A derivative of benzene

 

(57) Abstract:

Usage: in medicine as a drug. The inventive product is a derivative of benzene of formula I: wherein R1is a hydrogen atom, a lower alkyl or a group of the formula: -N(R7, R8), R2group of the formula: -N(R14)-C(=0)-N(R15,R16), R3group of the formula-O-(CH2)m-Y, where m is an integer of 1-6. Reagent 1: compound of the formula: . Reagent 2: compound of the formula: A= C(R1)-C(R2)=C(NN)(CH2)mY. 1 C. and 13 C.p. f-crystals, 1 Il., table 2.

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1. A derivative of benzene, the General formula

< / BR>
gdgt be the same or different, and where each of these groups is a hydrogen atom or lower alkyl;

R2the group described by formula

< / BR>
where R14R16may be the same or different and each may represent a hydrogen atom, lower alkyl or lower alkenylphenol group;

R3the group described by formula

-O-(CH2)m-Y

where m is an integer of 1-6;

Y 5-membered aromatic heterocyclic ring containing 1-4 nitrogen atom which may be substituted by a lower alkyl group, a phenyl, unsubstituted or substituted lower alkoxygroup, a lower alkyl group, CH2OH, nitrogroup, sulfopropyl, substituted lower alkyl, amino group, substituted sulfonylurea alkyl group, halogen, lower alkyl or lower alkenyl, replaced by carboxypropyl, naphthyl, substituted lower alkyl amino group, CH2SCH3CH2N(CH3)2, COOH, CONH2or condensed benzene c or benzocycloheptene ring; or Y 6-membered saturated heterocyclic ring containing 1-3 nitrogen atom which may be substituted by unsubstituted or substituted with halogen-phenyl;

And a group of the formula-CH=

In group-CH=

R5a hydrogen atom or a lower alkyl group.

2. Preprogram the group, described by the formula-NR7R8where R7and R8may be the same or different and each represents a hydrogen atom or lower alkyl;

R16a hydrogen atom, lower alkyl or lower alkenyl;

Y 5-membered aromatic heterocyclic ring containing 1-4 nitrogen atom which may be substituted by a lower alkyl group, a phenyl, unsubstituted or substituted lower alkoxygroup, a lower alkyl group, CH2OH, nitrogroup, sulfopropyl, substituted lower alkyl, amino group, substituted sulfonyl-lower alkyl group, halogen, lower alkyl or lower alkenyl, replaced by carboxypropyl, naphthyl, substituted lower alkyl, amino group, CH2SCH3CH2N(CH3)2, COOH, CONH2or fused with benzene or benzocycloheptene ring, or Y represents 6-membered saturated heterocyclic ring containing 1-3 nitrogen atom which may be substituted by unsubstituted or substituted with halogen by phenyl.

3. Connection on p. 2, wherein Ramethyl group.

4. Connection on p. 2, wherein Ra- dimethylaminopropan.

5. A connection is an Association under item 2, wherein R16an alkyl group containing 2-4 carbon atoms.

7. Connection on p. 2, wherein Y is a group of imidazolyl, which may be substituted.

8. Connection on p. 2, wherein Y is a group of imidazolyl, possibly substituted lower alkyl group, halogen atom or phenyl group.

9. Connection on p. 2, characterized in that Y duhsasana imidazolidine group, the substituents of which are selected from the group comprising lower alkyl groups containing 1-6 carbon atoms, halogen atoms and phenyl group.

10. Connection on p. 2, wherein Ramethyl, R16an alkyl group containing 1-6 carbon atoms, m is an integer from 1 to 6, and Y imidazole group, possibly bearing the substituent(s).

11. Connection on p. 2, wherein Ramethyl, R16an alkyl group containing 2-4 carbon atoms, m is an integer from 1 to 6, Y imidazolidinyl group which may bear one or more substituents selected from the group lower alkyl group containing 1-6 carbon atoms, halogen atom, and a phenyl group.

12. Connection on p. 2, characterized in that Y pipere a N-[2-{ 3-(5- ethyl-4-phenyl-1H-imidazol-1-yl)propoxy}-6-methyl-]fenilatilamina and having the formula

< / BR>
14. Connection on p. 2, selected from the group of N-[6-N,N-dimethylamino-2{3-(4-phenyl-1H-imidazol-1-yl)-propoxy} phenyl-N'-pencilmation

< / BR>
N-[6-N, N-dimethylamino-2-{ 3-(4-phenyl-1H-imidazol-1-yl)- propoxy}phenyl-N'-mutilation

< / BR>
N-[6-N, N-dimethylamino-2-{ 3/-(5-methyl-4-phenyl-1H-imidazol-1-yl)-propoxy}phenyl-N'-mutilation:

< / BR>
N-[6-N, N-dimethylamino-2-{ 3-(4-phenyl-1-imidazol-1-yl)-propoxy} phenyl-N'-mutilation

N-6[-{ 4- (4-phenyl-1H-imidazol-1-yl)butyl} -2-N,N-dimethylamino]-phenyl-N'-mutilation

< / BR>
N-[6-N, N-dimethylamino-2-{3-(4-phenylpiperazin-1-yl)propoxy}- phenyl-N'-pencilmation

< / BR>
N-[6-methyl-2-[3-{ -(1-methylethyl)-4-phenyl-1H-imidazol-1-yl)-propoxy} phenyl-N'-mutilation:

< / BR>
N-[6-methyl-2-{ 3-(5-chloro-4-phenyl-1H-imidazol-1-yl)propoxy}- phenyl-N'-pencilmation

< / BR>
N-[-6-methyl-2-{ 3-(5-methyl-4-phenyl-1H-imidazol-1-yl)propoxy}-phenyl-N'- pencilmation

< / BR>
N-[-6-(ethyl-2-{ 3-(5-methyl-4-phenyl-1H-imidazol-1-yl)propoxy}-phenyl-N'- pencilmation



 

Same patents:

The invention relates to chemical compounds with valuable properties, in particular derivatives of 2,3-dihydropyrano[2,3-b] pyridine of General formula

< / BR>
(I) where a lower alkylene;

R is a hydrogen atom or a group

A< / BR>
or their salts

The invention relates to novel condensed heterocyclic compounds or their salts, and their intermediate compounds, method of their production and the fungicide on their basis for the processing of agricultural and horticultural crops

The invention relates to new pyridine containing heterocyclic compounds, in particular new 1,3-dioxane-5-silt derived alkenovich acids containing pyridyloxy residue attached to position 4 of the 1,3-dioxane ring

The invention relates to new derivatives of glycerol General formula

where k=1 or 0;

Lower alkyl or arylalkyl;

R1acetyl, 2-alkoxybenzyl or aryl;

n=0 or an integer from 1 to 3;

The group G formula< / BR>
orX-

A is selected from groups of formula:

(1) -NH-(CH2)where R2, R3and R4lowest alkoxygroup;

(2) -NH-(CH2)SO2-NH-R5where R5hydrogen, alkyl, or CHp=1 or 2;

(3) -NX-R6where the X group is-CH - or a nitrogen atom; R6group-СОR7where R7alkyl or alkoxy, or a group-0-C0-NH-R8where R8alkyl;

(4) -NH< / BR>
(5) -NH-(CH2)3-OR10where R10alkyl;

(6) -NH-(CH2)10-NH-CO-NR11R12where R11and R12lower alkyl;

(7) -NH-CHNO

(9) -NH-(CH2)5-0-(CH2)5-0-(CH2)5-H

(10) -NH-(CH2)3-0-CO-NH-R14where R14alkyl;

(11) -NH-CH< / BR>
(12)CHwhere m=0 or from 1 to 6; R9, R15and R16the same or different and represent hydrogen or alkoxygroup, provided that when k=0, group a sure formula

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of bis-(4-alkylaminopiridinium-1)alkanes of formula (1) where X stands for lipophilic anion from the following group: triiodide I3, iodate IO3, perchlorate ClO4; Y stands for either linear or branched alkylene group, which contains 4 to 18 carbon atoms; R stands for either linear or branched alkyl, cycloalkyl or arylalkyl group, which contains 5 to 18 carbon atoms, to methods of preparation thereof and application thereof as antibacterial and antiviral substances.

EFFECT: new substances show useful biological properties.

10 cl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to production of bis(4-alkylaminopyridine-1) alkanes of formula I where R1 -s linear or branched alkyl, cycloalkyl or arylalkyl groups having from 4 to 18 carbons, preferably from 8 to 12 carbons, ideally - normal octyl, R2 - linear or branched alkylene groups having from 4 to 18 carbons, preferably from 8 to 14 carbons, ideally - 1,10 decandyl, X1, X2 - halogenanions (identical or diverse): fluoride-, chloride-, bromide-, iodideanions, ideally - chlorideanions through interreacting of 4-alkylaminopyridine of formula II with disubstituted alkylene of formula III X1-R2-X2 in a solvent at increased temperature with mole ratio of formula II compound to formula III compound equals 2:1, the process is carried out in anoxic environment, acetic acid or its mixture with water is used as a solvent, meanwhile the compound of formula II is treated with the compound of formula III in gradual and continuous way or portionwise, ensuring the reaction at temperature ranging from 90° to 130°C, ideally from 100 to 105°C.

EFFECT: preparation of bis(4-alkylaminopyridine-1) alkanes of high quality with higher yield at essential saving of expandable materials.

6 cl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing HIV protease inhibitor atazanavir sulphate in form of Form A crystals, which involves reacting a solution of a free base of atazanavir in an organic solvent in which atazanavir sulphate is virtually insoluble, at temperature ranging from 35°C to 55°C with a first portion of concentrated sulphuric acid in an amount sufficient for reaction with less than approximately 15 wt % free base of atazanavir, addition of nucleating centres of Form A atazanavir sulphate crystals, addition of an additional amount of concentrated sulphuric acid in several steps, where the acid is added at increasing rate to form atazanavir sulphate crystals and drying the atazanavir sulphate to form Form A crystals. A method of producing atazanavir sulphate in form of Form C crystals is also proposed.

EFFECT: improved method.

20 cl, 11 dwg, 6 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I , where R2 is selected from a group consisting of (1) phenyl, which is substituted with R2a, R2b and R2c, (2) furanyl, (3) C3-6 cycloalkyl; R2a, R2b and R2c are independently selected from a group consisting of (1) hydrogen, (2) halogen, (3) C1-6 alkyl, which is unsubstituted or substituted with (a) 1-6 halogen atoms, (4) -NR10R11, where R10 and R11 are hydrogen; R3 is C1-6 alkyl or C3-6 cycloalkyl, which is independently unsubstituted or substituted with 1-6 halogen atoms; R4 and R5 are hydrogen and m equals zero, R2 is directly bonded to a carbonyl; and to pharmaceutically acceptable salts thereof. The invention also pertains to compounds which are selected from the group, as well as a pharmaceutical composition.

EFFECT: obtaining novel biologically active compounds which are active as glycine transporter GlyT1 inhibitors.

10 cl, 14 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to 2,6-diazido-3,5-dicyanopyridine of formula (I), as well as synthesis method thereof, which involves reaction of a chloro-substituted derivative of 3,5-dicyanopyridine with an azidation agent in the medium of aqueous acetone, followed by extraction of the end product.

EFFECT: novel compound which can be used in synthesis of high-energy compounds is obtained and described.

2 cl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing N-methyl-4-benzylcarbamidopyridinium iodide (MBI), which is used as substance in medicinal agents, involving reaction of isonicotinic acid with benzylamine at temperature 160-185°C and molar ratio 1.0:1.2 and alkylation of the obtained benzylamide of isonicotinic acid with methyl iodide at 40-50°C and molar ratio 1.0:1.2.

EFFECT: high output of the end product and low solvent consumption.

2 cl, 2 tbl, 10 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In formula (I): X denotes a single bond or a binding group selected from -CO, -SO2-, -CS- or -CH2-; Y denotes a single bond or a divalent binding group obtained from a cyclic structure selected from benzene, pyridine, pyrimidine, pyrazole, imidazole, thiazole, thiophene, quinoline, benzoimidazole, benzothiazole, benzopyrazole, naphthalene and benzothiophene; X and Y are simultaneously single bonds; Z denotes a hydrogen atom or a substitute selected from a group A; m equals 1 or 2; n equals 0-3; in group A and group B, R, R' and R" can, respectively and independently, be identical or different and denote a hydrogen atom or -C1-6-alkyl; said -C1-6-alkyl can be substituted with a group selected from -OH, -O(C1-6-alkyl),-CONH2, -CONH(C1-6-alkyl), -CON(C1-6-alkyl)2, -NH2, -NH(C1-6-alkyl) and -N(C1-6-alkyl)2); Sus denotes a C3-C7 saturated or a C5-C10 unsaturated hydrocarbon ring or a nitrogen-containing C3-C7 heterocyclic ring containing 1-4 nitrogen atoms or containing an additional O, S atom; said C1-6 alkylene in groups A and B can be substituted in positions 1-3 with a -N(C1-6- alkyl)2 group, values of radicals R1, A1, T, B and Q are given in the claim. The invention also relates to a pharmaceutical composition containing said compounds, a PI3K inhibitor and a medicinal agent having PI3K inhibitor properties against a proliferative diseases such as a malignant tumour.

EFFECT: high efficiency of using the compounds.

21 cl, 645 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula (I), including any stereochemical isomer forms thereof, or a pharmaceutically acceptable salt thereof, , wherein A is phenyl or 6-member aromatic heterocycle containing 1 or 2 nitrogen atom; wherein said phenyl or 6-member aromatic heterocycle may be optionally condensed with phenyl; Z is CH2 or O; R1 is halogen, hydroxyl, C1-4alkyl, C1-4alkyloxy, or provided A is phenyl, then two neighbour substitutes R1 may be taken together to produce a radical of formula: -O-CH2-O- (a-1) or -O-CH2-CH2-O- (a-2); R2 is hydrogen or C1-4alkyl; each R3 and R4 independently is hydrogen, C1-6alkyl, C1-4alklyloxyC1-6alkyl or phenylC1-4alkyl; or R3 and R4 taken together with a nitrogen atom whereto attached form a radical of formula or , wherein X1 is CH2 or CHOH; and X2 is CH2, O or NR6; R5 is hydrogen, halogen, C1-4alkyl or C1-4alkyloxy; R6 is hydrogen, C1-4alkyl, C1-4alkylcarbonyl; n is equal to an integer 0, 1 or 2; provided the compound is other than , or a pharmaceutically acceptable salt thereof.

EFFECT: compounds are used to treat the diseases the treatment of which is affected, mediated or promoted by GHSlA-r receptor activation The present invention also refers to pharmaceutical compositions and an intermediate compound of formula II: .

22 cl, 10 tbl, 11 ex

FIELD: chemistry.

SUBSTANCE: invention relates to method of preparative obtaining 5-methoxypyridine amine-2, which is realised by substitution of bromine in 5-bromopyridine amine-2 by means of sodium methoxide under conditions of microwave initiation, with reaction proceeding in methanol with catalysis by microdisperse powder of copper (I) oxide at 120-150°C for 3-4 h.

EFFECT: elaboration of method of preparating obtaining 5-methoxypyridine amine-2 preparative obtaining.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 3,4,5-triazidopyridine-2,6-dicarbonitrile of formula (I) and the method of its production. 3,4,5- triazidopyridine-2,6-dicarbonitrile of formula (I) was produced by azidation of 3,4,5-trichloropyridine-2,6-dicarbonitrile with sodium azide in aqueous acetone.

EFFECT: invention can be used to produce new energy-intensive materials.

2 cl, 3 ex

FIELD: pharmaceutical industry, medicine.

SUBSTANCE: invention relates to compounds of formula I , wherein A, L, Y, and k are as defined in specification. Compounds of formula I have value pharmacological activity, in particular potent antithrombosis action and are useful in treatment and prophylaxis of cardiovascular diseases such as thromboembolia. They represent also reversible inhibitors of factor X and factor VIIa (blood coagulation enzymes). Also disclosed are methods for production of compounds I, uses thereof, in particular as active ingredients in pharmaceutical compositions, as well as medicines containing the same.

EFFECT: new pharmaceutical compositions for treatment and prophylaxis of cardiovascular diseases.

10 cl, 50 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of carboxylic acids of the formula: wherein Y is taken independently in each case among the group comprising C(O), N, CR1, C(R2)(R3), NR5, CH; q means a whole number from 3 to 10; A is taken among the group comprising NR6; E is taken among the group comprising NR7; J is taken among the group comprising O; T is taken among the group comprising (CH2)b wherein b = 0; M is taken among the group comprising C(R9)(R10), (CH2)u wherein u means a whole number from 0 to 3; L is taken among the group comprising NR11 and (CH2)n wherein n means 0; X is taken among the group comprising CO2H, tetrazolyl; W is taken among the group comprising C, CR15 and N; R1, R2, R3 and R15 are taken independently among th group comprising hydrogen atom, halogen atom, hydroxyl, alkyl, alkoxy-group, -CF3, amino-group, -NHC(O)N(C1-C3-alkyl)-C(O)NH-(C1-C3-alkyl), -NHC(O)NH-(C1-C6-alkyl), alkylamino-, alkoxyalkoxy-group, aryl, aryloxy-, arylamino-group, heterocyclyl, heterocyclylalkyl, heterocyclylamino-group wherein heteroatom is taken among N atom or O atom, -NHSO2-(C1-C3-alkyl), aryloxyalkyl; R4 is taken among the group comprising hydrogen atom, aryl, aralkyl, benzofuranyl, dihydrobenzofuranyl, dihydroindenyl, alkyl, benzodioxolyl, dihydrobenzodioxynyl, furyl, naphthyl, quinolinyl, isoquinolinyl, pyridinyl, indolyl, thienyl, biphenyl, 2-oxo-2,3-dihydro-1H-benzimidazolyl, pyrimidinyl and carbazolyl. Other values of radicals are given in the claimed invention. Also, invention relates to pharmaceutical composition used for inhibition binding α4β1-integrin in mammal based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof in aims for treatment or prophylaxis of diseases associated with α4β1-integrin.

EFFECT: improved method for inhibition, valuable medicinal properties of compounds.

33 cl, 7 tbl, 42 ex

FIELD: chemistry of organosilicon compounds, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds and their using in therapy. Invention describes compounds of the formula (I): wherein alternate values are given in the invention claim. These substances are claimed as compounds possessing antagonistic activity with respect to GnRH, and pharmaceutical composition comprising these compounds.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

28 cl, 3 ex

FIELD: chemistry of organosilicon compounds, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds and their using in therapy. Invention describes compounds of the formula (I): wherein radical are given in the invention claim. These substances are claimed as compounds possessing antagonistic activity with respect to GnRH, and pharmaceutical composition comprising these compounds.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

18 cl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: this invention relates to new compounds with formula (I) possessing the properties of mGLuR2 antagonists, to their obtainment methods, their application for production of medicines for prevention and treatment of disorders wherein mGLuR2 plays the activation role (in particular - central nervous system disorders). In formula (I) either any of X and Y represents N while the other represents CH or each of X and Y represents N; A represents aryl representing phenyl or 5- or 6-membered heteroaryl containing in the cycle 1-3 atoms selected from among nitrogen, oxygen or sulphur, the heteroaryl selected from among amidazolyl, [1,2,4] oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4] triazolyl, tiazolyl and pyrimidinyl, each of them substitutable by C1-6-alkyl; B represents H, cyano or represents a possibly substituted aryl selected from among phenyl or possibly substituted by 5- or 6-membered heteroaryl containing in the cycle 1-3 atoms selected from among nitrogen, oxygen or sulphur where the substitutes are selected from the group consisting of nitro, C1-6-alkyl, possibly substituted hydroxy, NRaRb where Ra and Rb independently represent H, C1-6-alkyl etc. R1 represents H, a halogen atom, C1-6-alkyl, possibly substituted hydroxy, C1-6-alcoxy, C1-6-halogenoalkyl, C3-6-cycloalkyl represents H cyano, a halogen atom, C1-6-halogenoalkyl, C1-6-alcoxy, C1-6-halogenoalcoxi-, C1-6-alkyl or C3-6-cycloalkyl R3 represents a halogen atom, H, C1-6-alcoxy, C1-6-halogenoalkyl, C1-6-alkyl, C3-6-cycloalkyl, C1-6-halogenoalcoxy R4 reprsents H or halogeno.

EFFECT: creation of new compounds of formula (I) possessing mGLuR2 antagonist properties.

104 cl, 465 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new imidazolone derivatives used as drugs being kinase inhibitors, described by formula (I), wherein; R1 represents a C1-C3 alkyl radical or a hydrogen atom, and/or an aryl radical, Ar1 is specified in or , R represents the group R2-S-, R2 is thereby specified in the radicals like T1-(CH2)n, wherein n=0, 1, 2 or 3, and T1 represents a metal, vinyl, alkyl, alkynyl, nitrile, C3- or C4-cycloalkyl radical, hal, Z-O, Z-CO, wherein Z represents C1-C3 alkyl or hal, hal represents F, Cl, Br or I, or the group CCl3, or the group R3-NH-, R3 is thereby specified in the radicals like T2-(CH2)n, wherein n=0, 1 or 2, and T2 represents a metal, vinyl radical, Z-O, Z-CONH-, -CH-(OZ)2, ZCO, wherein Z represents H or C1-C4 linear or branched alkyl, NH2, C3-cycloalkyl, aryl, substituted aryl, or R3 represents H, or the group R4-CONH-, R4 is thereby specified in C3-C5 branched alkyl, or Ar2- or Ar2-3-, Ar2 is specified in a phenyl radical, substituted phenyl or benzodioxolyl; and have IC50 less than 5 mcM.

EFFECT: invention also refers to pharmaceutical compositions based on the compounds of formula I for treating neurodegenerative disorders and to using these compounds as DYRKIA inhibitors.

11 cl, 2 tbl, 8 ex

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