hz).

(Example 23)

Ethyl 2-butyl-3-[4-[2-(4' -methoxybiphenyl-4 - carbylamine)-ethoxy]phenyl] propionate(ethyl ester of illustrative compounds N 4-179)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (540 mg), which is the product of reference example 6, 4'-methoxybiphenyl-4-carboxylic acid (420 mg) and carbonyldiimidazole (370 mg) and the reaction mixture was treated with obtaining the connection specified in the header (486 mg) as a white powder. So pl. 121-123oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,21-to 1.38 (4H, m), 1,42 is 1.70 (2H, m), of 2.51-of 2.72 (2H, m), 2,80-2,92 (IH, m), 3,86 (3H, s), a 3.87-to 3.92 (2H, m), 4,07 (2H, q, J=7.0 Hz), 4,14 (2H, t, J=5.0 Hz), 6,62 (1H, t, J=5.5 Hz), at 6.84 (2H, d, J=8.5 Hz), 7,00 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,55 (2H, d, J=8.5 Hz), a 7.62 (2H, d, J=8.5 Hz), 7,83 (2H, d, J=8,5 Hz).

(Example 24)

2-Butyl-3-[4-[2-(4'-methoxybiphenyl-4-carbylamine)ethoxy]-phenyl]propionic acid (illustrative compound N 4-179)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(4'-methoxybiphenyl-4-carbonyl is a solution of sodium hydroxide (1 N., 4,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (350 mg) as a pale orange powder. So pl. KZT 166.5-168oC. 1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J= 7.0 Hz), 1,23-of 1.40 (4H, m), USD 1.43 - 1,71 (2H, m), 2.57 m-2,78 (2H, m), 2,85-of 2.97 (1H, m), 3,86 (3H, s), 3,82-are 3.90 (2H, m), of 4.13 (2H, t, J=5.0 Hz), 6,69 (1H, t, J= 5.5 Hz), 6,83 (2H, d, J=8.5 Hz), 6,98 (2H, d, J=8.5 Hz), 7,10 (2H, d, J= 8.5 Hz), 7,55 (2H, d, J=8.5 Hz), 7,60 (2H, d, J=8.5 Hz), 7,81 (2H, d, J= 8,5 Hz).

(Example 25)

Ethyl 2-butyl-3-[4-[2-(4'-hydroxybiphenyl-4-carbylamine)-ethoxy]phenyl] propionate(ethyl ester of illustrative compounds N 4-206)

To a suspension of 4'-hydroxybiphenyl-4-carboxylic acid (383 mg) in dichloromethane (10 ml) at room temperature was added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (359 mg) and 1 - hydroxybenzotriazole (287 mg). The mixture was stirred for 4 hours at room temperature. Then the reaction mixture was added a solution of ethyl 3-[4-(2-aminoethoxy)phenyl] -2-butylphosphonate (500 mg), which is the product of reference example 6, in dichloromethane (10 ml). The mixture was stirred at room temperature for 2 hours and then left overnight. At the end of this time the reaction mixture was concentrated by evaporation. The residue was distributed between ethyl acetate is m sodium bicarbonate solution and saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/ethyl acetate = 5/1, receiving of the connection specified in the header (270 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7,0 Hz) and 1.15 (3H, t, J=7.0 Hz), to 1.21 to 1.37 (4H, m), 1,40-1,70 (2H, m), 2,55-of 2.64 (1H, m), 2,68 (1H, DD, J= 6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,88 (2H, q, J=5.0 Hz), of 4.05 (2H, KB, J=7,0 Hz), 4,14 (2H, t, J=5.0 Hz), 6,36 (1H, user.C) of 6.65 (1H, t, J= 5.0 Hz), 6,83 (2H, d, J=8.5 Hz), 6,93 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J= 8.5 Hz), 7,49 (2H, d, J=8.5 Hz), 7,60 (2H, d, J=8.5 Hz), 7,82 (2H, d, J=8,5 Hz).

(Example 26)

2-Butyl-3-[4-[2-(4'-hydroxybiphenyl-4-carbylamine) ethoxy] -phenyl] propionic acid (illustrative compound N 4-206)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(4'-hydroxybiphenyl-4-carbylamine)ethoxy] -phenyl] propionate (260 mg), which is the product of example 25 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2,20 ml) and the reaction mixture was treated with obtaining the connection specified in the header (230 mg) as a white powder. So pl. 182-184oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm of 0.79 (3H, t, J=6.5 Hz), 1,15-1,30 (4H, m), 1,34-1,53 (25 Hz), 7,53 (2H, d, J=8.5 Hz), 7,63 (2H, d, J=8.5 Hz), 7,87 (2H, d, J= 8.5 Hz), 8,63 (1H, t, J=5.5 Hz), being 9.61 (1H, s).

(Example 27)

2-Butyl-3-[4-[2-(4'-formylphenyl-4-carbylamine)ethoxy] -phenyl] propionic acid (illustrative compound N 4-207)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(4'-dimethoxybiphenyl-4-carbylamine)-ethoxy] phenyl]propionate (1.88 g), which is the product of reference example 11 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 6,80 ml) and the reaction mixture was treated with obtaining 2-butyl-3-[4-[2-(4'- dimethoxybiphenyl-4-carbylamine)ethoxy]phenyl]-propionic acid (1.78 g) as a pale brown solid product.

To a solution of this compound (521 mg) in acetone (15 ml) was added water (0.17 ml) and then at room temperature was added amberlyst 15 (100 mg). The mixture was left to stand for 40 minutes. Amberlyst 15 was removed by filtration and the filtrate was concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/methanol = 20/1 with getting the connection specified in the header, (336 mg) as a white solid product. So pl. 122-124oC.1H-NMR (270 MHz, CDCl3): ppm to 0.88 (3H, t, J= 7.0 Hz), of 1.20 to 1.37 (4H, m), 1,40-to 1.59 (1H, m), 1,61-18.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7,69 (2H, d, J=8.5 Hz), 7,76 (2H, d, J= 8.5 Hz), 7,89 (2H, d, J=8.5 Hz), of 7.97 (2H, d, J=8.5 Hz), 10,08 (1H, s).

(Example 28)

2-Butyl-3-[4-[2-(4'-hydroxymethyluracil-4 - carbylamine)-ethoxy]phenyl] propionic acid (illustrative compound N 4-211)

To a solution of 2-butyl-3-[4-[2-(4'-formylphenyl-4 - carbylamine)ethoxy] phenyl] propionic acid (366 mg) in ethanol (10 ml) at room temperature was added sodium borohydride (95%, 34 mg). The mixture was stirred for 1.5 hours. At the end of this time the reaction mixture was added 50% acetic acid. The mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. To the residue was added diisopropyl ether to obtain the connection specified in the header (331 mg) as colorless crystals. So pl. 111-113oC1H-NMR (270 MHz, deuterated methanol): ppm to 0.88 (3H, t, J=7.0 Hz), 1,22-of 1.39 (4H, m), 1,40-of 1.65 (2H, m), 2,52-2,61 (1H, m) to 2.67 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8.0 a, and 13.5 Hz), 3,80 (2H, t, J=5.5 Hz), of 4.16 (2H, t, J=5,5 Hz), and 4.68 (2H, s), 6.87 in (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,46 (2H, d, J= 8.5 Hz), 7,63 (2H, d, J=8.5 Hz), of 7.70 (2H, d, J=8.5 Hz), of 7.90 (2H, d, J=about acid (illustrative compound N 4-208)

It triethylamine (0,56 ml), dimethylaminohydrolase (167 mg) and tetraisopropoxide titanium (0,59 ml) was added a suspension of 2-butyl-3-[4-[2-(4'-formylphenyl-4-carbylamine)ethoxy] -phenyl] propionic acid (474 mg) in ethanol (20 ml) at room temperature to obtain a transparent solution. To the solution was added sodium borohydride (60 mg) and the mixture was stirred in nitrogen atmosphere for 18 hours. At the end of this time the reaction mixture was added 50% acetic acid. This mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. To the residue was added diisopropyl ether to obtain the connection specified in the header (135 mg) as colorless crystals. So pl. 125 - 127oC.1H-NMR (400 MHz, deuterated methanol): ppm of 0.87 (3H, t, J= 6.5 Hz), 1,22-to 1.38 (4H, m), 1.41 to of 1.62 (2H, m), 2,50 at 2.59 (1H, m) to 2.66 (1H, DD, J=6,0, and 13.5 Hz), 2,82 (1H, DD, J=8,5, and 13.5 Hz), of 2.86 (6H, s), of 3.78 (2H, t, J=5.5 Hz), to 4.15 (2H, t, J=5,5 Hz) to 4.33 (2H, s), 6.87 in (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,60 (2H, d, J=8.5 Hz), 7,76 (2H, d, J=8.5 Hz), 7,81 (2H, d, J=8.5 Hz), to 7.93 (2H, d, J=8,5 Hz).

(Example 30]

2-Butyl-3-[4-[2-(4'-carbonium, which is described in example 2, ethyl 2-butyl-3-[4-[2-(4'-methoxycarbonylmethyl-4-carbylamine)-ethoxy] phenyl] propionate (243 mg), which is the product of reference example 12, was subjected to contact with an aqueous solution of sodium hydroxide (1 N. and 1.83 ml) and the reaction mixture was treated with obtaining the connection specified in the header (163 mg) as a white powder. So pl. 199-201oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm of 0.83 (3H, t, J=6.5 Hz), of 1.18 to 1.31 (4H, m), 1,37-of 1.52 (2H, m), 2.40 a - 2,50 (1H, m), 2,61 (1H, DD, J=6,0, and 13.5 Hz), 2,74 (IH, DD, J= 8,5, and 13.5 Hz), 3,66 (2H, t, J=5.5 Hz), 4,10 (2H, t, J=5.5 Hz), 6.87 in (2H, d, J= 8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), the 7.85 (2H, d, J=8.0 Hz), 7,87 (2H, d, J= 8.0 Hz), to 7.99 (2H, d, J=8.5 Hz), with 8.05 (2H, DD, J=2.5 and 8.5 Hz), 8,78 (1H, d, J=5,5 Hz).

(Example 31)

Ethyl 2-butyl-3-[4-[2-(3'-methoxybiphenyl-4-carbylamine)-ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-212)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2 - aminoethoxy) phenyl]-2-butylphosphonate (620 mg), which is the product of reference example 6, 3'-methoxybiphenyl-4-carboxylic acid (456 mg) and carbonyldiimidazole (389 mg) and the reaction mixture was treated with obtaining the connection specified in the header, (740 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3

(Example 32)

2-Butyl-3-[4-[2-(3'-methoxybiphenyl-4-carbylamine)ethoxy] -phenyl] propionic acid (illustrative compound N 4-212)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(3'-methoxybiphenyl-4-carbylamine)ethoxy]-phenyl]propionate (730 mg), which is the product of example 31 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 4,50 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (520 mg) as a white powder. So pl. 107-109oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), 1,21-to 1.38 (4H, m), 1,45 - 1,71 (2H, m), 2,58-2,67 (IH, m), 2,71 (1H, DD, J to 6.5 and 13.5 Hz), 2,90 (1H, DD, J=8,5, and 13.5 Hz), 3,83-3,90 (5H, m), of 4.13 (2H, t, J=5.0 Hz), of 6.71 (1H, t, J=5.0 Hz), 6,83 (2H, d, J=8.5 Hz), 6,93 (1H, DD, J=2.5 and 8.0 Hz), 7,10 (2H, d, J=8.5 Hz), 7,12 (1H, d, J=2.5 Hz), 7,18 (2H, d, J= 8.0 Hz), 7,37 (IH, t, J=8.0 Hz), to 7.64 (2H, d, J-8.5 Hz), the 7.85 (2H, d, J= 8,5 Hz).

(Example 33)

Ethyl 2-butyl-3-[4-[2-(3'-hydroxybiphenyl-4 - carbylamine)-ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 4-213)

The reaction was conducted in the same manner as described in example 25, using e is biphenyl-4-carboxylic acid (450 mg), which is the product of reference example 13, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (443 mg) and 1-hydroxybenzotriazole (354 mg) and the reaction mixture was treated with obtaining the connection specified in the header (291 mg) as a white powder. So pl. 76-77,5oC.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,21-of 1.36 (4H, m), 1,40 was 1.69 (2H, m), 2,52-to 2.65 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), with 3.89 (2H, q, J=5.0 Hz), 4,06 (2H, q, J=7,0 Hz), 4,14 (2H, t, J=5.0 Hz), 6,10 (1H, s) 6,70 (1H, t, J=5.0 Hz), 6,83 (2H, d, J=8.5 Hz), 6,83-6,91 (1H, m), was 7.08 (2H, d, J= 8.5 Hz), 7,09-7,16 (2H, m), 7,31 (1H, t, J=8.0 Hz), 7,58 (2H, d, J=8.5 Hz), 7,83 (2H, d, J=8,5 Hz).

(Example 34)

2-Butyl-3-[4-[2-(3'-hydroxybiphenyl-4-carbylamine)ethoxy]-phenyl]propionic acid (illustrative compound N 4-213)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(3'-hydroxybiphenyl-4-carbylamine)ethoxy] -phenyl] propionate (350 mg), which is the product of example 33 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2,85 ml) and the reaction mixture was treated with obtaining the connection specified in the header (290 mg) as a white powder. So pl. 98-100oC.1H-NMR (270 MHz, CDCl3): ppm 0,84-to 0.89 (3H, m), 1,21-of 1.40 (4H, m), 1,45 by 1.68 (2H, m), of 2.51-2,90 (3H, m), 3,80-3,88 (2H, m), 4,12-4,20 (2H, m,), 6,82-6,92 (4-[2-(3'- formylphenyl-4 - carbylamine)ethoxy] -phenyl] propionic acid (illustrative compound N 4-214)

In the same way as described in example 27 ethyl 2-butyl-3-[4-[2-(3'-dimethoxybiphenyl-4-carbylamine)-ethoxy] phenyl]propionate (1,46 g), which is the product of reference example 14 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5.40 ml) and the reaction mixture was treated with obtaining 2-butyl-3-[4-[2-(3'-dimethoxybiphenyl-4-carbylamine)ethoxy]phenyl]-propionic acid (1.39 g) as a syrup. This compound (365 mg) was entered into the reaction, and the reaction mixture was treated in the same way as described in example 27, with the receipt of the connection specified in the header (335 mg) as a yellowish brown solid product.1H-NMR (270 MHz, CDCl3): ppm to 0.88 (3H, t, J=6.5 Hz), 1.18 to to 1.38 (4H, m), 1,40-of 1.78 (2H, m), 2,61 of 2.68 (1H, m), 2,73 (1H, DD, J=6,5, and 13.5 Hz), of 2.92 (1H, DD, J= 8.0 a, and 13.5 Hz), with 3.89 (2H, q, J=5.0 Hz), is 4.15 (2H, t, J=5.0 Hz), 6,69 (1H, user. t), 6,85 (2H, d, J=8.5 Hz), 7,11 (2H, d, J=8.5 Hz), to 7.64 (1H, t, J 8.0 Hz), 7,69 (2H, d, J=8.5 Hz), 7,86-to $ 7.91 (2H, m), 7,89 (2H, d, J=8,5 Hz) to 8.12 (1H, s), 10,10 (1H, s).

(Example 36)

Sodium 2-butyl-3-[4-[2-(3'-hydroxymethyluracil-4-carbonyl-amino)ethoxy] phenyl]propionic acid (illustrative compound N 4-218)

To a suspension of sodium 2-butyl-3-[4-[2-(3'-methoxyethoxymethyl-4 - carbylamine)ethoxy] phenyl] -propionate (238 mg), which is the product of (4 N., 1.2 ml). The mixture was left to stand over night. At the end of this time the reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/methanol = 20/1-10/1, to obtain the free acid. The connection specified in the header (140 mg) as a yellowish brown solid product was obtained by reaction of the free acid with sodium hydroxide. So pl. 124-126oC.1H-NMR (270 MHz, deuterated methanol): ppm of 0.87 (3H, t, J=7.0 Hz), 1.18 to 1.39 in (4H, m), 1,44-to 1.63 (2H, m), 2,32-2,47 (1H, m), of 2.51 (1H, DD, J=7,0, and 13.5 Hz), 2,85 (1H, DD, J= 6,0, and 13.5 Hz), 3,76 (2H, t, J=5.5 Hz), 4,14 (2H, t, J=5,5 Hz), and 4.68 (2H, s), at 6.84 (2H, d, J=8.5 Hz), 7,12 (2H, d, J=8.5 Hz), was 7.36 (1H, d, J= 7.5 Hz), 7,44 (1H, t, J=7.5 Hz), 7,56 (1H, d, J=7.5 Hz), 7,66 (1H, s), 7,72 (2H, d, J=8.5 Hz), of 7.90 (2H, d, J=8,5 Hz).

(Example 37)

Ethyl 2-butyl-3-[4-[2-(3'-formylphenyl-4-carbylamine)-ethoxy] phenyl] propionate(ethyl ester of illustrative compounds N 4-214)

The reaction was conducted in the same manner as described in example 5, using these is enyl-4-carboxylic acid (635 mg) and carbonyldiimidazole (500 mg), and the reaction mixture was treated with obtaining the connection specified in the header (506 mg) as pale brown oil.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,21-of 1.39 (4H, m), 1.41 to at 1.73 (2H, m), 2,53-of 2.66 (1H, m), 2,69 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,90 (2H, q, J= 5.0 Hz), 4,06 (2H, q, J=7,0 Hz) to 4.16 (2H, t, J=5.0 Hz), only 6.64 (1H, user. t), at 6.84 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), to 7.64 (1H, t, J=7.5 Hz), of 7.70 (2H, d, J=8.5 Hz), 7,86-a 7.92 (2H, m), of 7.90 (2H, d, J=8,5 Hz) to 8.12 (1H, s), 10,10 (1H, s).

(Example 38)

Ethyl 2-butyl-3-[4-[2-(3'-dimethylaminomethylphenol-4-carbylamine)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 4-215)

The reaction was conducted in the same manner as described in example 29, using ethyl 2-butyl-3-[4-[2-(3'-formylphenyl-4-carbylamine)ethoxy]phenyl] propionate (415 mg), which is the product of example 37, triethylamine (0,23 ml), dimethylaminohydrolase (139 mg), tetraisopropoxide titanium (0,49 ml) and borgert sodium (56 mg), and then the reaction mixture was treated with obtaining the connection specified in the header (263 mg) as a colourless syrup.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), of 1.20 to 1.37 (4H, m), 1,39 is 1.75 (2H, m), of 2.23 (6H, s), 2,55-2,63 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,52 (2H, s) to 3.89 (2H, kV, J=5.0 Hz), 4,06 (2H, q, J=7.0 Hz), is 4.15 (2H, t, J=5.0 Hz), 67,84 (2H, d, J=8,5 Hz).

(Example 39)

2-Butyl-3-[4-[2-(3'-dimethylaminomethylphenol-4-carbylamine)ethoxy] phenyl]propionic acid (illustrative compound N 4-215)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(3'-dimethylaminomethylphenol-4-carbylamine)-ethoxy] phenyl] propionate (263 mg), which is the product of example 38 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., and 1.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (121 mg) as a white powder. So pl. 95-97oC.1H-NMR (270 MHz, deuterated methanol): ppm 0,86 (3H, t, J=7.0 Hz), 1,14-of 1.34 (4H, m), 1,35-to 1.61 (2H, m), 2,46-to 2.57 (1H, m), 2,62 (1H, DD, J=6,5, and 13.5 Hz), 2,77 (6H, s), of 2.81 (1H, DD, J=8,5, and 13.5 Hz), 3,76 (2H, t, J=5.5 Hz), to 4.15 (2H, t, J=5.5 Hz), 4,25 (2H, s) 6,86 (2H, d, J= 8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,49 (1H, d, J=7.5 Hz), EUR 7.57 (1H, t, J= 7.5 Hz), 7,74-7,79 (1H, m), of 7.75 (2H, d, J-8.5 Hz), 7,82 (1H, s), to $ 7.91 (2H, d, J=8,5 Hz).

(Example 40)

Ethyl 2-butyl-3-[4-[2-(3' -carboxyphenyl-4 - carbylamine)-ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 4-217)

To a solution of ethyl 2-butyl-3- [4-[2-(3'-formylphenyl-4-carbylamine)ethoxy] phenyl]propionate (390 mg), which is the product of example 37, in acetonitrile (6 ml) was added sodium dihydrogenphosphate (24 mg) and water (0,3 is chlorite (104 mg). The mixture in an ice bath was stirred for 1 hour and then stirred at room temperature for 2.5 hours. Then the reaction mixture was extinguished sodium thiosulfate and the reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. To the residue was added diisopropyl ether to obtain the connection specified in the header (217 mg) as a white solid product.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=6.5 Hz) and 1.15 (3H, t, J=7.0 Hz), 1,20-of 1.39 (4H, m), 1,40-is 1.51 (1H, m), 1,53 by 1.68 (1H, m), of 2.51 2.63 in (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,83-of 3.95 (2H, m), of 4.05 (2H, q, J=7.0 Hz), 4,12-4,20 (2H, m), 6,70 (1H, user.t), at 6.84 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,53-to 7.61 (1H, m), 7,63-to 7.77 (2H, m), 7,79-7,94 (3H, m), 8,08-8,19 (1H, m), at 8.36 (1H, s).

(Example 41)

2-Butyl-3-[4-[2-(3'-carboxyphenyl-4-carbylamine)ethoxy] -phenyl] propionic acid (illustrative compound N 4-217)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(3'-carboxyphenyl-4-carbylamine)ethoxy] -phenyl] propionate (273 mg), which is the product of example 40 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 1,10 ml) and is of metal. So pl. 142-143oC.1H-NMR (270 MHz, deuterated methanol): ppm of 0.87 (3H, t, J=7.0 Hz), 1,20-of 1.44 (4H, m), 1,44-of 1.65 (2H, m), 2,49-2,60 (1H, m) to 2.66 (1H, DD, J=6,0, and 13.5 Hz), 2,82 (1H, DD, J=8,5, and 13.5 Hz), of 3.77 (2H, q, J 5.5 Hz), is 4.15 (2H, t, J=5.5 Hz), 6.87 in (2H, d, J=8.5 Hz), to 7.09 (2H, d, J= 8.5 Hz), 7,58 (1H, t, J=7.5 Hz), of 7.75 (2H, d, J=8.5 Hz), of 7.90 (1H, d, J= 7.5 Hz), to 7.93 (2H, d, J=8.5 Hz), of 8.04 (1H, d, J=7.5 Hz), 8,30 (1H, s), 8,72 (1H, user.t).

(Example 42)

Ethyl 2-butyl-3-[4-[2-(2'-methoxybiphenyl-4-carbylamine)-ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-219)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (643 mg), which is the product of reference example 6, 2'-methoxybiphenyl-4-carboxylic acid (500 mg) and carbonyldiimidazole (426 mg) and the reaction mixture was treated with obtaining the connection specified in the header (750 mg) as a pale yellow oil.1H-NMR (270 MHz, CDCl3): ppm of 0.91 (3H, t, J=6.5 Hz), of 1.20 (3H, t, J-7.0 Hz), 1,28-of 1.40 (4H, m), 1,45-of 1.73 (2H, m), 2,59-and 2.79 (2H, m), 2,85-of 2.97 (1H,m), 3,86 (3H, s), 3,93 (2H, q, J=5.0 Hz), 4,10 (2H, q, J=7.0 Hz), 4,18 (2H, t, J=5.0 Hz), to 6.67 (1H, t, J=5.0 Hz), 6,86 (2H, d, J=8.5 Hz), 7,06 (2H, t, J=8.0 Hz), 7,13 (2H, d, J=8.5 Hz), 7,35 - 7,44 (2H, m), the 7.65 (2H, d, J=8.0 Hz), 7,86 (2H, d, J=8.0 Hz).

(Example 43)

2-Butyl-3-[4-[2-(2'-methoxybiphenyl-4-carbylamine)ethoxy] -phenyl] propionic acid (Illus the Il-4-carbylamine)ethoxy] -phenyl] propionate (750 mg), which is the product of example 42 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (625 mg) as a pale orange powder. So pl. 190-192oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J= 7.0 Hz), 1,21-to 1.38 (4H, m), USD 1.43-1,71 (2H, m), 2,58-2,78 (2H, m), 2,85-of 2.97 (1H, m), of 3.80 (3H, s), a 3.87 (2H, q, J=5.0 Hz), of 4.13 (2H, t, J=5.0 Hz), to 6.67 (1H, t, J=5.0 Hz), 6,83 (2H, d, J=8.5 Hz), 6,98-7,06 (2H, m), 7,10 (2H, d, J=8.5 Hz), 7,28-7,38 (2H, m), to 7.59 (2H, d, J=8.5 Hz), 7,81 (2H, d, J=8,5 Hz).

(Example 44)

Ethyl 2-butyl-3-[4-[2-(2'-hydroxybiphenyl-4-carbylamine)-ethoxy]phenyl] propionate (ethyl ester of illustrative compounds 4-220 N)

The reaction was conducted in the same manner as described in example 25, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (249 mg), which is the product of reference example 6, 2'-hydroxybiphenyl-4-carboxylic acid (200 mg), which is the product of reference example 16, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (195 mg) and 1-hydroxybenzotriazole (138 mg) and the reaction mixture was treated with obtaining the connection specified in the header, (386 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=6.5 Hz), 1,16

(3H, t, J=7.0 Hz), 1,21-1,32 (4H,1 (4H, m), 7,21-7,28 (2H, m), 7,58 (2H, d, J=8.0 Hz), 7,88 (2H, d, J=8.0 Hz).

(Example 45)

Sodium 2-butyl-3-[4-[2-(2'-hydroxybiphenyl-4 - carbylamine)ethoxy]phenyl]propionate (illustrative compound N 4-220)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(2'-hydroxybiphenyl-4-carbylamine)ethoxy]phenyl]propionate (345 mg), which is the product of example 44 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2,82 ml) and the reaction mixture was treated with obtaining the crude free acid, which was subjected to thin-layer chromatography on silica gel, using as eluent dichloromethane/methanol = 10/1. The product was converted into the sodium salt of obtaining the connection specified in the header (200 mg) as colorless crystals. So pl. 153-156oC.1H-NMR of the free acid (270 MHz, CDCl3): ppm to 0.88 (3H, t, J=7.0 Hz), 1,25-of 1.37 (4H, m), 1,44-1,71 (2H, m), 2,55-2,78 (2H, m), of 2.86 (1H, DD, J= 8,5, and 13.5 Hz), 3,83 (2H, q, J=5.0 Hz), 4,10 (2H, t, J=5.0 Hz), 6,69-6,79 (1H, m), to 6.80 (2H, d, J=8,5 Hz), 6,95-7,10 (4H, m), 7,22-7,30 (2H, m), 7,55 (2H, d, J=8.0 Hz), 7,80 (2H, d, J=8,5 Hz).

(Example 46)

Ethyl 2-butyl-3-[4-[2-(2'-formylphenyl-4 - carbylamine)ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-221)

The reaction was conducted in the same manner as described in example 5, the 6, 2'-formylphenyl-4-carboxylic acid (350 mg) and carbonyldiimidazole (296 mg) and the reaction mixture was treated with obtaining the connection specified in the header, (314 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,19-of 1.33 (4H, m), 1.41 to its 1.68 (2H, m), 2,53-of 2.72 (2H, m), 2,87 (1H, DD, J= 8,5, and 13.5 Hz), 3,91 (2H, q, J=5.0 Hz), 4,01-4,20 (4H, m), 6,65-6,72 (1H, m), at 6.84 (2H, d, J= 8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,42-to 7.59 (4H, m), 7,63-of 7.70 (1H, m), 7,89 (2H, d, J=8.0 Hz), of 8.04 (1H, d, J=7.5 Hz), 9,96 (1H, s).

(Example 47)

2-Butyl-3-[4-[2-(2'-formylphenyl-4 - carbylamine)ethoxy] phenyl]propionic acid (illustrative compound N 4-221)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(2'-formylphenyl-4-carbylamine)ethoxy]phenyl]propionate (314 mg), which is the product of example 46 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 2.50 ml) and the reaction mixture was treated with obtaining the crude free acid, which was subjected to thin-layer chromatography on silica gel, using as eluent dichloromethane/methanol = 10/1, to obtain the compounds specified in the header, (152 mg) as a foam mass.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7.0 Hz), 1,22-of 1.40 (4H, m), 1,42 is 1.70 (2H, m), 2,55-2,78 (2H, m), is 2.88 (1H, DD, J=8,5, and 13.5 Hz), 3,83-3,93 (2H, m), 4,07-4,18 (2H, m), for 6.81 (2H, ="ptx2">

(Example 48)

Sodium 2-butyl-3-[4-[2-(4'-hydroxy-3', 5'-dimethylbiphenyl-4-carbylamine)ethoxy]phenyl]propionate (illustrative compound N 4-205)

In the same way as described in example 36, 2-butyl-3-[4-[2-(4'-methoxyethoxy-3', 5'-dimethylbiphenyl-4 - carbylamine)ethoxy]phenyl]propionic acid (1,00 g), which is the product of reference example 17 were subjected to interaction with a solution of hydrogen chloride in dioxane (4 N., 0,69 ml) and the reaction mixture was treated with obtaining the connection specified in the header (528 mg) as a pale brown solid product. So pl. 137-139oC. 1H-NMR (270 MHz, mixture CDCl3and deuterated methanol (10/3)): ppm of 0.85 (3H, t, J=7.0 Hz), 1,20-1,40 (5H, m), 1,43 is 1.60 (1H, m), and 2.27 (6H, s), 2,34-2,47 (1H, m), 2,52 (1H, DD, J=7,5, and 13.5 Hz), 2,85 (1H, DD, J=7,5, and 13.5 Hz), 3,74 (2H, t, J=5.5 Hz), 4,13 (2H, t, J=5.5 Hz), at 6.84 (2H, d, J=8.5 Hz), 7,12 (2H, d, J=8.5 Hz), a 7.62 (2H, d, J=8.5 Hz), to 7.84 (2H, d, J=8,5 Hz).

(Example 49)

Ethyl 2-butyl-3-[4-[2-(2-hydroxypyridine-5 - carbylamine)ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 4-193)

The reaction was conducted in the same manner as described in example 25, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (843 mg), which is the product of reference example 6, 6-hydroxynicotinic acid (400 mg), 1-(3-di is th the mixture was treated with obtaining connection specified in the header, (636 mg) as a white powder. So pl. 102-104oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7,0 Hz) of 1.17 (3H, t, J=7.0 Hz), 1,21-of 1.32 (4H, m), 1,40-1,70 (2H, m), 2,53-of 2.72 (2H, m), 2,80-only 2.91 (1H, m), 3,81 (2H, q, J=5.0 Hz), was 4.02-4,12 (4H, m), 6.42 per-of 6.52 (1H, m), 6,56 (1H, d, J=9.5 Hz), for 6.81 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,80 (1H, DD, J=2.5 and 9.5 Hz), 8,00 (1H, d, J=2.5 Hz).

(Example 50)

2-Butyl-3-[4-[2-(2-hydroxypyridine-5 - carbylamine)ethoxy]phenyl]propionic acid (illustrative compound N 4-193)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(2-hydroxypyridine-5-carbylamine)ethoxy]phenyl]propionate (300 mg), which is the product of example 49, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (240 mg) as a pale yellow powder. So pl. 69-71oC.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=7.0 Hz), 1,30-1,45 (4H, m), 1,50-1,79 (2H, m), 2.57 m) of 2.68 (1H, m), 2,77 (1H, d, J= 7.5 Hz), 3,68-of 3.77 (2H, m), EUR 4.00-4.09 to (2H, m), 6.42 per (1H, d, J=10.0 Hz), of 6.71 (2H, d, J=8.5 Hz), 7,05 (2H, d, J=8.5 Hz), 7,10-7,20 (1H, m), 7,75-7,80 (2H, m).

(Example 51)

Ethyl 2-butyl-3-[4-[2-(2-methoxypyridine-5 - carbylamine)ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-96)

The reaction was carried out in the same way that the description is knogo of example 6, 6-methoxynicotinic acid (400 mg) and carbonyldiimidazole (508 mg) and the reaction mixture was treated with obtaining the connection specified in the header (783 mg) as colorless crystals. So pl. 129-130oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), to 1.22 and 1.33 (4H, m), 1,40-1,70 (2H, m), 2,52-2,63 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,85 (2H, q, J= 5.0 Hz), of 4.00 (3H, s), 4,06 (2H, q, J=7.0 Hz), of 4.12 (2H, t, J=5.0 Hz), 6,46-6,55 (1H, m), is 6.78 (1H, d, J=8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), to 7.99 (1H, DD, J=2.5 and 8.5 Hz), 8,59 (1H, d, J=2.5 Hz).

(Example 52)

2-Butyl-3-[4-[2-(2-methoxypyridine-5 - carbylamine)ethoxy] phenyl]propionic acid (illustrative compound N 4-96)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(2-methoxypyridine-5-carbylamine)ethoxy] phenyl]propionate (500 mg), which is the product of example 51 were subjected to contact with an aqueous solution of sodium hydroxide (1 n, 4,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (293 mg) as a white powder. So pl. 144-145oC.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7.0 Hz), 1,24-of 1.40 (4H, m), 1,47 is 1.75 (2H, m), 2,62-2,90 (3H, m), 3,71-of 3.97 (2H, m), 3,98 (3H, s), 4,11-4.26 deaths (2H, m), 6.48 in-6,60 (1H, m), is 6.78 (1H, d, J=8.5 Hz), 6,85 (2H, d, J= 8.5 Hz), 7,11 (2H, d, J=8.5 Hz), 8,03 (1H, DD, J=2.5 and 8.5 Hz), 8,31 (1H, d, J=2.5 Hz).

illustrating connection N 4-98)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (156 mg), which is the product of reference example 6, 6-isopropoxytitanium acid (106 mg), which is the product of reference example 18, and carbonyldiimidazole (112 mg) and the reaction mixture was treated with obtaining the connection specified in the header (170 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,20-1,40 (10H, m), 1.41 to 1,71 (2H, m), 2,61-by 2.73 (2H, m), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,83 (2H, q, J= 5.0 Hz), of 4.05 (2H, q, J=7.0 Hz), 4,11 (2H, t, J=5.0 Hz), to 5.35 (2H, septet, J= 6.0 Hz), 6,56-6,62 (1H, m), 6,69 (1H, d, J=8.5 Hz), for 6.81 (2H, d, J= 8.5 Hz), 7,07 (2H, d, J=8.5 Hz), of 7.97 (1H, DD, J=2.5 and 8.5 Hz), 8,58 (1H, d, J=2.5 Hz).

(Example 54)

2-Butyl-3-[4-[2-(2-isopropoxypyridine-5-carbylamine)ethoxy] phenyl] propionic acid (illustrative compound N 4-98)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(2-isopropoxypyridine-5-carbylamine)ethoxy] phenyl]propionate (170 mg), which is the product of example 53, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 0.75 ml) and the reaction mixture was treated with obtaining the connection specified in the header (137 mg) as colorless crystals. So pl. 117-11 of 3.73-of 3.96 (2H, m), 4,10-4,22 (2H, m), 5,31 (2H, septet, J= 6.0 Hz), 6.48 in-to 6.57 (1H, m), 6,70 (1H, d, J=8.5 Hz), at 6.84 (2H, d, J=8.5 Hz), 7,11 (2H, d, J= 8.5 Hz), 8,00 (1H, DD, J=2.5 and 8.5 Hz), 8,35 (1H, d, J=2.5 Hz).

(Example 55)

Ethyl 2-butyl-3-[4-[2-(2-phenoxypyridine-5-carbylamine)ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-106)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (158 mg), which is the product of reference example 6, 6-phenoxyimino acid (125 mg) and carbonyldiimidazole (112 mg) and the reaction mixture was treated with obtaining the connection specified in the header (225 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7,0 Hz) and 1.15 (3H, t, J=7.0 Hz), 1,20-of 1.36 (4H, m), 1.41 to to 1.70 (2H, m), 2,52-of 2.72 (2H, m), 2,85 (1H, DD, J= 8,5, and 13.5 Hz), 3,78-to 3.89 (2H, m), 4,01-to 4.15 (4H, m), 6,65-PC 6.82 (3H, m), 6,92 (1H, d, J= 8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=7.5 Hz), 7,20-7,26 (1H, m), 7,38 was 7.45 (2H, m), 8,12. (1H, DD, J=2.5 and 8.5 Hz), 8,58 (1H, d, J=2.5 Hz).

(Example 56)

2-Butyl-3-[4-[2-(2-phenoxypyridine-5 - carbylamine)ethoxy]-phenyl]propionic acid (illustrative compound N 4-106)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(2-phenoxypyridine-5-carbylamine)ethoxy] phenyl]propionate (215 mg), which is the product of example 55 was subjected ot what ever got free acid, which was subjected to thin-layer chromatography on silica gel, using as eluent dichloromethane/methanol = 10/1, to obtain the compound indicated in heading (137 mg) as colorless crystals. So pl. 124-125oC.1H-NMR (270 MHz, CDCl3): ppm 0,85-0,95 (3H, m), 1,25-of 1.39 (4H, m), 1,40-1,71 (2H, m), 2,53-is 2.88 (3H, m), 3,70-of 3.97 (2H, m), 4,08-to 4.28 (2H, m), 6,58 of 6.68 (1H, m), for 6.81 (2H, d, J=8.5 Hz), 6,93 (1H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=8.5 Hz), 7,20-7,29 (1H, m), 7,39-of 7.48 (2H, m), 8,15 (1H, DD, J=8.5 Hz), 8,29 (1H, s).

(Example 57)

Ethyl 2-butyl-3-[4-[2-(the quinoline-3-carbylamine)ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-150)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (529 mg), which is the product of reference example 6, the quinoline-3-carboxylic acid (312 mg) and carbonyldiimidazole (350 mg) and the reaction mixture was treated with obtaining the connection specified in the header, (760 mg) as a yellow oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=6.5 Hz), of 1.16 (3H, t, J=7.0 Hz), to 1.22 to 1.37 (4H, m), 1,40-1,70 (2H, m), 2,55-2,63 (1H, m), 2,69 (1H, DD, J= 6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), of 3.95 (2H, q, J=5.0 Hz), 4,06 (2H, q, J=7,0 Hz), 4,19 (2H, t, J=5.0 Hz), 6,76-PC 6.82 (1H, m), 6,85 (2H, d, J= 8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,63 (1H, t, J=8.0 Hz), 7,78-a 7.85 (1H, m), 7,92 (1H, d, J=8.0 Hz), 8,16 (1H, d, J=8,0 and]phenyl]propionic acid (illustrative compound N 4-150)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(the quinoline-3-carbylamine)ethoxy] phenyl] propionate (760 mg), which is the product of example 57 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 6,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (386 mg) as a white powder. So pl. 245 - 248oC.1H-NMR of the free acid (270 MHz, CDCl3): ppm of 0.90 (3H, t, J= 7.0 Hz), of 1.28 to 1.48 (4H, m), 1,50-1,80 (2H, m), 2,58-2,90 (3H, m), 3,80-4,07 (2H, m), 4,20-4,39 (2H, m), 6,68-6,84 (1H, m), 6.87 in (2H, d, J=8.5 Hz), 7,12 (2H, d, J=8.5 Hz), a 7.62 (1H, t, J=8.0 Hz), 7,81 (1H, t, J=8.0 Hz), to $ 7.91 (1H, d, J=8.0 Hz), 8,13 (1H, d, J=8.0 Hz), to 8.70 (1H, s), 8,81 (1H, s).

(Example 59)

Ethyl 2-butyl-3-[4-[2-(indole-3-carbylamine)ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 4-143)

The reaction was conducted in the same manner as described in example 25, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (546 mg), which is the product of reference example 6, indole-3-carboxylic acid (300 mg), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (428 mg) and 1-hydroxybenzotriazole (342 mg) and the reaction mixture was treated with obtaining the connection specified in the header (650 mg) as a yellow oil.1H-NMR (270 MHz, CDCl3): of 0.87 ppm (3H) - Rev. C), of 4.05 (2H, q, J= 7.0 Hz), 4,17 (2H, t, J=5.0 Hz), 6,44 (1H, t, J=5.0 Hz), 6,86 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7.24 to 7,29 (2H, m), 7,41 was 7.45 (1H, m), 7,74 (1H, d, J=3.0 Hz), 7.95 is-to 7.99 (1H, m), 8,59-to 8.70 (1H, m).

(Example 60)

2-Butyl-3-[4-[2-(indole-3-carbylamine)ethoxy] phenyl]propionic acid (illustrative compound N 4-143)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(indole-3-carbylamine)ethoxy] phenyl] propionate (650 mg), which is the product of example 59, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (500 mg) as a white powder. So pl. 171-173oC.1H-NMR of the free acid (270 MHz, CDCl3): ppm 0,86 (3H, t, J= 7.0 Hz), to 1.22 to 1.37 (4H, m), 1,40 by 1.68 (2H, m), 2.40 a-2,62 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), 2,90 (1H, DD, J=8,5, and 13.5 Hz), 3,88 (2H, q, J=5.0 Hz), 4,17 (2H, t, J=5.0 Hz), was 6.73 (1H, t, J=5.0 Hz), 6,85 (2H, d, J=8.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7,17-7,24 (2H, m), 7,42-7,47 (1H, m), 7,78 (1H, d, J=3.0 Hz), 8,00-with 8.05 (1H, m).

(Example 61)

Ethyl 2-butyl-3-[4-[2-(4-N, N-diethylaminoethylamine)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 4-230)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (455 mg), which is the product of reference PI with obtaining connection specified in the header, (346 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), 1,13-of 1.20 (9H, m), of 1.24 to 1.37 (4H, m), 1,40-1,70 (2H, m), 2,53-2,63 (1H, m), 2,68 (1H, DD, J= 6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,39 (4H, q, J=7.0 Hz), 3,83 (2H, q, J=5.5 Hz), 4,01-to 4.14 (4H, m), 6,40 (1H, t, J=5.5 Hz), 6,63 (2H, d, J= 8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,66 (2H, d, J= 8,5 Hz).

(Example 62)

2-Butyl-3-[4-[2-(4-N, N-diethylaminoethylamine)ethoxy]phenyl]propionic acid (illustrative compound N 4-230)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(4-N, N-diethylaminoethylamine)ethoxy] phenyl]propionate (340 mg), which is the product of example 61 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2,20 ml) and the reaction mixture was treated with obtaining the connection specified in the header (257 mg) as a white powder. So pl. 76-78oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7,0 Hz) of 1.17 (6H, t, J= 7.0 Hz), 1,11-to 1.21 (4H, m), 1,45 is 1.70 (2H, m), 2.57 m-to 2.65 (1H, m), 2,70 (1H, DD, J=6,5, and 13.5 Hz), 2,90 (1H, DD, J=8.0 a, and 13.5 Hz), to 3.38 (4H, q, J=7.0 Hz), 3,80 (2H, q, J=5.0 Hz), 4,08 (2H, t, J=5.0 Hz), 6.48 in (1H, t, J=5.0 Hz), 6,62 (2H, d, J=8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), the 7.65 (2H, d, J=8,5 Hz).

(Example 63)

Ethyl 2-butyl-3-[4-[2-(4-piperidine-1-albenzaalbenza)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N]-2-butylphosphonate (428 mg), which is the product of reference example 6, 4-piperidine-1-eventing acid (300 mg) and carbonyldiimidazole (284 mg) and the reaction mixture was treated with obtaining the connection specified in the header (420 mg) as a white powder. So pl. 87-89oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7,0 Hz) and 1.15 (3H, t, J= 7.0 Hz), of 1.20 to 1.37 (4H, m), 1,40-of 1.73 (8H, m), 2,52-2,61 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,26-to 3.33 (4H, m), 3,83 (2H, q, J= 5.0 Hz), 4,01-4,16 (4H, m), 6.48 in (1H, t, J=5.0 Hz), PC 6.82 (2H, d, J=8.5 Hz), 6.87 in (2H, d, J=9.0 Hz), 7,07 (2H, d, J=8.5 Hz), to 7.67 (2H, d, J=9.0 Hz).

(Example 64)

2-Butyl-3-[4-[2-(4-piperidine-1-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 4-229)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(4-piperidine-1-albenzaalbenza)ethoxy]phenyl]propionate (370 mg), which is the product of example 63 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.30 ml) and the reaction mixture was treated with obtaining the connection specified in the header (324 mg) as a white powder. So pl. to 112.5-114oC.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=6.5 Hz), 1,28-of 1.44 (4H, m), 1,48-1,77 (8H, m), 2,61-2,69 (1H, m), 2,73 (1H, DD, J=6,5, and 13.5 Hz), of 2.92 (1H, DD, J=8.0 a, and 13.5 Hz), 3.27 to to 3.33 (4H, m), a-3.84 (2H, q, J= 5.0 Hz), 4,11 (2H, t, J=5.0 Hz), is 6.54 (1H, t, J=5.0 Hz), at 6.84 (2H, d, J=8.5 Hz), 6.89 in (2H, d, J=9.0 Hz), 7,l)amino)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 20-71)

To a solution of ethyl 2-butyl-3-[4-[2-(3-phenylpropylamine)ethoxy]phenyl]propionate (460 mg), which is the product of reference example 19, and 4-pyridine-2-eventological (341 mg) in dichloromethane (10 ml) at room temperature was added triethylamine (0,37 ml). Then the mixture was stirred for 5 hours at room temperature, the solvent is kept at reduced pressure. The residue was distributed between ethyl acetate and water, and an ethyl acetate layer was separated and dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/methanol = 19/1, receiving of the connection specified in the header (275 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J= 7.0 Hz), 1,12-2,05 (11H, m), 2,42-only 2.91 (5H, m), 3,35-4,30 (8H, m), 6,70-to 6.88 (2H, m), 7,00 - of 7.60 (10H, m), 7,73-a 7.85 (2H, m), 7,99-of 8.06 (2H, m), 8,72 (1H, d, J=5.0 Hz).

(Example 66)

Hydrochloride of 2-butyl-3-[4-[2-(N-(3-phenylpropyl)-(4-pyridine-2-aventyl)amino)ethoxy] phenyl]propionic acid (illustrative compound N 20-71)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[2-(N-(3-phenylpropyl)-(4-pyridine-2-aventyl)amino)ethoxy] phenyl] propionate (275 mg), which actionnow the mixture was processed. The connection specified in the header (230 mg) was obtained as a foamy mass by treating the product with a solution of dioxane sulfuric acid (4 BC).1H-NMR of the free acid (270 MHz, CDCl3): ppm to 0.92 (3H, t, J=7.0 Hz), 1,30-1,45 (4H, m), 1,50 is 2.10 (4H, m), 2,55-2,82 (5H, m), 3,48-a 3.83 (4H, m), 4,00 is 4.36 (2H, m), 6,57-6,86 (2H, m), 7,02-7,39 (10H, m), 7.68 per-7,89 (4H, m), 8,69 (1H, d, J=5.0 Hz).

(Example 67)

Ethyl 2-butyl-3-[4-[2-[N-butyl-(4-pyridine-2 - aventyl)amino]ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 20-53) the Reaction was carried out in the same manner as described in example 65, using ethyl 2-butyl-3-[4-[2-(butylamino)ethoxy] phenyl] propionate (390 mg), which is the product of reference example 20, 4-pyridine-2-eventological (340 mg) and triethylamine (0,37 ml) and the reaction mixture was treated with obtaining the connection specified in the header (165 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm 0,78-1,71 (19H, m), 2,55 - 2,77 (2H, m), 2,82-only 2.91 (1H, m), 3,34-3,47 (1H, m), 3,65-of 3.80 (3H, m), 3,83-of 3.94 (1H, m) 4,06 (2H, q, J= 7.0 Hz), 4,23-4,32 (1H, m), 6,68-6,91 (2H, m), 7,01-to 7.15 (2H, m), of 7.23-7,30 (1H, m), 7,43-7,81 (4H, m), 8,02 (2H, d, J=8.5 Hz), 8,70 (0,6 H, d, J=5.0 Hz), 8,90 (0,4 H, d, J=5.0 Hz).

(Example 68)

Hydrochloride of 2-butyl-3-[4-[2-[N-butyl-(4-pyridine-2 - aventyl)amino]ethoxy]phenyl]propionic acid (illustrative compound N 20-53)

The W is NAT (165 mg), which is the product of example 67, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., and 1.00 ml) and the reaction mixture was processed. The connection specified in the header (110 mg) was obtained as a foamy mass by treating the product with a solution of dioxane sulfuric acid (4 BC).1H-NMR of the free acid (270 MHz, CDCl3): ppm 0,80-a 1.01 (6H, m), 1,10-of 1.85 (10H, m), 2,60-to 2.85 (3H, m), 3,30-are 3.90 (4H, m), 4,11-to 4.38 (2H, m), 6,58-of 6.90 (2H, m), 7,02-7,14 (2H, m), 7,28-7,40 (3H, m), 7.68 per-of 7.90 (4H, m), 8,69 (1H, d, J= 5.0 Hz).

(Example 69)

Ethyl 2-butyl-3-[4-[3-(4-pyridine-2-albenzaalbenza)propoxy] phenyl]propionate (ethyl ester of illustrative compounds N 40-3)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(3-aminopropoxy)phenyl] -2-butylphosphonate (500 mg), which is the product of reference example 21, 4-pyridine-2-eventing acid (340 mg) and carbonyldiimidazole (333 mg) and the reaction mixture was treated with obtaining the connection specified in the header (178 mg) as a white powder. So pl. 110-112oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J= 7.0 Hz), to 1.21 and 1.33 (4H, m), 1,42 is 1.70 (2H, m), and 2.14 (2H, quintuplet, J=6.0 Hz), 2,53-by 2.73 (2H, m), 2,80-only 2.91 (1H, m), 3,71 (2H, q, J=6.0 Hz), 4,06 (2H, q, J=7.0 Hz), of 4.13 (2H, t, J=6.0 Hz), 6,76-to 6.80 (1H, m), 6,83 (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,25-to 7.32 (1H, m), 7, is solumina)propoxy] phenyl] propionic acid (illustrative compound N 40-3)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[3-(4-pyridine-2-albenzaalbenza)propoxy]phenyl]propionate (161 mg), which is the product of example 69 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 1,20 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (117 mg) as a white powder. So pl. 151-152oC.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=7.0 Hz), 1,28-of 1.44 (4H, m) and 1.51-of 1.64 (1H, m), 1,65-of 1.78 (1H, m), of 2.15 (2H, quintuplet, J=6.0 Hz), 2,58 of 2.92 (3H, m), 3,60-of 3.80 (2H, m), 4,15-is 4.21 (2H, m), at 6.84 (2H, d, J= 8.5 Hz), 6.87 in-to 6.95 (1H, m), 7,16 (2H, d, J=8.5 Hz), 7,30-to 7.35 (1H, m), 7,74-of 7.90 (6H, m), 8,69 (1H, d, J=5,5 Hz).

(Example 71)

Ethyl 2-butyl-3-[4-[3-[N-methyl-(4-pyridine-2 - aventyl)amino] propoxy] phenyl]propionate (ethyl ester of illustrative compounds N 20-80)

The reaction was conducted in the same manner as described in example 65, using ethyl 2-butyl-3-[4-(3-methylaminopropane)phenyl] propionate (380 mg), which is the product of reference example 22, 4-pyridine-2-eventological (360 mg) and triethylamine (0,40 ml) and the reaction mixture was treated with obtaining the connection specified in the header (259 mg) as a white powder. So pl. 58-60oC.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J= 7,0 Hz) and 1.15 (3H, t, J= 7.0 Hz), 1,20-to 1.38 (4H, m), 1,40-1,70 (2H, m), of 7.23-7,28 (1H, m), 7,41 - of 7.55 (2H, m), 7,70-7,81 (2H, m), to $ 7.91-of 8.06 (2H, m), 8,71 (1H, d, J=5.0 Hz).

(Example 72)

2-Butyl-3-[4-[3-[N-methyl-(4-pyridine-2 - aventyl)amino] propoxy]phenyl] propionic acid (illustrative compound N 20-80)

In the same way as described in example 2, ethyl 2-butyl-3-[4-[3-[N-methyl-(4-pyridine-2-aventyl)amino] propoxy]phenyl]propionate (200 mg), which is the product of example 71, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 1,20 ml) and the reaction mixture was treated with obtaining the connection specified in the header (127 mg) as a white powder. So pl. 110-112oC.1H-NMR (270 MHz, CDCl3): ppm of 0.91 (3H, t, J=7.0 Hz), 1,21-of 1.41 (4H, m), 1,48-to 1.61 (1H, m), 1,64 of-1.83 (1H, m), 1.93 and-of 2.23 (2H, m), 2,58-and 2.83 (3H, m), 3.00 and-3,17 (3H, m), 3,37-of 3.60 (1H, m), 3,68-4.26 deaths (3H, m), 6,66-7,01 (2H, m), 7,10-7,30 (2H, m), 7,33-of 7.60 (3H, m), 7,70-to 8.20 (4H, m), 8,76-9,05 (1H, m).

(Example 73)

Ethyl 2-propyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 3-35)

A solution of ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-propylphosphonate (2.20 g) in dioxane containing hydrochloric acid (4 N., 30 ml) was left to stand at room temperature for 40 minutes. At the end of this time the reaction mixture was concentrated under reduced pressure and the l 3-[4-(2-aminoethoxy)phenyl]-2-propyltrimethylammonium), 4-pyridine-2-eventing acid (1,21 g) and triethylamine (1.80 ml) in N,N-dimethylformamide (8.0 ml) in an ice bath was added a solution diethylthiophosphate (0,97 ml) in N,N-dimethylformamide (4.0 ml). The mixture was stirred in an ice bath for 1 hour and at room temperature for 3 hours. The reaction mixture was distributed between ethyl acetate and water, the ethyl acetate was separated, washed with saturated aqueous sodium bicarbonate and dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/ethyl acetate = 7/3, receiving of the connection specified in the header, (2.20 g) as a pale yellow powder. So pl. 90,5-92oC.1H-NMR (270 MHz, CDCl3): ppm to 0.88 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,21-1,71 (4H, m), 2,50-of 2.72 (2H, m), 2,80 of 2.92 (1H, m), 3,81-of 3.95 (2H, m), 4,00-421 (4H, m), 6,60-of 6.71 (1H, m), at 6.84 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,20-7,31 (1H, m), 7,70-7,80 (2H, m), 7,88 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 74)

2-Propyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 3-53)

In the same way as described in example 2, ethyl 2-propyl-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (2.10 g), 0 ml) and the reaction mixture was treated with obtaining connection specified in the header, (1,96 g) as a white powder. So pl. 81-82,5oC.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=7.0 Hz), 1,20-1,71 (4H, m), 2,55 is 2.75 (2H, m), 2,75 of 2.92 (1H, m), 3,74-are 3.90 (2H, m), a 4.03-421 (2H, m), of 6.71-6.89 in (3H, m), to 7.09 (2H, d, J=8.5 Hz), 7,21-7,31 (1H, m), 7,66-7,83 (4H, m), of 7.97 (2H, d, J=8.5 Hz), 8,71 (1H, d, J=4.5 Hz).

(Example 75)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl]-2-phenoxypropionate (ethyl ether illustrative compounds N 6-15)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate (666 mg), which is the product of reference example 4, biphenyl-4-carboxylic acid (400 mg) and carbonyldiimidazole (393 mg) and the reaction mixture was treated with obtaining the connection specified in the header (280 mg) as a white powder. So pl. 103-104,5oC.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 3,15-up 3.22 (2H, m) to 3.89 (2H, q, J=5.0 Hz), 4,13-4,22 (4H, m), 4,74 (1H, DD, J= 6,0, 7.5 Hz), 6,62 (1H, t, J=5.0 Hz), at 6.84 (2H, d, J=9.0 Hz), 6.87 in (2H, d, J= 9.0 Hz), 6,94 (1H, t, J=7.5 Hz), 7,19-of 7.25 (4H, m), 7,35 is 7.50 (3H, m), EUR 7.57-7,63 (2H, m), the 7.65 (2H, d, J=8.5 Hz), the 7.85 (2H, d, J=8,5 Hz).

(Example 76)

3-[4-[2-(Biphenyl-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid (illustrative compound N 6-15)

In the same way as described in example 2, ethyl 3-[4-[2-(biphenyl-4-carbonview with an aqueous solution of sodium hydroxide (1 N., 2,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (250 mg) as a white powder. So pl. 171-173oC.1H-NMR (270 MHz, CDCl3): ppm 3,20 (2H, d, J=6.5 Hz), 3,82-are 3.90 (2H, m), is 4.15 (2H, t, J=5.0 Hz), 4,71 (1H, t, J=6.5 Hz), 6,86 (4H, d, J=8.0 Hz), 6,91 (1H, t, J=7.5 Hz), 7,01 for 7.12 (1H, m), 7.18 in-7,27 (4H, m), 7,35 is 7.50 (3H, m), to 7.61 (2H, d, J=8.5 Hz), the 7.65 (2H, d, J=8.5 Hz), 7,88 (2H, d, J=8.0 Hz).

(Example 77)

Ethyl 3-[4-[2-(4'-forbiden-4-carbylamine)ethoxy]phenyl]-2-phenoxypropionate (ethyl ether illustrative compounds N 6-190)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate (1.63 g), which is the product of reference example 4, 4'-forbiden-4-carboxylic acid (1.20 g) and carbonyldiimidazole (1.08 g) and the reaction mixture was treated with obtaining the connection specified in the header, (915 mg) as a white powder. So pl. 99-101oC.1H-NMR (270 MHz, CDCl3): of 1.25 ppm (3H, t, J=7.0 Hz), 3,22-3,26 (2H, m), of 3.94 (2H, q, J=5.0 Hz), 4,20 (2H, t, J=5.0 Hz), 4,22 (2H, q, J= 7.0 Hz), 4,79 (1H, DD, J=5,5, 7.5 Hz), to 6.67 (1H, t, J=5.0 Hz), 6,86-6,93 (4H, m), of 6.96-7,01 (1H, m), 7,19 (2H, t, J=8.5 Hz), 7,28 (2H, d, J=8.5 Hz), to 7.59-to 7.68 (4H, m), 7,89 (2H, d, J=8,5 Hz).

(Example 78)

3-[4-[2-(4'-Forbiden-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid (illustrative connection of the Nile] -2-phenoxypropionate (915 mg), which is the product of example 77, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (866 mg) as a white powder. So pl. 195-196oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm is 3.08-3,17 (2H, m), 3,63 (2H, q, J=5.5 Hz), 4,10 (2H, t, J=5.5 Hz), a 4.83-4,89 (1H, m), 6,83 (2H, d, J=8.5 Hz), 6,88-to 6.95 (3H, m), 7.23 percent-7,39 (6H, m), 7,73-to 7.84 (4H, m), 7,95 (2H, d, J=8.0 Hz), the rate of 8.75 (1H, t, J=5,5 Hz).

(Example 79)

Ethyl 3-[4-[2-(4'-chlorobiphenyl-4-carbylamine)ethoxy]phenyl]-2-phenoxypropionate (ethyl ether illustrative compounds N 6-204)

To a solution of ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate (1.50 g), 4'-chlorobiphenyl-4-carboxylic acid (1,17 g) and triethylamine (0,70 ml) in tetrahydrofuran (20 ml) in an ice bath was added a solution diethylthiophosphate (0,76 ml) in tetrahydrofuran (10 ml). The mixture in an ice bath was stirred for 1 hour and at room temperature for 4 hours. At the end of this time the solvent is kept at reduced pressure. The residue was distributed between ethyl acetate and water, and an ethyl acetate layer was separated and washed with saturated aqueous solution of hydrogencarbonate sodium, and dried over anhydrous magnesium sulfate and concentric as eluent dichloromethane/ethyl acetate = 19/1, obtaining the connection specified in the header, (0,90 g) as a pale yellow oil.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 3,12-is 3.21 (2H, m), 3,79-are 3.90 (2H, m), 4,05-is 4.21 (4H, m), 4,69-rate 4.79 (1H, m), 6,68-of 6.78 (1H, m), 6,80-6,89 (4H, m), 6.90 to-of 6.96 (1H, m), 7,16-7,27 (4H, m), 7,41 (2H, d, J=8.5 Hz), 7,51 (2H, d, J=8.5 Hz), 7,58 (2H, d, J=8.5 Hz), to 7.84 (2H, d, J=8,5 Hz).

(Example 80)

3-[4-[2-(4'-Chlorobiphenyl-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid (illustrative compound N 6-204)

In the same way as described in example 2, ethyl 3-[4-[2-(4'-chlorobiphenyl-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionate (900 mg), which is the product of example 79 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (638 mg) as a white powder. So pl. 194,5-197oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 3,05 is 3.15 (2H, m), to 3.58-to 3.67 (2H, m), 4,01-4,12 (2H, m), 4.80 to 4,89 (1H, m), 6,78-to 6.95 (5H, m), 7.18 in-7,28 (4H, m), 7,55 (2H, d, J=8.5 Hz), 7,71-7,81 (4H, m), of 7.96 (2H, d, J=8.0 Hz), 8,71-8,79 (1H, m).

(Example 81)

Ethyl 3-[4-[2-(4'-triptorelin-4-carbylamine)ethoxy] phenyl] -2 - phenoxypropionate (ethyl ether illustrative compounds N 6-191)

The reaction was conducted in the same manner as described in example 5, using permitivitty-4-carboxylic acid (1.30 grams) and carbonyldiimidazole (0.95 g), and the reaction mixture was treated with obtaining the connection specified in the header (1.10 g) as a pale yellow oil.1H-NMR (270 MHz, CDCl3): of 1.25 ppm (3H, t, J=7.0 Hz), 3,18-of 3.25 (2H, m), of 3.95 (2H, q, J=5.0 Hz), 4,20 (2H, t, J=5.0 Hz), 4,22 (2H, q, J= 7.0 Hz), 4,79 (1H, DD, J=5,5, 7.5 Hz), 6,70 (1H, t, J=5.0 Hz), 6,82-6,98 (5H, m), 7,20-to 7.32 (4H, m), 7,65-7,76 (6H, m), to 7.93 (2H, d, J=8,5 Hz).

(Example 82)

3-[4-[2-(4'-Triptorelin-4-carbylamine)ethoxy] -phenyl] -2-phenoxypropionic acid (illustrative compound N 6-191)

In the same way as described in example 2, ethyl 3-[4-[2-(4'-triptorelin-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionate (1.10 g), which is the product of example 81 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (850 mg) as a white powder. So pl. 217-218,5oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 3,06-and 3.16 (2H, m), 3,66 (2H, q, J=5.5 Hz), 4,11 (2H, t, J=5.5 Hz), is 4.85 (1H, DD, J=5.0 and 7.5 Hz), 6,80-of 6.96 (5H, m), 7,20-7,28 (4H, m), a 7.85 (4H, d, J=8.5 Hz), 7,94-8,02 (4H, m), 8,80 (1H, t, J=5,5 Hz).

(Example 83]

Sodium 3-[4-[2-(4'-hydroxy-3', 5'-dimethylbiphenyl-4 - carbylamine)ethoxy]phenyl]-2-phenoxypropionate (illustrative compound N 6-205)

In the same way that opiat (330 mg), which is the product of reference example 24 was subjected to interaction with a solution of hydrogen chloride in dioxane (4n., 3,30 ml) and the reaction mixture was treated with obtaining the connection specified in the header (257 mg) as a white powder. So pl. 134-135oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm of 2.23 (6H, s), 2,90 (1H, DD, J=9,5, 14,5 Hz), 3,05 (1H, DD, J=1,5, 14,5 Hz), 3,61 (2H, q, J=5.5 Hz), 4,07 (2H, t, J= 5.5 Hz), 4,32 (1H, DD, J=1.5 and 9.5 Hz), 6,74 (2H, d, J=7.5 Hz), is 6.78 (1H, d, J=7.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=7.5 Hz), 7,19 (2H, d, J= 8.5 Hz), 7,31 (2H,s), 7,66 (2H, d, J=8.5 Hz), 7,89 (2H, d, J=8.5 Hz), 8,54 (1H, user.C) 8,68 (1H, user.t).

(Example 84)

Ethyl 3-[4-[2-(2-methoxypyridine-5-carbylamine)ethoxy] phenyl]-2 - phenoxypropionate (ethyl ether illustrative compounds N 6-96)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl] -2-phenoxypropionate (753 mg), which is the product of reference example 4, 6-methoxynicotinic acid (350 mg) and carbonyldiimidazole (445 mg) and the reaction mixture was treated with obtaining the connection specified in the header (355 mg) as a white powder. So pl. 114-116oC.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 3,17-3,20 (2H, m), 3,85 (2H, q, J=5.0 Hz), 3,98 (3H, s), of 4.12 (2H, t, J=5.0 Hz), 4,18 (2H, q, J=7.0 Hz), to 4.73 (1H, DD, J=6,0, 7,0 the x2">

(Example 85)

3-[4-[2-(2-Methoxypyridine-5-carbylamine)ethoxy] phenyl] -2 - phenoxypropionic acid (illustrative compound N 6-96)

In the same way as described in example 2, ethyl 3-[4-[2-(2-methoxypyridine-5-carbylamine)ethoxy] phenyl] -2-phenoxypropionate (330 mg), which is the product of example 84 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 2.50 ml) and the reaction mixture was treated with obtaining the connection specified in the header (260 mg) as colorless crystals. So pl. 145-146,5oC.1H-NMR (270 MHz, CD3Cl): ppm 3,18 is 3.23 (2H, m), 3,81 (2H, q, J=5.0 Hz), of 3.97 (3H, s), 4,14 (2H, t, J=5.0 Hz), 4,71 (1H, DD, J=5,5, 7,0 Hz), 6,76 (1H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 6,93 (1H, t, J=8.0 Hz), 7,02-7,11

(1H, m), 7,17-7,27 (4H, m), 8,02 (1H, DD, J=2.5 and 8.5 Hz), at 8.60 (1H, d, J=2.5 Hz).

(Example 86)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-(4 - isopropylphenoxy)propionate (ethyl ester of illustrative compounds N 7-15)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate (723 mg), which is the product of reference example 25, biphenyl-4-carboxylic acid (303 mg), diethylthiophosphate (0.25 ml) and triethylamine (0,47 ml), and reacts>NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7,0 Hz) to 1.21 (3H, t, J=7.0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3,15-3,20 (2H, m) to 3.89 (2H, q, J=5.0 Hz), is 4.15 (2H, t, J= 5.0 Hz), 4,20 (2H, q, J=7.0 Hz), 4,69 (1H, DD, J=5,5, 7.5 Hz), only 6.64 (1H, t, J= 5.0 Hz), 6,76 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J= 8.5 Hz), 7,24 (2H, d, J=8.5 Hz), 7,35-7,51 (3H, m), to 7.59-7,63 (2H, m), 7,66 (2H, d, J=8.5 Hz), 7,86 (2H, d, J=8,5 Hz).

(Example 87)

3-[4-[2-(Biphenyl-4-carbylamine)ethoxy] phenyl] -2-(4-isopropylphenoxy)propionic acid (illustrative compound N 7-15)

In the same way as described in example 2, ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-(4-isopropylphenoxy)propionate (630 mg), which is the product of example 86 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (510 mg) as a white powder. So pl. 172-173oC.1H-NMR (270 MHz, CD3Cl): ppm of 1.18 (6H, d, J=7,0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3,21 (2H, d, J=6.0 Hz), 3,86 (2H, q, J= 5.0 Hz), of 4.12 (2H, t, J=5.0 Hz), 4,78 (1H, t, J=6.0 Hz), of 6.68 (1H, t, J=5.0 Hz), 6,79 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J=8.5 Hz), 7,35-7,49 (3H, m), EUR 7.57 to 7.62 (2H, m), the 7.65 (2H, d, J=8.5 Hz), the 7.85 (2H, d, J=8,5 Hz).

(Example 88)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(4'-methoxybiphenyl-4-carbylamine)ethoxy]phenyl]propionate (ethyl ester illustrative-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate (723 mg), which is the product of reference example 25, 4'-methoxy-biphenyl-4-carboxylic acid (350 mg), diethylthiophosphate (0.25 ml) and triethylamine (0,47 ml) and the reaction mixture was treated with obtaining the connection specified in the header (600 mg) as a white powder. So pl. 116-117oC.1H-NMR (270 MHz, CDCl3): of 1.18 ppm (6N, d, J=7,0 Hz) of 1.20 (3H, t, J=7.0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3.15 and 3.21-in (2H, m), 3,86 (3H, s), 3,86-3,91 (2H, m), 4,14 (2H, t, J=5.0 Hz), 4,18 (2H, q, J=7.0 Hz), 4,69 (1H, DD, J= 6,0, 7,0 Hz), 6,62 (1H, t, J=5.0 Hz), 6,76 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), of 6.99 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J=8.5 Hz), 7,55 (2H, d, J=8.5 Hz), to 7.61 (2H, d, J=8.0 Hz), 7,83 (2H, d, J=8.0 Hz).

(Example 89)

2-(4-Isopropylphenoxy)-3-[4-[2-(4'-methoxybiphenyl-4-carbylamine)ethoxy]phenyl]propionic acid (illustrative compound N 7-179)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(4'-methoxybiphenyl-4-carbylamine)ethoxy] phenyl] propionate (580 mg), which is the product of example 88, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (450 mg) as a white powder. So pl. 159-160oC.1H-NMR (270 MHz, CD3Cl): ppm of 1.18 (6H, d, J= 6.5 Hz), 2.77-to 2,80 (1H, m), 3,18-of 3.27 (2H, m), 3,80-3,90 (5H, m), 4,10-4,18 (2H, m) is), to 7.59 (2H, d, J=8.0 Hz), 7,81 (2H, d, J=8.0 Hz).

(Example 90)

Ethyl 3-[4-[2-(4'-forbiden-4-carbylamine)ethoxy] phenyl] -2-(4-isopropylphenoxy)propionate (ethyl ester of illustrative compounds N 7-190)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate (723 mg), which is the product of reference example 25, 4'-forbiden-4-carboxylic acid (331 mg), diethyl cyanophosphonate (0.25 ml) and triethylamine (0,47 ml) and the reaction mixture was treated with obtaining the connection specified in the header (460 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7,0 Hz) of 1.20 (3H, t, J=7.0 Hz), 2,82 (1H, septet, J= 7.0 Hz), 3,12-3,18 (2H, m), 3,88 (2H, q, J=5.0 Hz), of 4.13 (2H, t, J= 5.0 Hz), 4,18 (2H, q, J=7.0 Hz), 4,69 (1H, DD, J=6,0, 7,0 Hz), 6,63 (1H, t, J= 5.0 Hz), to 6.75 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,00-7,29 (6H, m), 7,53-of 7.60 (2H, m), 7,60 (2H, d, J=8.5 Hz), to 7.84 (2H, d, J=8,5 Hz).

(Example 91)

3-[4-[2-(4'-Forbiden-4-carbylamine)ethoxy] phenyl] -2-(4 - isopropylphenoxy)propionic acid (illustrative compound N 7-190)

In the same way as described in example 2, ethyl 3-[4-[2-(4'-forbiden-4-carbylamine)ethoxy] phenyl] -2-(4-isopropylphenoxy)propionate (450 mg), which is the product of example 90, E-connection, specified in the header (380 mg) as a white powder. So pl. 192-193oC.1H-NMR (270 MHz, CD3Cl): ppm of 1.17 (6H, d, J= 7,0 Hz), 2,84 (1H, septet, J=7.0 Hz), 3,18 (2H, d, J=6.0 Hz), a-3.84 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), of 4.66 (1H, t, J=6.0 Hz), 6,77 (2H, d, J= 8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,10-7,19 (2H, m), 7,22-7,33 (3H, m), 7,55 to 7.62 (4H, m), of 7.90 (2H, d, J=8,5 Hz).

(Example 92)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(3'-methoxybiphenyl-4-carbylamine)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 7-212)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate (723 mg), which is the product of reference example 25, 3'-methoxybiphenyl-4-carboxylic acid (350 mg), diethylthiophosphate (0.25 ml) and triethylamine (0,47 ml) and the reaction mixture was treated with obtaining the connection specified in the header (700 mg) as a pale yellow oil. 1H-NMR (270 MHz, CDCl3): ppm to 1.22 (6H, d, J=7,0 Hz) of 1.24 (3H, t, J=7.0 Hz), 2,85 (1H, septet, J=7.0 Hz), 3,18-of 3.25 (2H, m), 3,91 (3H, s), 3,92-3,99 (2H, m), 4,12-to 4.28 (4H, m), to 4.73 (1H, DD, J=6,0, 7,0 Hz), 6,62-6,70 (1H, m), 6,79 (2H, d, J= 8.5 Hz), make 6.90 (2H, d, J=8.5 Hz), 6,97 (1H, DD, J=2.5 and 8.0 Hz), 7,12 (2H, d, J=8.5 Hz), 7,17 (1H, d, J=2.5 Hz), 7,20-7,30 (3H, m), 7,41 (1H, t, J=8.0 Hz), 7,69 (2H, d, J=8.5 Hz), 7,88 (2H, d, J=8,5 Hz).

(Example 93)

2-(4-EDINENIE N 7-212)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(3'-methoxybiphenyl-4-carbylamine)ethoxy] phenyl] propionate (700 mg), which is the product of example 92, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (310 mg) as a white powder. So pl. 138-139oC.1H-NMR (270 MHz, CD3Cl): ppm of 1.24 (6H, d, J= 7,0 Hz), 2,89 (1H, septet, J=7.0 Hz), with 3.27 (2H, d, J=6.0 Hz), 3,93 (3H, s), 3,84-of 3.96 (2H, m), 4,18 (2H, t, J=5.0 Hz), is 4.85 (1H, t, J=6.0 Hz), 6,74 (1H, t, J=5.0 Hz), 6,85 (2H, d, J=8.5 Hz), 6,91 (2H, d, J=8.5 Hz), of 6.99 (1H, DD, J=2.5 and 8.0 Hz), 7,16 (2H, d, J=8.5 Hz), 7,20-7,27 (2H, m), 7,29 (2H, d, J= 8.5 Hz), 7,44 (1H, t, J=8.0 Hz), of 7.70 (2H, d, J=8.0 Hz), of 7.90 (2H, d, J= 8.0 Hz).

(Example 94)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(2'-methoxybiphenyl-4-carbylamine)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 7-219)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate (723 mg), which is the product of reference example 25, 2'-methoxybiphenyl-4-carboxylic acid (350 mg), diethylthiophosphate (0.25 ml) and triethylamine (0,47 ml) and the reaction mixture was treated with obtaining compounds of the criminal code is a 7.0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3,15-3,20 (2H, m), 3,81 (3H, s), 3,88 (2H, q, J= 5.0 Hz), 4,14 (2H, t, J=5.0 Hz), 4,18 (2H, q, J=7.0 Hz), of 4.66-4.72 in (1H, m), 6,62 (1H, t, J=5.0 Hz), 6,76 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 6,98-7,10 (4H, m), 7,21-7,38 (4H, m), 7,60 (2H, d, J=8.0 Hz), 7,81 (2H, d, J=8.0 Hz).

(Example 95)

Sodium 2-(4-isopropylphenoxy)-3-[4-[2-(2'-methoxybiphenyl-4-carbylamine)ethoxy]phenyl]propionate (illustrative compound N 7-219)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(2'-methoxybiphenyl-4-carbylamine)ethoxy] phenyl] propionate (700 mg), which is the product of example 94, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (528 mg) as a white powder. So pl. 205-208oC.1H-NMR of the free acid (270 MHz, CD3Cl): ppm of 1.18 (6H, d, J=7,0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3,21 (2H, d, J= 6.5 Hz), 3,80 (3H, s), 3,86 (2H, q, J=5.0 Hz), of 4.12 (2H, t, J=5.0 Hz), 4,78 (1H, t, J=6.5 Hz), 6,66 (1H, t, J=5.0 Hz), 6,78 (2H, d, J=8.5 Hz), at 6.84 (2H, d, J=8.5 Hz), 6,97-7,07 (2H, m), 7,10 (2H, d, J=8.5 Hz), 7,22 (2H, d, J=8.5 Hz), 7,28-7,37 (2H, m), to 7.59 (2H, d, J=8.5 Hz), 7,80 (2H, d, J=8,5 Hz).

(Example 96)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(2-phenylpyridine-5-carbylamine)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 7-95)

The reaction was carried out I mg), which is the product of reference example 5, 6-phenyldiamine acid (438 mg) and carbonyldiimidazole (357 mg) and the reaction mixture was treated with obtaining the connection specified in the header (196 mg) as colorless crystals. So pl. 113-114oC.1H-NMR (270 MHz, CDCl3): ppm 1,10-of 1.23 (9H, m), 2,72-is 2.88 (1H, m), 3,12-3,19 (2H, m), 3,82-3,93 (2H, m), 4,10-to 4.23 (4H, m), 4,69 (1H, DD, J=5,5, 7.5 Hz), 6,61-6,69 (1H, m), of 6.75 (2H, d, J=8.5 Hz), 6,86 (2H, d, J= 8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,24 (2H, d, J=8.5 Hz), 7,41-7,53 (3H, m), 7,81 (1H, d, J=8.5 Hz), 8,00-8,08 (2H, m), 8,12-to 8.20 (1H, m), 9,01-9,39 (1H, m).

(Example 97)

2-(4-Isopropylphenoxy)-3-[4-[2-(2-phenylpyridine-5-carbylamine)ethoxy] phenyl]propionic acid (illustrative compound N 7-95)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(2-phenylpyridine-5-carbylamine)ethoxy]phenyl]propionate (169 mg), which is the product of example 96, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (126 mg) as colorless crystals. So pl. 174-176oC.1H-NMR (270 MHz, CD3Cl): ppm to 1.19 (6H, d, J= 7,0 Hz), 2,79-2,90 (1H, m), with 3.27 (2H, d, J=5.5 Hz), 3,71-3,88 (1H, m), 3,88-4,01 (1H, m), 4,28-and 4.40 (2H, m), 4,94 (1H, t, J=5.5 Hz), 6,50-6,59 (1H, m), at 6.84 (2H, d, J=8.5 Hz), to 6.95 (2H, d, J=8.5 Hz), 7,11 (2H, d, J=8,5 Hz)XI)-3-[4-[2-(2-(4-methoxyphenyl)pyridine-5 - carbylamine)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 7-233)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl] -2-(4-isopropylphenoxy)propionate (743 mg), which is the product of reference example 5 6-(4-methoxyphenyl)nicotinic acid (504 mg), which is the product of reference example 26, and carbonyldiimidazole (357 mg) and the reaction mixture was treated with obtaining the connection specified in the header (182 mg) as colorless crystals. So pl. 100-101oC.1H-NMR (270 MHz, CDCl3): ppm 1,13-of 1.23 (9H, m), 2,74-2,89 (1H, m), 3,12-3,19 (2H, m), 3,88 (3H, s), 3,86-3,93 (2H, m), 4,11-to 4.23 (4H, m), 4,69 (1H, DD, J=5,5, 7.5 Hz), 6,59-of 6.65 (1H, m), of 6.75 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,01 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J= 8.5 Hz), 7,24 (2H, d, J=8.5 Hz), 7,74 (1H, d, J=8.5 Hz), 8,00 (2H, d, J=8.5 Hz), 8,13 (1H, DD, J=2,0, 8.5 Hz), 9,01 (1H, d, J=2.0 Hz).

(Example 99)

2-(4-Isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)pyridine-5 - carbylamine]ethoxy]phenyl]propionic acid (illustrative compound N 7-233)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)pyridine-5 - carbylamine]ethoxy]phenyl]propionate (170 mg), which is the product of example 98, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.58 ml) and the reaction mixture was treated with obtaining compounds of the criminal code is 20 (6H, d, J=7,0 Hz), 2,78-2,90 (1H, m), with 3.27 (2H, d, J=5.5 Hz), 3,86 (3H, s), 3,70-4,01 (2H, m), 4,29-4,39 (2H, m), of 4.95 (1H, t, J=5.5 Hz), to 6.43-6,51 (1H, m), at 6.84 (2H, d, J=8.5 Hz), 6.90 to-7,00 (4H, m), 7,12 (2H, d, J=8.5 Hz), 7,30 (2H, d, J=8.5 Hz), 7,73 (1H, d, J=8.5 Hz), 7,80-7,88 (2H, m), 8,19 (1H, d, J= 2.5 Hz), of 8.27 (1H, DD, J=2.5 and 8.5 Hz).

(Example 100)

Ethyl 3-[4-[2-[2-(4-forfinal)pyridine-5-carbylamine] ethoxy]phenyl]-2-(4-isopropylphenoxy)propionate (ethyl ester of illustrative compounds N 7-231)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate (718 mg), which is the product of reference example 25, 6-(4-forfinal)nicotinic acid (330 mg), which is the product of reference example 27, diethylthiophosphate (0.25 ml) and triethylamine (0,47 ml) and the reaction mixture was treated with obtaining the connection specified in the header (560 mg) in the form of a white powder. So pl. 117-118oC. 1H-NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7,0 Hz) to 1.21 (3H, t, J=7.0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3,15-3,20 (2H, m), 3,90 (2H, q, J=5.0 Hz), 4,13-422 (4H, m), 4,69 (1H, DD, J=5,5, 7,0 Hz), 6,66 (1H, t, J=5.0 Hz), 6.75 in (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,14 - of 7.25 (4H, m), 7,76 (1H, d, J= 8.5 Hz), 8,00-8,07 (2H, m), 8,16 (1H, DD, J=2,0, 8.5 Hz), 9,03 (1H, d, J=2.0 Hz).

(Example 101)

3-[4-[2-[2-(4-Forfinal)pyridine-5-carbylamine]amatory described in example 2, ethyl 3-[4-[2-[2-(4-forfinal)pyridine-5-carbylamine] ethoxy]phenyl]-2-(4-isopropylphenoxy)propionate (540 mg), which is the product of example 100 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 3.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (495 mg) as a white powder. So pl. 199-200oC.1H-NMR (270 MHz, CD3Cl): ppm of 1.20 (6H, d, J=7,0 Hz), 2,84 (1H, septet, J=7.0 Hz), 3,20 is 3.23 (2H, m), 3,86 (2H, q, J= 5.5 Hz), is 4.21 (2H, t, J=5.5 Hz), 4,70 (1H, DD, J=5,5, 7,0 Hz), to 6.80 (2H, d, J=8.5 Hz), 6.89 in (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,13-7,30 (4H, m), 7,79 (1H, d, J=8.5 Hz), 7,92 (1H, t, J=5.5 Hz), 8,03-of 8.09 (2H, m), of 8.25 (1H, DD, J=2,0, 8.5 Hz), 9,12 (1H, d, J=2.0 Hz).

(Example 102)

Ethyl 3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] -phenyl] -2-(4-isopropylphenoxy)propionate (ethyl ester of illustrative compounds N 7-236)

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl] -2-(4-isopropylphenoxy)propionate (500 mg), which is the product of reference example 5 6-(2,2,3,3-tetrafluoropropoxy)nicotinic acid (375 mg), which is the product of reference example 28, and carbonyldiimidazole (240 mg) and the reaction mixture was treated with obtaining the connection specified in the header (137 mg) in the form), 4,08-of 4.25 (4H, m), 4,68-4,87 (3H, m), of 5.99 (1H, TT, J=4,5, 53 Hz), 6,63-6,89 (6H, m), was 7.08 (2H, d, J= 8.5 Hz), 7,22 (2H, d, J=8.5 Hz), with 8.05 (1H, DD, J=2.5 and 8.5 Hz), 8,58 (1H, d, J=2.5 Hz).

(Example 103)

Sodium 3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl] -2-(4-isopropylphenoxy)propionate (illustrative compound N 7-236)

In the same way as described in example 2, ethyl 3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl] -2-(4-isopropylphenoxy)propionate (73 mg), which is the product of example 102 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.13 ml) and the reaction mixture was treated with obtaining the connection specified in the header (51 mg) as colorless crystals. So pl. 204-207oC.1H-NMR (270 MHz, deuterated methanol): ppm 1,11-to 1.21 (6H, m), 2,77 (1H, septet, J=7.0 Hz), 2,99-3,17 (2H, m), of 3.73 (2H, t, J=5.5 Hz), of 4.12 (2H, t, J=5.5 Hz), 4,78-of 4.90 (3H, m), 6,30 (1H, TT, J=5,0, 53 Hz), 6,74 (2H, d, J=8,5 Hz), 6,85 (2H, d, J=8.5 Hz), 6,93 (1H, d, J=8.5 Hz), 7,01 (2H, d, J=8.5 Hz), 7,25 (2H, d, J=8.5 Hz), 8,13 (1H, DD, J=2.5 and 8.5 Hz), 8,64 (1H, d, J=2.5 Hz).

(Example 104)

(S)-2-(4-Isopropylphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (optically active compound illustrative compound N 7-35)

To a solution of 2-trimethylsilylmethyl(S)-2-(4-isopropylphenoxy)-3-[4-[2-(4-parahydrogen (4.0 ml) at room temperature was added a solution of tetrabutylammonium fluoride in tetrahydrofuran (1M, of 2.25 ml). 3 Quiroga mixture was stirred for 1 hour, the reaction mixture was concentrated under reduced pressure. The residue was separated between ethyl acetate and water. An ethyl acetate layer was washed with an aqueous solution chloroethanol acid (0,5 N.) and saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. The residue was purified by thin layer chromatography, using as eluent dichloromethane/methanol = 5/1. The product was led from diisopropyl ether to obtain the connection specified in the header (278 mg) as colorless crystals. So pl. 100-101oC. []D25+13,9o(c = 0.9, chloroform).1H-NMR (400 MHz, CDCl3): ppm of 1.11 (6H, d, J=7,0 Hz), is 2.74 (1H, septet, J= 7.0 Hz), 3,02-and 3.16 (2H, m), of 3.73-3,82 (2H, m), 3,98-4,07 (2H, m), 4.63 to-4,74 (1H, m), 6,69-to 6.80 (4H, m), 6,95-7,01 (3H, m), 7,11 (2H, d, J=8.0 Hz), 7,25-7,31(1H, m), to 7.68 (1H, d, J=8.0 Hz), 7,72-a 7.85 (3H, m), to 7.93 (2H, d, J= 8.0 Hz), 8,69 (1H, d, J=4.5 Hz).

(Example 105)

(R)-2-(4-Isopropylphenoxy)-3-[4-[2-(4-pyridine-2-eventelement)ethoxy] phenyl] propionic acid (optically active compound illustrative compound N 7-35)

The reaction was conducted in the same manner as described in example 104, using 2-trimethylsilylmethyl(R)-2-(4-isopropylphenoxy)-3-[4 and tetrabutylammonium fluoride in tetrahydrofuran (1M, 1.08 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (117 mg) as colorless crystals. So pl. 95-96oC. []D25situated 10.5o(c = 1.5, chloroform).1H-NMR (400 MHz, CDCl3): ppm of 1.11 (6H, d, J= 7,0 Hz), 2,73 (1H, septet, J=7.0 Hz), 3,02-and 3.16 (2H, m), of 3.73-3,82 (2H, m), 3,98-4,07 (2H, m), 4.63 to-4,74 (1H, m), 6,69-to 6.80 (4H, m), 6,95-7,02 (3H, m), 7,12 (2H, d, J= 8.0 Hz), 7,25-7,31(1H, m), the 7.65 (1H, d, J=8.0 Hz), 7,72-7,83 (3H, m), 7,88 (2H, d, J=8.0 Hz), to 8.70 (1H, d, J=4.5 Hz).

(Example 106)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-triptorelin-6-yl)benzoylamine] ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 7-227)

To a solution of 3-triptorelin-6-eventing acid (546 mg) in toluene (28,0 ml) at room temperature was added one drop of N,N-dimethylformamide and thionyl chloride (0.75 ml). Then the mixture was stirred for 4 hours at 85oC, the solvent drove and thionyl chloride azeotrope was evaporated to dryness with toluene under reduced pressure. To a solution of the residue obtained above and ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(4-isopropylphenoxy)propionate (201 mg), which is the product of reference example 5, in dichloromethane (10 ml) in an ice bath was added triethylamine (1.23 ml). Then the mixture was stirred for 30 minutes, the reaction mixture was concentrate is one sodium chloride and dried over anhydrous magnesium sulfate, and then was evaporated under reduced pressure. The residue was purified by chromatography on a column of silica gel using as eluent hexane/ethyl acetate = 3/2-1/1, to obtain the compound indicated in heading (570 mg) as a yellow foamy mass.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7,0 Hz) to 1.21 (3H, t, J=7.0 Hz), of 2.81 (1H, septet, J=7.0 Hz), 3,17 (2H, d, J=6.5 Hz), 3,90 (2H, q, J=5.0 Hz), 4,14 (2H, t, J=5.0 Hz), 4,18 (2H, t, J= 7.0 Hz), 4,70 (1H, t, J=6.5 Hz), to 6.67 (1H, user.t) of 6.75 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,24 (2H, d, J=8.5 Hz), 7,88 (1H, d, J= 8.5 Hz), to $ 7.91 (2H, d, J=8.5 Hz), 8,01 (1H, d, J=8,5 Hz) to 8.12 (2H, d, J=8.5 Hz), 8,99 (1H, s).

(Example 107)

2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-triptorelin-6-yl)benzoylamine] ethoxy]phenyl]propionic acid (illustrative compound N 7-227)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-triptorelin-6-yl)benzoylamine]ethoxy]phenyl]propionate (500 mg), which is the product of example 106 were subjected to contact with an aqueous solution of sodium hydroxide (1 n 1,60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (383 mg) as a white powder. So pl. 212-214oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 1,13 (6N, d, J=7,0 Hz), 2,78 (1H, septet, J=7.0 Hz), of 3.07 (1H, Is, J=8.5 Hz), 7.23 percent (2H, d, J=8.5 Hz), 8,02 (2H, d, J=8.5 Hz), of 8.27 (2H, d, J=8.5 Hz), 8.30 to-at 8.36 (2H, m), 8,84 (1H, user.t), the remaining 9.08 (1H, s).

(Example 108)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-nitropyridine-6-yl)benzoylamine]ethoxy]phenyl]propionic acid (ethyl ester of illustrative compounds N 7-228)

The reaction was conducted in the same manner as described in example 79, using ethyl 3-[4-(2-aminoethoxy)phenyl] -2-(4-isopropylphenoxy)propionate (290 mg), which is the product of reference example 5, 3-nitropyridine-6-eventing acid (277 mg), which is the product of reference example 32, diethylthiophosphate (of 0.18 ml) and triethylamine (0,29 ml) and the reaction mixture was treated with obtaining the connection specified in the header (379 mg) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7,0 Hz) to 1.21 (3H, t, J=7.0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3,17 (1H, d, J=5.0 Hz), 3,18 (1H, d, J=7.5 Hz), 3,90 (2H, q, J=5.0 Hz), 4,06-4,39 (4H, m), 4,69 (1H, DD, J= 5.0 and 7.5 Hz), of 6.68 (1H, user.t) of 6.75 (2H, d, J=8.5 Hz), 6,86 (2H, d, J= 8.5 Hz), 7,13 (2H, d, J=8.5 Hz), 7,24 (2H, d, J=8.5 Hz), to 7.93 (2H, d, J=8.5 Hz), 7,95 (1H, d, J=8.5 Hz), 8,17 (2H, d, J=8.5 Hz), 8,56 (1H, DD, J=2,0, 8,5 Hz), of 9.51 (1H, d, J=2.0 Hz).

(Example 109)

2-(4-Isopropylphenoxy)-3-[4-[2-[4-(3-nitropyridine-6 - yl)benzoylamine]ethoxy]phenyl]propionic acid (illustrative compound N 7-228)

In the same way that is described is that is the product of example 108, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 1.30 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (216 mg) as a white powder. So pl. 198-199oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm of 1.13 (6H, d, J=7,0 Hz), and 2.79 (1H, septet, J=7.0 Hz), of 3.07 (1H, d, J= 7.5 Hz), to 3.09 (1H, d, J=5.5 Hz), the 3.65 (2H, q, J=5.5 Hz), 4,11 (2H, t, J= 5.5 Hz), 4,78 (1H, DD, J=5,5, 7.5 Hz), 6,74 (2H, d, J=8.5 Hz), make 6.90 (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J=8.5 Hz), of 8.04 (2H, d, J=8.5 Hz), 8,31 (2H, d, J=8.5 Hz), at 8.36 (1H, d, J=8.5 Hz), to 8.70 (1H, DD, J=2,0, 8.5 Hz), 8,86 (1H, user.t), for 9.47 (1H, d, J=2.0 Hz).

(Example 110)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-methoxypyridine-6-yl)benzoylamine] ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 7-222)

The reaction was conducted in the same manner as described in example 106, using ethyl 3-[4-(2-aminoethoxy)phenyl] -2-(4-isopropylphenoxy)propionate (301 mg), which is the product of reference example 5, 3-methoxypyridine-6-eventing acid (195 mg), which is the product of reference example 33, thionyl chloride (0,31 ml) and triethylamine (0,36 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (199 mg) as a white powder. So pl. 118-119oC.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7.0 G(2H, kV, J=7,0 Hz), 4,69 (1H, DD, J=5.0 and 7.5 Hz), 6,63 (1H, user.t) 6,76 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J= 8.5 Hz), 7.23 percent (2H, d, J=8.5 Hz), 7,28 (1H, DD, J=3,0, 8.5 Hz), 7,71 (1H, d, J=8.5 Hz), 7,86 (2H, d, J=8.5 Hz), 8,01 (2H, d, J=8,5 Hz), to 8.41 (1H, d, J=3.0 Hz).

(Example 111)

2-(4-Isopropylphenoxy)-3-[4-[2-[4-(3-methoxypyridine-6 - yl)benzoylamine] ethoxy]phenyl]propionic acid (illustrative compound N 7-222)

In the same way as described in example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-methoxypyridine-6 - yl)benzoylamine] ethoxy]phenyl]propionate (210 mg), which is the product of example 110 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 0,72 ml) and the reaction mixture was treated with obtaining the connection specified in the header (185 mg) as a white powder. So pl. 145-146oC.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (6H, d, J=7,0 Hz), and 2.83 (1H, septet, J=7.0 Hz), up 3.22 (2H, d, J=6.0 Hz), 3,88 (2H, q, J=5.0 Hz), 3,91 (3H, s), 4,20 (2H, t, J=5.0 Hz), 4,82 (1H, t, J=6.0 Hz), of 6.65 (1H, user.t), 6,83 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,11 (2H, d, J= 8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7,32 (1H, DD, J=3,0, 9.0 Hz), to 7.67 (1H, d, J=9.0 Hz), of 7.75 (2H, d, J=8.5 Hz), 7,88 (2H, d, J=8,5 Hz), to 8.41 (1H, d, J=3.0 Hz).

(Example 112)

Ethyl 3-[4-[2-[4-(3-dimethylaminopyridine-6 - yl)benzoylamine]ethoxy]phenyl] -2-(4-isopropylphenoxy)propionate (ethyl ester of illustrative compounds N 7-225)

Reactions)propionate (370 mg), which is the product of reference example 5, 3-dimethylaminopyridine-6-eventing acid (221 mg), which is the product of reference example 34, thionyl chloride (0,34 ml) and triethylamine (0.51 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (456 mg) in the form of a foamy mass.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (6H, d, J=7,0 Hz) of 1.20 (3H, t, J=7.0 Hz), 2,82 (1H, septet, J=7.0 Hz), 3.04 from (6H, s), and 3.16 (1H, d, J=5.0 Hz), 3,17 (1H, d, J=7.5 Hz), 3,88 (2H, q, J=5.0 Hz), 4,14 (2H, t, J= 5.0 Hz), 4,18 (2H, q, J=7,0 Hz), 4,69 (1H, DD, J=5.0 and 7.5 Hz), 6,76 (2H, d, J= 8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,06 (1H, DD, J=2.5 and 9.0 Hz), was 7.08 (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J=8.5 Hz), 7,45 (1H, user.t) to 7.64 (1H, d, J= 9.0 Hz), 7,83 (2H, d, J=8.5 Hz), 8,00 (2H, d, J=8.5 Hz), 8,23 (1H, d, J= 2.5 Hz).

(Example 113)

3-[4-[2-[4-(3-Dimethylaminopyridine-6-yl)benzoylamine] ethoxy] phenyl] -2-(4-isopropylphenoxy)propionic acid (illustrative compound N 7-225)

In the same way as described in example 2, ethyl 3-[4-[2-[4-(3-dimethylaminopyridine-6-yl)benzoylamine] ethoxy] phenyl] -2-(4 - isopropylphenoxy)propionate (429 mg), which is the product of example 112 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 1.44 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (219 mg) as a white powder. So pl. 150-151oC.d, J=8,5, 14,5 Hz) and 3.15 (1H, DD, J= 4,5, 14,5 Hz), 3,76 (2H, t, J=5.5 Hz), 4,14 (2H, t, J=5.5 Hz), 4,58 (1H, DD, J= 4,5, 8.5 Hz), 6,74 (2H, d, J=8.5 Hz), 6.87 in (2H, d, J=8.5 Hz), 7,02 (2H, d, J=8.5 Hz), 7,22 (1H, DD, J=3,0, 9.0 Hz), 7.23 percent (2H, d, J= 8.5 Hz), 7,72 (1H, d, J=9.0 Hz), the 7.85-of 7.95 (4H, m), 8,11 (1H, d, J=3.0 Hz).

(Example 114)

Ethyl 2-(4-methylphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 14-11)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-methylphenoxy)propionate (798 mg), which is the product of reference example 35, 4-pyridine-2-eventing acid (365 mg), diethylthiophosphate (0,28 ml) and triethylamine (0,46 ml) and the reaction mixture was treated with obtaining the connection specified in the header (680 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.23 (3H, t, J=7.0 Hz), 2,28 (3H, s), 3,14-up 3.22 (2H, m), 3,88-of 3.96 (2H, m), 4,11-4,27 (4H, m), to 4.73 (1H, t, J=6.0 Hz), 6,62-of 6.71 (1H, m), 6,76 (2H, d, J=8.5 Hz), make 6.90 (2H, d, J=8.5 Hz), 7,05 (2H, d, J=8.5 Hz), 7,22-7,33 (3H, m), 7,78-7,83 (2H, m), 7,92 (2H, d, J=8.5 Hz), 8,11 (2H, d, J=8.5 Hz), 8,71-8,78 (1H, m).

(Example 115)

2-(4-Methylphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionic acid (illustrative compound N 14-11)

In the same way as described in example 2, ethyl 2-(4-methylphenoxy)-3-[4-Samadashvili with an aqueous solution of sodium hydroxide (1 N., 2,60 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (570 mg) as a white powder. So pl. 129-131oC.1H-NMR (270 MHz, CDCl3): ppm of 2.25 (3H, s), 3,21 (2H, d, J= 6.0 Hz), 3,81-are 3.90 (2H, m), 4,15-is 4.21 (2H, m), 4,80 (1H, t, J=6.0 Hz), 6,68 to 6.75 (1H, m), 6,79 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,03 (2H, d, J=8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7.29 trend and 7.36 (1H, m), 7,70-7,88 (4H, m), 7,92 (2H, d, J=8.5 Hz), 8,69-8,73 (1H, m).

(Example 116)

Ethyl 2-(4-tert-butylphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 138-8)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-tert-butylphenoxy)propionate (530 mg), which is the product of reference example 36, 4-pyridine-2-eventing acid (227 mg), diethylthiophosphate (of 0.18 ml) and triethylamine (0.33 ml) and the reaction mixture was treated with obtaining the connection specified in the header (370 mg) as a foamy mass.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7.0 Hz), 1,25 (9H, s), 3,15-3,20 (2H, m) to 3.89 (2H, q, J= 5.0 Hz), 4,10-422 (4H, m), 4,69 (1H, DD, J=5,5, 7.5 Hz), 6,66 (1H, t, J= 5.0 Hz), 6,76 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7.23 percent-7,30 (5H, m), 7,74-7,80 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 117)

2-(4-Tert-butylphenoxy)-3-[4-[2-(4-PIM, which is described in example 2, ethyl 2-(4-tert-butylphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (360 mg), which is the product of example 116 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (315 mg) as a white powder. So pl. 94-96oC.1H-NMR (270 MHz, CDCl3): ppm of 1.24 (9H, s), 3,20 (2H, d, J=6.0 Hz), 3,80-are 3.90 (2H, m), 4,13-4,20 (2H, m), 4,79 (1H, t, J=6.0 Hz), 6,76 (1H, t, J=5.0 Hz), PC 6.82 (2H, d, J=8.0 Hz), 6,85 (2H, d, J=8.0 Hz), 7,22 (2H, d, J=8.0 Hz), of 7.25 (2H, d, J=8.0 Hz), 7,28-to 7.35 (1H, m), 7,70-of 7.90 (4H, m), to $ 7.91 (2H, d, J=8.5 Hz), 8,73 (1H, d, J=4.5 Hz).

(Example 118)

Ethyl 2-(4-pertenece)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 138-56)

The reaction was conducted in the same manner as described in example 65, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(4-pertenece)propionate (2.10 g), which is the product of reference example 37, 4-pyridine-2-eventyrland hydrochloride (1.90 g) and triethylamine (2.20 ml) and the reaction mixture was treated with obtaining the connection specified in the header (2.50 g) as a white powder. So pl. 116-118oC.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J= 7.0 Hz), 3,17 (2H, d, J=6.5 Hz), 3,80-3,91 (2H, m), 4,08-is 4.21 (4H, m), 4,66 (1HP CLASS="ptx2">

(Example 119)

2-(4-Pertenece)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionic acid (illustrative compound N 138-56)

In the same way as described in example 2, ethyl 2-(4-pertenece)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (2,45 g), which is the product of example 118 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 15.0 ml) and the reaction mixture was treated with obtaining the connection specified in the header (2.30 g) as a white powder. So pl. 139-140,5oC.1H-NMR (270 MHz, CDCl3): ppm 3,20 (2H, d, J=6.5 Hz), 3,80-3,91 (2H, m), 4,16-4,22 (2H, m), 4,74 (1H, t, J=6.5 Hz), 6,69-6,77 (1H, m), 6,77-6,92 (6H, m), 7,19 (2H, d, J=8.5 Hz), 7,30-7,37 (1H, m), 7,69-7,80 (3H, m), 7,80-of 7.90 (3H, m) 8,71 (1H, d, J=4.0 Hz).

(Example 120)

Ethyl 2-(4-chlorophenoxy)-3-[4-[2-(4-pyridine-2-eventuallybecome]phenyl] propionate (ethyl ester of illustrative compounds N 138-72)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-chlorophenoxy)propionate (1,23 g), which is the product of reference example 38, 4-pyridine-2-eventing acid (539 mg), diethyl cyanophosphonate (0,41 ml) and triethylamine (0.68 ml) and the reaction mixture was treated with obtaining the connection specified in the RFQ), 3,17 (2H, d, J=6.5 Hz), 3,83-to 3.92 (2H, m), 4,08-is 4.21 (4H, m), 4,69 (1H, t, J=6.5 Hz), 6,60 of 6.68 (1H, m), of 6.75 (2H, d, J=8.5 Hz), 6.87 in (2H, d, J=8.5 Hz), 7,13-7,30 (5H, m), 7,72-7,79 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,70-8,73 (1H, m).

(Example 121)

2-(4-Chlorophenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 138-72)

In the same way as described in example 2, ethyl 2-(4-chlorophenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (950 mg), which is the product of example 120 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 3,49 ml) and the reaction mixture was treated with obtaining the connection specified in the header (834 mg) as colorless crystals. So pl. 155-156oC.1H-NMR (270 MHz, CDCl3): ppm is 3.21 (2H, d, J=6.0 Hz), 3,80-are 3.90 (2H, m), 4,12-4,22 (2H, m), was 4.76 (1H, t, J=6.0 Hz), 6,70-to 6.88 (5H, m), to 7.15 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8.5 Hz), 7,30-7,38 (1H, m), 7,79-of 7.90 (6H, m), 8,70-a total of 8.74 (1H, m).

(Example 122)

Ethyl 3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-(4-triptoreline)propionate (ethyl ester of illustrative compounds N 138-24)

To a solution of ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (332 mg), which is the product of reference example 39, 4-triptoreline (186 mg) and triphenylphosphine (300 mg) in that is a, of 0.52 ml) in toluene (3.0 ml). Then the mixture was stirred for 2 hours at room temperature, the reaction mixture was added triphenylphosphine (100 mg) and diethylazodicarboxylate (40% toluene solution, to 0.19 ml). The mixture was stirred for 18 hours. The reaction mixture was concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/ethyl acetate = 3/2, receiving of the connection specified in the header (283 mg, contains some impurities in the form of a white powder.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J= 7.0 Hz), 3,21 (2H, d, J=6.5 Hz), with 3.89 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J= 5.0 Hz), is 4.21 (2H, q, J=7.0 Hz), of 4.77 (1H, t, J=6.5 Hz), 6,66 (1H, user. t), to 6.88 (2H, d, J=8.5 Hz), make 6.90 (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J= 8.5 Hz), 7,26-7,34 (1H, m), 7,49 (2H, d, J=8.5 Hz), 7,75-7,83 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 123)

3-[4-[2-(4-Pyridine-2-albenzaalbenza)ethoxy] phenyl] -2-(4-triptoreline)propionic acid (illustrative compound N 138-24)

In the same way as described in example 2, ethyl 3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-(4-triptoreline)propionate (269 mg), which is the product of example 122 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.55 ml) and reacts the 54-155oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm to 3.02 (1H, DD, J=5.0 and 13.5 Hz), and 3.16 (1H, DD, J=2.0 a, and 13.5 Hz), 3,63 (2H, q, J= 5.5 Hz), 4,10 (2H, T, J=5.5 Hz), with 4.64 (1H, DD, J=2,0, 5,0 Hz), to 6.88 (2H, d, J=8.5 Hz), to 6.95 (2H, d,

J= 8.5 Hz), 7.23 percent (2H, d, J=8.0 Hz), 7,41 (1H, DD, J=6,0, 7.5 Hz), 7,54 (2H, d, J=8.5 Hz), 7,88-of 7.97 (1H, m), 7,98 (2H, d, J=8.5 Hz), with 8.05 (1H, d, J= 7.5 Hz), 8,18 (2H, d, J=8.0 Hz), to 8.70 (1H, d, J=3.5 Hz), 8,78 (1H, user. t).

(Example 124)

Ethyl 2-(4-methoxyphenoxy)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 8-35)

The reaction was conducted in the same manner as described in example 122 using ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (433 mg), which is the product of reference example 39, 4-methoxyphenol (247 mg), triphenylphosphine (523 mg) and diethylazodicarboxylate (40% toluene solution, of 0.65 ml) and the reaction mixture was treated with obtaining the connection specified in the header (320 mg) as a yellow oil.

1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 3,17 (2H, d, J= 6.5 Hz), and 3.72 (3H, s) to 3.89 (2H, q, J=5.5 Hz), 4,10-is 4.21 (4H, m), 4,63 (1H, t, J= 6.5 Hz), 6,66 (1H, t, J=5.5 Hz), 6.87 in (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J= 8.5 Hz), 7.23 percent-7,30 (1H, m), 7,40-of 7.70 (4H, m), 7,75-7,80 (2H, m), 7,88 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 125)

2-(4-Methoxyphenoxy)-3-[4-[2-(4-pyridine-2 - IV described in example 2, ethyl 2-(4-methoxyphenoxy)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (310 mg), which is the product of example 124 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (150 mg) as a white powder. So pl. of 67.5-70oC.1H-NMR (270 MHz, CDCl3): ppm 3,20 (2H, d, J=6.0 Hz), to 3.73 (3H, s), 3,82-to 3.92 (2H, m), 4,16-of 4.25 (2H, m), 4,74 (1H, t, J=6.5 Hz), 6,65-6,90 (7H, m), 7,21 (2H, d, J=8.5 Hz), 7,27-7,37 (1H, m), 7,70-7,89 (4H, m), to 7.93 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 126)

Ethyl 3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]-2-(4 - triftormetilfosfinov)propionate (ethyl ester of illustrative compounds N 138-40)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-(4 - triftormetilfosfinov) propionate (2,11 g), which is the product of reference example 40 was dissolved in a solution of hydrogen chloride in dioxane (4 N., 30 ml). The mixture was left to stand for 40 minutes at room temperature. Then the reaction mixture was concentrated under reduced pressure and the hydrogen chloride azeotrope was evaporated with toluene. The remainder, which represents ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(4-triptoreline-phenoxy)propionate hydrochloric acid, and 4-pyridine-2-eventuallity is,28 ml) and the mixture was stirred for 1 hour at the same temperature. The reaction mixture was concentrated under reduced pressure. The residue was separated between ethyl acetate and water, and an ethyl acetate layer was separated and washed with saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 2/3, receiving of the connection specified in the header (1.75 g) as colorless crystals. So pl. 87-88oC.1H-NMR (270 MHz, CDCl3): ppm of 1.17 (3H, t, J=7.0 Hz), 3,18 (2H, d, J=6.5 Hz), with 3.89 (2H, q, J=5.0 Hz), 4,10-of 4.25 (4H, m), 4,70 (1H, t, J=6.5 Hz), of 6.65 (1H, user.t), for 6.81 (2H, d, J= 8.5 Hz), to 6.88 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,14-7,31 (1H, m), 7.23 percent (2H, d, J=8.5 Hz), 7,72-of 7.82 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 127)

3-[4-[2-(4-Pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-(4 - triftormetilfosfinov)promonova acid (illustrative compound N 138-40)

In the same way as described in example 2, ethyl 3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] -2-(4 - triftormetilfosfinov)propionate (1.65 g), which is the product of example 126 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 5,54 ml) and the reaction mixture was treated with obtaining tonirovany methanol): and 3.16 ppm (1H, DD, J=8,0, 14,5 Hz), up 3.22 (1H, DD, J=4,5, 14,5 Hz), of 3.78 (2H, q, J=5,5 Hz) to 4.16 (2H, t, J=5.5 Hz), a 4.83 (1H, DD, J=4,5, 8.0 Hz), 6.89 in (2H, d, J=8.5 Hz), 6,91 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=8.5 Hz), from 7.24 (2H, d, J=8.5 Hz), of 7.36 was 7.45 (1H, m), 7,88-to 7.99 (2H, m), 7,94 (2H, d, J= 8.5 Hz), with 8.05 (2H, d, J=8.5 Hz), 8,64 (1H, d, J=5.0 Hz), 8,77 (1H, user. t).

(Example 128)

Ethyl 2-(4-cianfrocca)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 138-104)

The reaction was conducted in the same manner as described in example 126, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-(4 - cianfrocca)propionate (237 mg), which is the product of reference example 41, 4-pyridine-2-eventological (131 mg) and triethylamine (0,29 ml) and the reaction mixture was treated with obtaining the connection specified in the header (244 mg) in the form of syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J= 7.0 Hz), 3,21 (2H, d, J=6.5 Hz), with 3.89 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J= 5.0 Hz), 4,19 (2H, q, J=7.0 Hz), 4,79 (1H, t, J=6.5 Hz), of 6.65 (1H, user.t), to 6.88 (2H, d, J=8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7.24 to 7,31 (1H, m), 7,54 (2H, d, J=8.5 Hz), 7,70-to 7.84 (2H, m), 7,88 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 129)

2-(4-Cianfrocca)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 138-104)

In the same way as described in example 2, e of example 128, was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.92 ml) and the reaction mixture was treated with obtaining the connection specified in the header (184 mg) as colorless crystals. So pl. 92-93oC.1H-NMR (270 MHz, deuterated methanol): ppm 3,24 (2H, d, J=6.0 Hz), 3,86 (2H, q, J=5.5 Hz), 4,15-of 4.25 (2H, m), is 4.85 (1H, t, J= 6.0 Hz), 6,76 (1H, user.t), 6,85 (2H, d, J=8.0 Hz), 6,91 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8.5 Hz), 7,37 (1H, DD, J=5,0, 6,0 Hz), of 7.48 (2H, d, J= 7.5 Hz), 7,73 (3H, d, J=8.0 Hz), to 7.84 (2H, d, J=7.5 Hz), 7,87 (1H, DD, J= 6,0, 8.0 Hz), 8,71 (1H, d, J=5.0 Hz).

(Example 130)

Methyl 2-(4-methylthiophene)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (methyl ether illustrative compounds N 138-120)

The reaction was conducted in the same manner as described in example 126, using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-(4-methylthiophene)propionate (265 mg), which is the product of reference example 42, 4-pyridine-2-eventological (175 mg) and triethylamine (0,32 ml) and the reaction mixture was treated with obtaining the connection specified in the header (164 mg) as colorless crystals. So pl. 94-95oC.1H-NMR (270 MHz, CDCl3): to 2.41 ppm (3H, s), 3,17 (2H, d, J=6.5 Hz), 3,71 (3H, s) to 3.89 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), 4.72 in (1H, t, J=6.5 Hz), 6,66 (1H, user. t) 6,77 (2H, d, J=8.5 Hz), 6.87 in (2H, d, J=8.5 Hz), 7,18 (2H, the 131)

2-(4-Methylthiophene)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 138-120)

In the same way as described in example 2, methyl 2-(4-methylthiophene)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (203 mg), which is the product of example 130 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.74 ml) and the reaction mixture was treated with obtaining the connection specified in the header (153 mg) as colorless crystals. So pl. 168-169oC.1H-NMR (270 MHz, CDCl3): ppm 2.40 a (3H, s), up 3.22 (2H, d, J= 6.0 Hz), a 3.87 (2H, q, J=5.0 Hz), is 4.21 (2H, t, J=5.0 Hz), 4,80 (1H, t, J=6.0 Hz), 6,72 (1H, user.t), at 6.84 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7,34 (1H, DD, J= 5.0 and 7.0 Hz), 7,74 (1H, DD, J=7,0, 7.5 Hz), of 7.75 (2H, d, J=8.5 Hz), 7,83 (1H, d, J=7.5 Hz), of 7.90 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 132)

Methyl 2-(4-methysulfonylmethane)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionate (methyl ether illustrative compounds N 138-136)

The reaction was conducted in the same manner as described in example 126, using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-methysulfonylmethane)propionate (387 mg), which is the product of reference example 43, 4-pyridine-2-eventorganizer is the head, (278 mg) as colorless crystals. So pl. 80-81oC.1H-NMR (270 MHz, CDCl3): ppm to 2.99 (3H, s), 3,23 (2H, d, J=6.5 Hz), 3,74 (3H, s) to 3.89 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), is 4.85 (1H, t, J=6.5 Hz), of 6.65 (1H, user.t), to 6.88 (2H, d, J=8.5 Hz), 6,94 (2H, d, J=9.0 Hz), 7,21 (2H, d, J=8.5 Hz), 7.23 percent-7,38 (1H, m), 7,74-of 7.82 (2H, m), 7,82 (2H, d, J=9.0 Hz), 7,89 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,73 (1H, d, J=4.5 Hz).

(Example 133)

2-(4-Methysulfonylmethane)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)ethoxy] phenyl]propionic acid (illustrative compound N 138-136)

In the same way as described in example 2, methyl 2-(4-methysulfonylmethane)-3-[4-[2-(4-pyridine-2 - albenzaalbenza)ethoxy]phenyl]propionate (263 mg), which is the product of example 132 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.94 ml) and the reaction mixture was treated with obtaining the connection specified in the header (195 mg) as colorless crystals. So pl. 231-233oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 3,03-3,24 (2H, m), 313 (3H, s) to 3.64 (2H, q, J=5.5 Hz), 4,10 (2H, t, J=5.5 Hz), 5,10 (1H, DD, J=4,5, 7.5 Hz), make 6.90 (2H, d, J= 8.5 Hz), 7,07 (2H, d, J=9.0 Hz), 7,25 (2H, d, J=8.5 Hz), 7,40 (1H, DD, J= 5.0 and 7.5 Hz), 7,78 (2H, d, J=9.0 Hz), 7,92 (1H, DD, J=7,5, 8.0 Hz), 7,98 (2H, d, J=8.5 Hz), with 8.05 (1H, d, J=8.0 Hz), 8,18 (2H, d, J=8.5 Hz), to 8.70 (1H, d, J=5.0 Hz), 8,78 (1H, t, J=5,5 Hz).

(Example 134)

Ethyl 2-(4-pyridine-2-elfenix/BR> The reaction was conducted in the same manner as described in example 122 using ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionate (370 mg), which is the product of reference example 39, 4-(pyridin-2-yl)phenol (292 mg), triphenylphosphine (447 mg) and diethylazodicarboxylate (40% toluene solution, of 0.56 ml) and the reaction mixture was treated with obtaining the connection specified in the header (500 mg) in the form of a colorless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), up 3.22 (2H, d, J=6.0 Hz), with 3.89 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), 4,18 (2H, q, J= 7.0 Hz), 4,82 (1H, t, J=6.0 Hz), 6,66 (1H, t, J=5.0 Hz), to 6.88 (2H, d, J=8.5 Hz), to 7.93 (2H, d, J=8.5 Hz), 7,10-7,30 (3H, m), 7,45-7,80 (5H, m), 7,89 (4H, d, J= 8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,63 (1H, d, J=4.5 Hz), 8,71 (1H, d, J=4.5 Hz).

(Example 135)

2-(4-Pyridine-2-elfenix)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionic acid (illustrative compound N 138-264)

In the same way as described in example 2, ethyl 2-(4-pyridine-2-elfenix)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (500 mg), which is the product of example 134 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (390 mg) as a white powder. So pl. 98-101oC.1

(Example 136)

Ethyl 2-(3-pertenece)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl] propionate (ethyl ester of illustrative compounds N 138-88)

The reaction was conducted in the same manner as described in example 122 using ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (500 mg), which is the product of reference example 39, 3-terfenol (258 mg), triphenylphosphine (604 mg) and diethylazodicarboxylate (40% toluene solution, 0.75 ml) and the reaction mixture was treated with obtaining the connection specified in the header (524 mg) as a white powder. So pl. 133-134,5oC.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 3,18 (2H, d, J=6.5 Hz), 3,81-to 3.92 (2H, m), 4,10-4,22 (4H, m), 4.72 in (1H, t, J=6.5 Hz), 6,51-6,70 (4H, m), to 6.88 (2H, d, J=8.5 Hz), 7,11-7,30 (4H, m), 7,71-of 7.82 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 137)

2-(3-Pertenece)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionic acid (illustrative compound N 138-88)

In the same way as described in example 2, ethyl 2-(3-pertenece)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (500 mg), which is a product of when Tivoli getting connection specified in the header, (410 mg) as a white powder. So pl. to 136.5-138oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 3,00-3,20 (2H, m), 3,56-3,70 (2H, m), 4,01-4,12 (2H, m), 4,90-5,00 (1H, m), 6,62-to 6.80 (3H, m) 6,91 (2H, d, J=8.5 Hz), 7,16-7,31 (3H, m), 7,37-the 7.43 (1H, m), a 7.85-8,08 (4H, m), 8,19 (2H, d, J=8.5 Hz), to 8.70 (1H, d, J=5.0 Hz), 8,71-8,82 (1H, m).

(Example 138)

Ethyl 2-(3,5-divergence)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 138-168)

The reaction was conducted in the same manner as described in example 122 using ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionate (400 mg), which is the product of reference example 39, 3,5-diferena (240 mg), triphenylphosphine (483 mg) and diethylazodicarboxylate (40% toluene solution, of 0.60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (460 mg) as a white powder. So pl. 146-147oC.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7.0 Hz), 3,18 (2H, d, J=6.5 Hz), with 3.89 (2H, d, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), 4,19 (2H, q, J=7.0 Hz), and 4.68 (1H, t, J=6.5 Hz), of 6.31-of 6.45 (3H, m), of 6.66 (1H, t, J=5.0 Hz), 6,86 (2H, d, J=8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7,26-7,31 (1H, m), 7,75-7,80 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 139)

2-(3,5-Divergence)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propertyfinance)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (410 mg), which is the product of example 138, subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (350 mg) as a white powder. So pl. of 149.5-151oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 3,05-of 3.25 (2H, m), the 3.65 (2H, d, J=5.5 Hz), 4,11 (2H, t, J=5.5 Hz), to 5.08 (1H, t, J=5.5 Hz), of 6.65 (2H, d, J=9.0 Hz), 6,70-6,83 (1H, m) 6,91 (2H, d, J=7.5 Hz), 7.23 percent (2H, d, J=7.5 Hz), 7,38 was 7.45 (1H, m), of 7.90-8,10 (4H, m), 8,18 (2H, d, J=8.5 Hz), to 8.70 (1H, d, J=4.5 Hz), 8,79 (1H, t, J=5.0 Hz).

(Example 140)

Ethyl 2-(3,4-divergence)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 138-152)

The reaction was conducted in the same manner as described in example 122 using ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (312 mg), which is the product of reference example 39, 3,4-diferena (187 mg), triphenylphosphine (377 mg) and diethylazodicarboxylate (40% toluene solution, of 0.65 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (213 mg) as a white powder. So pl. 133-134oC.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7.0 Hz), 3,17 (2H, d, J=6.5 Hz), 3,90 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), 4,18 (2H, q, J= 7.0 Hz), with 4.64 (1H, t, J=6.5 Hz), 6.48 in-6,60 (1H, m)8,72 (1H, d, J=5.0 Hz).

(Example 141)

2-(3,4-Divergence)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 138-152)

In the same way as described in example 2, ethyl 2-(3,4-divergence)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (281 mg), which is the product of example 140 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 1.02 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (246 mg) as a white powder. So pl. 135-136oC.1H-NMR (270 MHz, CDCl3): ppm 3,20 (2H, d, J=6.5 Hz), 3,80 (2H, q, J=5,5 Hz) to 4.23 (2H, t, J=5.5 Hz), to 4.73 (1H, t, J=6.5 Hz), 6,56 of 6.66 (1H, m), 6,68-6,77 (2H, m) 6,86 (2H, d, J=8.5 Hz), 7,00 (1H, q, J= 9.5 Hz), 7,19 (2H, d, J=8.5 Hz), was 7.36 (1H, DD, J=5,5, 7.5 Hz), 7,74 (1H, d, J=7.5 Hz), 7,74 (2H, d, J=8.5 Hz), 7,84-7,87 (1H, m), 7,88 (2H, d, J=8.5 Hz), 8,71 (1H, d, J=4.5 Hz).

(Example 142)

Ethyl 2-(3,4,5-tryptophanate)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 138-184)

The reaction was conducted in the same manner as described in example 122 using ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (385 mg), which is the product of reference example 39, 3,4,5-tryptophanol (262 mg), triphenylphosphine (465 mg) and diet the data in the header, (415 mg) as a white powder. So pl. 150-152oC. 1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J=7,0 Hz), and 3.16 (2H, d, J= 6.5 Hz), 3,90 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), 4,19 (2H, q, J= 7.0 Hz), to 4.62 (1H, t, J=6.5 Hz), 6,41-6,50 (2H, m), of 6.66 (1H, t, J=5.0 Hz), to 6.88 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8.5 Hz), 7,25-7,30 (1H, m), 7,73-7,81 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 143)

2-(3,4,5-Tryptophanate)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionic acid (illustrative compound N 138-184)

In the same way as described in example 2, ethyl 2-(3,4,5-tryptophanate)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (380 mg), which is the product of example 142 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (320 mg) as a white powder. So pl. 144-146oC.1H-NMR (270 MHz, CDCl3): ppm 3,16 is 3.23 (2H, m), 3,80-are 3.90 (2H, m), 4,17-of 4.25 (2H, m), of 4.66 (1H, t, J=6.0 Hz), 6,41-to 6.58 (2H, m), 6.75 in-PC 6.82 (1H, m), at 6.84 (2H, d, J=8.5 Hz), 7,17 (2H, d, J=8.5 Hz), 7,38 (1H, t, J=6.0 Hz), 7,70-of 7.90 (6H, m), 8,72 (1H, d, J=5.0 Hz).

(Example 144)

Ethyl 2-Pantothenate-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (ethyl ester of illustrative compounds N 138-200)

The reaction was carried out in the same way, which is on the verge is the product of reference example 39, pentafluorophenol (424 mg), triphenylphosphine (604 mg) and diethylazodicarboxylate (40% toluene solution, 1,10 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (918 mg, containing some impurity) in the form of a white powder. 1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J=7.0 Hz), 3,12-to 3.33 (2H, m), 3,82-of 3.94 (2H, m), 4,10-4,27 (4H, m), 4,91 (1H, DD, J= 5.0 and 7.5 Hz), 6,62-6,72 (1H, m), to 6.88 (2H, d, J=8.5 Hz), 7.18 in-7,30 (3H, m), 7,70-7,80 (2H, m), of 7.90 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 145)

2 Pantothenate-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionic acid (illustrative compound N 138-200)

In the same way as described in example 2, ethyl 2-Pantothenate-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionate (910 mg), which is the product of example 144, subjected to contact with an aqueous solution of sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (240 mg) as a white powder. So pl. 145-146oC.1H-NMR (270 MHz, CDCl3): ppm 3,19-to 3.41 (2H, m), 3.75 to-4,10 (2H, m), 4,21-432 (2H, m), 5,04 (1H, t, J=6.0 Hz), 6,70-6,85 (1H, m), of 6.90 (2H, d, J=8.5 Hz), 7,26 (2H, d, J=8.5 Hz), 7,38-7,46 (1H, m), 7.68 per-7,81 (3H, m), 7,81-7,98 (3H, m), 8,77 (1H, d, J=4.5 Hz).

(Example 146)

Methyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2 the way that described in example 73, using methyl 3-[4-(2-tert-butoxycarbonyl-aminoethoxy)phenyl] -2-(4-pertenece)propionate (314 mg), which is the product of reference example 44, biphenyl-4-carboxylic acid (158 mg), diethylthiophosphate (0,12 ml) and triethylamine (0,30 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (276 mg) as a white powder. So pl. 105-106oC.1H-NMR (270 MHz, CDCl3): ppm 3,17 (2H, d, J=6.5 Hz), and 3.72 (3H, s) to 3.89 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), and 4.68 (1H, t, J=6.5 Hz), 6,63 (1H, user. t) 6,76 (2H, DD, J=4,0, 9.0 Hz), to 6.88 (2H, d, J=8.5 Hz), 6,91 (2H, t, J=9.0 Hz), 7,22 (2H, d, J=8.5 Hz), 7,41 (1H, t, J=7.0 Hz), 7,44 (1H, t, J=7.0 Hz), 7,47 (1H, t, J=7.0 Hz), to 7.61 (2H, d, J=7,0 Hz), 7,66 (2H, d, J=8.5 Hz), the 7.85 (2H, d, J=8,5 Hz).

(Example 147)

3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-(4-pertenece)propionic acid (illustrative compound N 138-51)

In the same way as described in example 2, methyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-(4-pertenece)propionate (266 mg), which is the product of example 146 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 1,04 ml) and the reaction mixture was treated with obtaining the connection specified in the header (241 mg) as colorless crystals. So pl. 162-163oC.1H-NMR (270 MHz, CDCl3

(Example 148)

Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[6-(4-methoxyphenyl)pyridine-3 - carbylamine] ethoxy] phenyl] -2-methylpropionate (ethyl ether illustrative compounds N 34-40)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)-2-methylpropionate (400 mg), which is the product of reference example 45, 6-(4-methoxyphenyl)nicotinic acid (208 mg), which is the product of reference example 26, diethylthiophosphate (0,14 ml) and triethylamine (0,23 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (355 mg) as colorless crystals. So pl. 92-94oC. 1H-NMR (270 MHz, CDCl3): ppm 1,01 of 1.28 (9H, m) of 1.36 (3H, s), was 2.76-2.91 in (1H, m), 3,10 (1H, d, J=14,0 Hz), 3,26 (1H, d, J=14,0 Hz), a 3.87 (3H, s), 3,81-of 3.94 (2H, m), 4,10-4,27 (4H, m), 6,60 of 6.68 (1H, m), of 6.75 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,01 (2H, d, J=9.0 Hz), 7,06 (2H, d, J=8.5 Hz), 7,19 (2H, d, J=8.5 Hz), 7,74 (1H, d, J=8.5 Hz), 8,01 (2H, d, J=8.5 Hz), 8,13 (1H, DD, J=2,0, 8.5 Hz), 9,01 (1H, d, J=2.0 Hz).

(Example 149)

2-(4-Isopropylphenoxy)-3-[4-[2-(2-(4-methoxyphenyl)pyridine-5-carbylamine] is an example 2, ethyl 2-(4-isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)pyridine-5-carbylamine]ethoxy]phenyl]-2-methylpropionate (341 mg), which is the product of example 148 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 1.14 ml) and the reaction mixture was treated with obtaining the connection specified in the header (144 mg) as colorless crystals. So pl. 194-196oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm to 1.15 (6H, d, J=7,0 Hz), 1.27mm (3H, s), 2,72-2,89 (1H, m), 3,06 (1H, d, J=13.5 Hz), 3,17 (1H, d, J=13.5 Hz), 3,61-3,70 (2H, m), 3,83 (3H, s), 4,08-4,16 (2H, m), 6,74 (2H, d, J=8,5 Hz), 6,91 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,12 (2H, d, J=8.5 Hz), 7,17 (2H, d, J=8.5 Hz), 8,01 (1H, d, J=8,5 Hz) to 8.12 (2H, d, J=8.5 Hz), 8,24 (1H, DD, J=2,0, 8.5 Hz), 8,86-to 8.94 (1H, m), 9,05 (1H, d, J=2.0 Hz).

(Example 150)

Ethyl 3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine]ethoxy] phenyl] -2-(4-isopropylphenoxy)-2-methylpropionate (ethyl ether illustrative compounds N 34-43)

The reaction was conducted in the same manner as described in example 73, using ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)-2-methylpropionate (600 mg), which is the product of reference example 45, 6-(2,2,3,3-tetrafluoropropoxy)nicotinic acid (344 mg), which is the product of reference example 28, diethylthiophosphate (0,21 ml) is in the form of a colourless oil.1H-NMR (400 MHz, CDCl3): to 1.16 ppm of 1.28 (9H, m) to 1.37 (3H, s), and 2.83 (1H, septet, J=7.0 Hz), 3,11 (1H, d, J=13.5 Hz), 3,26 (1H, d, J=13.5 Hz), 3,83-to 3.89 (2H, m), 4,10-4,18 (2H, m), is 4.21 (2H, q, J=7.0 Hz), and 4.75 (2H, t, J= 12,5 Hz), 6,00 (1H, TT, J=4,5, 53 Hz), 6,53-6,60 (1H, m), of 6.75 (2H, d, J=8.5 Hz), for 6.81-of 6.90 (3H, m), 7,06 (2H, d, J=8.5 Hz), 7,19 (2H, d, J=8.5 Hz), 8,07 (1H, d, J=8.5 Hz), 8,59 (1H, s).

(Example 151)

3-[4-[2-[2-(2,2,3,3-Tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl] -2-(4-isopropylphenoxy)-2-methylpropionate acid (illustrative compound N 34-43)

In the same way as described in example 2, ethyl 3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl] -2-(4-isopropylphenoxy)-2-methylpropionate (210 mg), which is the product of example 150 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 0.51 ml) and the reaction mixture was treated with obtaining the connection specified in the header (140 mg) as colorless crystals. So pl. 173-175oC.1H-NMR (400 MHz, CDCl3/deuterated methanol = 20/1): ppm of 1.20 (6H, d, J=7,0 Hz) of 1.40 (3H, s) 2,84 (1H, septet, J=7.0 Hz), 3,13 (1H, d, J=14,0 Hz), 3,26 (1H, d, J=14,0 Hz), 3,80-to 3.89 (2H, m), 4,14-4,20 (2H, m), 4,78 (2H, t, J= 12,5 Hz), 6,00 (1H, TT, J=4,5, 53 Hz), 6,80-6,92 (5H, m), to 7.09 (2H, d, J= 8.5 Hz), 7,22 (2H, d, J=8.5 Hz), of 8.09 (1H, d, J=8.5 Hz), 8,55 (1H, s).

(Example 152)

Methyl 2-phenylthio-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] the dryer is th described in example 126, using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-phenylthiophene (209 mg), which is the product of reference example 46, 4-pyridine-2-eventological (135 mg) and triethylamine (0,27 ml) and the reaction mixture was treated with obtaining the connection specified in the header (146 mg) as colorless crystals. So pl. 102-104oC.1H-NMR (270 MHz, CDCl3): to 3.00 ppm (1H, DD, J=6,0, and 13.5 Hz), 3,14 (1H, DD, J=9,0, 13.5 Hz), to 3.58 (3H, s), 3,86 (1H, DD, J=6,0, 9.0 Hz), 3,90 (2H, q, J=5.0 Hz), is 4.15 (2H, t, J=5.0 Hz), of 6.65 (1H, user.t), 6,85 (2H, d, J=8.5 Hz), 7,12 (2H, d, J= 8.5 Hz), 7,16-7,37 (4H, m), 7,38-of 7.48 (2H, m), 7,71-7,81 (2H, m), 7,89 (2H, d, J=8.5 Hz), with 8.05 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 153)

2 Phenylthio-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionic acid (illustrative compound N 17-11)

In the same way as described in example 2, methyl 2-phenylthio-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (150 mg), which is the product of example 152, subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.58 ml) and the reaction mixture was treated with obtaining the connection specified in the header (138 mg) as colorless crystals. So pl. 75-77oC.1H-NMR (270 MHz, CDCl3): to 3.00 ppm (1H, DD, J=5.0 and 13.5 Hz), 3,11 (1H, DD, J=a 10.5, and 13.5 Hz), 3,82 (2H, t, J=5.0 Hz), a 3.87 (1H, DD, J= is), to 7.61 (2H, d, J=8.5 Hz), 7,71 (1H, d, J= 8.0 Hz), 7,82-7,89 (1H, m), 7,87 (2H, d, J=8.5 Hz), 8,63 (1H, d, J=5.0 Hz).

(Example 154)

Methyl 3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-(pyridine-3-yloxy)propionate (methyl ether illustrative compounds N 138-216)

The reaction was conducted in the same manner as described in example 126, using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(pyridine-3-yloxy)propionate (345 mg), which is the product of reference example 47, 4-pyridine-2-eventyrland hydrochloride (261 mg) and triethylamine (0,60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (271 mg) as colorless crystals. So pl. 101-103oC.1H-NMR (270 MHz, CDCl3): ppm up 3.22 (2H, d, J=6.5 Hz), to 3.73 (3H, s), 3,90 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J=5.0 Hz), 4,78 (1H, t, J=6.5 Hz), 6,66 (1H, user.t), to 6.88 (2H, d, J=8.5 Hz), 7,09-to 7.18 (2H, m), 7,22 (2H, d, J=8.5 Hz), 7,26-7,33 (1H, m), 7,73-of 7.82 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,16 compared to 8.26 (2H, m), 8,72 (1H, d, J=5.0 Hz).

(Example 155)

3-[4-[2-(4-Pyridine-2-albenzaalbenza)ethoxy] phenyl] -2-(pyridine-3-yloxy)propionic acid (illustrative compound N 138-216)

In the same way as described in example 2, methyl 3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] -2-(pyridine-3-yloxy)propionate (248 mg), which is the product of example 154, getting a connection, specified in the header, (212 mg) as colorless crystals. So pl. 194-196oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm is 3.10 (1H, DD, J=8,5, 14,5 Hz), 3,18 (1H, DD, J=4,0, 14,5 Hz) to 3.64 (2H, q, J=5.5 Hz), 4,10 (2H, t, J=5.5 Hz), 5,04 (1H, DD, J=4,0, 8.5 Hz), 6,91 (2H, d, J=8.5 Hz), 7,25 (2H, d, J=8.5 Hz), 7,26 (1H, DD, J=6,5, 8.0 Hz), 7,27 (1H, d, J=6.5 Hz), 7,40 (1H, DD, J=4,5, 8.0 Hz), 7,92 (1H, t, J= 8.0 Hz), 7,98 (2H, d, J=8.5 Hz), with 8.05 (1H, d, J=8.0 Hz), 8,14 (1H, s), 8,18 (2H, d, J=8,5 Hz), 8,18 (1H, d, J=8.0 Hz), to 8.70 (1H, d, J=4.5 Hz), 8,79 (1H, user.t).

(Example 156)

Methyl 2-(benzoxazol-2-ylthio)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (methyl ether illustrative compounds N 138-248)

The reaction was conducted in the same manner as described in example 126, using methyl 2-(benzoxazol-2-ylthio)-3-[4-(2-tert-butoxycarbonylamino)phenyl] propionate (665 mg), which is the product of reference example 48, 4-pyridine-2-eventyrland hydrochloride (444 mg) and triethylamine (0,81 ml) and the reaction mixture was treated with obtaining the connection specified in the header (582 mg) as a foam mass.1H-NMR (270 MHz, CDCl3): ppm 3,30 (1H, DD, J=7,5, 15,0 Hz), the 3.35 (1H, DD, J=7,5, 15,0 Hz), 3,71 (3H, s), 3,88 (2H, q, J= 5.0 Hz), of 4.13 (2H, t, J=5.0 Hz), of 4.77 (1H, t, J=7.5 Hz), of 6.68 (1H, user.t) 6,86 (2H, d, J=8.5 Hz), 7,18 (2H, d, J=8.5 Hz), 7.24 to 7,38 (3H, m), 7,42 (1H, d, J=7.5 Hz), 7,60 (1H, d, J=6.0 Hz), 7,75-of 7.82 (2H, m), 7,89 (2H, d, J=8, which amino)ethoxy] phenyl]propionic acid (illustrative compound N 138-248)

In the same way as described in example 2, methyl 2-(benzoxazol-2-ylthio)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]propionate (361 mg), which is the product of example 156 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 1.30 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (248 mg) as colorless crystals. So pl. 66-67oC.1H-NMR (270 MHz, deuterated methanol): ppm 3,20-to 3.36 (2H, m in), 3.75 (2H, t, J=5.5 Hz), 4,10 (1H, t, J=5.5 Hz), 4,19 (1H, t, J= 5.5 Hz), 6,85 (1H, d, J=8.5 Hz), 6.89 in (1H, d, J=8.5 Hz), to 7.15 (1H, d, J= 8.5 Hz), 7,21 (2H, d, J=8.5 Hz), 7,28 (1H, t, J=4.5 Hz), 7,40 (1H, DD, J= 4,5, 8.5 Hz), of 7.48 (1H, DD, J=4,0, 5,0 Hz), 7,54 (1H, DD, J=4,0, 5,0 Hz), 7,92 (2H, d, J=4.0 Hz), 7,95 (2H, d, J=8.5 Hz), of 8.06 (2H, d, J=8.5 Hz), 8,64 (1H, d, J=4.5 Hz).

(Example 158)

Methyl 2-benzyloxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (methyl ether illustrative compounds N 138-232)

The reaction was conducted in the same manner as described in example 126, using methyl 2-benzyloxy-3-[4-(2-tert-butoxycarbonylamino)phenyl] propionate (195 mg), which is the product of reference example 49, 4-pyridine-2-eventyrland hydrochloride (127 mg) and triethylamine (0.25 ml) and the reaction mixture was treated with obtaining the connection specified in the header (106 mg) in VI(3H, C) 3,91 (2H, q, J=5.0 Hz), 4,10 (1H, DD, J=5,5, 7.5 Hz), 4,17 (2H, t, J= 5.0 Hz), 4,37 (1H, d, J=12.0 Hz), of 4.66 (1H, d, J=12.0 Hz), of 6.68 (1H, user. t) 6,86 (2H, d, J=8.5 Hz), to 7.15 (2H, d, J=8.5 Hz), 7,19 (2H, d, J=8.0 Hz), 7,22-7,37 (4H, m), 7,76-7,83 (2H, m), of 7.90 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 159)

2-Benzyloxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionic acid (illustrative compound N 138-232)

In the same way as described in example 2, methyl 2-benzyloxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (94 mg), which is the product of example 158, subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.36 ml) and the reaction mixture was treated with obtaining the connection specified in the header (86 mg) as colorless crystals. So pl. 138-139oC.1H-NMR (270 MHz, CDCl3): ppm 3,01 (1H, DD, J=7,0, 14,5 Hz), of 3.12 (1H, DD, J=5,0, 14,5 Hz), 3,90 (2H, q, J=5.5 Hz), 4,18 (1H, DD, J= 5.0 and 7.0 Hz), 4,20 (2H, t, J=5.5 Hz), 4,48 (1H, d, J=11.5 Hz), of 4.67 (1H, d, J=11.5 Hz), 6,69 (1H, user.t), 6,85 (2H, d, J=8.5 Hz), 7,16 (2H, d, J= 8.5 Hz), 7,22-the 7.43 (6H, m), of 7.75 (1H, d, J=8.0 Hz), 7,79 (1H, DD, J=8,0, 9.0 Hz), 7,81 (2H, d, J=8.5 Hz), 8,00 (2H, d, J= 8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 160)

2-(3-Phenylpropyl)-2-[4-[3-(4-pyridine-2-albenzaalbenza)propyl]phenyl]propionic acid (illustrative compound N 77-3)

To a solution of dibenzyl 2-(3-phenylpropyl)-2-[4-[3-(4-´┐ŻNola (20 ml) was added palladium on carbon (5%, 0.12 g). The mixture was stirred in hydrogen atmosphere at 60oC for 5 hours. The catalyst was then removed by filtration, the filtrate was concentrated. The residue was dissolved in 2-methoxyethanol (10 ml). The solution was stirred at 150oC for 4 hours and then concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/methanol = 9/1, receiving of the connection specified in the header (330 mg) as crystals. So pl. 118-119oC.1H-NMR (270 MHz, CDCl3): ppm 1,75-to 1.82 (4H, m), 1,99 (2H, quintuplet, J=7.5 Hz), 2,58-2,77 (6H, m), 2,96 (1H, DD, J=of 11.0 to 15.0 Hz), 3,51 (2H, dt, J=5,5, 7.5 Hz), 6,16 (1H, user.t, J=5.5 Hz), 7,12-to 7.18 (6H, m), 7.23 percent-7,33 (4H, m), 7,60 (2H, d, J=8.0 Hz), 7,71 (1H, DD, J= 1,0, 8.0 Hz), 7,80 (1H, DD, J=2,0, 8.0 Hz), to 7.93 (2H, d, J=8.5 Hz), 8,65-8,67 (1H, m).

(Example 161)

Ethyl 3-[3-chloro-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-phenoxypropionate (ethyl ether illustrative compounds N 139-24)

The reaction was conducted in the same manner as described in example 126, using methyl 3-[4-(2-tert-butoxycarbonylamino)-3-chlorophenyl]-2-phenoxypropionate (738 mg), which is the product of reference example 51, 4-pyridine-2-eventyrland hydrochloride (445 mg) and triethylamine (0,89 ml) and the reaction mixture was treated with obtaining the who(1H, d, J=5.5 Hz), 3,17 (1H, d, J=7,0 Hz), 3,93 (2H, q, J= 5.0 Hz), 4,19 (2H, q, J=7.0 Hz), 4,22 (2H, t, J=5.0 Hz), to 4.73 (1H, DD, J= 5,5, 7,0 Hz), 6,83 (2H, d, J=8.5 Hz), 6,91 (1H, d, J=8.5 Hz), to 6.95 (1H, t, J= 8.0 Hz), 7,18 (1H, DD, J=2,0, 8.5 Hz), 7,24 (2H, t, J=8.0 Hz), 7,26-7,33 (1H, m), 7,35 (1H, d, J=2.0 Hz), to 7.77-a 7.85 (2H, m), a 7.85 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 162)

3-[3-chloro-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] -2-phenoxypropionic acid (illustrative compound N 139-24)

In the same way as described in example 2, ethyl 3-[3-chloro-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-phenoxypropionate (540 mg), which is the product of example 161 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., to 1.98 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (404 mg) as colorless crystals. So pl. 59-61oC.1H-NMR (270 MHz, CDCl3): ppm 3,19 (2H, d, J=6.0 Hz), 3,83-3,98 (2H, m) to 4.23 (2H, user.t), 4,79 (1H, t, J=6.0 Hz), 6,86 (2H, d, J= 8.0 Hz), 6.87 in (1H, d, J=8.5 Hz), 6,93 (1H, t, J=8.0 Hz), 7,12 (1H, DD, J= 2,0, 8.5 Hz), 7.23 percent (2H, t, J=8.0 Hz), 7,33 (1H, DD, J=4,5, 7.5 Hz), was 7.36 (1H, d, J=2.0 Hz), 7,72 (1H, d, J=8.0 Hz), 7,80 (2H, d, J=8.5 Hz), to 7.84 (1H, DD, J=7,5, 8.0 Hz), to $ 7.91 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 163)

Ethyl 3-[3-bromo-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-2-phenoxypropionate (ethyl ether illustrative compounds N 141-23)1
H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7,0 Hz), and 3.16 (1H, d, J=5.5 Hz), 3,17 (1H, d, J=7,0 Hz), of 3.94 (2H, q, J=5.0 Hz), 4,19

(2H, q, J= 7.0 Hz), 4,22 (2H, t, J=5.0 Hz), to 4.73 (1H, DD, J=5,5, 7,0 Hz), 6,82-6,98 (1H, m), 6,83 (2H, d, J=8.5 Hz), to 6.88 (1H, d, J=8.5 Hz), to 6.95 (1H, t, J= 7.5 Hz), 7,21-to 7.32 (1H, m), 7,24 (2H, DD, J=7,5, 8.0 Hz), 7,25 (1H, DD, J= 2,0, 8.5 Hz), 7,52 (1H, d, J=2.0 Hz), 7,76-7,80 (2H, m), 7,95 (2H, d, J=8.5 Hz), 8,08 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 164)

3-[3-Bromo-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] -2 - phenoxypropionic acid (illustrative compound N 141-23)

In the same way as described in example 2, ethyl 3-[3-bromo-4-[2- (4-pyridine-2-albenzaalbenza)ethoxy] phenyl] -2-phenoxypropionate (237 mg), which is the product of example 163 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., of 0.80 ml) and the reaction mixture was treated with obtaining the connection specified in the header (174 mg) as colorless crystals. So pl. 83-84oC.1H-NMR (270 MHz, deuterated methanol): ppm of 3.12 (1H, DD, J=7,5, of 14.0 Hz), 3,20 (1H, DD, J=5,0, of 14.0 Hz), 3,81 (2H, t, J=5.5 Hz), 4,24 (2H, t, J=5.5 Hz), a 4.86 (1H, DD, J1H, DD, J= 4,5, 8.0 Hz), 7,52 (1H, d, J=2.0 Hz), to 7.93 (1H, t, J=4.5 Hz), 7,95 (2H, d, J=8.5 Hz), with 8.05 (2H, d, J=8.5 Hz), 8,64 (1H, d, J=4.5 Hz).

(Example 165)

Ethyl 3-[3-nitro-4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl]- 2-phenoxypropionate(ethyl ether illustrative compounds N 142-23)

The reaction was conducted in the same manner as described in example 126, using methyl 3-[3-nitro-4-(2-tert-butoxycarbonylamino)phenyl]-2 - phenoxypropionate (723 mg), which is the product of reference example 53, 4-pyridine-2-eventyrland hydrochloride (465 mg) and triethylamine (0,85 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (843 mg) as a foamy mass.1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J= 7.0 Hz), 3,24 (2H, d, J=6.0 Hz), of 3.96 (2H, q, J=5.0 Hz), is 4.21 (2H, q, J= 7.0 Hz), or 4.31 (2H, t, J=5.0 Hz), was 4.76 (1H, t, J=6.0 Hz), 6,83 (2H, d, J=8.5 Hz), of 6.96 (1H, t, J=7.5 Hz), 7,05 (1H, d, J=8.5 Hz), to 7.09 (1H, user. t), 7,22-7,30 (1H, m), 7,24 (2H, DD, J=7,5, 8.0 Hz), 7,53 (1H, DD, J= 2.5 and 8.5 Hz), 7,75-7,80 (2H, m), 7,88 (1H, d, J=2.5 Hz), of 7.97 (2H, d, J=8.5 Hz), of 8.09 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=4.5 Hz).

(Example 166)

3-[3-Nitro-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] -2 - phenoxypropionic acid (illustrative compound N 142-23)

In the same way as described in example 2, ethyl 3-[3-nitro-4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl] -2-phenoxypropionate (1 N., to 0.80 ml) and the reaction mixture was treated with obtaining the connection specified in the header (137 mg) as colorless crystals. So pl. 178-179oC.1H-NMR (270 MHz, CDCl3/deuterated methanol = 1/9): ppm up 3.22 (1H, DD, J=8,0, 14,5 Hz), 3,26 (1H, DD, J=5,0, 14,5 Hz), a-3.84 (2H, q, J=5.0 Hz), 4,36 (2H, t, J=5.0 Hz), a 4.83 (1H, DD, J=5.0 and 8.0 Hz), 6,85 (2H, d, J=8.0 Hz), 6,92 (1H, t, J=7.5 Hz), of 7.23 (2H, DD, J=7,5, 8.0 Hz), 7,24 (1H, d, J=6.5 Hz), 7,40 (1H, DD, J to 4.5, and 6.5 Hz), 7,58 (1H, DD, J=2,0, 8.5 Hz), to 7.84 (1H, d, J=2.0 Hz), to $ 7.91 (1H, t, J=8.5 Hz), 7,92 (1H, t, J= 4.5 Hz), of 7.96 (2H, d, J=8.5 Hz), 8,03 (2H, d, J=8.5 Hz), 8,65 (1H, d, J= 4.5 Hz).

(Example 167)

Methyl (S)-2-benzyloxycarbonylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate (methyl ether illustrative compounds N 144-63)

The reaction was conducted in the same manner as described in example 73, using methyl (S)-2-benzyloxycarbonylamino-3-[4-(2-tert-butoxycarbonylamino)phenyl] propionate (368 mg), which is the product of reference example 54, 4-pyridine-2-eventing acid (175 mg), diethylthiophosphate (0,13 ml) and triethylamine (0,22 ml) and the reaction mixture was treated with obtaining the connection specified in the header (300 mg) as colorless crystals. So pl. 150-151oC.1H-NMR (270 MHz, CDCl3): ppm 2,90-of 3.12 (2H, m), and 3.72 (3H, s), 3,82-of 3.94 (2H, m), and 0.15 (2H, t, J=5.0 Hz), 4,55-4,69 (1H, m), 5,09 (2H, ABq, J= 12.5 G=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 168)

(S)-2-benzyloxycarbonylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]-phenyl] propionic acid (illustrative compound N 144-63)

In the same way as described in example 2, methyl (S)-2-benzyloxycarbonylamino-3-[4-[2- (4-pyridine-2-albenzaalbenza)ethoxy] phenyl]-propionate (200 mg), which is the product of example 167 were subjected to contact with an aqueous solution of sodium hydroxide (1 N., 0,72 ml) and the reaction mixture was treated with obtaining the connection specified in the header (144 mg) as a foamy mass.1H-NMR (270 MHz, CDCl3): is 3.08 ppm (2H, d, J=5.0 Hz), 3,68-4,00 (2H, m), 4,08-4,30 (2H, m), 4,55-4,69 (1H, m), 5,11 (2H, s), lower than the 5.37 (1H, d, J=8.0 Hz), 6,70-of 6.90 (3H, m), of 6.99 (2H, d, J=8.5 Hz), 7,20-7,41 (6H, m), 7,70-7,93 (6H, m), to 8.70 (1H, d, J=4.5 Hz).

(Example 169)

Methyl (S)-2-propylamino-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl]propionate (methyl ether illustrative compounds N 144-13)

The reaction was conducted in the same manner as described in reference example 1 (d) using methyl (S)-2-benzyloxycarbonylamino-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl]propionate (1,53 g) and palladium on carbon (5%, 150 mg) and the reaction mixture was treated with obtain methyl (S)-2-amino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] -phenyl] propionamide (0,24 ml) and potassium carbonate (387 mg). The mixture was stirred at 70oC for 16 hours. The reaction mixture was distributed between ethyl acetate and water, an ethyl acetate layer was separated and dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel using dichloromethane/methanol = 19/1, receiving of the connection specified in the header (196 mg) as colorless crystals. So pl. 86-87oC.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7.5 Hz), 1,39-to 1.59 (2H, m), 2,39-2,60 (2H, m), 2,90 (2H, d, J=7,0 Hz), 3,48 (1H, t, J=7,0 Hz) to 3.64 (3H, s), a 3.87-of 3.95 (2H, m), 4,10-4,20 (2H, m), 6,60-of 6.71 (1H, m) 6,86 (2H, d, J=8.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7,25-7,30 (1H, m), 7,78-7,80 (2H, m), 7,89 (2H, d, J=8.5 Hz), of 8.09 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5.0 Hz).

(Example 170)

(S)-2-propylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionic acid (illustrative compound N 144-13)

In the same way as described in example 2, methyl (S)-2-propylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] -phenyl] propionate (169 mg), which is the product of example 169 was subjected to contact with an aqueous solution of sodium hydroxide (1 N., 0,73 ml) and the reaction mixture was treated with obtaining the connection specified in the header (144 mg) as colorless crystals. So pl. 242-244oC.1H-, is), 2,31-of 2.50 (1H, m), 2,70-of 2.81 (2H, m), 3,30-to 3.41 (1H, m), to 3.58-and 3.72 (2H, m), 4,00-4,12 (2H, m), to 6.80 (2H, d, J=8.5 Hz), 7,12 (2H, d, J=8.5 Hz), 7,37 was 7.45 (1H, m), 7,88-8,11 (4H, m), 8,19 (2H, d, J=8.5 Hz), to 8.70 (1H, d, J=4.5 Hz), 8,80-8,88 (1H,

(Example 171)

Ethyl 2-phenylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate (ethyl ester of illustrative compounds N 144-68)

The reaction was conducted in the same manner as described in example 122 using 2-(4-pyridine-2-albenzaalbenza)ethanol, which is the product of reference example 61, ethyl 3-(4-hydroxyphenyl)-2-(phenylamino)propionate, which is the product of reference example 55(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 172)

2 Phenylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]-phenyl] propionic acid (illustrative compound N 144-68)

Ethyl 2-phenylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate is hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 173)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl]-2-phenylaminopropyl (ethyl ether illustrative compounds N 144-67)

The reaction was conducted in the same manner as described in example 122 using 2-(biphenyl-4-carb the EPA 55(b); triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 174)

3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -phenyl-aminopropionic (illustrative compound N 144-67)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl]-2-phenylaminopropyl, which is the product of example 173, hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 175)

Ethyl 2-ethylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl]propionate hydrochloride (ethyl ether illustrative compounds N 144-8)

(a) Ethyl 2-(N-tert-tertbutoxycarbonyl)ethylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 122 using 2-(4-pyridine-2-albenzaalbenza)ethanol, which is the product of reference example 61, ethyl 2-(N-tert-butoxycarbonyl)ethylamino-3-(4-hydroxyphenyl) propionate, which is the product of reference example 59(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(b) Ethyl 2-ethylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate hydrochloride (ethyl ether illustrational] propionate was treated with a solution of hydrogen chloride in dioxane (4 B.C.) to obtain the compounds specified in the header.

(Example 176)

2 Ethylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]-phenyl] propionate (illustrative compound N 144-8)

Ethyl 2-ethylamino-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy] phenyl] propionate hydrochloride, which is the product of example 175(b), hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 177)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine) ethoxy]phenyl]-2-Ethylenediamine hydrochloride (ethyl ether illustrative compounds N 144-7)

(a) Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-(N-tert-butoxycarbonyl) Ethylenediamine

The reaction was conducted in the same manner as described in example 122 using 2-(biphenyl-4-carbylamine)ethanol, ethyl 2-(N-tert-butoxycarbonyl)ethylamino-3-(4-hydroxyphenyl)- propionate, which is the product of reference example 59(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(b) Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-Ethylenediamine hydrochloride (ethyl ether illustrative compounds N 144-7)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2- (N-tert-butoxycarbonyl)ethylamine the receiving connection, specified in the header.

(Example 178)

3-[4-[2-(Biphenyl-4-carbylamine)ethoxy] phenyl]-2-ethylamino-propionic acid (illustrative compound N 144-7)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-Ethylenediamine hydrochloride, which is the product of example 177(b), hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 179)

Ethyl 2-(N-ethyl-N-phenylamino)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] -phenyl]propionate (ethyl ester of illustrative compounds N 144-33)

The reaction was conducted in the same manner as described in example 122 using 2-(4-pyridine-2-albenzaalbenza)ethanol, which is the product of reference example 61, ethyl 2-(N-ethyl-N-phenylamino)-3-(4-hydroxyphenyl)propionate, which is the product of reference example 56(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 180)

2-(N-ethyl-M-phenylamino)-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy]phenyl]propionic acid (illustrative compound N 144-33)

Ethyl 2-(N-ethyl-N-phenylamino)-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] phenyl] propionate, which is the product of example 179, hydrolyzed in hydrox-(biphenyl-4-carbylamine) ethoxy]phenyl]-2-(N-ethyl-N-phenylamino)propionate (ethyl ester of illustrative compounds N 144-32)

The reaction was conducted in the same manner as described in example 122 using 2-(biphenyl-4 - carbylamine)ethanol, ethyl 2-(N-ethyl-N-phenylamino)-3-(4 - hydroxyphenyl)propionate, which is the product of reference example 56(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 182)

3-[4-[2-(biphenyl-4-carbylamine) ethoxy] phenyl] -2-(N-ethyl-N-phenylamino)-propionic acid (illustrative compound N 144-32)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-(N-ethyl-N-phenylamino)propionate, which is the product of example 181, hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 183)

Ethyl 2-propylamino-3-[4-[2-(4-pyridine-2 - albenzaalbenza)-ethoxy]phenyl] propionate hydrochloride (ethyl ether illustrative compounds N 144-13)

(a) Ethyl 2-(N-tert-butoxycarbonyl)propylamino-3-[4-[2-(4-pyridine - 2-albenzaalbenza)-ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 122 using 2-(4-pyridine-2 - albenzaalbenza)ethanol, which is the product of reference example 61, ethyl 2-(N-tert-butoxycarbonyl) propylamino-3-(4-hydroxyphenyl)-propionate, which is a PR in the header.

(b) Ethyl 2-propylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy]phenyl] propionate hydrochloride (ethyl ether illustrative compounds N 144-13)

Ethyl 2-(N-tert-butoxycarbonyl)propylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy]phenyl]propionate, which is the product of example 183(a), treated with a solution of hydrogen chloride in dioxane (4 BC) with the receipt of the connection specified in the header.

(Example 184)

2 Propylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)ethoxy] -phenyl] propionic acid (illustrative compound N 144-13)

Ethyl 2-propylamino-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionate hydrochloride, which is the product of example 183(b) hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 185)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-Propylenediamine hydrochloride (ethyl ether illustrative compounds N 144-12)

(a) Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-(N-tert-butoxycarbonyl) Propylenediamine

The reaction was conducted in the same manner as described in example 122 using 2-(biphenyl-4-carbylamine) ethanol, ethyl 2-(N-tert-butoxycarbonyl)propylamino-3-(4-hydroxyphenyl)probIem connection specified in the header.

(b) Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-Propylenediamine hydrochloride (ethyl ether illustrative compounds N 144-12)

Ethyl 2-(N-tert-butoxycarbonyl)propylamino-3-[4-[2-(4- phenylbenzoate)ethoxy]phenyl]propionate, which is the product of example 185(a), treated with a solution of hydrogen chloride in dioxane (4 BC) with the receipt of the connection specified in the header.

(Example 186)

3-[4-[2-(Biphenyl-4-carbylamine)ethoxy] phenyl] -2-propylamino-propionic acid (illustrative compound N 144-12)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine) ethoxy]phenyl]-2-Propylenediamine hydrochloride, which is the product of example 185(b), hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 187)

Ethyl 2-(N,N-diethylamino)-3-[4-[2-(4-pyridine-2-benzoylamino)- ethoxy]phenyl]propionate (ethyl ester of illustrative compounds N 144-28)

The reaction was conducted in the same manner as described in example 122 using 2-(4-pyridine-2-albenzaalbenza) ethanol, which is the product of reference example 61, ethyl 2-(N,N-diethylamino)-3-(4-hydroxyphenyl)propionate, which is the product of reference example 58, Trifan
2-(N, N-Diethylamino)-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy] phenyl] propionic acid (illustrative compound N 144-28)

Ethyl 2-(N,N-diethylamino)-3-[4-[2-(4-pyridine-2-benzoylamino)ethoxy]phenyl] propionate, which is the product of example 187, hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 189)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine) ethoxy]phenyl]-2-(N,N-diethylamino)propionate (ethyl ester of illustrative compounds N 144-27)

The reaction was conducted in the same manner as described in example 122 using 2-(biphenyl-4-carbylamine) ethanol, ethyl 2-(N,N-diethylamino)-3-(4-hydroxyphenyl)propionate, which is the product of reference example 58, triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 190)

3-[4-[2-(Biphenyl-4-carbylamine) ethoxy] phenyl] -2-(N, N-diethylamino)propionic acid (illustrative compound N 144-27)

Ethyl 2-(N, N-diethylamino)-3-[4-[2-(4-phenylbenzoate)-ethoxy] phenyl] propionate, which is the product of example 189, hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 191)

Ethyl 3-[4-[2-(4-pyridine-2-albenza rowdily the same way that described in example 122 using 2-(4-pyridine-2-albenzaalbenza)ethanol, which is the product of reference example 61, ethyl 3-(4-hydroxyphenyl)-2-(pyrrol-1-yl)propionate, which is the product of reference example 57(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 192)

3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy] phenyl] -2-(pyrrol-1-yl)propionic acid (illustrative compound N 144-38)

Ethyl 3-[4-[2-(4-pyridine-2-albenzaalbenza) ethoxy] phenyl]-2-(pyrrol-1-yl)propionate, which is the product of example 191, hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Example 193)

Ethyl 3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-(pyrrol-1-yl)propionate (ethyl ester of illustrative compounds N 144-37)

The reaction was conducted in the same manner as described in example 122 using 2-(biphenyl-4-carbylamine)ethanol, ethyl 3-(4-hydroxyphenyl)-2-(pyrrol-1-yl)propionate, which is the product of reference example 57(b), triphenylphosphine and diethylazodicarboxylate with getting the connection specified in the header.

(Example 194)

3-[4-[2-(Biphenyl-4-carbylamine) ethoxy]phenyl]-2-(pyrrol-1-yl) the ol-1-yl)propionate, which is the product of example 193, hydrolyzed with sodium hydroxide in methanol to obtain the connection specified in the header.

(Reference example 1)

Ethyl 2-ethoxy-3-[4-(2 - preliminaty)phenyl]propionate

(a) N-[2-(methanesulfonate)ethyl] phthalimide

To a solution of N-(2-hydroxyethyl)phthalimide (19.1 g) in anhydrous dichloromethane (200 ml) was added methanesulfonamide (12.7 g), then in the mixture in an ice bath was added dropwise a triethylamine (20 ml). The mixture was stirred at room temperature for 4 hours. At the end of this time the reaction mixture was concentrated under reduced pressure. The remainder of the solid product was washed with ethyl acetate and water and then was led from ethyl acetate to give the desired compound (18.2 g). So pl. 138-139oC.1H-NMR (270 MHz, CDCl3): ppm to 3.02 (3H, s), of 4.05 (2H, t, J=5.5 Hz), of 4.49 (2H, t, J=5.5 Hz), 7,70-7,80 (2H, m), 7,83-to 7.93 (2H, m).

(b) Ethyl 3-(4-benzyloxyphenyl)lactate

To a solution of ethyl 3-(4-hydroxyphenyl)lactate (22,4 g) in dimethylformamide (220 ml) was added benzylbromide (21,9 g) and potassium carbonate (35,3 g). The mixture was stirred at 50oC for 2 hours. The reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated and dried over sulfate managalam, using as eluent hexane/ethyl acetate = 7/3, to give the desired compound (31.0 g) as a pale yellow oil.

(C) Ethyl 3-(4-benzyloxyphenyl)-2-ethoxypropionate

To a solution of ethyl 3-(4-benzyloxyphenyl)lactate (10.30 g), which is the product of reference example 1(b), in a mixture with N,N-dimethylacetamide (50 ml) and toluene (50 ml), was added sodium hydride (55% suspension in oil, of 1.65 g). The mixture was stirred at 40oC for 30 minutes. In the reaction mixture was added ethyliodide (3,3 ml) and toluene (5 ml). This mixture was stirred at 40oC for 2 hours. At the end of this time the reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated, dried over anhydrous magnesium sulfate and evaporated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 5/1, to give the desired compound (5.50 g) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm 1,11-of 1.26 (6H, m), 2,95 (2H, d, J=6.5 J Hz) to 3.36 (1H, quintuplet, J=7,0 Hz), 3,60 (1H, quintuplet, J=7,0 Hz), of 3.97 (1H, t, J=6.5 Hz), is 4.15 (2H, q, J=7.0 Hz), of 5.05 (2H, s), 6.89 in (2H, d, J=8.5 Hz), 7,16 (2H, d, J=8,5 Hz) 7,30-of 7.48 (5H, m).

(d) Ethyl 2-ethoxy-3-hydroxyphenylpropionic

To a solution of ethyl 3-(4-benzyloxy lady on carbon (5%, 0,70 g). The mixture was stirred in hydrogen atmosphere at 40oC for 2 hours. At the end of this time the catalyst was removed by filtration and the filtrate was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was dried over anhydrous magnesium sulfate and then concentrated under reduced pressure to give the desired product (3.80 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.12 ppm of 1.28 (6H, m), 2,95 (2H, d, J=6.5 Hz), 3,37 (1H, quintuplet, J= 7,0 Hz), 3,60 (1H, quintuplet, J=7,0 Hz) to 3.99 (1H, t, J=6.5 Hz), 4,19 (2H, q, J=7.0 Hz), 5,38 (1H, s), 6.73 x (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8,5 Hz).

(e) Ethyl 2-ethoxy-3-[4-(2-fallimentare)phenyl] propionate

To a solution of ethyl 2-ethoxy-3-hydroxyphenylpropionic (1,00 g), which is the product of reference example 1(d), in a mixture of dimethylacetamide (10 ml) and toluene (10 ml) was added sodium hydride (55% suspension in oil, 200 mg). The mixture was stirred at room temperature for 20 minutes. In the reaction mixture were added N-[2-(methanesulfonate)ethyl]phthalimide (1.50 g), which is the product of reference example 1(a), and the mixture was stirred at 70oC for 2.5 hours and then at 60oC for 24 hours. At the end of this time the reaction was evaporated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent benzene/ethyl acetate = 8/1, receiving of the connection specified in the header (0.31 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm 1,09 of 1.28 (6H, m), of 2.92 (2H, d, J=6.5 Hz), 3,37 (1H, quintuplet, J= 7,0 Hz) to 3.58 (1H, quintuplet, J=7,0 Hz), 3,93 (1H, t, J=6.5 Hz), 4,06-of 4.25 (6H, m), 6,79 (2H, d, J=8.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7.68 per-to $ 7.91 (4H, m).

(Reference example 2)

Ethyl 2-(3-phenylpropyl)-3-[4-(2-preliminaty)phenyl]- propionate

(a) Diethyl 2-(4-benzyloxybenzyl)-2-(3 - phenylpropyl)malonate

To a solution of diethyl 2-(3-phenylpropyl)malonate (2,78 g) in a mixture of N,N-dimethylacetamide (10 ml) and toluene (20 ml) was added sodium hydride (55% suspension in oil, of 0.48 g). The mixture was stirred at room temperature for 30 minutes. In the reaction mixture was added 4-benzyloxybenzoate (2,45 g) and the mixture was stirred at room temperature for 30 minutes and then at 60oC for 30 minutes. At the end of this time the reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated and dried over anhydrous magnesium sulfate, and concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 9/1, m), 1,76-of 1.85 (2H, m), 2,61 (2H, t, J=6.5 Hz), 3,14 (2H, s), is 4.15 (4H, dq, J= 1,5, 7,0 Hz), free 5.01 (2H, s), 6,79 (2H, d, J=8.5 Hz), 6.89 in (2H, d, J=8.5 Hz), 7,15-7,44 (10H, m).

(b) Ethyl 2-(4-benzyloxybenzyl)-5-phenylvaleric

To a solution of diethyl 2-(4-benzyloxybenzyl)-2-(3-phenylpropyl)malonate (3,91 g) in a mixture of 2-methoxyethanol (30 ml) and water (3 ml) was added potassium hydroxide (2.00 g). The mixture was stirred at 130oC on an oil bath for 1.5 hours. At the end of this time the reaction mixture was distributed between ethyl acetate and water, and the mixture was acidified with an aqueous solution of hydrochloric acid (6 BC). An ethyl acetate layer was separated and washed with an aqueous solution of sodium chloride, dried over anhydrous magnesium sulfate and concentrated. The solution remaining syrup in xylene (20 ml) was stirred for 1 hour and then concentrated. To a solution of the syrup residue of 2-(4-benzyloxybenzyl)- 5-phenylalaninol acid in ethanol (40 ml) was added concentrated sulfuric acid (1 ml). The mixture was stirred at 80oC for 3 hours and left to stand at room temperature for 16 hours. At the end of this time the reaction mixture was concentrated and the residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated, dried over anhydrous magnesium sulfate and concentrated the dosa is 0 (4H, m), 2,53-a 2.71 (4H, m), 2,82-2,90 (1H, m), Android 4.04 (2H, q, J=7.0 Hz), 5,04 (2H, s), 6.87 in (2H, d, J=8.5 Hz), 7,05 (2H, d, J=8.5 Hz), 7,10-7,44 (10H, m).

(C) Ethyl 2-(4-hydroxybenzyl)-5-phenylvaleric

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 2-(4-benzyloxybenzyl)-5-phenylvaleric (of 3.32 g) and palladium on carbon (5%, 0.40 g) and the reaction mixture was treated to give the desired compound (2,56 g) as a syrup.1H-NMR (270 MHz, CDCl3): to 1.14 ppm (3H, t, J=7.0 Hz), 1,50-1,75 (4H, m), 2,53-a 2.71 (4H, m), 2,78-2,87 (1H, m), of 4.05 (2H, q, J=7.0 Hz), 6,70 (2H, d, J=8.5 Hz), 6,98 (2H, d, J=8.5 Hz), 7,12-7,29 (5H, m).

(d) Ethyl 2-(3-phenylpropyl)-3-[4-(2-preliminaty) phenyl]-propionate

The reaction was conducted in the same manner as described in reference example 1(e), using ethyl 2-(4-hydroxybenzyl)-5-phenylvaleric (1.42 g), which is the product of reference example 2(C), sodium hydride (55% suspension in oil, 228 mg) and N-[2-(methanesulfonate)ethyl]phthalimide (1,25 d), which is the product of reference example 1(a), and the reaction mixture was treated to give the desired compound (1,34 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.12 (3H, t, J=7.0 Hz), (1,46 is 1.70 (4H, m), 2,50-2,70 (4H, m), was 2.76-2,89 (1H, m), was 4.02 (2H, q, J=7.0 Hz), 4,10 (2H, t, J=5.5 Hz), 4,19 (2H, t, J=5.5 Hz), 6,77 (2H, d, J=8.5 Hz), 7,00 (2H, d, J=8.5 Hz), 7,10-7,20 (3H, m), 7,21-7,29 (2H, m)Ionut

(a) Diethyl 2-(4-methoxybenzylidene)malonate

To a solution of 4-methoxysalicylaldehyde (16.2 g) in ethanol (160 ml) was added piperidine (1.5 ml) and diethylmalonate (14.9 ml). The mixture was boiled under reflux for 7 hours. At the end of this time the reaction mixture was added ethyl acetate, the ethyl acetate was washed with an aqueous solution of hydrochloric acid (0.8 n), saturated aqueous sodium bicarbonate, and saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate, and then concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 9/1-3/1, to give the desired compound (5,00 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.33 (6H, t, J=7.0 Hz), 3,48 (3H, s), the 4.29 (2H, q, J= 7.0 Hz), 4,36 (2H, q, J=7.0 Hz), 5,20 (2H, s), 7,03 (2H, d, J=9.0 Hz), 7,42 (2H, d, J=9.0 Hz), to 7.67 (1H, s).

(b) Diethyl 2-(4-methoxyethoxymethyl)malonate

The reaction was conducted in the same manner as described in reference example 1(d), using diethyl 2-(4-methoxyethoxymethyl)malonate (to 4.98 g) and palladium on carbon (5%, 0.50 g) and the reaction mixture was treated to give the desired compound (5,00 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.24 (6H, t, J=7.0 Hz), 3,18 (2H, d, J=8.0 Hz), 3,49 (3H, benzyl)-2-(2-phenoxyethyl) malonate

The reaction was conducted in the same manner as described in reference example 2(a), using diethyl 2-(4 - methoxyethoxymethyl)malonate (1,58 g), which is the product of reference example 3(b), sodium hydride (55% suspension in oil, 0.24 g) and 2-phenoxyethylamine (1,23 g) and the reaction mixture was treated to give the desired compound (1,72 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.22 (6H, t, J=7.5 Hz), 2,30 (2H, t, J=6.5 Hz), 3,30 (2H, s), 3,47 (3H, s) 4,08 (2H, t, J=6.5 Hz), 4,19 (4H, q, J=7.5 Hz), 5,14 (2H, s), 6,84-of 6.96 (5H, m), 7,05 (2H, d, J=9.0 Hz), 7,16-7,30 (2H, m).

(d) Ethyl 2-(4-hydroxybenzyl)-4-phenoxybutyric

The reaction was conducted in the same manner as described in reference example 2(b), using diethyl 2-(4-methoxyethoxymethyl)-2-(2-phenoxyethyl)malonate (1,71 g) and potassium hydroxide, and the reaction mixture was treated to give the desired compound (1.25 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.13 (3H, t, J=7.0 Hz), 1,90-of 2.20 (2H, m), 2,74 are 2.98 (3H, m), 3,90-to 4.14 (4H, m), 4,71 (1H, s), 6,74 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 6,93 (1H, t, J=7.5 Hz), 7,05 (2H, d, J=8.5 Hz), 7,22-7,30 (2H, m).

(e) Ethyl 2-(2-phenoxyethyl)-3-[4-[2-(tetrahydropyran-2 - yloxy)ethoxy]phenyl] propionate

To a solution of ethyl 2-(4-hydroxybenzyl)-4-phenoxybutyric (620 mg), which is the product of reference example 3(d) in 2-butanone (8 ml) dobavljalo. In the reaction mixture was added dimethylacetamide (10 ml) and the mixture was stirred at 100oC for 1.5 hours. At the end of this time the reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and then concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 4/1, to give the desired compound (738 mg) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.13 (3H, t, J= 7.0 Hz), 1,50 is 2.10 (8H, m), 2,73 are 2.98 (3H, m), 3,48-to 3.58 (1H, m), of 3.77-4,17 (9H, m), 4,71 (1H, t, J=3.5 Hz), PC 6.82-6.87 in (4H, m), 6,93 (1H, t, J=7.5 Hz), to 7.09 (2H, d, J=8.5 Hz), of 7.23-7.29 trend (2H, m).

(f) Ethyl 3-[4-(2-hydroxyethoxy) phenyl]-2-(2 - phenoxyethyl)-propionate

To a solution of ethyl 2-(2-phenoxyethyl)-3-[4-[2- (tetrahydropyran-2-yloxy)ethoxy] phenyl] propionate (738 mg), which is the product of reference example 3(e), in ethanol (10 ml) was added monohydrate p-toluensulfonate acid (0,40). The mixture was stirred at room temperature for 2 hours. At the end of this time the reaction mixture was concentrated. The residue was distributed between ethyl acetate and saturated aqueous sodium bicarbonate. Atelast chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 7/3-3/2, to give the desired compound (503 mg) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.13 (3H, t, J=7.0 Hz), 1,90-2,10 (3H, m), 2,75-3,00 (3H, m), 3,92-4,11 (8H, m), PC 6.82-6.87 in (4H, m), 6,93 (1H, t, J=7.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7.23 percent-7,29 (2H, m).

(g) Ethyl 3-[4-(2-methanesulfonamido) phenyl] -2-(2 - phenoxyethyl) propionate

To a solution of ethyl 3-[4-(2-hydroxyethoxy)phenyl]-2-(2-phenoxyethyl)propionate (503 mg), which is the product of reference example 3(f), in anhydrous dichloromethane (10 ml) was added triethylamine (0,29 ml) and methanesulfonamide (0,12 ml). The reaction mixture was stirred at room temperature for 2 hours. At the end of this time the reaction mixture was concentrated. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated and dried over anhydrous magnesium sulfate and then concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 2/1-3/2, to give the desired compound (632 mg) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.13 (3H, t, J= 7.0 Hz), 1,90-of 2.20 (2H, m), 2,75-3,00 (3H, m) to 3.09 (3H, s), 3,89-was 4.02 (2H, m), 4,07 (2H, q, J=7.0 Hz), 4,20-to 4.23 (2H, m), 4,54-4,58 (2H, m), to 6.80-6.87 in (4H, m), 6,93 (1H, t, J-7.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7.23 percent-7,30 (2H, m).

(the) phenyl]-2-(2-phenoxyethyl)propionate, which is the product of reference example 3(g), in dimethylformamide (8 ml) was added sodium azide (0.29 grams). The mixture was stirred at 70oC for 2 hours. At the end of this time the reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated, dried over anhydrous magnesium sulfate and then concentrated to give the desired compound (546 mg) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.13 (3H, t, J=7.0 Hz), 1,90-of 2.20 (2H, m), 2,75-3,00 (3H, m) to 3.58 (2H, t, J=5.0 Hz), 3,89-4,14 (6H, m), for 6.81-6.87 in (4H, m), 6,93 (1H, t, J=7.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7,22-7,30 (2H, m).

(i) Ethyl 3-[4-(2-aminoethoxy) phenyl]-2-(phenoxyethyl) propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy) phenyl]-2-(2-phenoxyethyl)propionate (538 mg) and palladium on carbon (5%, 500 mg) and the reaction mixture was treated with obtaining the connection specified in the header (476 mg) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.13 (3H, t, J=7,0 Hz) of 1.66 (2H, user. C) 1,90-of 2.21 (2H, m), 2,75-3,07 3H, m), is 3.08 (2H, t, J=5.0 Hz), 3,90-4,12 (6H, m), 6,82-to 6.88 (4H, m), 6,93 (1H, t, J=7.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7.23 percent-7,30 (2H, m).

(Reference example 4)

Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate

(a) Diethyl 2-(4-benzyloxybenzyl)-2-proximalen

Reacts-benzyloxybenzoate (2,59 g) and sodium hydride (55% suspension in oil, 530 mg) and the reaction mixture was treated to give the desired compound (3,10 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.12 ppm (6H, t, J=7.0 Hz), of 3.57 (2H, s), is 4.15 (4H, q, J=7.0 Hz), 5,02 (2H, s), 6,84-7,14 (6H, m), 7,22-7,41 (8H, m).

(b) Ethyl 3-(4-benzyloxyphenyl)-2-phenoxypropionate

The reaction was conducted in the same manner as described in reference example 2(b), using diethyl 2-(4-benzyloxybenzyl)-2-proximalen (3,10 g) and potassium hydroxide (2.10 g) and the reaction mixture was treated with syrup 3-(4-benzyloxyphenyl)-2-phenoxypropionic acid to give the desired compound (2.10 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (3H, t, J= 7.0 Hz), 3,11-3,20 (2H, m) to 4.16 (2H, q, J=7.0 Hz), 4,74 (1H, DD, J= 5,5, 6,5 Hz), 5,04 (2H, s), at 6.84 (2H, d, J=8.0 Hz), 6,91 (2H, d, J=8.5 Hz), 6,92-6,97 (1H, m), 7,05-to 7.09 (1H, m), 7,22 (2H, d, J=8.5 Hz), 7,20-the 7.43 (6H, m).

(C) Ethyl 3-(4-hydroxyphenyl)-2-phenoxypropionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-phenoxypropionate (2.10 g), which is the product of reference example 4(b), and palladium on carbon (5%, 0.32 g) and the reaction mixture was treated to give the desired compound (1.01 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J= 7.0 Hz), 3,10-3,24 (2H, m) to 4.17 (2H, q, J=7.0 Hz), 4,74 (1H, the 2-phenoxy-3-[4-[2-(tetrahydropyran-2-yloxy) ethoxy] -phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 3-(4-hydroxyphenyl)-2-phenoxypropionate (3.33 g), which is the product of reference example 4 (C), 2-(2 - bromoethoxy)tetrahydropyran (7,27 g) and potassium carbonate (6,41 g) in dimethylacetamide, and the reaction mixture was treated to give the desired compounds (a 4.53 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 1,50-of 1.88 (6H, m), 3,16-3,20 (2H, m), 3,48 of 3.56 (1H, m), 3,76-3,93 (2H, m), 4,00-is 4.21 (5H, m), 4,69 was 4.76 (2H, m), 6,83 (2H, d,

J= 8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 6,94 (1H, t, J=7.0 Hz), 7.18 in-7,26 (4H, m).

(e) Ethyl 3-[4-(2-hydroxyethoxy)phenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-phenoxy-3-[4-[2- (tetrahydropyran-2-yloxy)ethoxy] phenyl] propionate (a 4.53 g), which is the product of reference example 4(d), and monohydrate p-toluensulfonate acid (2.70 g) and the reaction mixture was treated to give the desired compound (3.28 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 1,98-2,02 (1H, user. C), 3,14-3,20 (2H, m), 3,90-4,00 (2H, m) 4,06 (2H, t, J=4.5 Hz), 4,17 (2H, q, J=7.0 Hz), 4,74 (1H, DD, J=6,0, 7.5 Hz), 6,82-to 6.88 (4H, m), to 6.95 (1H, t, J=7.0 Hz), 7,21-7,26 (4H, m).

(f) Ethyl 3-[4-(2-methanesulfonamido)phenyl]-2-phenoxypropionate

) phenyl]-2-phenoxypropionate (3,27 g), which is the product of reference example 4(e), triethylamine (2,07 ml) and methanesulfonamide (0,84 ml) and the reaction mixture was treated to give the desired compound (4,20 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), of 3.07 (3H, s), 3,19 (2H, d, J=7,0 Hz), 4,14-of 4.25 (4H, m), 4,56 (2H, t, J=4.5 Hz), 4,74 (1H, t, J=7.0 Hz), at 6.84 (4H, d. J=8.5 Hz), to 6.95 (1H, t, J=7.0 Hz), 7,20-7,29 (4H, m).

(g) Ethyl 3-[4-(2-azidoethoxy)phenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 3-[4-(2-methanesulfonamido)phenyl]-2-phenoxypropionate (4,00 g), which is the product of reference example 4(f), and sodium azide (1,93 g) and the reaction mixture was treated to give the desired compound (3,40 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 3,14-up 3.22 (2H, m) to 3.58 (2H, t, J=5.0 Hz), of 4.13 (2H, t, J=5.0 Hz), 4,18 (2H, q, J=7.0 Hz), 4,74 (1H, dd. J=6,0, 7.5 Hz), 6,82-6,97 (5H, m), 7,21-7,29 (4H, m).

(h) Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl]-2-phenoxypropionate (3,40 g), which is the product of reference example 4(g), and palladium on carbon (5%, 350 mg) and the reaction mixture was treated with obtaining connection is Hz), 3,14-3,20 (2H, m), 3,90-to 4.15 (2H, m) to 4.17 (2H, q, J=7.0 Hz), 4,74 (1H, dd. J=6,0, 7,0 Hz), at 6.84 (4H, d, J=8.5 Hz), 6,94 (1H, t, J=7.5 Hz), 7,19-7,30 (4H, m).

(Reference example 5)

Ethyl 3-[4-(2-aminoethoxy)phenyl] -2-(4-isopropylphenoxy)-propionate

(a) Diethyl 2-(4-isopropylphenoxy)malonate

To a solution of 4-isopropylphenol (15.0 g) in a mixture of dimethylformamide (63 ml) and toluene (75 ml) was added sodium hydride (55% suspension in oil, with 5.22 g). The mixture was stirred at room temperature for 1 hour. In the reaction mixture was added diethyl 2-gloryland (18.5 g). The mixture was stirred at 60oC for 2.5 hours. At the end of this time the reaction mixture was added ethyl acetate. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and then concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 4/1, to give the desired compound (21,5 g) as a syrup.1H-NMR (270 MHz, CDCl3): to 1.21 ppm (6H, d, J=7,0 Hz), 2,81-2,95 (1H, m), 3,85 (6H, s), a total of 5.21 (1H, s), to 6.88 (2H, d, J= 8.5 Hz), to 7.15 (2H, d, J=8,5 Hz).

(b) Diethyl 2-(4-benzyloxybenzyl)-2-(4-isopropylphenoxy)-malonate

The reaction was conducted in the same manner as described in reference example 2(a), socialshare (19.7 g) and sodium hydride (55% suspension in oil, of 3.53 g) and the reaction mixture was treated to give the desired compound (32,3 g) as a syrup.1H-NMR (270 MHz, CDCl3): to 1.21 ppm (6H, d, J=6.5 Hz), 2,79 of 2.92 (1H, m), 3,55 (2H, s), 3,68 (6H, s), 5,02 (2H, s) 6,86 (4H, d, J=8.5 Hz), to 7.09 (4H, d, J=8.5 Hz), 7,30-the 7.43 (5H, m).

(C) Diethyl 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy) malonate

The reaction was conducted in the same manner as described in reference example 1 (d), using diethyl 2-(4-benzyloxybenzyl)-2-4-isopropylphenoxy)malonate (32,3 g), which is the product of reference example 5(b), and palladium on carbon (5%, 2.00 g) and the reaction mixture was treated to give the desired compounds of 25.2 g) in the form of syrup.1H-NMR (270 MHz, CDCl3): to 1.21 ppm (6H, d, J=7,0 Hz), of 2,75 2,95 (1H, m), of 3.54 (2H, s), 3,68 (6H, s), is 4.93 (1H, user. C) 6,69 (2H, d, J=8.5 Hz), 6.87 in (2H, d, J=8.5 Hz),? 7.04 baby mortality (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8,5 Hz).

(d) Ethyl 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionate

The reaction was conducted in the same manner as described in reference example 2(b), using diethyl 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)malonate of 25.2 g), which is the product of reference example 5(C), and potassium hydroxide (20,0 g) and the reaction mixture was treated with crystals of 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionic acid to give the desired compounds =5,5, 7.5 Hz), of 4.77 (1H, user.C) 6,76 (4H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,17 (2H, d, J=8,5 Hz).

(e) Ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy]phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 3-(4-hydroxyphenyl)-2-(4 - isopropylphenoxy)propionate (14.8 g), which is the product of reference example 5(d), 2-(2-bromoethoxy)tetrahydropyran (28,2 g) and potassium carbonate (24,9 g) in dimethylformamide, and the reaction mixture was treated to give the desired compound (20.6 g) in the form of syrup.

(f) Ethyl 3-[4-(2-hydroxyethoxy)phenyl]-2-(4-isopropylphenoxy) propionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-(4-isopropylphenoxy)-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy] -phenyl] propionate (20.6 g), which is the product of reference example 5(e), and monohydrate p-toluensulfonate acid (a 7.85 g) and the reaction mixture was treated to give the desired compound (16.2 g) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm 1,15-1,22 (9H, m), 2,75-3,00 (1H, m), 3,12-3,20 (2H, m), 3,90-3,99 (2H, m) 4,06 (2H, t, J=4.5 Hz), 4,17 (2H, q, J= 7.5 Hz), 4,69 (1H, DD, J=5,5, 7.5 Hz), 6,76 (2H, d, J=8.5 Hz), at 6.84 (2H, d, J=8,5 Hz)that was 7.08 (2H, d, J=8.5 Hz), 7,22 (2H, d, J=8,5 Hz).

(g) Ethyl 2-(4-isopropylphenoxy)-3-[4-cnom example 3(g), using ethyl 3-[4-(2-hydroxyethoxy)phenyl] -2-(4-isopropylphenoxy)propionate (16.2 g), which is the product of reference example 5(f), triethylamine (12.1 ml) and methanesulfonamide (of 5.05 ml) and the reaction mixture was treated to give the desired compound (19.6 g) in the form of syrup.1H-NMR (270 MHz, CDCl3): ppm 1,16-of 1.23 (9H, m), 2,72-2,90 (1H, m), of 3.07 (3H, s), 3,12-3,19 (2H, m), 4,10-to 4.23 (4H, m), 4,51-4,58 (2H, m), 4,69 (1H, DD, J= 5,5, 7.5 Hz), 6,76 (2H, d, J=8.5 Hz), 6,83 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7.23 percent (2H, d, J=8,5 Hz).

(h) Ethyl 3-[4-(2-azidoethoxy)phenyl]-2-(4 - isopropylphenoxy)-propionate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 2-(4-isopropylphenoxy)-3-[4-(2-methanesulfonamido)phenyl] -propionate (19.6 g), which is the product of reference example 5(g), and sodium azide (7,06 g) and the reaction mixture was treated to give the desired compound (15,8 g) as a syrup.

(i) Ethyl 3-[4-(2-aminoethoxy) phenyl]-2-(4 - isopropylphenoxy)-propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl] -2-(4-isopropylphenoxy)propionate (15,8 g), which is the product of reference example 5(h), and palladium on carbon (5%, 1.60 g) and the reaction mixture was treated with polumesecari)phenyl]-2-butylphosphonate

(a) Diethyl 2-(4-benzyloxybenzyl)-2-butylmalonate

The reaction was conducted in the same manner as described in reference example 2(a), using diethyl 2-butylmalonate (2.16 g), 4-benzyloxybenzyl chloride (2,44 g) and sodium hydride (55% suspension in oil, 480 mg) and the reaction mixture was treated to give the desired compound (3,67 g) as crystals. So pl. 73oC.1H-NMR (270 MHz, CDCl3): ppm of 0.91 (3H, t, J=7,0 Hz) of 1.24 (6H, t, J= 7.0 Hz), 1,20-to 1.38 (4H, m), 1,74 and 1.80 (2H, m), 3,18 (2H, s), 4,11-to 4.23 (4H, m), 5,02 (2H, s) 6,86 (2H, d, J-8.5 Hz), of 6.99 (2H, d, J=8.5 Hz), 7,31-7,44 (5H, m).

(b) Ethyl 2-(4-benzyloxybenzyl)caproate

The reaction was conducted in the same manner as described in reference example 2(b), using diethyl 2-(4-benzyloxybenzyl)-2-butylmalonate (of 3.60 g), which is the product of reference example 6(a), and potassium hydroxide (2.00 g) and the reaction mixture was treated with crystals of 2-(4-benzyloxybenzyl)-2-Caproic acid to give the desired compound (2,71 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7,0 Hz) to 1.14 (3H, t, J= 7.0 Hz), 1,20-1,70 (6H, m), of 2.51 - of 2.72 (2H, m), 2,85 (1H, DD, J=8,5, and 13.5 Hz), of 4.05 (2H, q, J=7.0 Hz), to 5.03 (2H, s), to 6.88 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,31 was 7.45 (5H, m).

(C) Ethyl 2-(4-hydroxybenzyl)caproate

The reaction was carried out in the same way, which is described in the reference b), and palladium on carbon (5%, 0.40 g) and the reaction mixture was treated to give the desired compound (1.90 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,20-of 1.35 (4H, m), 1,40-1,70 (2H, m), 2,53-of 2.72 (2H, m), 2,84 (1H, DD, J= 8,5, and 13.5 Hz), 4,06 (2H, q, J=7 Hz), is 4.93 (1H, s), 6,72 (2H, d, J=8.5 Hz), 7,02 (2H, d, J-8.5 Hz).

(d) Ethyl 2-butyl-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy]-phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 2-(4-hydroxybenzyl)caproate (2,40 g), which is the product of reference example 6(C), 2-(2-bromoethoxy)tetrahydropyran (1.63 g) and potassium carbonate (3,23 g) in dimethylacetamide, and the reaction mixture was treated to give the desired compound (2,47 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,21-of 1.36 (4H, m), 1,38-1,90 (8H, m), of 2.51 2.63 in (1H, m) to 2.67 (1H, DD, J=6,5, and 13.5 Hz), 2,85 (1H, DD, J=8,5, and 13.5 Hz), 3,48 of 3.56 (1H, m), 3.72 points-of 3.94 (3H, m), 3,96-4,16 (4H, m), 4,70 (1H, t, J=3.5 Hz), 6,83 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8,5 Hz).

(e) Ethyl 2-butyl-3-[4-(2-hydroxyethoxy)phenyl]propionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-butyl-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy]phenyl] propionate (2,47 g), which is the product of reference example 6(d), is inane (1.44 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), of 1.20 to 1.37 (3H, m), 1,39 is 1.70 (3H, m), 2,08 (1H, user.C) of 2.51 2.63 in (1H, m), 2,68 (1H, DD, J= 6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,89-4,00 (2H, m), as 4.02-4,11 (4H, m), PC 6.82 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8,5 Hz).

(f) Ethyl 2-butyl-3-[4-(2-methanesulfonylaminoethyl)- phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 2-butyl-3-[4-(2-hydroxyethoxy)phenyl]propionate (1.44 g), which is the product of reference example 6(e), triethylamine (2,04 ml) and methanesulfonyl chloride (0,76 ml) and the reaction mixture was treated to give the desired compound (1.65 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,22-of 1.39 (4H, m), 1,40-1,70 (2H, m), 2,52-2,61 (1H, m), 2,69 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), to 3.09 (3H, s) 4,06 (2H, q, J=7,0 Hz)that is 4.21 (2H, t, J=4.5 Hz), 4,55 (2H, t, J=4.5 Hz), for 6.81 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8,5 Hz).

(g) Ethyl 3-[4-(2-azidoethoxy)phenyl]-2-butylphosphonate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 2-butyl-3-[4-(2-methanesulfonamido)phenyl]propionate (1.65 g), which is the product of reference example 6(f), and sodium azide (0.95 g) and the reaction mixture was treated to give the desired compound (1,62 g) as a syrup.1

(h) Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl]-2-butylphosphonate (1,62 g), which is the product of reference example 6 (g), and palladium on carbon (5%, 243 mg) and the reaction mixture was treated with obtaining the connection specified in the header (1,49 g) as a syrup.

(Reference example 7)

Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-methyl-2-(3-phenylpropyl)-propionate

(a) Diethyl 2-methyl-2-(3-phenylpropyl)malonate

The reaction was conducted in the same manner as described in reference example 2(a), using diethyl 2-methylmalonate (3,48 g), 3-phenylpropylamine (3.98 g) and sodium hydride (55% suspension in oil, 0.96 g) and the reaction mixture was treated to give the desired compound (4,63 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.22 (6H, t, J=7,0 Hz) of 1.34 (3H, s), 1,50-to 1.63 (2H, m), 1,88-of 1.94 (2H, m), 2,62 (2H, t, J=7.5 Hz), 4,16 (4H, q, J=7.0 Hz), 7,15-7,30 (5H, m).

(b) Ethyl 2-methyl-5-phenylvaleric

The reaction was conducted in the same manner as described in reference example 2(b), using diethyl 2-methyl-2-(3-phenylpropyl)malonate (4,63 g) and the hydroxide is Mr (270 MHz, CDCl3): to 1.14 ppm (3H, d, J=7,0 Hz) of 1.24 (3H, t, J=7.0 Hz), 1,37-and 1.54 (1H, m), 1,55-to 1.87 (3H, m), 2,37 is 2.44 (1H, m), 2,61 (2H, t, J=7.5 Hz), of 4.12 (2H, q, J=7.0 Hz), 7,10-to 7.35 (5H, m).

(C) Ethyl 2-(4-benzyloxybenzyl)-2-methyl-5-phenylvaleric

To a solution of Diisopropylamine (3,23 g) in anhydrous tetrahydrofuran (60 ml) was added dropwise a solution of n-utility in hexane (1.65 M, with 19.4 ml) for 20 minutes at -60oC. the Mixture was stirred at 0oC for 30 minutes. To this mixture was added dropwise a solution of 2-methyl-5-phenylvaleric (7,05 g) in anhydrous tetrahydrofuran (30 ml) for 20 minutes at -70oC and the mixture was stirred at -70oC for 40 minutes. To the reaction mixture was added dropwise a solution of 4-benzyloxybenzaldehyde (9,68 g) in anhydrous tetrahydrofuran (80 ml) at -70oC. the Mixture was stirred at -70oC for 3 hours. At the end of this time the reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 15/1, to give the desired compound (1.88 g) in the form=13.5 Hz), 4,08 (2H, q, J=7.0 Hz), free 5.01 (2H, s), at 6.84 (2H, d, J=8.5 Hz), 6,97 (2H, d, J=8.5 Hz), 7,14-7,49 (10H, m).

(d) Ethyl 2-(4-hydroxybenzyl)-2-methyl-5-phenylvaleric

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 2-(4-benzyloxybenzyl)-2-methyl-5-phenylvaleric (1.88 g), which is the product of reference example 7(C), and palladium on carbon (5%, 0.28 g) and the reaction mixture was treated to give the desired compound (1,58 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.06 (3H, s) of 1.20 (3H, t, J=7.0 Hz), 1,35-of 1.85 (4H, m), 2,56 of 2.68 (2H, m) 2,60 (1H, d, J= 13.5 Hz), 2,92 (1H, d, J=13.5 Hz), 4.09 to (2H, q, J=7.0 Hz), 5,18 (1H, user.C) of 6.68 (2H, d, J=8.5 Hz), 6,91 (2H, d, J=8.5 Hz), 7,05 and 7.36 (5H, m).

(e) Ethyl 2-methyl-2-(3-phenylpropyl)-3-[4-[2-(tetrahydropyran-2-yloxy) ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 2-(4-hydroxybenzyl)-2-methyl-5-phenylvaleric (1,58 g), which is the product of reference example 7(d), 2-(2-bromoethoxy)tetrahydropyran (0,94 g) and potassium carbonate (1.86 g) in dimethylacetamide, and the reaction mixture was treated to give the desired compound (1.64 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.05 ppm (3H, s) to 1.21 (3H, t, J= 7,10 Hz), 1,35-1,90 (10H, m), 2,50-of 2.64 (2H, m), 2,62 (1H, d, J=13.5 Hz), with 2.93 (1H, d, J=13.5 Hz), 3.45 points of 3.56 (1H, m), 3,67-4,15 (the Teal-2-(3 - phenylpropyl)propionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-methyl-2-(3-phenylpropyl)-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy] phenyl] -propionate (1.64 g), which is the product of reference example 7(e), and monohydrate p-toluensulfonate acid (0.68 g) and the reaction mixture was treated to give the desired compound (0.95 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.06 (3H, s) to 1.21 (3H, t, J=7.0 Hz), 1,38-to 1.82 (4H, m), 2,04 (1H, user.C) 2,56-to 2.65 (3H, m) to 2.94 (1H, d, J= 13.5 Hz), a 3.87-of 3.97 (2H, m), 3,99-to 4.14 (4H, m), 6,79 (2H, d, J=8.5 Hz), 6,98 (2H, d, J=8.5 Hz), 7,10-7,31 (5H, m).

(g) Ethyl 3-[4-(2-methanesulfonamido)phenyl] -2-methyl-2-(3-phenyl-propyl)propionate

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 3-[4-(2-hydroxyethoxy)phenyl]-2-methyl-2-(3-phenylpropyl)propionate (0.95 g), which is the product of reference example 7(f), triethylamine (1.07 ml) and methanesulfonamide (0,40 ml) and the reaction mixture was treated to give the desired compound (1,16 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.05 ppm (3H, s) to 1.21 (3H, t, J=7.0 Hz), 1,38-to 1.82 (4H, m) at 2.59 (2H, t, J=7.0 Hz), 2,62 (1H, d, J=13.5 Hz), to 2.94 (1H, d, J= 13.5 Hz), is 3.08 (3H, s), 4.09 to (2H, q, J=7.0 Hz), is 4.21 (2H, t, J=4.5 Hz), 4,56 (2H, t, J= 4.5 Hz), 6,77 (2H, d, J=8.5 Hz), 6,99 (2H, l, J=8.5 Hz), 7,15-7,31 (5H, m).

(h) Ethyl 3-[EN in reference example 3(h), using ethyl 3-[4-(2-methanesulfonamido)phenyl]-2-methyl-2-(3-phenylpropyl)-propionate (1,16 g), which is the product of reference example 7 (g), and sodium azide (0.50 g) and the reaction mixture was treated to give the desired compound (0,86 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 1.06 (3H, s) to 1.21 (3H, t, J=7.0 Hz), 1,38-to 1.82 (4H, m), 2,56-to 2.65 (3H, m) to 2.94 (1H, d, J=13.5 Hz), to 3.58 (2H, t, J=5.0 Hz), 4,05-to 4.14 (4H, m), is 6.78 (2H, d, J=8.5 Hz), of 6.99 (2H, d, J=8.5 Hz), 7,15-7,31 (5H, m).

(i) Ethyl 3-[4-2-aminoethoxy)phenyl]-2-methyl-2-(3-phenylpropyl)propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl] -2-methyl-2-(3-phenylpropyl)propionate (0,86 g), which is the product of reference example 7(h), and palladium on carbon (5%, 129 mg) and the reaction mixture was treated with obtaining the connection specified in the header (to 0.80 g) as a syrup.

(Reference example 8)

Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-methyl-2-phenoxypropionic

(a) Ethyl 3-(4-benzyloxyphenyl)-2-methyl-2-phenoxypropionic

The reaction was conducted in the same manner as described in reference example 7(C), using ethyl 2-phenoxypropionate (x 6.15 g), 4-benzyloxybenzaldehyde (9,62 g) and dicyclohexylamine (5,78 g) instead of Diisopropylamine, and the reaction with the H, t, J=7.0 Hz), of 1.40 (3H, s), 3,11 (1H, d, J=14,0 Hz), or 3.28 (1H, d, J=14,0 Hz), 4,19 (2H, q, J=7.0 Hz), 5,04 (2H, s), 6.75 in-7,02 (5H, m), 7,11-7,47 (9H, m).

(b) Ethyl 3-(4-hydroxyphenyl)-2-methyl-2-phenoxypropionic

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-methyl-2-phenoxypropionate (equal to 4.97 g), which is the product of reference example 8(a), and palladium on carbon (5%, 0.75 g) and the reaction mixture was treated to give the desired compounds (of 3.85 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J= 7.0 Hz), of 1.40 (3H, s), 3,10 (1H, d, J=14,0 Hz), 3,24 (1H, d, J=14,0 Hz), 4,20 (2H, q, J=7.0 Hz), 6,13 (1H, user.C) 6,74 (2H, d, J=8.5 Hz), 6,83 (2H, d, J=8.5 Hz), of 6.96 (1H, t, J=7.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,20 (2H, DD, J=7,5, 8,5 Hz).

(C) Ethyl 2-methyl-2-phenoxy-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy]phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 3-(4-hydroxyphenyl)-2-methyl-2-phenoxypropionate (1.55 g), which is the product of reference example 8(b), 2-(2-bromoethoxy)tetrahydropyran (1.08 g) and potassium carbonate (2.14 g) in dimethylacetamide, and the reaction mixture was treated to give the desired compound (1.60 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7,0 Hz) of 1.39 (3H, s), 1,45-1,90 (6H, m), 3,11 (1H, d, J=13,5 P CLASS="ptx2">

(d) Ethyl 3-[4-(2-hydroxyethoxy) phenyl]-2-methyl-2 - phenoxypropionic

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-methyl-2-phenoxy-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy] phenyl] propionate (1.60 g), which is the product of reference example 8(C), and monohydrate p-toluensulfonate acid (0,70 g) and the reaction mixture was treated to give the desired compound (1.10 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J=7.0 Hz), of 1.40 (3H, s), is 2.09 (1H, user.C) 3,11 (1H, d, J=13.5 Hz), or 3.28 (1H, d, J=13.5 Hz), 3,91-4,00 (2H, m), 4,07 (2H, t, J=4.5 Hz), is 4.21 (2H, q, J=7.0 Hz), for 6.81-6.90 to (4H, m), 6,97 (1H, t, J=7.5 Hz), 7,13-7,28 (4H, m).

(e) Ethyl 3-[4-(2-methanesulfonamido) phenyl]-2-methyl-2-phenoxypropionic

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 3-[4-(2-hydroxyethoxy) phenyl]-2-methyl-2-phenoxypropionate (1.10 g), which is the product of reference example 8(d), triethylamine (0,49 ml) and methanesulfonamide (0.25 ml) and the reaction mixture was treated to give the desired compound (1.42 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J=7.0 Hz), of 1.40 (3H, s), of 3.07 (3H, s), 3,11 (1H, d, J=14,0 Hz), 3,29 (1H, d, J=14,0 Hz), 4,17-of 4.25 (4H, m), 4,56 (2H, t, J=4.5 Hz), for 6.81-6,93 (4H, m), 6,98 (1H, t, J=7.5 Hz), 7,17-7,26 (4H, m).

(f) e is in reference example 3(h), using ethyl 3-[4-(2-methanesulfonamido)phenyl]-2-methyl-2-phenoxypropionate (1.42 g), which is the product of reference example 8(e), and sodium azide (0.66 g) and the reaction mixture was treated to give the desired compound (0,82 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.22 (3H, t, J= 7.0 Hz), of 1.40 (3H, s), 3,12 (1H, d, J=14,0 Hz), 3,29 (1H, d, J= 14,0 Hz) to 3.58 (2H, t, J=5.0 Hz), of 4.13 (2H, t, J=5.0 Hz), 4,20 (2H, q, J= 7.0 Hz), PC 6.82-6.89 in (4H, m), 6,97 (1H, t, J=7.5 Hz), 7,17-7,27 (4H, m).

(g) Ethyl 3-[4-(2-aminoethoxy) phenyl]-2-methyl-2-phenoxypropionic

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2 - azidoethoxy)phenyl]-2-methyl-2-phenoxypropionate (0,82 g), which is the product of reference example 8(f), and palladium on carbon (5%, 123 mg) and the reaction mixture was treated with obtaining the connection specified in the header (0,76 g) as a syrup.

(Reference example 9)

3-[4-(2-aminoethoxy)phenyl]-2-(4-isopropylphenoxy)-2-methylpropionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(4-isopropylphenoxy)-2-methylpropionic

The reaction was conducted in the same manner as described in reference example 7(C), using ethyl 2-(4-isopropylphenoxy)propionate (4,72 g) and 4-benzyloxybenzyl chloride (6,00 g) and dicyclohexylamine (3.62 in) instead of diisopropyl the Hz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz) to 1.21 (3H, t, J=7.5 Hz), to 1.38 (3H, s), and 2.83 (1H, septet, J=7.0 Hz), 3,11 (1H, d, J=13.5 Hz) at 3.25 (1H, d, J=13.5 Hz), 4,20 (2H, q, J=7.5 Hz), of 5.05 (2H, s), of 6.75 (2H, d, J=8,5 Hz), 6,91 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,18 (2H, d, J=8.5 Hz), 7,30 was 7.45 (5H, m).

(b) Ethyl 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-(4-isopropylphenoxy)-2-methylpropionate book (6.16 g), which is the product of reference example 9(a), and palladium on carbon (5%, and 1.00 g) and the reaction mixture was treated with obtaining the connection specified in the header (4,18 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz) to 1.22 (3H, t, J=7.5 Hz), to 1.38 (3H, s), and 2.83 (1H, septet, J=7.0 Hz), 3,10 (1H, d, J=13.5 Hz), 3,24 (1H, d, J= 13.5 Hz), 4,20 (2H, q, J=7.5 Hz), to 4.81 (1H, s), 6.75 in (4H, d, J=8,5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=8,5 Hz).

(C) Ethyl 2-(4-isopropylphenoxy)-2-methyl-3-[4-[2-(tetrahydropyran - 2-yloxy)-ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)-2 - methylpropionate (1,00 g), which is the product of reference example 9(b), 2-(2-bromoethoxy)tetrahydropyran (1.84 g) and potassium carbonate (1,62 g) in dimethylacetamide, and implement the SUB>): of 1.20 ppm (6H, d, J= 7,0 Hz) of 1.23 (3H, t, J=7.0 Hz), of 1.36 (3H, s), 1,48-1,90 (6H, m), and 2.83 (1H, septet, J=7.0 Hz), 3,10 (1H, d, J=13.5 Hz) at 3.25 (1H, d, J=13.5 Hz), 3,48 is 3.57 (1H, m), 3,78-of 3.96 (2H, m), 4,01-of 4.25 (5H, m), 4,70-to 4.73 (1H, m), of 6.75 (2H, d, J=8.5 Hz), 6,86 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,17 (2H, d, J=8,5 Hz).

(d) Ethyl 2-(4-isopropylphenoxy)-3-[4-(2-hydroxyethoxy)-phenyl] -2-methylpropionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-(4-isopropylphenoxy)-2-methyl-3-[4-[2-(tetrahydropyran-2-yloxy)-ethoxy]phenyl]propionate (1.06 g), which is the product of reference example 9(C), and monohydrate p-toluensulfonate acid (0,60 g) and the reaction mixture was treated to give the desired compound (0.66 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz) of 1.23 (3H, t, J=7,0 Hz) to 1.37 (3H, s), a 2.01 (1H, t, J=6.0 Hz), and 2.83 (1H, septet, J=7.0 Hz), 3,11 (1H, d, J=13.5 Hz), 3,26 (1H, d, J=13.5 Hz), 3,93-4,00 (2H, m), 4,05-4,10 (2H, m), is 4.21 (2H, q, J=1.0 Hz), to 6.75 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,19 (2H, d, J-8.5 Hz).

(e) Ethyl 2-(4-isopropylphenoxy)-3-[4-(2-methanesulfonamido)phenyl] -2-methylpropionate

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 2-(4-isopropylphenoxy)-3-[4-(2-hydroxyethoxy)phenyl]-2-methyl-propionate (0.66 g), which is the product of reference primeomega compound (0.64 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz) of 1.23 (3H, t, J=7,0 Hz) to 1.37 (3H, s), and 2.83 (1H, septet, J=7.0 Hz), to 3.09 (3H, s), 3,11 (1H, d, J=13.5 Hz), 3,26 (1H, d, J=13.5 Hz), is 4.21 (2H, q, J 7.0 Hz), 4,22-4.26 deaths (2H, m), 4,55-4,59 (2H, m), of 6.75 (2H, d, J=8.5 Hz), 6,83 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8,5 Hz).

(f) Ethyl 3-[4-(2-azidoethoxy)phenyl]-2-(4-isopropylphenoxy)-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 2-(4-isopropylphenoxy)-3-[4-(2-methanesulfonylaminoethyl)-phenyl] -2-methylpropionate (0, 64 g), which is the product of reference example 9(e), and sodium azide (0.27 g) and the reaction mixture was treated to give the desired compound (0.56 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz) of 1.23 (3H, t, J=7,0 Hz) to 1.37 (3H, s), and 2.83 (1H, septet, J=7.0 Hz), 3,11 (1H, d, J=13.5 Hz), 3,26 (1H, d, J= 13.5 Hz) and 3.59 (2H, t, J=5.0 Hz), 4,14 (2H, t, J=5.0 Hz), is 4.21 (2H, q, J= 7,0 Hz), to 6.75 (2H, d, J=8.5 Hz), 6,85 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,19 (2H, d, J=8,5 Hz).

(g) Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(4-isopropylphenoxy)-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl]-2-(4-isopropylphenoxy)-2-methylpropionate (0.56 g), which is the product of reference example 9(f), and palladium on carbon (5%, 60 mg), and reacts who MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz) of 1.23 (3H, t, J=7,0 Hz) to 1.37 (3H, s), and 1.63 (2H, user.C), and 2.83 (1H, septet, J=7.0 Hz), is 3.08 (2H, t, J=5.0 Hz), 3,10 (1H, d, J=13.5 Hz) at 3.25 (1H, d, J=13.5 Hz), 3,92 is 4.13 (2H, m), is 4.21 (2H, q, J= 7.0 Hz), to 6.75 (2H, d, J=8.5 Hz), at 6.84 (2H, d, J=8.5 Hz), 7,06 (2H, l, J=8.5 Hz), 7,18 (2H, d, J=8,5 Hz).

(Reference example 10)

Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butyl-2-methylpropionate

(a) Ethyl 2-(4-benzyloxybenzyl)-2-metaloprokat

The reaction was conducted in the same manner as described in reference example 7(C), using ethyl 2-(4-benzyloxybenzyl)caproate (2,04 g) and methyliodide (1,12 ml) instead of 4-benzyloxybenzaldehyde, and cyclohexylethylamine (1,48 ml) instead of Diisopropylamine, and the reaction mixture was treated to give the desired compound (1.80 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7,0 Hz) of 1.06 (3H, s), 1,10-of 1.45 (8H, m), 1,63-to 1.79 (1H, m), 2.63 in (1H, d, J=13.5 Hz), 2,96 (1H, d, J=13.5 Hz), 4,10 (2H, q, J=7.0 Hz), to 5.03 (2H, s) 6,86 (2H, d, J=8.5 Hz), 7,02 (2H, d, J=8.5 Hz), 7,25-7,46 (5H, m).

(b) Ethyl 2-butyl-3-(4-hydroxyphenyl)-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 2-(4-benzyloxybenzyl)-2-metaloprokat (3,95 g), which is the product of reference example 10(a), and palladium on carbon (5%, 0.40 g) and the reaction mixture was treated to give the desired is 61 (1H, d, J=13.5 Hz), 2,95 (1H, d, J=13.5 Hz), 4,10 (2H, q, J=7.0 Hz), 4,80 (1H, user.C) of 6.71 (2H, d, J=8.5 Hz), of 6.96 (2H, d, J=8,5 Hz).

(C) Ethyl 2-butyl-2-methyl-3-[4-[2-(tetrahydropyran-2 - yloxy)ethoxy]phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 2-butyl-3-(4-hydroxyphenyl)-2-methylpropionate (2,95 g), which is the product of reference example 10(b), 2-(2 - bromoethoxy)tetrahydropyran (of 4.66 g) and potassium carbonate (4,62 g) in dimethylacetamide, and the reaction mixture was treated to give the desired compound (4,18 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7.0 Hz), of 1.05 (3H, s), 1,11 was 1.43 (8H, m), 1,47-1,90 (7H, m), 2,62 (1H, d, J=13.5 Hz), 2,95 (1H, d, J=13.5 Hz), 3,48 is 3.57 (1H, m), 3,64-4,18 (7H, m), 4,67-4,72 (1H, m), for 6.81 (2H, d, J=8.5 Hz), 7,00 (2H, d, J=8,5 Hz).

(d) Ethyl 2-butyl-3-[4-(2-hydroxyethoxy)phenyl]-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-butyl-2-methyl-3-[4-[2- (tetrahydropyran-2-yloxy)ethoxy] -phenyl] propionate (4,18 g), which is the product of reference example 10(C), and monohydrate p-toluensulfonate acid (2,61 g) and the reaction mixture was treated to give the desired compound (2,73 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=7,0 Hz) of 1.06 (3H, s) of 1.10 to 1.47 (8H, m), 1S="ptx2">

(e) Ethyl 2-butyl-3-[4-(2-methanesulfonamido)phenyl]-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 2-butyl-3-[4-(2 - hydroxyethoxy)phenyl]-2-methylpropionate (2,73 g), which is the product of reference example 10(d), triethylamine (of 1.85 ml) and methanesulfonyl chloride (0.75 ml) and the reaction mixture was treated to give the desired compound (3,17 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7,0 Hz) of 1.06 (3H, s), 1,10-of 1.44 (8H, m), 1,66 and 1.80 (1H, m), 2,62 (1H, d, J=13.5 Hz), 2,97 (1H, d, J=13.5 Hz), is 3.08 (3H, s), 4,11 (2H, q, J=7.5 Hz), 4,20-to 4.23 (2H, m), 4,54-4,58 (2H, m), 6,79 (2H, d, J=8.5 Hz), 7,03 (2H, d, J=8,5 Hz).

(f) Ethyl 3-[4-(2-azidoethoxy) phenyl]-2-butyl-2 - methylpropionate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 2-butyl-3-[4-(2-methanesulfonamido)phenyl]-2-methylpropionate (3,17 g), which is the product of reference example 10(e), and sodium azide (1.60 g) and the reaction mixture was treated to give the desired compound (2,80 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=7,0 Hz) of 1.06 (3H, s), 1,10-of 1.44 (8H, m), 1,66-of 1.78 (1H, m), 2.63 in (1H, d, J= 13.5 Hz), 2,96 (1H, d, J=13.5 Hz), to 3.58 (2H, t, J=5.0 Hz), 4,11 (2H, q, J= 7.5 Hz), of 4.12 (2H, t, J=5.0 Hz), for 6.81 (2H, d, J=8.5 Hz), 7,03 (2H, d, J-8.5 Hz).

(g) Ethyl 3-[4-(2-minimera 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl]- 2-butyl-2-methylpropionate (2,73 g), which is the product of reference example 10(f), and palladium on carbon (5%, 270 mg) and the reaction mixture was treated with obtaining the connection specified in the header (2,42 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7,0 Hz) of 1.06 (3H, s), 1,10-of 1.43 (9H, m), 1,71 (2H, user.C) 2,62 (1H, d, J=13.5 Hz), 2,96 (1H, d, J=13.5 Hz), of 3.07 (2H, t, J= 5.0 Hz), 3,91-4,10 (2H, m), 4,11 (2H, q, J=7.0 Hz), to 6.80 (2H, d, J=8.5 Hz), 7,01 (2H, d, J=8,5 Hz).

(Reference example 11)

Ethyl 2-butyl-3-[4-[2-(4'-dimethoxybiphenyl-4-carbylamine)ethoxy] phenyl]propionate

(a) Methyl 4'-dimethoxybiphenyl-4-carboxylate

To a solution of methyl 4'-formylphenyl-4-carboxylate (2.00 g) in methanol (20 ml) was added meteorophobia (4,55 ml) and amberlyst 15 (200 mg). The mixture was left to stand at room temperature for 14 hours. Amberlyst was removed by filtration and the filtrate was concentrated under reduced pressure. Excess meteorophobia azeotropic toluene was evaporated. The residue was led from diisopropyl ether to give the desired compound (2,23 g) as colorless crystals. So pl. 76-77oC.1H-NMR (270 MHz, CDCl3): ppm 3,37 (6H, s), of 3.94 (3H, s), the 5.45 (1H, s), 7,55 (2H, d, J= 8.5 Hz), to 7.64 (2H, d, J= 8.5 Hz), to 7.67 (2H, d, J=8.5 Hz), 8,11 (2H, d, J=8,5 EY described in example 2, using methyl 4'-dimethoxybiphenyl-4-carboxylate (1.89 g), which is the product of reference example 11(a), and aqueous sodium hydroxide (1 N., 9,90 ml) and the reaction mixture was treated to give the desired compound (1.80 g) as colorless crystals. So pl. 164oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm of 3.28 (6H, s), the 5.45 (1H, s), 7,51 (2H, d, J= 8.5 Hz), 7,76 (2H, d, J= 8.5 Hz), 7,81 (2H, d, J - 8.5 Hz), 8,02 (2H, d, J= 8,5 Hz).

(C) Ethyl 2-butyl-3-[4-[2-(4'-dimethoxybiphenyl-4-carbylamine)ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (1,81 g), which is the product of reference example 6, 4'-dimethoxybiphenyl-4-carboxylic acid (1.68 g), which is the product of reference example 11(b), and carbonyldiimidazole (1.20 g) and the reaction mixture was treated to give the desired compound (2,77 g) as a pale brown solid product.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,22-of 1.36 (4H, m), 1,38-1,49 (1H, m) and 1.51-1,71 (1H, m), 2,52-2,63 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), to 3.36 (6H, s), 3,88 (2H, q, J=5.0 Hz), of 4.05 (2H, q, J=7.0 Hz), 4,14 (2H, t, J=5.0 Hz), the 5.45 (1H, s), of 6.65 (1H, user.t), 6,83 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,54 (2H, d, J=8.5 Hz), a 7.62 (2H, iluvenis-4-carbylamine) ethoxy] phenyl]propionate

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (375 mg), which is the product of reference example 6, 4'-methoxycarbonylmethyl-4-carboxylic acid (328 mg) and carbonyldiimidazole (225 mg) and the reaction mixture was treated with obtaining the connection specified in the header (257 mg) as colorless crystals. So pl. 93-95oC.1H-NMR (270 MHz, CDCl3): ppm 0,86 (3H, t, J=6.5 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,21-of 1.36 (4H, m), 1,40-to 1.67 (2H, m), 2,52-2,63 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), is 2.88 (1H, DD, J=8,5, and 13.5 Hz), with 3.89 (2H, t, J=5.0 Hz), of 3.95 (3H, s), of 4.05 (2H, q, J=7.0 Hz), is 4.15 (2H, t, J=5.0 Hz), 6,63 (1H, user.C) at 6.84 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J= 8.5 Hz), to 7.68 (2H, d, J-8.5 Hz), 7,69 (2H, d, J=8.5 Hz), 7,88 (2H, d, J=8,5 Hz) to 8.12 (2H, d, J=8,5 Hz).

(Reference example 13)

3'-Hydroxybiphenyl-4-carboxylic acid to a solution of methyl 3'-methoxybiphenyl-4-carboxylate (2.00 g) in anhydrous dichloromethane (10 ml) was added a solution of tribromide boron in dichloromethane (1 N., 24,8 ml) at -70oC. the Mixture was stirred at room temperature for 4 hours and the reaction mixture on an ice bath was added a mixture of ice and water, and then the mixture was stirred for 30 minutes. The reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and leaders introduce pressure. The residue was led from a mixture of hexane and diisopropyl ether to obtain the connection specified in the header (1,82 g) as pale yellow crystals. So pl. 250 -

253oC.1H-NMR (270 MHz, CDCl3): ppm 6,89 (1H, d, J=8.0 Hz), 7,11 (1H, d, J=8.0 Hz), 7,13 (1H, s), 7,28 (1H, t, J=8.0 Hz), to 7.64 (2H, d, J=8,5 Hz) to 8.12 (2H, d, J=8,5 Hz).

(Reference example 14)

Ethyl 2-butyl-3-[4-[2-(3'-dimethoxybiphenyl-4-carbylamine)ethoxy] -phenyl]propionate

(a) Methyl 3'-formylphenyl-4-carboxylate

To a solution of 3-formylphenylboronic acid (3.00 g) and methyl 4-bromobenzoyl acid (4,30 g) in a mixture of toluene (30 ml), ethanol (50 ml) and saturated aqueous solution of hydrogencarbonate sodium (30 ml) at room temperature was added a solution of tetrakis(triphenylphosphine) palladium (297 mg). The mixture was boiled under reflux for 2 hours at 100oC. the Reaction mixture was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was washed with a saturated aqueous solution of sodium chloride, and dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was led from diisopropyl ether to obtain the connection specified in the header (3,37 g) as colorless crystals. So pl. 95-97oC. 1

(b) Methyl 3'-dimethoxybiphenyl-4-carboxylate

The reaction was conducted in the same manner as described in example 11(a) using methyl 3'-formylphenyl-4-carboxylate (1.60 g), which is the product of reference example 14(a), meteorophobia (3,64 ml) and amberlyst 15 (160 mg) and the reaction mixture was treated to give the desired compound (1,91 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm 3,37 (6H, c), of 3.94 (3H, s), 5,46 (1H, s), 7,47 (1H, d, J= 4.5 Hz), 7,49 (1H, d, J= 2.5 Hz), EUR 7.57-to 7.64 (1H, m), to 7.68 (2H, d, J= 8.5 Hz), 7,72 (1H, s), 8,11 (2H, d, J=8,5 Hz).

(C) the 3'-Dimethoxybiphenyl-4-carboxylic acid

The reaction was conducted in the same manner as described in example 2, using methyl 3'-dimethoxybiphenyl-4-carboxylate (1,91 g), which is the product of reference example 14(b), and aqueous sodium hydroxide (1 N., 10.0 ml) and the reaction mixture was treated to give the desired compound (1.55 g) as colorless crystals. So pl. 130-131oC.1H-NMR (270 MHz, CDCl3): ppm to 3.38 (6H, s), of 5.48 (1H, s), 7,49 (1H, d, J= 5.0 Hz), 7,49 (1H, d, J= 3.5 Hz), to 7.59-7,66 (1H, m), 7,73 (2H, d, J= 8.5 Hz), of 7.75 (1H, s), 8,19 (2H, d, J=8,5 Hz).

(d) Ethyl 2-butyl-3-[4-[2-(3'-dimethoxybiphenyl-4-carbylamine)ethoxy]phenyl] propionate

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2 is iphenyl-4-carboxylic acid (1.44 g), which is the product of reference example 14(C), and carbonyldiimidazole (1,03 g) and the reaction mixture was treated to give the desired compound (2,72 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), to 1.21 and 1.35 (4H, m), 1,39-of 1.56 (1H, m), 1,58 - to 1.67 (1H, m), 2,53-to 2.65 (1H, m), 2,69 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,37 (6H, s), the 3.89 (2H, q, J=5.0 Hz), 4,06 (2H, q, J=7.0 Hz), is 4.15 (2H, t, J=5.0 Hz), the 5.45 (1H, s), only 6.64 (1H, user.t), at 6.84 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,46 (1H, d, J=5.0 Hz), 7,47 (1H, d, J=3.0 Hz), 7,54-to 7.61 (1H, m), to 7.68 (2H, d, J=8.5 Hz), 7,71 (1H, s), a 7.85 (2H, d, J=8,5 Hz).

(Reference example 15)

Sodium 2-butyl-3-[4-[2-(3'-methoxyethoxymethyl-4-carbylamine)ethoxy]phenyl]propionate

(a) Methyl 3'-hydroxymethyluracil-4-carboxylate

To a solution of methyl 3'-formylphenyl-4-carboxylate (720 mg), which is the product of reference example 14 (a), in ethanol (50 ml) was added sodium borohydride (132 mg) at room temperature. The mixture was stirred in nitrogen atmosphere for 50 minutes. The reaction mixture was extinguished 50% acetic acid and concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was washed saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and the concentration of the compound (522 mg) as colorless crystals. So pl. 88-89oC.1H-NMR (270 MHz, CDCl3): ppm of 3.95 (3H, s), rate 4.79 (2H, s), 7,40 (1H, d, J=7.5 Hz), 7,47 (1H, t, J= 7.5 Hz), 7,56 (1H, d, J=7.5 Hz), to 7.64 (1H, s), to 7.67 (2H, d, J=8.5 Hz), 8,11 (2H, d, J=8,5 Hz).

(b) Methyl 3'-methoxyethoxymethyl-4-carboxylate

To a solution of methyl 3'-hydroxymethyluracil-4-carboxylate (504 mg), which is the product of reference example 15(a), in bezvodnom dichloromethane (10 ml) was added chloromethylation ether (0,24 ml) and diisopropylethylamine (0,74 ml) at 0oC. the Mixture was stirred at 0oC for 1 hour and then left to stand at room temperature for 14 hours. The reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was washed saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 2/1, to give the desired compound (467 mg) as colorless crystals. So pl. 54-55oC. 1H-NMR (270 MHz, CDCl3): ppm 3,44 (3H, s), of 3.94 (3H, s), of 4.67 (2H, s), and 4.75 (2H, s), 7,39 (1H, d, J=7.5 Hz), 7,46 (1H, t, J= 7.5 Hz), 7,56 (1H, d, J=7.5 Hz), 7,63 (1H, s), to 7.67 (2H, d, J=8.5 Hz), 8,11 (2H, d the way which is described in example 2, using methyl 3'-methoxyethoxymethyl-4-carboxylate (445 mg), which is the product of reference example 15(b), and aqueous sodium hydroxide (1 N., 3,10 ml) and the reaction mixture was treated to give the desired compound (342 mg) as colorless crystals. So pl. 126-127oC.1H-NMR (270 MHz, CDCl3): to 3.45 ppm (3H, s), and 4.68 (2H, s), was 4.76 (2H, s), 7,41 (1H, d, J=7.5 Hz), 7,47 (1H, t, J= 7.5 Hz), 7,58 (1H, d, J=7.5 Hz), to 7.64 (1H, s), 7,71 (2H, d, J=8.5 Hz), 8,17 (2H, d, J=8,5 Hz).

(d) Ethyl 2-butyl-3-[4-[2-(3'-methoxyethoxymethyl-4-carbylamine)ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (358 mg), which is the product of reference example 6, 3'-methoxyethoxymethyl-4-carboxylic acid (333 mg), which is the product of reference example 15 (C), and carbonyldiimidazole (238 mg) and the reaction mixture was treated to give the desired compound (573 mg) as a brown syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,22-of 1.39 (4H, m), 1,40-is 1.51 (1H, m), 1,54-to 1.67 (1H, m), 2,53-2,63 (1H, m), 2,68 (1H, DD, J= 6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,44 (3H, s), 3,88 (2H, q, J= 5.0 Hz), of 4.05 (2H, q, J=7.0 Hz), 4,14 (2H, t, J=5.0 Hz), of 4.67 (2H, s), 4,74 (2H, s), 6,69 (1H, user.t), at 6.84 (2H, d,ptx2">

(e) Sodium 2-butyl-3-[4-[2-(3'-methoxyethoxymethyl-4-carbylamine)ethoxy]phenyl] propionate

The reaction was conducted in the same manner as described in example 2, using ethyl 2-butyl-3-[4-[2-(3'-methoxyethoxymethyl-4-carbylamine)ethoxy] phenyl] - propionate (573 mg), which is the product of reference example 15(d), and aqueous sodium hydroxide (1 N., 2.00 ml) and the reaction mixture was treated to give the desired compound (472 mg) as a white powder. So pl. 216-218oC.1H-NMR (270 MHz, deuterated methanol): ppm of 0.85 (3H, t, J=7.0 Hz), 1,17-of 1.40 (4H, m), 1,46 is 1.60 (2H, m), 2,36 is 2.46 (1H, m), 2,52 (1H, DD, J=7,0, and 13.5 Hz), of 2.86 (1H, DD, J=7,5, and 13.5 Hz), to 3.41 (3H, s), of 3.77 (2H, t, J=5.5 Hz), to 4.14 (2H, t, J=5.5 Hz), of 4.66 (2H, s), to 4.73 (2H, s), at 6.84 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=8.5 Hz), 7,38 (1H, d, J=7.5 Hz), was 7.45 (1H, t, J=7.5 Hz), 7,60 (1H, d, J=7.5 Hz), 7,66 (1H, s), 7,72 (2H, d, J=8.5 Hz), to $ 7.91 (2H, d, J=8,5 Hz).

(Reference example 16)

2'-Hydroxybiphenyl-4-carboxylic acid

The reaction was conducted in the same manner as described in example 2 using methyl 2'-hydroxybiphenyl-4-carboxylate (498 mg) and aqueous sodium hydroxide (1 N. , 4,81 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (434 mg) as colorless crystals. So pl. 176-178oC.1H-NMR (270 MHz, CDCl3/deuterated methanol = methoxyethoxy-3', 5'-dimethylbiphenyl-4-carbylamine)ethoxy]phenyl]propionic acid

(a) Methyl 4'-methoxyethoxy-3',5'-dimethylbiphenyl-4-carboxylate

To a suspension of magnesium (327 mg) in tetrahydrofuran (45 ml) was added dropwise a solution of 5-bromo-2 - methoxyethoxy-1,3-xylene (at 3.35 g) in tetrahydrofuran (7.0 ml) for 15 minutes at 65oC. the Mixture was stirred at 80oC for 1 hour to obtain a Grignard reagent. This solution was added dropwise to a solution of triethylborane (2.00 ml) in bezvodnom diethyl ether (20 ml) for 30 minutes at -50oC. the Mixture was stirred at room temperature for 2 hours. At the end of this time the reaction was suppressed by hydrogensulfate potassium and distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. The residue was led from diisopropyl ether to obtain 4'-methoxyethoxy-3',5'-dimetilfenil borate (1.04 g) as colorless crystals. The reaction was conducted in the same manner as described in reference example 14(a), using 4'-methoxyethoxy-3',5'-dimetilfenil Borat, obtained above, (1.04 g), methyl 4-bromobenzoyl Ki is about connections (1,36 g) as colorless crystals. So pl. 100-101oC.1H-NMR (270 MHz, CDCl3): ppm is 2.37 (6H, s) to 3.64 (3H, s), 3,93 (3H, s), free 5.01 (2H, s), 7,28 (2H, s), to 7.61 (2H, d, J= 8.5 Hz), 8,07 (2H, d, J=8,5 Hz).

(b) 4'-Methoxyethoxy-3',5'-dimethylbiphenyl-4-carboxylic acid

The reaction was conducted in the same manner as described in example 2 using methyl 4'-methoxyethoxy-3',5'-dimethylbiphenyl-4-carboxylate (1.24 g), and aqueous sodium hydroxide (1 N., 8,20 ml) and the reaction mixture was treated to give the desired compound (0,99 g) as colorless crystals. So pl. 153-154oC.1H-NMR (270 MHz, CDCl3): ppm of 2.38 (6H, s) to 3.64 (3H, s), 5,02 (2H, s), 7,30 (2H, s), the 7.65 (2H, d, J= 8.5 Hz), 8,14 (2H, d, J=8,5 Hz).

(C) Ethyl 2-butyl-3-[4-[2-(4'-methoxyethoxy-3', 5'-dimethylbiphenyl-4-carbylamine)ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (880 mg), which is the product of reference example 6, 4'-methoxyethoxy-3',5'-dimethylbiphenyl-4-carboxylic acid (859 mg), which is the product of reference example 17(b), and carbonyldiimidazole (577 mg) and the reaction mixture was treated to give the desired compound (1.18 g) as colorless crystals. So pl. 70-71oC.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J= 7.0 G is H, kV, J=7,0 Hz), 4,14 (2H, t, J= 5.0 Hz), 5,00 (2H, s), 6,62 (1H, user.t), 6,83 (2H, d, J-8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,60 (2H, d, J=8.5 Hz), 7,82 (2H, d, J=8,5 Hz).

(d) 2-Butyl-3-[4-[2-(4'-methoxyethoxy-3', 5 - dimethylbiphenyl-4-carbylamine)-ethoxy]phenyl] propionic acid

The reaction was conducted in the same manner as described in example 2, using ethyl 2-butyl-3-[4-[2-(4'-methoxyethoxy-3', 5'-dimethylbiphenyl-4-carbylamine)ethoxy] phenyl]propionate (1.01 g), which is the product of reference example 17(C), and an aqueous solution of sodium hydroxide (1 n of 3.60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (1,00 g) in the form of foam powder.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J= 7.0 Hz), 1,21-of 1.39 (4H, m), 1,40-1,70 (2H, m) to 2.35 (6H, s), 2,56-to 2.65 (1H, m), 2,71 (1H, DD, J=6,5, and 13.5 Hz), 2,89 (1H, DD, J=8,5, and 13.5 Hz), 3,63 (3H, s), 3,86 (2H, q, J=5.0 Hz), of 4.12 (2H, t, J=5.0 Hz), 5,00 (2H, s), of 6.73 (1H, user. t), PC 6.82 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,58 (2H, d, J=8.5 Hz), 7,81 (2H, d, J=8,5 Hz).

(Reference example 18)

6-Isopropoxyaniline acid

(and) Isopropyl 6-isopropoxyaniline

To a solution of 6-chloronicotinamide (1.56 g) in isopropanol (20 ml) was added cesium carbonate (7,94 g). The mixture was boiled under reflux for 3 hours. The reaction mixture was concentrated under reduced pressure. The remainder of the distribution is, and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 4/1, to give the desired compound (143 mg) as a colourless liquid.1H-NMR (270 MHz, CDCl3): of 1.36 ppm (12H, d, J=6.5 Hz), 5,24 (1H, septet, J=6.5 Hz), of 5.39 (1H, septet, J=6.5 Hz), of 6.68 (1H, d, J=8,5 Hz) to 8.12 (1H, DD, J=2.5 and 8.5 Hz), 8,81 (1H, d, J=2.5 Hz).

(b) 6-Isopropoxyaniline acid

The reaction was conducted in the same manner as described in example 2, using isopropyl 6-isopropoxyaniline (130 mg), which is the product of reference example 18(a), and an aqueous solution of sodium hydroxide (1 N., of 0.87 ml) and the reaction mixture was treated with obtaining the connection specified in the header (106 mg) as crystals.1H-NMR (270 MHz, CDCl3): ppm to 1.38 (6H, d, J= 6.0 Hz), 5,42 (1H, septet, J=6.0 Hz), was 6.73 (1H, d, J=8.5 Hz), 8,18 (1H, DD, J=2.5 and 8.5 Hz), of 8.92 (1H, d, J=2.5 Hz).

(Reference example 19)

Ethyl 2-butyl-3-[4-[2-(3-phenylpropylamine)ethoxy]phenyl]-propionate

To a solution of ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (500 mg), which is the product of reference example 6, in ethanol (10 ml) was added 3-phenylpropionaldehyde (0,23 ml), sodium cyanoborohydride (117 mg) and acetic acid (one drop). The mixture was stirred at room temperature Chechenia and water and the layers were separated. An ethyl acetate solution was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/methanol = 19/1, to give the desired compound (460 mg) as a pale yellow oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7,0 Hz) and 1.15 (3H, t, J=7.0 Hz), 1,23-of 1.32 (4H, m), 1,40-of 1.95 (4H, 681 m), 2,52-of 3.00 (9H, m), 3,99-4.09 to (4H, m), to 6.80 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,15-7,31 (5H, m).

(Reference example 20)

Ethyl 2-butyl-3-[4-[2-(butylamino)ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in reference example 19, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-butylphosphonate (500 mg), which is the product of reference example 6, butylaldehyde (0.15 ml), sodium cyanoborohydride (107 mg) and acetic acid (one drop) and the reaction mixture was treated with obtaining the connection specified in the header (390 mg) as a yellow oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), were 0.94 (3H, t, J=7.5 Hz), of 1.17 (3H, t, J=7.0 Hz), 1,22-1,73 (10H, m), 2,52-of 3.00 (5H, m), 3,20 of 3.28 (2H, m), 3,99-4,20 (4H, m), at 6.84 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8,5 Hz).

(Reference example 21)

Ethyl 3-[4-(3-aminopropoxy)phenyl]-2-butylphosphonate

(a) 2-butyl-3-[4-[3-(tetrahydropyran-2-yloxy)plesae ethyl 2-(4-hydroxybenzyl)caproate (3,02 g), 2-(3-bromopropane)-tetrahydropyran (3,23 g) and potassium carbonate (5,00 g) and the reaction mixture was treated to give the desired compound (4.42 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7,0 Hz) and 1.15 (3H, t, J= 7.0 Hz), 1,22-1,35, (4H, m), 1,47-of 1.88 (8H, m) to 2.06 (2H, quintuplet, J= 6.0 Hz), 2,52-2,63 (1H, m) to 2.67 (1H, DD, J=6,5, and 13.5 Hz), 2,85 (1H, DD, J= 8,5, and 13.5 Hz), of 3.46-3,61 (2H, m), 3,80-of 3.97 (2H, m), 4,01-4,10 (4H, m), 4,60 (1H, t, J=3.5 Hz), to 6.80 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8,5 Hz).

(b) Ethyl 2-butyl-3-[4-(3-hydroxypropoxy)phenyl]propionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-butyl-3-[4-[3- (tetrahydropyran-2-yloxy)propoxy]phenyl] propionate (4.42 g) and monohydrate p-toluensulfonate acid (to 2.57 g) and the reaction mixture was treated to give the desired compound (3,02 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,22-of 1.35 (4H, m), 1,40-1,70 (2H, m), 1.77 in (1H, t, J=5.5 Hz), 2,03 (2H, quintuplet, J=5.5 Hz), 2,53-to 2.65 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 3,86 (2H, q, J=5.5 Hz), was 4.02-4,17 (4H, m), for 6.81 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8,5 Hz).

(C) Ethyl 2-butyl-3-[4-(3-methanesulfonylaminoethyl)-phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 2-butyl-3-[4-(3-hydroxyprop is whether to give the desired compound (3,49 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J= 7.0 Hz), 1,22-of 1.34 (4H, m), 1,40-1,70 (2H, m), of 2.21 (2H, quintuplet, J= 6.0 Hz), 2,52-of 2.64 (1H, m), 2,68 (1H, DD, J=6,5, and 13.5 Hz), of 2.86 (1H, DD, J=8,5, and 13.5 Hz), 2,98 (3H, s)that was 4.02-4,11 (4H, m), of 4.44 (2H, t, J= 6.0 Hz), to 6.80 (2H, d, J=8.5 Hz), 7,07 (2H, d, J-8.5 Hz).

(d) Ethyl 3-[4-(3-azithromax)phenyl]-2-butylphosphonate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 2-butyl-3-[4-(3-methanesulfonamido)phenyl]propionate (2,98 g) and sodium azide (1.50 g) and the reaction mixture was treated to give the desired compound (2,45 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), of 1.20 to 1.34 (4H, m), 1,40-1,70 (2H, m), 2,03 (2H, quintuplet, J=6.5 Hz), of 2.51 2.63 in (1H, m) to 2.67 (1H, DD, J=6,5, and 13.5 Hz), 2,85 (1H, DD, J=8,5, and 13.5 Hz), 3,51 (2H, t, J=6.5 Hz), was 4.02 (2H, t, J=6.5 Hz), of 4.05 (2H, q, J=7.0 Hz), to 6.80 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8,5 Hz).

(e) Ethyl 3-[4-(3-aminopropoxy)phenyl]-2-butylphosphonate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(3-azithromax) phenyl]- 2-butylphosphonate (2,45 g) and palladium on carbon (5%, 250 mg) and the reaction mixture was treated to give the desired compound (1,62 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J=6.5 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,22-of 1.34 (4H, m),BR> Ethyl 2-butyl-3-[4-(3-methylaminopropane)phenyl]propionate

To a solution of ethyl 2-butyl-3-[4-(3-methanesulfonyl-oxopropoxy)phenyl]propionate (500 mg), which is the product of reference example 21(C), in toluene (10 ml) was added a solution of methylamine in methanol (40%, 5.0 ml). The mixture was stirred at 90oC for 2 days. The reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate solution was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent dichloromethane/methanol = 5/1, receiving of the connection specified in the header (389 mg) as a pale yellow oil.1H-NMR (270 MHz, CDCl3): ppm of 0.87 (3H, t, J= 6.5 Hz), 1,15 (1,5 H, t, J=7.0 Hz), 1,16 (1,5 H, t, J=7.0 Hz), 1,22-of 1.35 (4H, m), 1,42 is 1.70 (2H, m), 1,92-2,02 (1H, m), 2,17-of 2.27 (1H, m), 2,52-3,09 (8H, m), 3,92-4,10 (4H, m), of 6.73-for 6.81 (2H, m), 7,00-to 7.09 (2H, m).

(Reference example 23)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-propylphosphonate

(a) Diethyl 2-(4-benzyloxybenzyl)-2-propylmalonate

The reaction was conducted in the same manner as described in reference example 2(a), using diethyl 2-propylmalonate (of 5.00 g), 4-benzyloxy the desired compound (9.80 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 0.92 (3H, t, J=7,0 Hz) of 1.23 (6H, t, J=7.0 Hz), 1,23-to 1.38 (2H, m), 1,71 and 1.80 (2H, m), 3,18 (2H, s), 4,08-is 4.21 (4H, m), 5,02 (2H, s) 6,86 (2H, d, J=8.5 Hz), of 6.99 (2H, d, J=8.5 Hz), 7,30-of 7.48 (5H, m).

(b) 3-(4-benzyloxyphenyl)-2-propylphosphonate acid

The reaction was conducted in the same manner as described in reference example 2(b), using diethyl 2-(4-benzyloxybenzyl)-2 - propylmalonate (9,85 g), which is the product of reference example 23(a), and potassium hydroxide (5,25 g) and the reaction mixture was treated to give the desired compound (3,96 g) in the form of brownish crystals. So pl. 83-85oC.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, t, J=7.0 Hz), 1,24 is 1.70 (4H, m), 2,59-of 3.00 (3H, m), of 5.03 (2H, s), make 6.90 (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,21-of 7.48 (5H, m).

[(C) Ethyl 3-(4-benzyloxyphenyl)-2-propylphosphonate ()

To a solution of 3-(4-benzyloxyphenyl)-2-propylamino acid (3,90 g), which is the product of reference example 23(b), in N,N-dimethylformamide (40 ml) was added 1,8-diazabicyclo[5,4,0]undec-7-ene (2,34 ml) and ethyliodide (1,57 ml). The reaction mixture was stirred at 60oC for 4 hours. The reaction mixture was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue cleaned obtaining the desired compound (4,00 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7,0 Hz) to 1.14 (3H, t, J=7.0 Hz), 1,20-1,70 (4H, m), 2,56-2,62 (1H, m), 2,68 (1H, DD, J=6,0, 13,0 Hz), of 2.86 (1H, DD, J=8.0 a, 13,0 Hz), of 4.05 (2H, q, J=7.0 Hz), to 5.03 (2H, s), to 6.88 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,28-7,47 (5H, m).

(d) Ethyl 3-(4-hydroxyphenyl)-2-propylphosphonate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-propylphosphonate (4,00 g) and palladium on carbon (5%, 0.40 g) and the reaction mixture was treated to give the desired compound (3,10 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 0.89 (3H, t, J=7,0 Hz) and 1.15 (3H, t, J=7.0 Hz), 1,21 is 1.70 (4H, m), 2,53-of 2.72 (2H, m), 2,84 (1H, DD, J=8,5, 13,0 Hz), of 4.05 (2H, q, J=7.0 Hz), 4.75 V-4,82 (1H, m), 6,72 (2H, d, J=8.5 Hz), 7,02 (2H, d, J=8,5 Hz).

(e) Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-propylphosphonate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(4-hydroxyphenyl)- 2-propylphosphonate (1.65 g), which is the product of reference example 23(d), tert-butyl 2-gidroxiatilkrahmal (5,63 g), triphenylphosphine (9,16 g) and diethylazodicarboxylate (6,14 ml) and the reaction mixture was treated to give the desired compound (2,22 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 0.88 (3H, t, J=7.0 Hz), of 1.16 (3H, t, J=7.0 Hz), 1,20-1,70 (4H, m) of 1.45 (9H, s), 2,55-a 2.71 (2H, t example 24)

3-[4-[2-(4'-Methoxyethoxy-3',5' -dimethylbiphenyl-4-carbylamine)ethoxy] phenyl]-2 - phenoxypropionic acid

(a) Ethyl 3-[4-[2-(4'-methoxyethoxy-3', 5'-dimethylbiphenyl-4-carbylamine) ethoxy]phenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in example 5, using ethyl 3-[4-(2-aminoethoxy)phenyl]-2-phenoxypropionate (2,07 g), which is the product of reference example 4, 4'-methoxyethoxy-3',5'-dimethylbiphenyl-4-carboxylic acid (1.50 g), which is the product of reference example 17(b), and carbonyldiimidazole (1.10 g) and the reaction mixture was treated to give the desired compound (720 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), a 2.36 (6H, s) 3,18 (1H, d, J=5.5 Hz), 3,19 (1H, d, J=7.5 Hz), to 3.64 (3H, s), 3,88 (2H, q, J=5.0 Hz), is 4.15 (2H, t, J=5.0 Hz), 4,18 (2H, q, J=7.0 Hz), 4,74 (1H, DD, J=5,5, 7.5 Hz), 5,00 (2H, s), is 6.61 (1H, user.t), 6,83 (2H, d, J=8.5 Hz), 6.87 in (2H, d, J=8.5 Hz), 6,94 (1H, t, J=7.5 Hz), 7,20-7,30 (6H, m), 7,60 (2H, d, J=8.5 Hz), 7,82 (2H, d, J=8,5 Hz).

(b) 3-[4-[2-(4'-Methoxyethoxy-3', 5' -dimethylbiphenyl-4-carbylamine)ethoxy]-phenyl]-2 - phenoxypropionic acid

The reaction was conducted in the same manner as described in example 2, using ethyl 3-[4-[2-(4'-methoxyethoxy-3', 5'-dimethylbiphenyl-4-carbylamine)-ethoxy]phenyl]-2-phenoxy-propionate (720 mg), colibacilli getting connection specified in the header, (520 mg) as a white powder. So pl. 142-143oC.1H-NMR (270 MHz, deuterated methanol): ppm of 2.35 (6H, s), 3,14 (1H, d, J=7.5 Hz), and 3.16 (1H, d, J= 4.5 Hz), of 3.60 (3H, s), of 3.77 (2H, q, J=5,5 Hz) to 4.16 (2H, t, J=5.5 Hz), a 4.86 (1H, DD, J=4,5, 7.5 Hz), 5,00 (2H, s), 6,83 (2H, d, J=7.5 Hz), 6,86-6,93 (1H, m), of 6.90 (2H, d, J=8.5 Hz), 7,19 (2H, d, J=7.5 Hz), 7,24 (2H, d, J= 8.5 Hz), 7,33 (2H, s), the 7.65 (2H, J=8.5 Hz), 7,86 (2H, d, J=8.5 Hz), 8,68 (1H, user.t).

(Reference example 25)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)propionate

To a solution of ethyl 3-(4-hydroxyphenyl)-2-(4 - isopropylphenoxy)propionate (18.2 g), which is the product of reference example 5(d), in a mixture of N,N-dimethylformamide (200 ml) and toluene (100 ml) was added potassium carbonate (23,5 g) at room temperature. To this suspension was added dropwise a solution of tert-butyl 2-methanesulfonylaminoethyl (12.2 g) in toluene (40 ml) at 70oC and the mixture was stirred at the same temperature for 2 hours. Later in the reaction mixture was added a solution of tert-butyl 2-methanesulfonylaminoethyl (12.2 g) in a mixture of N,N - dimethylformamide (10 ml) and toluene (40 ml) and the mixture was stirred at 70oC during the night. The reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was washed with a saturated aqueous solution is attended by chromatography on a column of silica gel, using as eluent toluene/ethyl acetate = 20/1 - hexane/ethyl acetate = 3/1, to give the desired compound (18.7 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (6H, d, J=7,0 Hz) of 1.45 (9H, s), 2,82 (1H, septet, J-7.0 Hz), and 3.16 (1H, d, J=5.0 Hz), 3,18 (1H, d, J=7.5 Hz), 3,52 (2H, q, J=5.0 Hz), 3,99 (2H, t, J=5.0 Hz), 4,18 (2H, q, J= 7.0 Hz), 4,69 (1H, DD, J=5.0 and 7.5 Hz), equal to 4.97 (1H, user.t) 6,76 (2H, d, J= 8.5 Hz), for 6.81 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,21 (2H, d, J=8,5 Hz).

(Reference example 26)

6-(4-Methoxyphenyl) nicotinic acid

The reaction was conducted in the same manner as described in example 2, using methyl 6-(4-methoxyphenyl)nicotinate (3,95 g) and an aqueous solution of sodium hydroxide (1 N., 32,5 ml) and the reaction mixture was treated with obtaining the connection specified in the header (2,63 g) as colorless crystals. So pl. 252 - 253oC.1H-NMR (270 MHz, CDCl3): ppm of 3.84 (3H, s), was 7.08 (2H, d, J= 9.0 Hz), of 8.04 (1H, d, J-8.5 Hz), 8,14 (2H, d, J=9.0 Hz), of 8.27 (1H, DD, J= 2.5 and 8.5 Hz), which is 9.09 (1H, d, J=2.5 Hz).

(Reference example 27)

6-(4-Forfinal) nicotinic acid

The reaction was conducted in the same manner as described in example 2, using methyl 6-(4-forfinal)nicotinate (390 mg) and aqueous sodium hydroxide solution (1 N. , 5,00 ml) and the reaction mixture was treated with obtaining the connection specified in the header (345 m,29 (2H, m), 8,32 (1H, DD, J=2,0, 8.5 Hz), 9,13 (1H, d, J=2.0 Hz).

(Reference example 28)

6-(2,2,3,3-tetrafluoropropoxy)nicotinic acid

The reaction was conducted in the same manner as described in reference example 1(C), using 2,2,3,3-tetrafluoropropanol (5,23 ml), sodium hydride (55% suspension in oil, 1,91 g) and methyl 6-chloronicotinate (5,00 g), and treated with obtaining crude methyl 6-(2,2,3,3-tetrafluoropropoxy) nicotinate (5,42 g) as a colourless oil. The reaction was conducted in the same manner as described in example 2, using the crude product described above (2.70 g), and aqueous sodium hydroxide solution (2n., 15 ml) and the reaction mixture was treated with obtaining raw connection specified in the header (1.60 g). This product used in example 102 and 150 without further purification.

(Reference example 29)

2-Trimethylsilylmethyl (S)-2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridine-2-yl-benzoylamine)ethoxy]phenyl]propionate

(a) (S)-4-benzyl-3-[(4-isopropylphenoxy)acetyl] oxazolidin-2-he

To a solution of 4-isopropylthioxanthone acid (15.0 g) in dichloromethane (75 ml) was added oxalicacid (16,8 ml) and N,N-dimethylformamide (three drops) at room temperature. The reaction mixture was stirred for 1.5 hours. The reaction mixture koncentrere pressure.

To a solution of (S)-4-benzyloxypyridine-2-she (12.4 g) in tetrahydrofuran (150 ml) was added dropwise a solution of n-butyl lithium in hexane (1,61 N., 48,0 ml) at -78oC, and the mixture was stirred at the same temperature for 30 minutes. To this solution was added a solution of 4-isopropylphenoxy-chloride, which was obtained above in tetrahydrofuran (100 ml) at -78oC. the Mixture was stirred at 0oC for 1 hour. The reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was washed with an aqueous solution of hydrochloric acid (1 ad), saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium chloride. An ethyl acetate solution was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was led from a mixture of hexane/ethyl acetate = 6/1 to give the desired compound (20,9 g) as colorless crystals. So pl. of 104.5-105oC.1H-NMR (270 MHz, CDCl3): ppm of 1.23 (6H, d, J=7,0 Hz), 2,79 of 2.92 (2H, m) to 3.36 (1H, DD, J= 3,0 and 13.5 Hz), 4,24-4,37 (2H, m), 4,68-4,78 (1H, m), with 5.22 (2H, s) 6,91 (2H, d, J=8.5 Hz), 7,13-7,38 (7H, m).

(b) (S)-4-benzyl-3-[(2S, 3R)-3-(4-benzyloxyphenyl)- 3-hydroxy-2-(4-isopropylphenoxy)propionyl]oxazolidin-2-he

To a solution of (S)-4-benzyl-3-[(4-isopropyl-phenoxy)acetyl]oxazolidin-2-it (20,0 g) 0oC. the Mixture was stirred at the same temperature for 1 hour. In the reaction mixture was added dropwise a solution of 4-benzyloxybenzaldehyde (13,2 g) in dichloromethane (20 ml) at -78oC and then stirred at the same temperature for 40 minutes. The reaction mixture was further stirred at 0oC for 1 hour. At the end of this time the reaction mixture was added a mixture of saturated aqueous sodium chloride solution/methanol = 1/1 (50 ml) and aqueous hydrogen peroxide solution (31%)/methanol = 2/1 (150 ml) and was stirred for 1 hour. The mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was washed with an aqueous solution of hydrochloric acid (1 ad), saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 3/1-1/1, to give the desired compound (25,7 g) as a foamy mass.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (6H, d, J=7,0 Hz), 2,73 (1H, DD, J=a 9.5 and 13.5 Hz), 2,85 (1H, septet, J=7.0 Hz), of 3.07 (1H, DD, J=3,0 and 13.5 Hz), to 3.58 (1H, t, J=8,5 4 (2H, d, J=8.5 Hz), 7.23 percent-7,44 (10H, m).

(s) (S)-4-benzyl-3-[(2S, 3R)-3-hydroxy-3-(4 - hydroxyphenyl)-2-(4-isopropylphenoxy)propionyl]oxazolidin-2-he

The reaction was conducted in the same manner as described in reference example 1(d), using (3)-4-benzyl-3-[(2S,3R)-3-(4-benzyloxyphenyl)-3-hydroxy-2-(4-isopropylphenoxy) -propionyl] oxazolidin-2-he (25,0 g), which is the product of reference example 29(b), and palladium on carbon (5%, 2.50 g) and the reaction mixture was treated to give the desired compound (19.1 g) in the form of a frothy mass.1H-NMR (270 MHz, CDCl3): to 1.21 ppm (6H, d, J=7,0 Hz), was 2.76 (1H, DD, J=9,0, 13.5 Hz), 2,85 (1H, septet, J=7.0 Hz), of 3.07 (1H, DD, J= 3,0 and 13.5 Hz), 3,17 (1H, d, J=4.5 Hz), to 3.73 (1H, t, J=8.5 Hz), Android 4.04 (1H, d, J=8.5 Hz), 4,25 is 4.35 (1H, m), 5,07 (1H, t, J=5.0 Hz), 5,52 (1H, s), 6,18 (1H, d, J= 5.5 Hz), 6,78 (2H, d, J=8.5 Hz), 6,92 (2H, d, J=8.5 Hz), 7,02 for 7.12 (2H, m), 7,14 (2H, d, J=8.5 Hz), 7,22-7,29 (3H, m), 7,32 (2H, d, J=8,5 Hz).

(d) (S)-4-benzyl-3-[(S)-3-(4-hydroxyphenyl)-2-(4 - isopropyl-phenoxy)propionyl]-oxazolidin-2-he

To a solution of (S)-4-benzyl-3-[(2S, 3R)-3-hydroxy-3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionyl] oxazolidin-2-it (18.0 g), which is the product of reference example 29(C), triperoxonane acid (150 ml), was added triethylsilane (30,2 ml) at room temperature. The mixture was stirred for 18 hours. The reaction mixture concentration is atny layer was washed with a saturated aqueous solution of sodium bicarbonate, aqueous solution of hydrochloric acid (1 BC) and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 3/1, to give the desired compound (10.7 g) as colorless crystals. So pl. 142 - 143oC.1H-NMR (400 MHz, CDCl3): ppm to 1.19 (6H, d, J=7,0 Hz), 2,75-is 2.88 (2H, m), 3,10-is 3.21 (3H, m), a 4.03 (1H, t, J=8.0 Hz), 4,17 (1H, d, J=9.0 Hz), 4,48-4,55 (1H, m), 4,89 (1H, s), between 6.08 (1H, DD, J=5,5, 8.0 Hz), 6,74 (2H, d, J=8.5 Hz), 6,83 (2H, d, J=8.5 Hz), 7,05-7,16 (4H, m), 7,21 and 7.36 (5H, m).

(e) 2-Trimethylsilylmethyl (S)-3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionate

To a suspension of (S)-4-benzyl-3-[(3)-3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionyl] oxazolidin-2-she (10.6 g), which is the product of reference example 29(d), in a mixture of methanol (140 ml) and tetrahydrofuran (15 ml) was added dropwise a mixture of an aqueous solution of lithium hydroxide (1 N., 57,0 ml) and aqueous hydrogen peroxide solution (31%, 6,34 ml). Then the mixture was stirred at room temperature for 6 hours, the reaction mixture was added a solution of dithionite sodium (10.1 g) in water (50 ml) and the mixture was stirred for 1 hour. The reaction mixture was concentrated at pangenetor washed with dichloromethane and distributed between aqueous hydrochloric acid and ethyl acetate. An ethyl acetate layer was separated, dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. The residue was led from hexane to obtain (S)-3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionic acid (6,00 g) as a white powder. To a suspension of this carboxylic acid (4,43 g) in dichloromethane (100 ml) was added oxalicacid (5.50 ml) and N,N-dimethylformamide (5 drops) at room temperature. The mixture was stirred for 1 hour. At the end of this time the reaction mixture was concentrated under reduced pressure. The remainder of the azeotropic drove, using toluene to remove excess reagent. To a solution of the residue in dichloromethane (50 ml) was added 2-trimethyl-semilateral (9,06 ml). This mixture was stirred at room temperature for 15 hours. To the mixture was added triethylamine (4,40 ml) and 4-N,N-dimethylaminopyridine (155 mg). This mixture was stirred at room temperature for 2 hours. The reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was washed saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified with what giving the desired compound (5.30 g) as a pale yellow oil.1H-NMR (270 MHz, CDCl3): ppm 0,00 (9H, s) to 0.92 (2H, t, J=8,5 Hz) of 1.18 (6H, d, J=7,0 Hz), of 2.81 (1H, septet, J=7.0 Hz), 3,10-3,17 (2H, m), 4,19 (2H, t, J=8.5 Hz), of 4.66 (1H, DD, J= 6,0, 7,0 Hz), 6.73 x (2H, d, J=8.5 Hz), 6,74 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), to 7.15 (2H, d, J=8,5 Hz).

(f) 2-Trimethylsilylmethyl(3)-3-[4-(2-tert-butoxycarbonyl-aminoethoxy)phenyl]-2-(4-isopropylphenoxy) propionate

The reaction was conducted in the same manner as described in reference example 25 using 2-trimethylsilylmethyl (S)-3-(4 - hydroxyphenyl)-2-(4-isopropyl-phenoxy)propionate (4,80 g), which is the product of reference example 29(e), tert-butyl 2-methanesulfonylaminoethyl (7,17 g) and potassium carbonate (of 8.28 g) and the reaction mixture was treated to give the desired compound (5,94 g) as a colourless oil.

[]25D-6,0o(C = 0.9, chloroform).1H-NMR (400 MHz, CDCl3): ppm 0,00 (9H, s) of 0.91 (2H, t, J=8,5 Hz) of 1.17 (6H, d, J=7,0 Hz) of 1.45 (9H, s), of 2.81 (1H, septet, J=7.0 Hz), is 3.08-3,18 (2H, m), 3.45 points-of 3.54 (2H, m), 3,93-4,00 (2H, m), 4,10-of 4.25 (2H, m) and 4.65 (1H, DD, J=5,5, 7.5 Hz), 4,93-5,00 (1H, m), 6,74 (2H, d, J=8.5 Hz), to 6.80 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8,5 Hz).

(g) 2-Trimethylsilylmethyl (S)-2-(4-isopropylphenoxy)-3-[4- [2-(4-pyridine-2-yl-benzoylamine)ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 73, using 2-trimethylsilylmethyl (S)-Loto (382 mg), diethylthiophosphate (0,29 ml) and triethylamine (0,53 ml) and the reaction mixture was treated with obtaining the connection specified in the header (of 0.62 g) as a colourless oil.

[]25D-3,0o(C = 0,7, chloroform).1H-NMR (400 MHz, CDCl3): of 0.05 ppm (9H, s) 0,97 (2H, t, J=8.5 Hz), 1,15-of 1.23 (6H, m), 2,86 (1H, septet, J=7.0 Hz), 3,14 is 3.23 (2H, m), 3,85-of 3.95 (2H, m), 4,15-4,27 (4H, m), 4,70 (1H, DD, J= 5,5, 7.5 Hz), 6,64-6,74 (1H, m), 6,79 (2H, d, J=8.5 Hz), make 6.90 (2H, d, J= 8.5 Hz), 7,12 (2H, d, J=8.5 Hz), 7.24 to 7,34 (3H, m), 7,76-to 7.84 (2H, m), to 7.93 (2H, d, J=8.5 Hz), 8,11 (2H, d, J=8.5 Hz), 8,76 (1H, d, J=5.0 Hz).

(Reference example 30)

2-Trimethylsilylmethyl (R)-2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridine-2-yl-benzoylamine) ethoxy]phenyl]propionate

(a) (R)-4-benzyl-3-[(4-isopropylphenoxy)acetyl]oxazolidin-2-he

The reaction was conducted in the same manner as described in reference example 29(a), using 4-isopropylphenoxy acid (14.1 g), oxacillin (15,8 ml), (R)-4-benzyloxypyridine-2-he (11,7 g) and a solution of n-utility in hexane (1,61 N. , 45,0 ml) and the reaction mixture was treated to give the desired compound (18.6 g) as colorless crystals. So pl. 104,5-105,5oC.1H-NMR (400 MHz, CDCl3): ppm of 1.23 (6H, d, J=7,0 Hz), 2,80-only 2.91 (2H, m) to 3.36 (1H, DD, J=3,0 and 13.5 Hz), 4,28 (1H, DD, J=3,0, 9,0 Hz) to 4.33 (1H, DD, J= 8,0, 9.0 Hz), 4,68-4,78 (1H, m), with 5.22 (2H, s) 6,91 (2H, d, J= 8.5 Hz), 7,14-7,38 (7H, m).

/BR>The reaction was conducted in the same manner as described in reference example 29(b), using (R)-4-benzyl-3-[(4-isopropylphenoxy)acetyl]oxazolidin-2-he (10.0 g), which is the product of reference example 30(a), a solution of dibutylphthalate in dichloromethane (1M, 34,0 ml), triethylamine (5,11 ml) and 4-benzyloxybenzaldehyde (6.60 g) and the reaction mixture was treated to give the desired compound (12.1 g) as a foamy mass.1H-NMR (270 MHz, CDCl3): to 1.21 ppm (6H, d, J=7,0 Hz), 2,73 (1H, DD, J=9,0, 13.5 Hz), 2,85 (1H, septet, J=7.0 Hz), 3,02-of 3.12 (1H, m), 3,53-3,63 (1H, m), 3,93-4,01 (1H, m), 4,21-4,32 (1H, m), 5,02-5,12 (3H, m), 6,18 (1H, d, J=6.0 Hz), 6,88-7,46 (18H, m).

(C) (R)-4-benzyl-3-[(2R, 3S)-3-hydroxy-3-(4 - hydroxyphenyl)-2-(4-isopropylphenoxy)propionyl]oxazolidin-2-he

The reaction was conducted in the same manner as described in reference example 1(d), using (R)-4-benzyl-3-[(2R,3S)-3-(4-benzyloxyphenyl)-3-hydroxy-2-(4-isopropylphenoxy)- propionyl] oxazolidin-2-he (9.00 g), which is a product

reference example 30(b) and palladium on carbon (5%, of 1.80 g) and the reaction mixture was treated to give the desired compounds (of 7.48 g) in the form of a frothy mass.1H-NMR (270 MHz, CDCl3): to 1.21 ppm (6H, d, J=7,0 Hz) of 2.75 (1H, DD, J= 9,0, 13.5 Hz), 2,85 (1H, septet, J=7.0 Hz), 3,05-3,14 (2H, m), 3,70-with 3.79 (1H, m), to 4.01-4.09 to (1H, m), 4.26 deaths is 4.35 (1H, m), 5,04-5,12 (1H, m), 5,34 (l)-2-(4 - isopropyl-phenoxy)propionyl]-oxazolidin-2-he

The reaction was conducted in the same manner as described in reference example 29(d), using (R)-4-benzyl-3-[(2R,3S)-3-hydroxy-3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)-propionyl] oxazolidin-2-he (7,00 g), which is the product of reference example 30(C), and triethylsilane (18.8 ml) and the reaction mixture was treated to give the desired compound (4,89 g) as colorless crystals. So pl. 147-148oC.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (6H, d, J=7.0 Hz), 2.71 to is 2.88 (2H, m), 3,09-up 3.22 (3H, m), 3,97-4,07 (1H, m), is 4.15 (1H, DD, J= 2.5 and 7.0 Hz), 4,47-of 4.57 (1H, m), 4,88 (1H, s), between 6.08 (1H, d, J= 5,5, 8.0 Hz), 6.75 in (2H, d, J=8.5 Hz), 6,83 (2H, d, J=8.5 Hz), 7,05-7,30 (9H, m).

(e) 2-Trimethylsilylmethyl (R)-3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)propionate

The reaction was conducted in the same manner as described in reference example 29(e), using (R)-4-benzyl-3-[(R)-3-(4-hydroxyphenyl)-2-(4-isopropyl-phenoxy)propionyl] oxazolidin-2-he (of 3.78 g), which is the product of reference example 30(d), an aqueous solution of lithium hydroxide (1 N., of 20.6 ml) and aqueous hydrogen peroxide solution (31%, and 2.26 ml), and the reaction mixture was treated with obtaining (R)-3-(4-hydroxyphenyl)-2-(4 - isopropylphenoxy)propionic acid (2,18 g) as a white powder. This acid (1,95 g) reacted with oxalylamino (2,73 ml) and 2-trimethylsilylethynyl (4,66 ml), and reaktsionny (of 2.26 g) as a colourless oil. 1H-NMR (270 MHz, CDCl3): ppm 0,00 (9H, s) to 0.92 (2H, t, J=8,5 Hz) of 1.18 (6H, d, J= 7,0 Hz), of 2.81 (1H, septet, J=7.0 Hz), 3,07-3,18 (2H, m), 4,11-of 4.25 (2H, m), 4,70 (1H, DD, J=5,5, 7,0 Hz), of 5.75 (1H, s), 6,72 (2H, d, J= 8.5 Hz), to 6.75 (2H, d, J=8.5 Hz), 7,07 (2H, d, J=8.5 Hz), 7,12 (2H, d, J= 8,5 Hz).

(f) 2-Trimethylsilylmethyl (R)-3-[4-(2-tert-butoxycarbonylamino) phenyl]-2-(4-isopropylphenoxy)propionate

The reaction was conducted in the same manner as described in reference example 25 using 2-trimethylsilylmethyl (R)-3-(4 - hydroxyphenyl)-2-(4-isopropyl-phenoxy) propionate (221 mg), which is the product of reference example 30(e), tert-butyl 2-methanesulfonylaminoethyl (330 mg) and potassium carbonate (381 mg) and the reaction mixture was treated to give the desired compound (264 mg) as a colourless oil.

[]25D+6,8o(C = 0.9, chloroform).1H-NMR (270 MHz, CDCl3): ppm 0,00 (9H, s) of 0.93 (2H, t, J=8,5 Hz) to 1.19 (6H, d, J=7,0 Hz) of 1.45 (9H, s), 2,82 (1H, septet, J=7.0 Hz), of 3.10-3.20 (2H, m), 3.43 points-of 3.54 (2H, m), 3,98 (2H, t, J= 5.0 Hz), 4,11-of 4.25 (2H, m), of 4.66 (1H, DD, J=5,5, 7,0 Hz), 4,91-free 5.01 (1H, m), of 6.75 (2H, d, J=8.5 Hz), for 6.81 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,22 (2H, d, J=8,5 Hz).

(g) 2-Trimethylsilylmethyl (R)-2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridine-2-yl-benzoylamine)ethoxy]phenyl]propionate

The reaction was conducted in the same manner as described in example 73, using 2-trimethylbenzoic acid (143 mg), diethylthiophosphate (0,11 ml) and triethylamine (0.10 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (307 mg) as a colourless oil.

[]25D+2,8o(C = 2,1, chloroform).1H-NMR (400 MHz, CDCl3): of 0.05 ppm (9H, s) 0,97 (2H, t, J=8.5 Hz), 1.18 to 1.22 respectively (6H, m), 2,85 (1H, septet, J=7.0 Hz), 3.15 and is 3.23 (2H, m) to 3.92 (2H, q, J=5.0 Hz), 4,15-4,30 (4H, m), 4,71 (1H, DD, J= 5,5, 7.5 Hz), 6,64 - 6,74 (1H, m), 6,79 (2H, d, J=8.5 Hz), 6.89 in (2H, d, J=8.5 Hz), 7,11 (2H, d, J=8.5 Hz), 7,26-7,34 (3H, m), 7,78-7,83 (2H, m), to 7.93 (2H, d, J=8.5 Hz), 8,10 (2H, d, J=8.5 Hz), the rate of 8.75 (1H, d, J=5.0 Hz).

(Reference example 31)

3-Triptorelin-6-Albertina acid

(a) Methyl 3-triptorelin-6-eventout

To a suspension bisbenzimidazole (119 mg) and 1,4-bidimensionality (131 mg) in toluene (10 ml) was added 4-methoxycarbonylamino acid (541 mg) and 2-chloro-5-triptorelin (718 mg) at room temperature, and the mixture was added ethanol (5 ml) and saturated aqueous sodium hydrogen carbonate solution (5 ml). This mixture was boiled under reflux for 5 hours at 100oC. the Reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and koncentrirane is in the form of a white powder, which contained some impurities.1H-NMR (270 MHz, CDCl3): ppm of 3.96 (3H, s), to $ 7.91 (1H, d, J= 8.5 Hz), of 8.04 (1H, d, J= 8,5 Hz) to 8.12 (2H, d, J= 8.5 Hz), 8,18 (2H, d, J=8.5 Hz), 8,98 (1H, s).

(b) 3-Triptorelin-6-Albertina acid

The reaction was conducted in the same manner as described in example 2, using methyl 3-triptorelin-6-eventout (791 mg) and aqueous sodium hydroxide solution (1 BC, the ceiling of 5.60 ml) and the reaction mixture was treated with obtaining the connection specified in the header (546 mg), which contains some impurities, and used in example 106 without further purification.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm with 8.05 (1H, d, J= 8.5 Hz), 8,10 (2H, d, J=8.5 Hz), 8,29 (2H, d, J= 8.5 Hz), 8,35 (1H, d, J=8.5 Hz), 9,10 (1H, s).

(Reference example 32)

3-Nitropyridine-6-Albertina acid

(a) Methyl 3-nitropyridine-6-eventout

The reaction was conducted in the same manner as described in reference example 14(a), using 4-ethoxycarbonylphenyl boric acid (3,24 g), 2-bromo-5-nitropyridine and 4.75 g) and tetrakis(triphenylphosphine) palladium (1.04 g) and processed to give the desired compound (3,67 g) as colorless crystals. So pl. 197-199oC.1H-NMR (270 MHz, CDCl3): ppm of 3.97 (3H, s), 7,98 (1H, d, J=8.5 Hz), 8,19 (4H, s), 8,58 (1H, DD, J=2.5 and 8.5 Hz), at 9.53 (1H, d, J=2.5 n in example 2, using methyl 3-nitropyridine-6-eventout (545 mg), which is the product of reference example 32(a), and an aqueous solution of sodium hydroxide (1 N., and 3.16 ml) at 90oC, and the reaction mixture was treated with obtaining the connection specified in the header (370 mg) as colorless crystals. So pl. 262 to 264oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 8,11 (2H, d, J= 8.0 Hz), with 8.33 (2H, d, J=8.0 Hz), at 8.36 (1H, d, J=8.0 Hz), 8,71 (1H, DD, J= 2,0, 8.0 Hz), 9,48 (1H, d, J=2.0 Hz).

(Reference example 33)

3-Methoxypyridine-6-Albertina acid

(a) Methyl 3-aminopyridine-2-eventout

The reaction was conducted in the same manner as described in reference example 1(d) using methyl 3-nitropyridine-6-eventout (1.13 g), which is the product of reference example 32(a), and palladium on carbon (221 mg), and was treated to give the desired compound (738 mg) as colorless crystals. So pl. 188-189oC.1H-NMR (270 MHz, CDCl3): a 3.83 ppm (2H, user. C) 3,93 (3H, s), 7,06 (1H, DD, J=3,0, 8.5 Hz), to 7.61 (1H, d, J= 8.5 Hz), 7,98 (2H, d, J=8.5 Hz), of 8.09 (2H, d, J=8.5 Hz), to 8.20 (1H, d, J=3.0 Hz).

(b) Methyl 3-methoxypyridine-6-eventout

To a suspension of methyl 3-aminopyridine-6-eventout (425 mg) and sodium bromide (383 mg) in water at 0oC (10 ml) was added concentrated sulfuric acid (0,14 ivali at the same temperature for 15 minutes. At the end of this time the reaction mixture was added a solution amigorena acid and concentrated sulfuric acid (of 0.21 ml) in water (1.60 ml) and the mixture was stirred at 80oC for 1.5 hours and at room temperature for 1 hour and then left to stand for 14 hours. the pH of the reaction mixture was brought to pH 8 with an aqueous solution of sodium hydroxide (1 BC ). After addition of a solution of acetic anhydride (2.00 ml) and the mixture was stirred at room temperature for 30 minutes. The reaction mixture was distributed between ethyl acetate and water and an ethyl acetate layer was separated, washed with saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate. An ethyl acetate layer was away under reduced pressure to obtain a mixture (457 mg), methyl 5-acetoxypiperidine-2-eventuate and methyl 5-hydroxypyridine-2-eventuate. The reaction was conducted in the same manner as described in example 2, using a mixture obtained above, and an aqueous solution of sodium hydroxide (1 N., 2.10 ml) and the reaction mixture was treated with a 5-hydroxypyridine-2-eventing acid as a white powder. The reaction was conducted in the same manner as described in reference example 1C, using 5-hydroxypyridine-2-eventing acid, PI to give the desired compound (429 mg) as colorless crystals So pl. 130-132oC.1H-NMR (270 MHz, CDCl3): ppm 3,93 (3H, s), of 3.94 (3H, s), 7,30 (1H, DD, J=3,0, 9.0 Hz), 7,74 (1H, d, J= 9.0 Hz), 8,02 (2H, d, J=8,5 Hz) to 8.12 (2H, d, J=8.5 Hz), 8,43 (1H, d, J=3.0 Hz).

(C) 3-Methoxypyridine-6-Albertina acid

The reaction was conducted in the same manner as described in example 2, using methyl 3-methoxypyridine-6-eventout (249 mg), which is the product of reference example 33(b), and aqueous sodium hydroxide solution (1 N., 1,20 ml) and the reaction mixture was treated with obtaining the connection specified in the header, (206 mg) as colorless crystals. So pl. 221-223oC.1H-NMR (270 MHz, CDCl3/deuterated methanol = 3/1): ppm of 3.94 (3H, s), 7,35 (1H, DD, J= 3,0, 8.5 Hz), of 7.75 (1H, d, J= 8.5 Hz), of 7.96 (2H, d, J=8.5 Hz), 8,13 (2H, d, J= 8.5 Hz), scored 8.38 (1H, d, J=3.0 Hz).

(Reference example 34)

3-Dimethylaminopyridine-6-Albertina acid

(a) Methyl 3-dimethylaminopyridine-6-eventout

To a suspension of methyl 3-nitropyridine-6-eventout (519 mg) in a mixture of methanol (25 ml) and 2-methoxyethanol (5 ml) was added an aqueous solution of formaldehyde (35%, 3,20 ml) and palladium on carbon (5%, 640 mg). The mixture was stirred in hydrogen atmosphere at 50oC for 3 days. The catalyst was removed by filtration and the filtrate was concentrated under reduced pressure. The residue was distributed IU the sodium and saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was led from diisopropyl ether to give the desired product (288 mg) as colorless crystals. So pl. 161-163oC.1H-NMR (270 MHz, CDCl3): ppm was 3.05 (6H, s), 3,93 (3H, s), 7,05 (1H, DD, J= 3,0, 8.5 Hz), 7,66 (1H, d, J=8.5 Hz), 8,00 (2H, d, J=8.5 Hz), of 8.09 (2H, d, J= 8.5 Hz), 8,24 (1H, d, J=3.0 Hz).

(b) 3-Dimethylaminopyridine-6-Albertina acid

The reaction was conducted in the same manner as described in example 2, using methyl 3-dimethylaminopyridine-6-eventout (277 mg), which is the product of reference example 34(a) and aqueous solution of sodium hydroxide (1 N., 2,20 ml) and the reaction mixture was treated with obtaining the connection specified in the header (237 mg) as colorless crystals. So pl. 234-236oC.1H-NMR (270 MHz, deuterated dimethyl sulfoxide): ppm 3,01 (6H, s), 7,18 (1H, DD, J= 3,0, 9.0 Hz), 7,87 (1H, d, J= 9.0 Hz), of 7.97 (2H, d, J= 8.5 Hz), 8,10 (2H, d, J= 8.5 Hz), 8,23 (1H, d, J=3.0 Hz).

(Reference example 35)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2- (4-methylphenoxy) propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-methanesulfonylaminoethyl

To a solution of ethyl 3-(4-benzyloxyphenyl)lactate (3,32 g), which is the product of reference example 1(b), in anhydrous dichloromethane (30 ml) was added methanesulfonyl chloride (0,94 ml). To see this is an increase of 3 hours. The reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was led from hexane to give the desired product (of 3.60 g) as colorless crystals. So pl. 81-83oC. 1H-NMR (270 MHz, CDCl3): ppm of 1.27 (3H, t, J=7.0 Hz), 2,80 (3H, s), 3,02 be 3.29 (2H, m), are 4.24 (2H, q, J=7.0 Hz), of 5.05 (2H, s), of 5.05-5,14 (1H, m), 6,93 (2H, d, J=8.5 Hz), 7,17 (2H, d, J=8.5 Hz), 7,28 was 7.45 (5H, m).

(b) Ethyl 3-(4-benzyloxyphenyl)-2-(4-methylphenoxy)propionate

To a solution of ethyl 3-(4-benzyloxyphenyl)-2-methanesulfonylaminoethyl (11.1 g), which is the product of reference example 35(a), and p-cresol (2.85 g) in N,N - dimethylformamide (110 ml) was added potassium carbonate (8,09 g). This mixture was stirred at 70oC for 16 hours. The reaction mixture was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 9/1, to give the desired compound (2,84 g) as a colourless oil.1H-NMR (270 MHz, CDCl, Is, J=8.5 Hz), 7,26 (2H, d, J=8.5 Hz), 7,32-of 7.60 (5H, m).

(C) Ethyl 3-(4-hydroxyphenyl)-2-(4-methylphenoxy)propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-(4 - methylphenoxy)propionate (2,84 g), which is the product of reference example 35(b), and palladium on carbon (284 mg) and the reaction mixture was treated to give the desired compounds of 2.27 g) as a syrup. NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J= 7,0 Hz in), 2.25 (3H, s), 3,09-3,18 (2H, m) to 4.16 (2H, q, J=7.0 Hz), with 4.64-4.72 in (1H, m), was 4.76 (1H, user.C), 6,65-6,79 (4H, m), 7,02 (2H, d, J=8.5 Hz), 7,16 (2H, d, J=8,5 Hz).

(d) Ethyl 3-[4-(2-tert-butoxycarbonylamino) phenyl]-2-(4-methylphenoxy) propionate

The reaction was conducted in the same manner as described in reference example 25, using ethyl 3-(4-hydroxyphenyl)-2-(4-methylphenoxy) propionate (300 mg), which is the product of reference example 35(C), tert-butyl 2-methanesulfonylaminoethyl (598 mg) and potassium carbonate (691 mg) and the reaction mixture was treated with obtaining the connection specified in the header (261 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), a 1.45 (9H, s), of 2.25 (3H, s), 3,12-3,18 (2H, m), 3,45-3,55 (2H, m) to 3.99 (2H, t, J= 5.0 Hz), 4,17 (2H, q, J=7.0 Hz), 4,69 (1H, DD, J=5,5, 7.5 Hz), 4,96 (1H, user.C) 6,72 (2H, d, J=8.5 Hz), 6,82 (is aminoethoxy)phenyl] -2-(4-tert-butylphenoxy) propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(4-tert-butylphenoxy) propionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(4-benzyloxyphenyl)lactate (5,00 g), which is the product of reference example 1(b), 4-tertbutylphenol (2.50 g), triphenylphosphine (5,24 g) and a solution of diethylazodicarboxylate in toluene (40%, 8,80 ml) and the reaction mixture was treated to give the desired compound (3.00 g) as a colourless oil. 1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 1.26 in (9H, s), 3,12-is 3.21 (2H, m) to 4.17 (2H, q, J=7.0 Hz), 4,70 (1H, DD, J=5,5, 7.5 Hz), 5,04 (2H, s) 6,76 (2H, d, J=8.5 Hz), make 6.90 (2H, d, J=8.5 Hz), 7,20-7,26 (4H, m), 7,31 was 7.45 (5H, m).

(b) Ethyl 2-(4-tert-butylphenoxy)-3-(4-hydroxyphenyl) propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-(4 - tert-butylphenoxy) propionate (3.00 g), which is the product of reference example 36(a), and palladium on carbon (5%, 300 mg) and the reaction mixture was treated to give the desired compound (2.37 g) as a colourless oil. NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 1.26 in (9H, s), 3,13-3,20 (2H, m), 4,18 (2H, q, J= 7.0 Hz), 4,69 (1H, DD, J=5,5, 7.5 Hz), to 4.81 (1H, user.C) to 6.75 (2H, d, J= 8.5 Hz), 6,76 (2H, d, J=8.5 Hz), 7,17 (2H, d, J=8.5 Hz), 7,24 (2H, d, J=8,5 Hz).

(C) Ethyl 3-[4-(2-tert-butoxy described in reference example 25, using ethyl 2-(4-tert-butylphenoxy)-3-(4-hydroxyphenyl) propionate (2.37 g), which is the product of reference example 36(b), tert-butyl 2-methanesulfonylaminoethyl (of 3.60 g) and potassium carbonate (4,78 g) and the reaction mixture was treated with obtaining the connection specified in the header, (3.13 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7.0 Hz), 1.26 in (9H, s) of 1.45 (9H, s), 3,13-3,19 (2H, m), 3,51 (2H, q, J= 5.0 Hz), 3,99 (2H, t, J=5.0 Hz), 4,18 (2H, q, J=7.0 Hz), of 4.66-4.72 in (1H, m), 4,90-5,02 (1H, m), 6,76 (2H, d, J=8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), 7,22 (2H, d, J=8.5 Hz), 7,24 (2H, d, J=8,5 Hz).

(Reference example 37)

Ethyl 3-[4-(2-aminoethoxy)phenyl] -2-(4-pertenece)propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(4 - pertenece) propionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(4-benzyloxyphenyl)lactate (10.0 g), which is the product of reference example 1(b), 4-terfenol (4.15 g), triphenylphosphine (10.6 g) and diethylazodicarboxylate (6,40 ml) and the reaction mixture was treated to give the desired compound (7,00 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (3H, t, J=7,0 Hz), and 3.16 (2H, d, J=6,5 Hz) to 4.16 (2H, q, J= 7.0 Hz), of 4.66 (1H, t, J=6.5 Hz), 5,04 (2H, s), 6,72-to 6.80 (2H, m), 6.89 in-6,97 (4H, m), 7,21 (2H, d, J=8.5 Hz), 7,31-of 7.48 (5H, m).

(b) Ethyl 2-(4-pertenece)-3-(4-hydrocodone reference example 37(a), in a solution of hydrogen bromide in acetic acid (25%, 70 ml) was stirred at room temperature for 3 hours. The reaction mixture was concentrated under reduced pressure. To a solution of the residue in ethanol (70 ml) was added potassium carbonate (6.90 to g). This mixture was stirred at room temperature for 4 hours. The reaction mixture was concentrated under reduced pressure. The residue was distributed between ethyl acetate and water and the layers were separated. An ethyl acetate layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 9/1-4/1, to give the desired compound (2,75 g) as a white powder. So pl. 80-81oC.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7,0 Hz) and 3.15 (2H, d, J 6.5 Hz), 4,17 (2H, q, J= 7,0 Hz) and 4.65 (1H, t, J=6.5 Hz), was 4.76 (1H, s) of 6.71-to 6.80 (4H, m), 6.87 in-6,95 (2H, m), 7,16 (2H, d, J=8,5 Hz).

(C) Ethyl 2-(4-pertenece)-3-[4-[2-(tetrahydropyran-2-yloxy)ethoxy] phenyl]propionate

The reaction was conducted in the same manner as described in reference example 3(e), using ethyl 2-(4-pertenece)-3-(4-hydroxyphenyl) propionate (2,75 g), which is the product of reference example 37(b), 2-(2-bromoethoxy)tetrahydropyran (2,08 g) and the carb is oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 1,48-1,90 (6H, m), and 3.16 (2H, d, J=6.5 Hz), 3,49 is 3.57 (1H, m), of 3.77-of 3.95 (2H, m), 4,00-is 4.21 (5H, m), 4,60-to 4.73 (2H, m), 6,74 - 6,79 (2H, m), 6,84-to 6.95 (4H, m), 7,20 (2H, d, J=8,5 Hz).

(d) Ethyl 2-(4-pertenece)-3-[4-(2-hydroxyethoxy)- phenyl]propionate

The reaction was conducted in the same manner as described in reference example 3(f), using ethyl 2-(4-pertenece)-3-[4- [2-(tetrahydropyran-2-yloxy)ethoxy] -phenyl] propionate (3.75 g), which is the product of reference example 37(C), and monohydrate p-toluensulfonate acid (2.15 g) and the reaction mixture was treated to give the desired compound (2,68 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.25 ppm (3H, t, J=7.0 Hz), to 2.06 (1H, t, J=6.5 Hz), 3,20 is 3.23 (2H, m), 3,98-was 4.02 (2H, m), 4,10-4,13 (2H, m), 4,22 (2H, q, J=7.0 Hz), 4,71 (1H, DD, J=6,0, 7,0 Hz), 6,80-7,00 (6H, m), 7,25-7,28 (2H, m).

(e) Ethyl 2-(4-pertenece)-3-[4-(2-methanesulfonamido)phenyl] propionate

The reaction was conducted in the same manner as described in reference example 3(g), using ethyl 2-(4-pertenece)-3-[4-(2-hydroxyethoxy)phenyl]propionate (2,68 g), which is the product of reference example 37(d), triethylamine (1,61 ml) and methanesulfonamide (0,65 ml) and the reaction mixture was treated to give the desired compound (3,17 g) as a pale yellow oil.1H-NMR (2 6,74-OF 6.96 (6H, m), of 7.23 (2H, d, J=8,5 Hz).

(f) Ethyl 3-[4-(2-azidoethoxy)phenyl]-2-(4-pertenece)- propionate

The reaction was conducted in the same manner as described in reference example 3(h), using ethyl 2-(4-pertenece)-3-[4-(2-methanesulfonamido)phenyl] propionate (3,16 g), which is the product of reference example 37(e), and sodium azide (1.45 g) and the reaction mixture was treated to give the desired compound (2.67 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 3,17 (2H, d, J=6.5 Hz), to 3.58 (2H, t, J= 5.0 Hz), 4,08-to 4.23 (4H, m), of 4.66 (1H, t, J=6.5 Hz), 6,74-of 6.96 (6H, m), 7,20-of 7.25 (2H, m).

(g) Ethyl 3-[4-(2-aminoethoxy)phenyl]-2-(4-pertenece)- propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-[4-(2-azidoethoxy)phenyl]-2-(4-pertenece)propionate (2,60 g), which is the product of reference example 37(f), and palladium on carbon (5%, 250 mg) and the reaction mixture was treated with obtaining the connection specified in the header (2.30 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 2,99 is 3.15 (2H, m), and 3.16 (2H, d, J=6.5 Hz), of 3.97 (2H, t, J=5.0 Hz), 4,17 (2H, q, J=7.0 Hz), of 4.66 (1H, t, J=6.5 Hz), 6,72-of 6.96 (6H, m) and 7.1-7,27 (2H, m).

(Reference example 38)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-chlorosomes, that described in reference example 35(b), using ethyl 3-(4-benzyloxyphenyl)-2 - methanesulfonylaminoethyl (8,82 g), which is the product of reference example 35(a), 4-chlorophenol (3.00 g) and potassium carbonate (6,44 g) and the reaction mixture was treated to give the desired compounds (of 5.99 g) as colorless crystals. So pl. 63-64oC.1H-NMR (270 MHz, CDCl3): ppm of 1.18 (3H, t, J=7.0 Hz), 3,17 (2H, d, J= 6,5 Hz) to 4.16 (2H, q, J=7.0 Hz), 4,69 (1H, t, J=6.5 Hz), 5,04 (2H, s), of 6.75 (2H, d, J=9.0 Hz), 6,91 (2H, d, J=8.5 Hz), 7,13-of 7.23 (4H, m), 7,25-of 7.55 (5H, m).

(b) Ethyl 2-(4-chlorophenoxy)-3-(4-hydroxyphenyl)propionate

The reaction was conducted in the same manner as described in referential example 37(b), using ethyl 3-(4-benzyloxyphenyl)-2-(4-chlorophenoxy)propionate (of 5.99 g), which is the product of reference example 38(a), a solution of hydrogen bromide in acetic acid (25%, 60 ml) and potassium carbonate (4.68 g) and the reaction mixture was treated to give the desired compound (3,85 g) as colorless crystals. So pl. 90-93oC.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7,0 Hz), and 3.16 (2H, d, J=6.5 Hz),) to 4.17 (2H, q, J=7.0 Hz), 4,69 (1H, t, J= 6.5 Hz), of 4.95 (1H, user.C) 6,76 (4H, d, J=8.5 Hz), to 7.15 (2H, d, J=8.5 Hz), 7,18 (2H, d, J=8,5 Hz).

(C) Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-(4-chlorophenoxy) propionate

The reaction was carried out t is which is the product of reference example 38(b), tert-butyl 2-gidroxiatilkrahmal (1.27 g), triphenylphosphine (of 2.06 g) and diethylazodicarboxylate (1,37 g) and the reaction mixture was treated with obtaining the connection specified in the header (to 1.14 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), a 1.45 (9H, s), 3,17 (2H, t, J=6.5 Hz), 3.43 points is 3.57 (2H, m) to 3.99 (2H, t, J=5.0 Hz), 4,17 (2H, q, J=7.0 Hz), 4,69 (1H, t, J=6.5 Hz), 4,96 (1H, user.C) 6,76 (2H, d, J=8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), 7,10-7,20 (4H, m).

(Reference example 39)

Ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy]phenyl]propionate

(a) Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-hydroxypropionate

The reaction was conducted in the same manner as described in reference example 25, using ethyl 4-hydroxyphenylacetate (224 mg), tert-butyl 2-methanesulfonylaminoethyl (638 mg) and potassium carbonate (737 mg) and the reaction mixture was treated with obtaining the connection specified in the header, (205 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.29 (3H, t, J=7.0 Hz), a 1.45 (9H, s), of 2.72 (1H, d, J=6.0 Hz), only 2.91 (1H, DD, J=6,5, of 14.0 Hz), of 3.07 (1H, DD, J=4,5, of 14.0 Hz), 3,52 (2H, q, J=5.0 Hz), 3,99 (2H, t, J=5.0 Hz), 4,22 (2H, q, J=7.0 Hz), 4,39 (1H, DDD, J=4,5, 6,0, 6.5 Hz), to 4.98 (1H, user. t), PC 6.82 (2H, d, J=8.5 Hz), 7,13 (2H, d, J=8,5 Hz).

(b) Ethyl 2-hydroxy-3-[4-[2-(4-pyridine-2-albenzaalbenza)-ethoxy]phenyl] propionate

Re is hydroxy)phenyl]-2 - hydroxypropionate (168 mg), 4-pyridine-2-eventological (126 mg) and triethylamine (0,28 ml) and the reaction mixture was treated with obtaining the connection specified in the header (188 mg) as colorless crystals. So pl. 97-99oC.1H-NMR (270 MHz, CDCl3): ppm of 1.29 (3H, t, J=7.0 Hz), 2,92 (1H, d, J= 6,5, of 14.0 Hz), of 3.07 (1H, DD, J=4,5, of 14.0 Hz), 3,90 (2H, q, J=5.0 Hz), of 4.16 (2H, t, J= 5.0 Hz), 4,22 (2H, q, J=7.0 Hz), 4,39 (1H, DD, J=4,5, 6.5 Hz), 6,66 (1H, user.t), 6,87 (2H, d, J=8.5 Hz), to 7.15 (2H, d, J=8.5 Hz), 7,27-to 7.32 (1H, m), 7,73-to 7.84 (2H, m), 7,89 (2H, d, J=8.5 Hz), 8,07 (2H, d, J=8.5 Hz), 8,73 (1H, d, J=5.0 Hz).

(Reference example 40)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-triftormetilfosfinov)propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(4-triftormetilfosfinov)-propionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(4-benzyloxyphenyl)lactate (4,50 g), which is the product of reference example 1(b), 4-cryptomaterial (2,33 ml), triphenylphosphine (4.71 g) and a solution of diethylazodicarboxylate in toluene (40%, 8,15 ml) and the reaction mixture was treated to give the desired compound (4,19 g) as colorless crystals. So pl. 34-36oC.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J= 7.0 Hz), 3,18 (2H, d, J=6.5 Hz), 4,18 (2H, q, J=7.0 Hz), 4,70 (1H, t, J=6.5 Hz), 5,04 (2H, s), PC 6.82 (2H, d, J=8.5 Hz), 6,91 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,21 the Yu was performed in the same way, that described in reference example 37(b), using ethyl 3-(4-benzyloxyphenyl)-2-(4-triftormetilfosfinov)propionate (4,08 g), which is the product of reference example 40(a), a solution of hydrogen bromide in acetic acid (25%, 40 ml) and potassium carbonate (1.68 g) and the reaction mixture was treated to give the desired compound (2,98 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J= 7.0 Hz), 3,17 (2H, d, J=6.5 Hz), 3,50 (1H, user.C) 4,18 (2H, q, J=7.0 Hz), 4,70 (1H, t, J=6.5 Hz), 6,76 (2H, d, J=8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), to 7.15 (2H, d, J=8,5 Hz).

(C) Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-(4-triftormetilfosfinov)propionate

The reaction was conducted in the same manner as described in reference example 25, using ethyl 3-(4-hydroxyphenyl)-2-(4-triftormetilfosfinov)propionate (2,93 g), tert-butyl 2-methanesulfonylaminoethyl (4,73 g) and potassium carbonate (5,46 g) and the reaction mixture was treated with obtaining the connection specified in the header, (2.28 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), the 1.44 (9H, s) 3,18 (2H, d, J=6.5 Hz), 3,51 (2H, q, J=5.0 Hz), 3,99 (2H, t, J=5.0 Hz), 4,19 (2H, q, J=7.0 Hz), 4,70 (1H, t, J=6.5 Hz), equal to 4.97 (1H, user.t), for 6.81 (2H, d, J=8.5 Hz), 6,83 (2H, d, J=8.5 Hz), was 7.08 (2H, d, J=8.5 Hz), 7,21 (2H, d, J=8,5 Hz).

(Reference example 41)

Ethyl 3-[4-(2-what phenoxy)propionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(4-benzyloxyphenyl)lactate (1.01 g), which is the product of reference example 1(b), 4-cyanoprop (481 mg), triphenylphosphine (1.06 g) and a solution of diethylazodicarboxylate in toluene (40%, to 0.73 ml) and the reaction mixture was treated to give the desired compound (619 mg) as a colorless oil. 1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), 3,21 (2H, d, J=6.5 Hz), 4,17 (2H, q, J=7.0 Hz), 4,79 (1H, t, J=6.5 Hz), 5,04 (2H, s), to 6.88 (2H, d, J= 8.5 Hz), 6,91 (2H, d, J=8.5 Hz), 7,19 (2H, d, J=8.5 Hz), 7,28-of 7.48 (5H, m), 7,54 (2H, d, J=8,5 Hz).

(b) Ethyl 2-(4-cianfrocca)-3-(4-hydroxyphenyl)propionate

The reaction was conducted in the same manner as described in reference example 1(d), using ethyl 3-(4-benzyloxyphenyl)-2-(4-cianfrocca)propionate (376 mg), which is the product of reference example 41(a), and palladium on carbon (5%, 65 mg) and the reaction mixture was treated with obtaining the connection specified in the header (293 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J=7.0 Hz), 3,19 (2H, d, J=6.5 Hz), 4,18 (2H, q, J=7.0 Hz), 4,78 (1H, t, J=6.5 Hz), 6,76 (2H, d, J=8.5 Hz), to 6.88 (2H, d, J=9.0 Hz), 7,14 (2H, d, J=8.5 Hz), a 7.62 (2H, d, J=9.0 Hz).

(C) Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-cianfrocca) propionate

The reaction is enyl) propionate (293 mg), tert-butyl 2-methanesulfonylaminoethyl (560 mg) and potassium carbonate (520 mg) and the reaction mixture was treated with obtaining the connection specified in the header (245 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7.0 Hz), a 1.45 (9H, s), 3,21 (2H, d, J=6.5 Hz), 3,52 (2H, q, J=5.0 Hz), 3,99 (2H, t, J=5.0 Hz), 4,19 (2H, q, J=7.0 Hz), 4,79 (1H, t, J=6.5 Hz), equal to 4.97 (1H, user.t), 6,83 (2H, d, J=8.5 Hz), to 6.88 (2H, d, J=8.5 Hz), 7,20 (2H, d, J=8.5 Hz), 7,55 (2H, d, J=8,5 Hz).

(Reference example 42)

Methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-methylthiophene)propionate

The reaction was conducted in the same manner as described in example 122 using methyl 3-[4-(2-tert - butoxycarbonylamino)phenyl]-2-hydroxypropionate (389 mg), which was obtained by the same method described in reference example 39(a), 4-methylthiophenol (241 mg), triphenylphosphine (463 mg) and a solution of diethylazodicarboxylate in toluene (40%, at 0.31 ml) and the reaction mixture was treated to give the desired compound (265 mg) as a colourless oil, which contains some impurities.1H-NMR (270 MHz, CDCl3): ppm of 1.45 (9H, s), 2,43 (3H, s), 3,17 (2H, d, J=6.5 Hz), 3,52 (2H, q, J=5.0 Hz), and 3.72 (3H, s) to 3.99 (2H, t, J=5.0 Hz), 4.72 in (1H, t, J=6.5 Hz), to 4.98 (1H, user.t) is 6.78 (2H, d, J=8.5 Hz), PC 6.82 (2H, d, J=8.5 Hz), 7,20 (4H, d, J=8,5 Hz).

(Reference example 43)

Methyl 3-[GE way that described in example 122 using methyl 3-[4-(2-tert - butoxycarbonylamino)phenyl]-2-hydroxypropionate (518 mg), which was obtained in the same way as described in reference example 39(a), 4-methansulfonate (394 mg), tributylphosphine (0,57 ml) instead of triphenylphosphine and 1,1'-(azodicarbon)dipiperidino (578 mg) instead of diethylazodicarboxylate, and the reaction mixture was treated to give the desired compound (441 mg) as a foamy mass.1H-NMR (270 MHz, CDCl3): ppm of 1.44 (9H, s) of 3.00 (3H, s), up 3.22 (2H, d, J=6.5 Hz), 3,51 (2H, q, J=5.0 Hz), 3,74 (3H, s) to 3.99 (2H, t, J=5.0 Hz), 4,84 (1H, t, J=6.5 Hz), equal to 4.97 (1H, user. t), 6,83 (2H, d, J=8.5 Hz), 6,94 (2H, d, J=9.0 Hz), 7,19 (2H, d, J=8.5 Hz), 7,82 (2H, d, J=9.0 Hz).

(Reference example 44)

Methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-pertenece)propionate

The reaction was conducted in the same manner as described in example 122 using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]- 2-hydroxypropionate (420 mg), which was obtained in the same way as described in reference example 39(a), 4-terfenol (284 mg), triphenylphosphine (666 mg) and a solution of diethylazodicarboxylate in toluene (40%, 1,10 ml) and the reaction mixture was treated to give the desired compound (314 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3: ), 6,83 (2H, d, J= 8.5 Hz), 6,92 (2H, DD, J=8,0, 9.0 Hz), 7,20 (2H, d, J=8,5 Hz).

(Reference example 45)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-(4-isopropylphenoxy)-2-methylpropionate

The reaction was conducted in the same manner as described in reference example 25, using ethyl 3-(4-hydroxyphenyl)-2-(4-isopropylphenoxy)-2-methylpropionate (4,85 g), which is the product of reference example 9(b), tert-butyl 2-methanesulfonylaminoethyl (of 8.47 g) and potassium carbonate (9,78 g) and the reaction mixture was treated with obtaining the connection specified in the header, (6,23 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): to 1.15 ppm of 1.28 (9H, m) to 1.37 (3H, s) of 1.45 (9H, s), and 2.83 (1H, septet, J=7.0 Hz), 3,10 (1H, d, J=13.5 Hz) at 3.25 (1H, d, J=13.5 Hz), 3.46 in-to 3.58 (2H, m) 4,00 (2H, t, J=5.0 Hz), is 4.21 (2H, q, J=7.0 Hz), 4,95-of 5.05 (1H, m), of 6.75 (2H, d, J= 8.5 Hz), for 6.81 (2H, d, J=8.5 Hz), 7,06 (2H, d, J=8.5 Hz), 7,17 (2H, d, J= 8,5 Hz).

(Reference example 46)

Methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-phenyl-thiopropionate

The reaction was conducted in the same manner as described in example 122 using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2 - hydroxypropionate (366 mg), which was obtained by the same method described in reference example 39(a), thiophenol (0.17 ml), triphenylphosphine (438 mg) and a solution of diethylester the form of colorless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.45 (9H, s) of 3.00 (1H, DD, J=6,5, and 13.5 Hz), of 3.13 (1H, DD, J=a 9.5 and 13.5 Hz), 3,52 (2H, t, J=5.0 Hz), to 3.58 (3H, s), 3,86 (1H, DD, J=6,5, 9.5 Hz), 3,98 (2H, t, J=5.0 Hz), 5,00 (1H, user.t), to 6.80 (2H, d, J=8.5 Hz), 7,10 (2H, d, J=8.5 Hz), 7,30-7,40 (3H, m), 7,41-7,56 (2H, m).

(Reference example 47)

Methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2- (pyridine-3-yloxy) propionate

The reaction was conducted in the same manner as described in example 122 using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl]-2-hydroxypropionate (404 mg), which was obtained by the same method described in reference example 39(a), 3 hydroxypyridine (227 mg), triphenylphosphine (938 mg) and a solution of diethylazodicarboxylate in toluene (40%, of 0.65 ml) and the reaction mixture was treated to give the desired compound (345 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.44 (9H, s), 3,21 (2H, d, J=6.5 Hz), 3,52 (2H, q, J=5.0 Hz), 3,74 (3H, s) to 3.99 (2H, t, J=5.0 Hz), 4,78 (1H, t, J= 6.5 Hz), 4,96 (1H, user.t), at 6.84 (2H, d, J=8.5 Hz), 7,11 (1H, d, J=8.5 Hz), 7,18 (1H, DD, J=5.0 and 8.5 Hz), 7,20 (2H, d, J=8.5 Hz), 8,23 (1H, d, J= 5.0 Hz), 8,24 (1H, s).

(Reference example 48)

Methyl 2-(benzoxazol-2-ylthio)-3-[4-(2-tert-butoxycarbonylamino)phenyl] propionate

The reaction was conducted in the same manner as described in example 122 using methyl 3-[4-(2-tert-butoxycarbonylamino mercaptobenzoxazole (277 mg), tributylphosphine (0,46 ml) instead of triphenylphosphine and 1,1'- (azodicarbon)dipiperidino (460 mg) instead of diethylazodicarboxylate, and the reaction mixture was treated to give the desired compound (665 mg) as a colourless oil, which contains some impurities.1H-NMR (270 MHz, CDCl3): ppm of 1.46 (9H, s), 3,26 (1H, DD, J= 7,0, of 14.0 Hz), the 3.35 (1H, DD, J=7,5, of 14.0 Hz), 3,51 (2H, q, J=5.0 Hz), 3,71 (3H, s), of 3.96 (2H, t, J=5.0 Hz), was 4.76 (1H, DD, J=7,0, 7.5 Hz), 4,89 (1H, user.t), for 6.81 (2H, d, J=8.0 Hz), 7,17 (2H, d, J=8.0 Hz), 7,22-7,29 (2H, m), the 7.43 (1H, d, J=7.5 Hz), 7,60 (1H, d, J=6.0 Hz).

(Reference example 49)

Methyl 2-benzyloxy-3-[4-(2-tert-butoxycarbonylamino)-phenyl] propionate

The reaction was conducted in the same manner as described in reference example 1(C) using methyl 3-[4-(2-tert-butoxycarbonylamino)phenyl] -2-hydroxypropionate (398 mg), which was obtained by the same method described in reference example 39(a), benzylbromide (0,28 ml), hydride (55% suspension in oil, 168 mg) and tetrabutylammonium iodide (43 mg) and the reaction mixture was treated to give the desired compound (133 mg) as a colorless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.46 (9H, s), 2,99 (1H, d, J=7.5 Hz), 3,00 (1H, d, J=5.5 Hz), 3,53 (2H, q, J=5.0 Hz), 3,71 (3H, s), of 4.00 (2H, t, J= 5.0 Hz), 4.09 to (1H, DD, J=5,5, 7.5 Hz), 4,37 (1H, d, J=12.0 Hz) and 4.65 (1H, d, J=12.0 Hz), 5,00 (1H, user.t), for 6.81 (2H, d, J=8,5-pyridine-2-albenzaalbenza)propyl] benzyl]malonate

(a) 4-(3-Benzyloxycarbonylamino)benzyl alcohol

To a suspension of lithium aluminum hydride (of 4.00 g) in tetrahydrofuran (180 ml) in an ice bath was added dropwise a solution of methyl 4-(2-cyanoethyl)benzoate (10.0 g) in tetrahydrofuran (80 ml). The mixture was stirred at room temperature for 1 hour and at 60oC for 3 hours. In the reaction mixture was sequentially added water (4 ml), aqueous sodium hydroxide solution (15%, 4 ml) and water (12 ml) and the mixture was stirred for 1 hour. The insoluble product in the reaction mixture were removed by filtration and washed with tetrahydrofuran. In the mixture of filtrate was added N-benzyloxycarbonyl-5-norbornene-2,3-dicarboximide (16.5 g) and a solution of tetrahydrofuran, and the mixture was stirred at room temperature for 3 hours. The reaction mixture was concentrated. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride and saturated aqueous sodium bicarbonate, dried over anhydrous magnesium sulfate and concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 1/1, to give the desired compound (5,67 is), the 4.65 (2H, s), and 4.75 (1H, user.C) 5,09 (2H, s), 7,16 (2H, d, J=8.0 Hz), 7,26 and 7.36 (7H, m).

(b) 4-[3-(4-Pyridine-2-albenzaalbenza)propyl]alcohol

To a solution of 4-(3-benzyloxycarbonylamino)-benzyl alcohol (1,00 g), which is the product of reference example 50 (a), in ethanol (20 ml) was added palladium on carbon (5%, 0.15 g). The mixture was stirred in hydrogen atmosphere at room temperature for 2 hours. The catalyst was removed by filtration and the filtrate was concentrated to obtain 4-(3-aminopropyl)benzyl alcohol resin. The reaction was conducted in the same manner as described in example 5, using 4-(3-aminopropyl)benzyl alcohol, 4-pyridine-2-eventing acid (668 mg) and carbonyldiimidazole (650 mg) and the reaction mixture was treated to give the desired compound (0.74 g) as colorless crystals. So pl. 118-120oC. 1H-NMR (270 MHz, CDCl3): 2,00 ppm (2H, quintuplet, J=7.5 Hz), a 2.75 (2H, t, J=7.5 Hz),

of 3.53 (2H, dt, J=6,5, 7,5 Hz) and 4.65 (2H, s), 6,10 (1H of user.C), 7,20-7,31 (5H, m), 7,72-7,80 (4H, m), 8,02 (2H, d, J=8.5 Hz), 8,71 (1H, d, J=5.0 Hz).

(C) 4-[3-(4-pyridine-2-albenzaalbenza)propyl] benzylchloride

To a solution of 4-[3-(4-pyridine-2-albenzaalbenza)-propyl] alcohol (0.74 g) in dichloromethane (20 ml) was sequentially added methanesulfonamide (294 mg) and triethylamine (0.37 to mlotok was distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated to obtain crystals. The crystals were washed with a small amount of diisopropyl ether to give the desired compound (0.68 g). So pl. 115-117oC.1H-NMR (270 MHz, CDCl3): ppm of 1.99 (2H, quintuplet, J=7.5 Hz), a 2.75 (2H, t, J=7.5 Hz), 3,53 (2H, dt, J=6,5, 7.5 Hz), x 6.15 (1H, user. C), 7,21-7,34 (5H, m), 7,76-of 7.82 (4H, m), of 8.06 (2H, d, J=8.5 Hz), 8,70-8,73 (1H, m).

(d) Dibenzyl 2-(3-phenylpropyl)-2-[4-[3-(4-pyridine-2-albenzaalbenza)propyl]benzyl]malonate

The reaction was conducted in the same manner as described in reference example 2(a), using 4-[3-(4-pyridine-2-albenzaalbenza)propyl] benzylchloride (488 mg), which is the product of reference example 50(C), sodium hydride (55% suspension in oil, 64 mg) and benzyl (3-phenylpropyl)malonate (540 mg) and the reaction mixture was treated with obtaining the connection specified in the header, (0.65 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm 1,44 is 1.58 (2H, m), 1,78-to 1.87 (2H, m), with 1.92 (2H, t, J=7.5 Hz), 2,52 (2H, t, J=7.5 Hz), to 2.65 (2H, t, J= 7.5 Hz), 3,19 (2H, s), 3,49 (2H, dt, J=6,0, 7.5 Hz), of 5.05 (1H, d, J= 12.0 Hz), 5,09 (1H, d, J=12.0 Hz), 6,16 (1H, user.t, J=6.0 Hz), 6,78 (2H, d, J= 8.0 Hz), of 6.96 (2H, d, J=8.0 Hz), 7,05 (2H, d, J=8.0 Hz), 7,17-to 7.35 (14H, m), 7,76-of 7.82 (4H, m), of 8.06 (2H, d, J=8.5 Hz), 8,71 (1H, d, J=5.0 Hz).

(a) Ethyl 3-(3-chloro-4-hydroxyphenyl)-2-phenoxypropionate

To a solution of ethyl 3-(4-hydroxyphenyl)-2-phenoxypropionate (1,43 g) in diethyl ether (20 ml) was added dropwise a solution of sulfurylchloride (of 0.71 ml) in diethyl ether (5 ml) at room temperature. The mixture was stirred for 8 hours and left to stand over night. The reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 10/3, to give the desired compound (1,09 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J=7,0 Hz) and 3.15 (1H, d, J=5.0 Hz), and 3.16 (1H, d, J= 7.5 Hz), 4,19 (2H, q, J=7.0 Hz), to 4.73 (1H, DD, J=5.0 and 7.5 Hz), 5,49 (1H, s), at 6.84 (2H, d, J=8.0 Hz), 6,94 (1H, d, J=8.5 Hz), of 6.96 (1H, t, J= 8.0 Hz), 7,12 (1H, DD, J=2,0, 8.5 Hz), 7,25 (2H, t, J=8.0 Hz), 7,28 (1H, d, J 2.0 Hz).

(b) Ethyl 3-[4-(2-tert-butoxycarbonylamino)-3-chlorophenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(3-chloro-4-hydroxyphenyl)-2-phenoxypropionate (761 mg), which is the product of reference is that in toluene (40%, 2,69 ml) and the reaction mixture was treated to give the desired compound (1,03 g) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7.0 Hz), a 1.45 (9H, s) and 3.15 (1H, d, J=5.5 Hz), and 3.16 (1H, d, J=7.5 Hz),2 of 3.56 (2H, q, J=5.0 Hz), of 4.05 (2H, t, J=5.0 Hz), 4,19 (2H, q, J=7.0 Hz), to 4.73 (1H, DD, J=5,5, 7.5 Hz), of 5.06 (1H, user.t), at 6.84 (2H, d, J=8.0 Hz), 6,85 (1H, d, J=8.5 Hz), of 6.96 (1H, t, J=8.0 Hz), to 7.15 (1H, DD, J=2,0, 8.5 Hz), 7,25 (2H, t, J=8.0 Hz), 7,33 (1H, d, J=2.0 Hz).

(Reference example 52)

Ethyl 3-[3-bromo-4-(2-tert-butoxycarbonylamino)phenyl] -2-phenoxypropionate

(a) Ethyl 3-(3-bromo-4-hydroxyphenyl)-2-phenoxypropionate

To a solution of ethyl 3-(4-hydroxyphenyl)-2-phenoxypropionate (1,43 g), which is the product of reference example 4 (C) in chloroform (20 ml), was added N-bromosuccinimide (1.12 g) at room temperature. The mixture was stirred at 70oC for 4 hours and concentrated under reduced pressure. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 4/1, to give the desired compound (1,41 g) in the, =7,0 Hz), 4.72 in (1H, DD, J=5,5, 7,0 Hz), the 5.45 (1H, user.C) at 6.84 (2H, d, J=8.0 Hz), 6,94 (1H, d, J=8.5 Hz), of 6.96 (1H, t, J=8.0 Hz), 7,16 (1H, DD, J=2,0, 8.5 Hz), 7,25 (2H, t, J=8.0 Hz), 7,42 (1H, d, J=2.0 Hz).

(b) Ethyl 3-[3-bromo-4-(2-tert-butoxycarbonylamino)-phenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(3-bromo-4-hydroxyphenyl)-2-phenoxypropionate (374 mg), which is the product of reference example 52(a), tert-butyl 2-gidroxiatilkrahmal (403 mg), triphenylphosphine (672 mg) and a solution of diethylazodicarboxylate in toluene (40%, of 1.16 ml) and the reaction mixture was treated to give the desired compound (466 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm to 1.21 (3H, t, J=7.0 Hz), a 1.45 (9H, s) and 3.15 (1H, d, J=5.5 Hz), and 3.16 (1H, d, J= 7,0 Hz), of 3.56 (2H, q, J=5.0 Hz), Android 4.04 (2H, t, J=5.0 Hz), 4,19 (2H, q, J= 7.0 Hz), 4.72 in (1H, DD, J=5,5, 7,0 Hz), to 5.08 (1H, user.t), PC 6.82 (1H, d, J=8.5 Hz), 6,85 (2H, d, J=8.0 Hz), of 6.96 (1H, t, J=7.5 Hz), 7,20 (1H, DD, J=2,0, 8.5 Hz), 7,25 (2H, DD, J=7,5, 8.0 Hz), to 7.50 (1H, d, J=2.0 Hz).

(Reference example 53)

Ethyl 3-[4-(2-tert-butoxycarbonylamino)-3-nitrophenyl]-2 - phenoxypropionate

(a) Ethyl 3-(4-hydroxy-3-nitrophenyl)-2-phenoxypropionate

To a solution of ethyl 3-(4-hydroxyphenyl)-2-phenoxypropionate (1,00 g), which is the product of reference example 4(C), in a mixture of dichloromethane (4.0 ml) is spending sodium (297 mg) at room temperature. The mixture was stirred for 2.5 hours at the same temperature and left to stand for 14 hours. The reaction mixture was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent hexane/ethyl acetate = 4/1, to give the desired compound (935 mg) as a colourless oil.1H-NMR (270 MHz, CDCl3): ppm of 1.23 (3H, t, J=7.0 Hz), 3,23 (2H, d, J=6.0 Hz), is 4.21 (2H, q, J= 7.0 Hz), was 4.76 (1H, t, J=6.0 Hz), 6,83 (2H, d, J=8.0 Hz), 6,97 (1H, t, J= 7.5 Hz), 7,11 (1H, d, J=8.5 Hz), 7,25 (2H, DD, J=7,5, 8.0 Hz), 7,56 (1H, DD, J=2,0, 8.5 Hz), 8,08 (1H, d, J=2.0 Hz).

(b) Ethyl 3-[4-(2-tert-butoxycarbonylamino)-3 - nitrophenyl]-2-phenoxypropionate

The reaction was conducted in the same manner as described in example 122 using ethyl 3-(4-hydroxy-3-nitrophenyl)-2-phenoxypropionate (270 mg), which is the product of reference example 53(a), tert-butyl 2-gidroxiatilkrahmal (322 mg), triphenylphosphine (535 mg) and a solution of diethylazodicarboxylate in toluene (40%, with 0.93 ml) and the reaction mixture was treated with obtaining desire, Is, J=6.0 Hz), of 3.57 (2H, q, J= 5.0 Hz), 4,14 (2H, t, J=5.0 Hz), is 4.21 (2H, q, J=7.0 Hz), was 4.76 (1H, t, J=6.0 Hz), 5,14 (1H, user.t), 6,83 (2H, d, J=8.0 Hz), 6,97 (1H, t, J= 7.5 Hz), 7,00 (1H, d, J=8.5 Hz), 7,25 (2H, DD, J=7,5, 8.0 Hz), to 7.50 (1H, DD, J=2,0, 8.5 Hz), the 7.85 (1H, d, J=2.0 Hz).

(Reference example 54)

Methyl (S)-2-benzyloxycarbonylamino-3-[4-(2-tert-butoxycarbonylamino)phenyl]propionate

The reaction was conducted in the same manner as described in reference example 25, using methyl ester of N-benzyloxycarbonyl-L-tyrosine (4.94 g), tert-butyl 2-methanesulfonylaminoethyl (8,97 g) and potassium carbonate (10.4 g) and the reaction mixture was treated with obtaining the connection specified in the header (of 3.32 g) as colorless crystals. So pl. 89-91oC.1H-NMR (270 MHz, CDCl3): of 1.62 ppm (9H, s), 3.00 and-3,10 (2H, m), 3,48 of 3.56 (2H, m), and 3.72 (3H, s), 3,98 (2H, t, J=5.0 Hz), 4,56-and 4.68 (1H, m), 4,99 (1H, user.C) to 5.10 (2H, ABq, J= 12,5 Hz, =0,03 ppm), 5,15-5,24 (1H, m), 6,79 (2H, d, J=8.5 Hz), 7,00 (2H, d, J=8.5 Hz), 7.23 percent-7,41 (5H, m).

(Reference example 55)

Ethyl 3-(4-hydroxyphenyl)-2-(phenylamino)propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(phenylamino) propionate

A mixture of ethyl 3-(4-benzyloxyphenyl)-2 - methansulfonate-propionate (4,00 g) and aniline (5 ml) was stirred at 110oC for 24 hours. The reaction mixture was purified by chromatography on a column of silica gel, IP is UP>H-NMR (270 MHz, CDCl3): ppm of 1.17 (3H, t, J=7 Hz), 3.00 and-3,14 (2H, m), of 4.12 (2H, dq, J=1,5, 7 Hz), 4,30 (1H, t, J=6 Hz), 5,04 (2H, s), 6,60 (2H, J=8.5 Hz), was 6.73 (1H, t, J=7.5 Hz), 6.89 in (2H, d, J=8.5 Hz), to 7.09 (2H, d, J=8.5 Hz), 7,16 (2H, d, J=8.5 Hz), 7,31-7,44 (5H, m).

(b) Ethyl 3-(4-hydroxyphenyl)-2-(phenylamino)propionate

To a solution of ethyl 3-(4-benzyloxyphenyl)-2-(phenylamino)propionate (3.94 g), which is the product of reference example 55(a), in a mixture of ethanol (40 ml) and tetrahydrofuran (20 ml) was added palladium on carbon (5%, 0,80 g).

The mixture was stirred in hydrogen atmosphere at 50oC for 6 hours. The catalyst was removed by filtration and the filtrate was concentrated. The residue was purified by chromatography on a column of silica gel, using as eluent ethyl acetate/hexane = 1/2, obtaining the connection specified in the header (2,95 g) as a syrup.1H-NMR (270 MHz, CDCl3): ppm to 1.19 (3H, t, J= 1 Hz), 3.00 and-3,13 (2H, m), 4,13 (2H, dq, J=1, 7 Hz), 4,30 (1H, user.t, J=6 Hz), 4,88 (1H, user.C) 6,60 (2H, d, J=8 Hz), of 6.71-6,76 (3H, m), 7,03 (2H, d, J=8 Hz), 7,14-7,20 (2H, m).

(Reference example 56)

Ethyl 3-(4-hydroxyphenyl)-2-(N - ethyl-N-phenylamino) propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(N-ethyl-N-phenylamino)- propionate

The reaction was conducted in the same manner as described in reference example 55(a), using ethyl 3-(4-benzylated mixture of the desired compounds and N-ethylaniline (6,30 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.07 ppm (3H, t, 3H, J=7 Hz), to 1.14 (3H, t, J=7 Hz), 3,01 is-3.45 (4H, m), 4.09 to (2H, q, J= 7 Hz), 4,39 (1H, t, J=7.5 Hz), 5,02 (2H, s), 6,66 to 6.75 (3H, m), 6.87 in (2H, d, J=8 Hz), 7,10 (2H, d, J=8.5 Hz), 7,15-of 7.25 (2H, m), 7,31-7,44 (5H, m).

(b) Ethyl 2-(N-ethyl-N-phenylamino)-3-(4-hydroxyphenyl)propionate

The reaction was conducted in the same manner as described in reference example 55(b) using a mixture (6,30 g), which is the product of reference example 56(a), and the reaction mixture was treated with obtaining the connection specified in the header, (2.37 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.07 ppm (3H, t, J=7 Hz) and 1.15 (3H, t, J=7 Hz), 3,05 (1H, DD, J=8, 14 Hz), 3,26 (1H, d, d, J= 7,5, 14 Hz), 3,30-of 3.46 (2H, m), 4,10 (2H, q, J=7 Hz), to 4.38 (1H, t, J=8 Hz), and 4.75 (1H, user. C) 6,67-6,79 (5H, m), 7,05 (2H, d, J=8.5 Hz), 7.18 in-7,26 (2H, m).

(Reference example 57)

Ethyl 3-(4-hydroxyphenyl)-2-(pyrrol-1-yl)propionate

(a) Ethyl 3-(4-benzyloxyphenyl)-2-(pyrrol-1-yl)propionate

To a solution of ethyl 3-(4-benzyloxyphenyl)-2-aminopropionic (3,30 g) in dichloromethane (80 ml) was added 1,4-dichloro-1,4-diethoxybutane (3,30 g) and then the mixture was added amberlyst A-21 (20 g). The mixture was stirred at room temperature for 18 hours and the reaction mixture was filtered. The filtrate was concentrated and the residue was purified by chromatography on a column of silica gel, using as3): ppm to 1.19 (3H, t, J= 7 Hz), 3,19 (1H, DD, J=8,5, 14 Hz), to 3.34 (1H, DD, J=7, 14 Hz), 4,14 (2H, q, J=7 Hz), and 4.68 (1H, DD, J=7, 8.5 Hz), free 5.01 (2H, s), x 6.15 (2H, t, J=2 Hz), 6.73 x (2H, t, J=2 Hz), at 6.84 (2H, d, J=8.5 Hz), 6,94 (2H, d, J=8.5 Hz), 7,28-the 7.43 (5H, m).

(b) Ethyl 3-(4-hydroxyphenyl)-2-(pyrrol-1-yl)propionate

The reaction was conducted in the same manner as described in reference example 55(b), using ethyl 3-(4-benzyloxyphenyl)-2-(pyrrol-1-yl)propionate (1,00 g) obtained in reference example 57(a), and palladium on carbon (5%, 0.12 g) and the reaction mixture was treated with obtaining the connection specified in the header (0.71 g) as a syrup.1H-NMR (270 MHz, CDCl3): of 1.20 ppm (3H, t, J= 7 Hz), 3,18 (1H, DD, J=8,5, 14 Hz), to 3.33 (1H, DD, J=7, 14 Hz), is 4.15 (2H, q, J=7 Hz), of 4.67 (1H, DD, J-7, 8.5 Hz), 4,80 (1H, s), 6,14 (2H, t, J=2 Hz), of 6.71 (2H, d, J=8.5 Hz), 6,72 (2H, d, J=2 Hz), to 6.88 (2H, d, J=8,5 Hz).

(Reference example 58)

Ethyl 2-(N,N-diethylamino)-3-(4-hydroxyphenyl)propionate

To a solution of the hydrochloride of the ethyl ester of DL-tyrosine (491 mg) in methanol (5 ml) was added acetic acid (0.3 ml) and acetaldehyde (0.5 ml). To the mixture was added cyanoborohydride sodium (126 mg) and the mixture was stirred at room temperature for 2 hours. At the end of this time the reaction mixture was concentrated. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated, p is ri reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent methanol/dichloromethane = 1/20, to give the desired compound (420 mg) as a syrup. 1H-NMR (270 MHz, CDCl3): of 1.02 ppm (6H, t, J=7 Hz), of 1.16 (3H, t, J=7 Hz), 2,53 (2H, sextet, J=7 Hz), and 2.79 (2H, sextet, J=7 Hz), of 2.81 (1H, DD, J=6 and 13.5 Hz), 2,99 (1H, DD, J=9 and 13.5 Hz), 3,55 (1H, DD, J=6, 9 Hz), was 4.02-4,11 (2H, m), 6,72 (2H, d, J-8.5 Hz), 7,02 (2H, d, J=8,5 Hz).

(Reference example 59)

Ethyl 2-N-(tert-butoxycarbonyl)ethylamino-3-(4-hydroxyphenyl)-propionate

(a) Ethyl 2-ethylamino-3-(4-hydroxyphenyl)propionate

The reaction was conducted in the same manner as described in referential example 9 by using the hydrochloride of the ethyl ester of DL-tyrosine (983 mg), acetaldehyde (0,26 ml) and sodium cyanoborohydride (100 mg) and the reaction mixture was treated to give the desired compound (515 mg) in the form of a syrup, which was left to stand to obtain crystals. So pl. 87-89oC.1H-NMR (270 MHz, CDCl3): ppm of 1.08 (3H, t, J=7 Hz), of 1.18 (3H, t, J=7 Hz), 2,48-of 2.72 (2H, m), 2,82-2,96 (2H, m), 3,50 (1H, t, J=7 Hz), 4,11 (2H, q, J=7 Hz), of 6.68 (2H, d, J=8.5 Hz), 7,01 (2H, d, J=8,5 Hz).

(b) Ethyl 2-N-(tert-butoxycarbonyl)ethylamino-3-(4 - hydroxyphenyl)propionate

To a solution of ethyl 2-ethylamino-3-(4-hydroxyphenyl)propionate (569 mg), which is the product sulochna the amine (1 ml). The mixture was stirred at room temperature for 4 hours. At the end of this time the reaction mixture was concentrated. The residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by chromatography on a column of silica gel, using as eluent ethyl acetate/hexane = 1/2, obtaining the connection specified in the header (663 mg) as a syrup.1H-NMR (270 MHz, CDCl3): ppm of 0.90 (3H, user. t, J=7 Hz), to 1.21 to 1.31 (3H, m) of 1.45 (9H, s), 3,15-3,37 (1H, m), is 3.08 (1H, DD, J=10, 14 Hz), 3,15-3,37 (1H, m), 3,24 (1H, DD, J=5, 14 Hz), 3,85-4,30 (3H, m), 6,76 (2H, user. d, J=8.5 Hz), 7,00-7,11 (2H, m).

(Reference example 60)

Ethyl 2-N-(tert-butoxycarbonyl)propylamino-3-(4-hydroxyphenyl) propionate

(a) Ethyl 3-(4-hydroxyphenyl)-2-Propylenediamine

The reaction was conducted in the same manner as described in reference example 59(a), using the hydrochloride of the ethyl ester of DL-tyrosine, Propionaldehyde and sodium cyanoborohydride, and the reaction mixture was treated to give the desired compound.

(b) Ethyl 2-N-(tert-butoxycarbonyl)propylamino-3-(4-hydroxyphenyl) propionate

The reaction was carried out in the same way, which is described in Ref the aqueous example 60(a), and tert-BUTYLCARBAMATE, and the reaction mixture was treated with obtaining the connection specified in the header.

(Reference example 61)

2-(4-pyridine-2-albenzaalbenza) ethanol

To a suspension of 4-pyridine-2-eventological (254 mg) in dichloromethane (2 ml) was added triethylamine (0,14 ml). To the mixture was added a solution of ethanolamine (to 0.060 ml) in dichloromethane (3 ml). This mixture was stirred for 30 minutes. At the end of this time the reaction mixture was concentrated and the residue was distributed between ethyl acetate and water. An ethyl acetate layer was separated and washed with aqueous sodium chloride, dried over anhydrous magnesium sulfate, and concentrated to obtain crystals. The crystals were washed with isopropyl ether to obtain the connection specified in the header (111 mg). So pl. = 86-88oC.1H-NMR (270 MHz, CDCl3): ppm 2,52 (1H, t, J=4.5 Hz), 3,68 (2H, dt, J=5.0 and 5.5 Hz), 3,88(2H, dt, J=4,5, 5,5 Hz), of 6.68 (1H, user. C), 7,24-7,33 (1H, m), to 7.77-of 7.82 (1H, m), of 7.90 (2H, d, J=8.5 Hz), of 8.09 (2H, d, J=8.5 Hz), 8,72 (1H, d, J=5 Hz).

[Test sample]

The effect on the suppression of blood glucose (Method 1)

Each composition, primitively powder feed F-2 (Funabashi Farm) were administered to male KK mice with hyperglycemia, weight was 40 g or more, with a coefficient of 0.01 Roscovan food. Then each mouse under anesthesia from the tail vein took a blood sample and centrifuged. Thus obtained glucose in blood plasma was determined using Glucoloader F (Product of A & T Co., Ltd.).

Reduction of blood glucose was estimated in accordance with the following equation:

< / BR>
The results are summarized in table 156.

Data table 156 shows that the compounds according to this invention have excellent hypoglycemic activity.

Preparative example

(1) Capsules

The compound of example 2 of 10 mg

Lactose - 110 mg

Corn starch - 58 mg

Magnesium stearate 2 mg 180 mg

Powders of all components above were mixed and passes through a sieve of 60 mesh (standard mesh to Tyier). The powder mixture (180 mg) were loaded into gelatin capsules (N 3) to produce capsules.

(2) Tablets

The compound of example 2 of 10 mg

Lactose - 85 mg

Corn starch - 34 mg

Melkokristallicheskie cellulose 20 mg

Magnesium stearate 1 mg to 150 mg

Powders of all components mentioned above are mixed and pressed into the machine to obtain tablets (150 mg). If necessary, the tablets may be coated with sugar or film.
Hydroxypropylcellulose - 1 mg - 1000 mg

Powders of all components above were mixed and moistened with clean water, was grained using a uniform granulator and dried to obtain granules.

Industrial application

Derivatives amidocarbonyl acid, their pharmacologically acceptable salts and their pharmaceutically acceptable esters of the present invention are used as a prophylactic agent and/or therapeutic agent for diabetes, hyperlipemia, obesity, weakened glucose tolerance, glucose tolerance non-IGT (NGT), hypertension, fatty liver, diabetic complications, arteriosclerosis, diabetes, pregnancy, polycystic ovary syndrome and cell damage caused by atherosclerosis, epiphyseal osteomyelitis, rheumatoid arthritis, allergic diseases, asthma, cancer, autoimmune diseases, pancreatitis, osteoporosis, cataracts, things like that. T T T T$

1. Derived amidocarbonyl acid of the formula (I)

< / BR>
where R1represents a hydrogen atom, alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms or aracelio group containing from 7 to 12 atoms of plastics technology: turning & the 6 carbon atoms;

R3represents (i) hydrogen atom, (ii) halogen atom, or (iii) a nitro-group;

R4represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms;

Z represents alkylenes group with a straight or branched chain, containing from 1 to 6 carbon atoms;

W represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) alloctype containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (vi) aralkylated containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 atoms ug is Oh, a straight or branched alkyl group, containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, (x) straight or branched monoalkylamines, in which the alkyl group contains from 1 to 4 carbon atoms, (xi) aralkylamines containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group;

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents defined below, when W represents (i) a straight or branched monoalkylamines, in which the alkyl group contains from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, the content is from 1 to 5 substituents , defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (vi) aralkylated containing from 7 to 12 carbon atoms, which may contain from 1 to 5 substituents defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms, which may contain from 1 to 5 substituents defined below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered heterogroup, containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 mixing the Torah alkyl group contains from 1 to 4 carbon atoms, (ii) arachidonoylethanolamine in which kalkilya group contains from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents defined below, aryl group;

Deputy represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (vi) straight or branched allylthiourea, containing from 1 to 4 carbon atoms, (vii) straight or branched alkylsulfonyl containing from 1 to 4 carbon atoms, (viii) halogen atom, (ix) cyano, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (xi) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents , which may be the same or different, as defined below, (Lenno below, on the aryl group, (xiii) mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents defined below, and (xiv) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom;

Deputy represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group containing from 1 to 4 carbon atoms, (vi) straight or branched aliphatic acyl group containing from 1 to 5 carbon atoms, (vii) halogen atom, (viii) the nitro-group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, and (xi) dialkylaminoalkyl gr is ├╝ the same or different and each contains from 1 to 4 carbon atoms, and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms;

Y represents a single bond, an oxygen atom or a sulfur atom;

or their pharmacologically acceptable salts or their pharmaceutically acceptable esters.

2. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom, alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms, or aracelio group containing from 7 to 9 carbon atoms.

3. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom, alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

4. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom.

5. Derivatives amidocarbonyl acid according to any one of paragraphs.1-4, their pharmacologically acceptable salt or their pharmacologists which contains from 2 to 4 carbon atoms.

6. Derivatives amidocarbonyl acid according to any one of paragraphs.1-4, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R2represents an ethylene group.

7. Derivatives amidocarbonyl acid according to any one of paragraphs.1-6, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R3represents a hydrogen atom.

8. Derivatives amidocarbonyl acid according to any one of paragraphs.1-7, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R4represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

9. Derivatives amidocarbonyl acid according to any one of paragraphs.1-7, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R4represents a hydrogen atom or methyl group.

10. Derivatives amidocarbonyl acid according to any one of paragraphs.1-7, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R4represents a hydrogen atom.

11. Derivatives amidocarbonyl acid according to any one of paragraphs.1-10, their pharmacologically acceptable salts or ICAEW, containing from 1 to 4 carbon atoms.

12. Derivatives amidocarbonyl acid according to any one of paragraphs.1-10, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where Z is a methylene group.

13. Derivatives amidocarbonyl acid according to any one of paragraphs.1-12, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where W represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) alloctype containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 1defined below, aryl group, (vi) aralkylated group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (vii) aryloxyalkyl is stitely1defined below, and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy1represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (vi) straight or branched allylthiourea, containing from 1 to 4 carbon atoms, (vii) straight or branched alkylsulfonyl containing from 1 to 4 carbon atoms, (viii) halogen atom, (ix) cyano, (x) straight or branched dialkylamino carbon (xi) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1that may be the same or different, as defined below, (xii) alloctype containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (xiii) mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents1defined below, and (xiv) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy1represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group containing from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms.

14. Derivatives amidocarbonyl acid according to any one of paragraphs.1-12, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where W represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) aryloxy group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 2defined below, aryl group, (vi) aralkylated containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents2defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2defined below, and the alkyl group is a straight or branched alkyl group containing what eroatoms, selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy2represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (vi) straight or branched allylthiourea, containing from 1 to 4 carbon atoms, (vii) straight or branched alkylsulfonyl containing from 1 to 4 carbon atoms, (viii) halogen atom, (ix) cyano, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (xi) aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2to the of Lerida, which may contain from 1 to 3 substituents2defined below, aryl group, (xiii) mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents2defined below, and (xiv) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy2represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iv) straight or branched hydroxyalkyl group containing from 1 to 4 carbon atoms, (v) halogen atom, (vi) a nitro-group, (vii) formyl group, (viii) carboxyl group, (ix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (x) dialkylaminoalkyl group, in which dieta, which may be the same or different, and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

15. Derivatives amidocarbonyl acid according to any one of paragraphs.1-12, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where W represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) aryloxy group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents 3defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3defined below, aryl group, (vi) aralkylated containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 arestable a straight or branched alkyl group, containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy3represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (v) straight or branched, alkylthio group containing from 1 to 4 carbon atoms, (vi) a straight or branched alkylsulfonyl containing from 1 to 4 carbon atoms, (vii) halogen atom, (viii) cyano, (ix) pyridyloxy group.

16. Derivatives amidocarbonyl acid according to any one of paragraphs.1-12, their pharmacologically acceptable salts or their pharmaceutically acceptable esters of the kind, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) fenoxaprop, which may contain from 1 to 3 substituents4defined below, on the phenyl group; (iv) phenylthiourea, which may contain from 1 to 3 substituents4defined below, on the phenyl group; (v) Uralkaliy group containing 7 to 10 carbon atoms, (vi) aralkylated containing 7 to 10 carbon atoms, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms and the alkyl group is a straight or branched alkyl group containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy4represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl g to 4 carbon atoms, (iv) a straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (v) straight or branched, alkylthio group containing from 1 to 4 carbon atoms, (vi) straight or branched alkylsulfonyl containing from 1 to 4 carbon atoms, (vii) halogen atom, (viii) cyano and (ix) pyridyloxy group.

17. Derivatives amidocarbonyl acid according to any one of paragraphs.1-12, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where W is phenoxy group which may contain one Deputy5defined below, on the phenyl group; Deputy5represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iv) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (v) straight or branched allylthiourea containing from 1 to 4 carbon atoms, (vi) straight or branched alkylsulfonyl, soderjatsya amidocarbonyl acid according to any one of paragraphs.1-12, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where W represents fenoxaprop, which may contain one Deputy6defined below, on the phenyl group; Deputy6represents a group selected from methyl, ethyl, ISO-propyl, tert-butilkoi, triptorelin, metaxylene and triptoreline groups, and fluorine atom and chlorine atom.

19. Derivatives amidocarbonyl acid according to any one of paragraphs.1-18, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where X is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents7defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents7defined below, Deputy7represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing OTE from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (vi) straight or branched allylthiourea containing from 1 to 4 carbon atoms, (vii) straight or branched alkylsulfonyl group containing from 1 to 4 carbon atoms, (viii) halogen atom, (ix) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (x) phenyl group, which may contain from 1 to 3 substituents3defined below, (xi) fenoxaprop, which may contain from 1 to 3 substituents 3defined below, (xii) pyridyloxy group, which may contain from 1 to 3 substituents3defined below, and (xiii) mono - or decillions, 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy 3represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxy who or branched hydroxyalkyl group, containing from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, and (xi) dialkylaminoalkyl group, in which dialkylamino includes two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

20. Derivatives amidocarbonyl acid according to any one of paragraphs.1-18, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where X is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents8defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents8defined below, Deputy 8represents Gruppman carbon (ii) a straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (vi) straight or branched allylthiourea containing from 1 to 4 carbon atoms, (vii) halogen atom, (viii) straight or branched dialkylamino, in which each alkyl group may be the same or different, and each contains from 1 to 4 carbon atoms, (ix) phenyl group, which may contain from 1 to 3 substituents4defined below, (x) fenoxaprop, which may contain from 1 to 3 substituents4defined below, (xi) pyridyloxy group, which may contain from 1 to 3 substituents4defined below, and (xii) mono - or decillions, 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy4represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms is a hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group containing from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, and (xi) dialkylaminoalkyl group, in which dialkylamino includes two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

21. Derivatives amidocarbonyl acid according to any one of paragraphs.1-18, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where X is an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents9defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, is UP>9
represents a group selected from the group including (i) hydroxyl group, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) straight or branched halogenated alkoxygroup containing from 1 to 4 carbon atoms, (iv) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (v) phenyl group, which may contain from 1 to 3 substituents5defined below, (vi) fenoxaprop, which may contain from 1 to 3 substituents 5defined below, (vii) pyridyloxy group, which may contain from 1 to 3 substituents5defined below and (viii) mono - or decillions, 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy 5represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv)percent hydroxyalkyl group, containing from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, and (xi) dialkylaminoalkyl group

in which dialkylamino includes two straight or branched alkyl group comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

22. Derivatives amidocarbonyl acid according to any one of paragraphs.1-18, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where X represents a phenyl, indolenine, pyridyloxy or pinolillo group, which may contain from 1 to 3 substituents 11defined below, Deputy11represents a group selected from the group including (i) hydroxyl group, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) straight or branched halogenated alkoxygroup containing 1 to be the same or different, and each contains from 1 to 4 carbon atoms, (v) phenyl group, which may contain from 1 to 3 substituents7defined below, (vi) fenoxaprop, which may contain from 1 to 3 substituents7defined below, (vii) pyridyloxy group, which may contain from 1 to 3 substituents7defined below and (viii) mono - or decillions, 5-10-membered saturated heterocyclic group containing 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy7represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched hydroxyalkyl group containing from 1 to 4 carbon atoms, (vi) halogen atom, (vii) a nitro-group, (viii) formyl group, (ix) carboxyl group, (x) straight or branched dialkylamino, in which each alkyl group may be the same or different, and each contains the or branched alkyl group, comprising from 1 to 4 carbon atoms, which may be the same or different, and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms.

23. Derivatives amidocarbonyl acid according to any one of paragraphs.1-18, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where X represents a phenyl group which may contain one Deputy12defined below, Deputy12represents a group selected from the group comprising methyl group, ISO-propyl and hydroxyl group, a fluorine atom, a chlorine atom and group diethylamino, phenyl group (the phenyl group may be substituted by 1-3 substituents, which may be the same or different, selected from the group comprising methyl, ethyl, triptorelin, hydroxyl, methoxy, ethoxy, isopropoxy, triptoreline, methylendioxy and hydroxymethylene group, a fluorine atom, a chlorine atom and a nitro, formyl, cyano, carboxyl, dimethylamino, diethylamino and N,N-dimethylaminomethylene group), phenoxy and pyridyloxy group (Peregrina group may be substituted by methyl, ethyl, triptorelin, methoxy, atopy), and piperidino group; or X represents pyridyloxy group which may have one Deputy13defined below, Deputy13represents a group selected from the group comprising methyl, ISO-propyl, methoxy, ethoxy, isopropoxy, 2,2,3,3-tetrafluoropropoxy, allylthiourea containing one or two carbon atoms, alkylsulfonyl group containing one or two carbon atoms, phenyl group (the phenyl group may be substituted by methyl, ethyl, triptorelin, methoxy, ethoxy or isopropoxy, a fluorine atom, a chlorine atom or a nitro-group, dimethylaminopropoxy or diethylaminopropyl) and fenoxaprop.

24. Derivatives amidocarbonyl acid according to any one of paragraphs.1-18, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where X represents biphenylyl group (each phenyl group may be substituted by one Deputy, who may be the same or different, selected from the group comprising methyl, triptorelin, hydroxyl, methoxy and hydroxymethylene group, a fluorine atom, a chlorine atom and formyl, carboxyl, nitro, dimethylamino, and N,N-dimethylaminomethylene group), the feast is the fact that methyl, ethyl, triptorelin, hydroxyl, methoxy, ethoxy, isopropoxy and cryptometer, fluorine atom, chlorine atoms and nitro, dimethylamino and diethylaminopropyl) or phenylpyridine group (the phenyl group may be substituted by one Deputy, selected from the group comprising methyl, ethyl, triptorelin, methoxy, ethoxy and isopropoxy, a fluorine atom, a chlorine atom and a nitro and dimethylamino group).

25. Derivatives amidocarbonyl acid according to any one of paragraphs.1-24, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where Y represents a single bond or an oxygen atom.

26. Derivatives amidocarbonyl acid according to any one of paragraphs.1-24, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where Y represents an oxygen atom.

27. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms; R2represents alkylenes group with a straight or branched chain, containing from 2 to 4 atomboy a hydrogen atom or alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms; Z represents alkylenes group with a straight or branched chain, containing from 1 to 4 carbon atoms; W represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) alloctype containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents 1defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (vi) aralkylated group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents1defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms which may have from 1 to 3 substituents1and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 atombender from the group including an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy1such, as defined in paragraph 13;

X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents7defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents7defined below; Deputy7such, as defined in paragraph 19; and Y represents a single bond or an oxygen atom.

28. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1-4 carbon atoms; R2represents alkylenes group with a straight or branched chain, containing from 2 to 4 carbon atoms;3represents a hydrogen atom, atom run by the chain, containing from 1 to 4 carbon atoms; Z represents a methylene group; W represents (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) aryloxy group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents2defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 2defined below, aryl group, (vi) aralkylated containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents2defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms which may have from 1 to 3 substituents 2and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroaromatics is whether (ix) mono - or decillions, 5-10-membered heterogroup containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom; Deputy2such, as defined in paragraph 14; X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents8defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents8defined below; Deputy 8such, as defined in paragraph 20; and Y represents an oxygen atom.

29. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms; R2represents alkylenes group with a straight or branched chain, containing from 2-4 carbon atoms; R3represents a hydrogen atom, a halogen atom or a nitro-group; R4represents a hydrogen atom or alkyl group with straight or robbery (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (iii) aryloxy group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3defined below, aryl group, (iv) killigrew containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents3defined below, aryl group, (v) Uralkaliy group containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents 3defined below, aryl group, (vi) aralkylated containing from 7 to 12 carbon atoms, which may contain from 1 to 3 substituents3defined below, aryl group, (vii) aryloxyalkyl the group in which the aryl group contains from 6 to 10 carbon atoms which may have from 1 to 3 substituents 3and the alkyl group is an alkyl group with straight or branched chain, containing from 1 to 4 carbon atoms, (viii) mono - or decillions, 5-10-membered heteroepitaxy containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, a nitrogen atom and a sulfur atom, or (ix) mono - or decillions, 5-10-membered Gotha and a sulfur atom; Deputy3such, as defined in paragraph 15; X represents an aryl group containing from 6 to 10 carbon atoms, which may contain from 1 to 3 substituents9defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group comprising an oxygen atom, nitrogen atom and sulfur atom, which may contain from 1 to 3 substituents9defined below; Deputy 9such, as defined in paragraph 21; and Y represents an oxygen atom.

30. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom; R2represents an ethylene group; R3represents a hydrogen atom; R4represents a hydrogen atom; Z represents a methylene group; W represents fenoxaprop, which may contain one Deputy5defined below, on the phenyl group, Deputy 5such, as defined in paragraph 17; X represents a phenyl group which may have one Deputy12defined below, Deputy12such as defined in point is who, Deputy13such, as defined in paragraph 23; and Y represents an oxygen atom.

31. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom; R2represents an ethylene group; R3represents a hydrogen atom; R4represents a hydrogen atom; Z represents a methylene group; W represents fenoxaprop, which may contain one Deputy 6defined below, on the phenyl group, Deputy6such, as defined in paragraph (18; X represents biphenylyl group (the substituents on each phenyl group may be the same or different and each is selected from the group comprising methyl, triptorelin, hydroxyl, methoxy and hydroxymethylene group, a fluorine atom, a chlorine atom or formyl, carboxyl, nitro, dimethylamino, and N,N-dimethylaminomethylene group), pyridylamino group (Peregrina group may be substituted by one Deputy, selected from the group comprising methyl, ethyl, triptorelin, methoxy, ethoxy, isopropoxy and cryptometer, a fluorine atom, atom chlena one Deputy, selected from methyl, ethyl, triptorelin, methoxy, ethoxy and isopropoxy, fluorine atom, chlorine atom, nitro and dimethylamino group); and Y represents an oxygen atom.

32. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts or their pharmaceutically acceptable esters, where R1represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1-6 carbon atoms; R2represents alkylenes group with a straight or branched chain, containing from 1-6 carbon atoms; R3represents (i) hydrogen atom, (ii) halogen atom, or (iii) a nitro-group; R4represents a hydrogen atom or alkyl group with straight or branched chain, containing from 1-6 carbon atoms; Z represents alkylenes group with a straight or branched chain, containing from 1 to 4 carbon atoms; W represents ethyl, through boutelou, pentelow, methoxy, ethoxy, propoxy, isopropoxy, methylthio, ethylthio, propylthio, isopropylthio, phenoxy, 4-methylphenoxy, 4-ethylenoxy, 4-isopropylphenoxy, 4-methoxyphenoxy, 4-chlorophenoxy, phenylthio, benzyl, fenetylline, 3-phenylpropyl or 4-phenylbutyl 1 to 3 substituents , defined below, or mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms selected from the group containing oxygen atom, nitrogen atom and sulfur atom, which may include 1 to 3 substituents defined below, Deputy represents a group selected from the group comprising (i) an alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, (ii) straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, (iii) hydroxyl group, (iv) alkoxygroup straight or branched chain, containing from 1 to 4 carbon atoms, (v) straight or branched allylthiourea containing from 1 to 4 carbon atoms, (vi) straight or branched alkylsulfonyl containing from 1 to 4 carbon atoms, (vii) halogen atom, (viii) straight or branched dialkylamino, in which each alkyl group may be the same or different and each contains from 1 to 4 carbon atoms, (ix) aryl group, containing from 6 to 10 carbon atoms (the aryl group may be substituted by straight or branched alkyl group with straight or branched chain, containing from 1 to 6 carbon atoms, straight or rasvet the branched chain, containing from 1 to 4 carbon atoms), (x) alloctype containing from 6 to 10 carbon atoms (the aryl group may be substituted by straight or branched alkyl group containing from 1 to 6 carbon atoms, straight or branched halogenated alkyl group containing from 1 to 4 carbon atoms, straight or branched alkoxygroup containing from 1 to 4 carbon atoms or a halogen atom), and (xi) a mono - or decillions, 5-10-membered heteroaryl group containing from 1 to 4 heteroatoms, selected from the group containing an oxygen atom, nitrogen atom and sulfur atom; and Y represents a single bond, an oxygen atom or a sulfur atom.

33. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts and their pharmaceutically acceptable esters, selected from the following group of compounds:

2 ethoxy-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] -2-propylphosphonate acid,

2-butyl-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] -phenyl] propionic acid,

3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-butyl-propionic acid,

2-butyl-3-[4-[2-(4'-formylphenyl-4-carbylamine)ethoxy] f the OIC acid,

2-butyl-3-[4-[2-(4'-carboxyphenyl-4-carbylamine)ethoxy]phenyl]propionic acid,

2-butyl-3-[4-[2-(3'-methoxybiphenyl-4-carbylamine)ethoxy] phenyl]propionic acid,

2-butyl-3-[4-[2-(3'-hydroxybiphenyl-4-carbylamine)ethoxy]phenyl]propionic acid,

2-butyl-3-[4-[2-(2'-methoxybiphenyl-4-carbylamine)ethoxy] phenyl]propionic acid,

2-butyl-3-[4-[2-(4'-hydroxy-3,5-dimethylbiphenyl-4-carbylamine)ethoxy] phenyl]propionic acid,

2-butyl-3-[4-[2-(2-methoxypyridine-5-carbylamine)ethoxy] phenyl] propionic acid,

2-butyl-3-[4-[2-(4-diethylaminobenzylidene)ethoxy]phenyl]propionic acid,

2-butyl-3-[4-[3-(4-pyridyl-2-albenzaalbenza)propoxy] phenyl] propionic acid,

2 phenoxy-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

3-[4-[2-(biphenyl-4-carbylamine)ethoxy]phenyl]-2-phenoxypropionic acid,

3-[4-[2-(4'-forbiden-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid,

3-[4-[2-(4'-chlorobiphenyl-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid,

3-[4-[2-(4'-triptorelin-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl] propionic, coprophiliacs)-3-[4-[2-(2-phenylpyridine-5-carbylamine)ethoxy] phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)-pyridine-5-carbylamine]ethoxy]phenyl]propionic acid,

3-[4-[2-[2-(4-forfinal)pyridine-5-carbylamine] ethoxy]phenyl]-2-(4-isopropylphenoxy)propionic acid,

3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl]-2-(4-isopropylphenoxy)propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-triptorelin-6-yl)benzoylamine]ethoxy]phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-nitropyridine-6-yl)benzoylamine] ethoxy]phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-methoxypyridine-6-yl)benzoylamine] ethoxy]phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-dimethylaminopyridine-6-yl)benzoylamine]ethoxy]phenyl]propionic acid,

2-(4-methoxyphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(3-phenylpropyl)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-methylphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-tert-butylphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl]propionic acid,

2-(4-pertenece)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,
enocsi)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl]propionic acid,

2-(4-triftormetilfosfinov)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl]propionic acid,

2-(3-pertenece)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(3,5-divergence)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(3,4-divergence)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(3,4,5-tryptophanate)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl]propionic acid,

2-(2,3,4,5,6-Pantothenate)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl]propionic acid,

2-methyl-2-phenoxy-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-isopropylphenoxy)-2-methyl-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)-pyridine-5-carbylamine]ethoxy]phenyl]-2-methylpropionate acid and

3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl]-2-(4-isopropylphenoxy)-2-methylpropionate acid.

34. Derivatives amidocarbonyl acid on p. 1, their pharmacologically acceptable salts and their pharmaceutically acceptable esters, selected from the following group of compounds:

2 ethoxy-3-[4-[2-(4-pyridyl-2-Alben the IP acid,

2-butyl-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-butyl-3-[4-[2-(4'-formylphenyl-4-carbylamine)ethoxy] phenyl] propionic acid,

2-butyl-3-[4-[2-(4'-hydroxy-3,5-dimethylbiphenyl-4-carbylamine)ethoxy] phenyl]propionic acid,

2 phenoxy-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-phenoxy-propionic acid,

3-[4-[2-(4'-forbiden-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid,

3-[4-[2-(4'-chlorobiphenyl-4-carbylamine)ethoxy] phenyl] -2-phenoxypropionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl] propionic acid,

3-[4-[2-(biphenyl-4-carbylamine)ethoxy] phenyl] -2-(4-isopropylphenoxy)propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-(2-phenylpyridine-5-carbylamine)ethoxy] phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)-pyridine-5-carbylamine]ethoxy]phenyl]propionic acid,

3-[4-[2-[2-(4-forfinal)pyridine-5-carbylamine] ethoxy]phenyl]-2-(4-isopropylphenoxy)propionic acid,

3-[4-[2-[2-(2,2,3,3-tetrafluoropropoxy)pyridine-5-carbylamine] ethoxy] phenyl]-2-(4-isopropylphenoxy)propionic keys is>/BR>2-(4-isopropylphenoxy)-3-[4-[2-[4-(3-dimethylaminopyridine-6-yl)benzoylamine]ethoxy]phenyl]propionic acid,

2-(4-methoxyphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-methylphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-tert-butylphenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl]propionic acid,

2-(4-pertenece)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-chlorophenoxy)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-triptoreline)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl]propionic acid,

2-(4-triftormetilfosfinov)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl]propionic acid,

2-(3-pertenece)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(3,4,5-tryptophanate)-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl]propionic acid,

2-methyl-2-phenoxy-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy] phenyl] propionic acid,

2-(4-isopropylphenoxy)-2-methyl-3-[4-[2-(4-pyridyl-2-albenzaalbenza)ethoxy]phenyl]propionic acid,

2-(4-isopropylphenoxy)-3-[4-[2-[2-(4-methoxyphenyl)-pyridine-5-carbylamine]etock]-2-(4-isopropylphenoxy)-2-methylpropionate acid.

35. Derived amidocarbonyl acid, its pharmacologically acceptable salt and a pharmacologically acceptable ester according to any one of paragraphs.1-34 as an active ingredient of medicines intended to reduce the level of glucose in the blood.

36. Pharmaceutical composition having hypoglycemic activity, characterized in that it contains as active ingredient amidocarbonyl acid, its pharmacologically acceptable salt and a pharmacologically acceptable ester specified in paras.1-34.

37. The pharmaceutical composition according to p. 36 for reducing blood glucose level.

38. A way of reducing glucose levels in the blood of warm-blooded animals which consists in the introduction of the specified warm-blooded animal a pharmacologically effective amount of the active ingredient, where the specified ingredient is a derivative of amidocarbonyl acid, its pharmaceutically acceptable salts or its pharmaceutically acceptable ester, specified in clauses.1-34.

 

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