Derivatives benzothiophen-1,1-dioxides, the way they are received and drug


C07D337/08 - condensed with one six-membered ring

 

The invention relates to a derivative benzothiophen-1,1-dioxides and their additive salts with acids of formula 1where mean R1is methyl, ethyl, propyl, butyl; R2- H, HE; R3- the rest of the saccharide, and the rest of the saccharide in case you need one - or multiply substituted by one or more protective for saccharides group; R4is methyl, ethyl, propyl, butyl; R5is methyl, ethyl, propyl, butyl; Z is - (C= O)n-C1-C16-alkyl-NH-, a covalent bond; n = 1. The compounds can be used as hypolipidemic agents. Also described is a method of obtaining compounds and medicinal products based on them. 3 C. and 10 C.p. f-crystals, 1 table.

Description text in facsimile form (see graphic part).

Claims

1. Derivatives benzothiophen-1,1-dioxides of the formula I

where R1is methyl, ethyl, propyl, butyl;

R2- H, HE;

R3- the rest of the saccharide, and the rest of the saccharide, if necessary single or multiply substituted by one or more protective for saccharides group;

R4is methyl, ethyl, propyl, butyl;

R5is methyl, ethyl, propylparaben salt.

2. The compounds of formula I on p. 1, wherein one or more residues have the following meanings:

R1is ethyl, propyl,butyl;

R2- H, OH;

R3- the rest of the saccharide, and the rest of the saccharide in case you need one - or multi-substituted protective for saccharides group;

R4is methyl, ethyl, propyl, butyl;

R5is methyl, ethyl, propyl, butyl;

Z -(C=O)n-C1-C16-alkyl-NH, covalent bond;

n - 1;

and their pharmaceutically acceptable salts.

3. The compounds of formula I under item 1 or 2, characterized in that one or more residues have the following meanings:

R1- ethyl, butyl;

R2- HE;

R3- the rest of the saccharide, and the rest of the saccharide in case you need one - or multi-substituted protective for saccharides group;

R4is methyl;

R5is methyl;

Z is a covalent bond;

and their pharmaceutically acceptable salts.

4. The compound of formula I according to one or more paragraphs.1-3, characterized in that the compound has the following structure

as well as its pharmaceutically acceptable salt.

5. The compound of formula I according to one or more paragraphs.1-3, characterized in that the connection has lspool obtain compounds of the formula I according to one or more paragraphs.1-5, namely, that the amine of formula II

where R1, R2, R4and R5have shown in the formula I value, is subjected to the interaction with the compound of the formula III

where R3and Z have the meanings given in formula I,

with the elimination of water and formation of the compounds of formula I and the compound obtained of the formula I, if necessary, transferred to the pharmaceutically acceptable salt.

7. A drug that promotes the secretion of bile acids containing one or more compounds of one or more paragraphs.1-3.

8. Compounds according to one or more paragraphs.1-5, suitable as pharmaceuticals for the treatment of lipid metabolism disorders.

9. Compounds according to one or more paragraphs.1-5, suitable as pharmaceuticals for the treatment or prevention of gallstones.

10. Compounds according to one or more paragraphs.1-5, suitable for the preparation of drugs for the treatment of hyperlipidemia.

11. Compounds according to one or more paragraphs.1-5, suitable for the preparation of drugs for effects on the level of serum cholesterol.

12. Compounds according to one or more paragraphs.1-5, suitable d is one or more paragraphs.1-5, suitable for the preparation of drugs for treatment or prevention of gallstones.

 

Same patents:

The invention relates to substituted derivatives of benzo (b) thiepin-1,1-dioxides and their additive salts with acids of the formula I, in which R1is methyl, ethyl, propyl, butyl; R2- H, HE; R3a balance of amino acids, the remainder of diaminoanisole, and the balance of amino acids, the remainder of diaminoanisole in case you need one - or multi-substituted aminoadenine group; R4is methyl, ethyl, propyl, butyl; R5is methyl, ethyl, propyl, butyl; Z is a covalent bond

The invention relates to benzodiapines General formula I, their derivatives and analogues

The invention relates to a heterocyclic derivative benzocyclobutene General formula I, where R1IT denotes, C1-C6alkoxy; R2represents C1-C6alkyl; R3represents C1-C6alkyl, -(CH2)1-2-aryl, where aryl is phenyl, CH2-(C3-C7) cycloalkyl; R4and R5at the same time or in distinction from each other denote H, Cl, F, C1-C6alkyl, HE, C1-C6alkoxy, -(CH2)0-2-aryl, -O-(CH2)0-2-aryl, April is phenyl, unsubstituted or one-deputizing, -SOP(R6R7)

The invention relates to optically active derivative benzodiapine formula I, where R represents a lower alkyl group; R1and R2independently represent a lower alkyl group or together represent lower alkylene, which has excellent osteoinductive action, it is useful as a prophylactic or therapeutic agent against bone disease

The invention relates to medicine, in particular to plants with nephrolithiasis action, and can be used for the treatment and prevention of urolithiasis

The invention relates to substituted derivatives of benzo (b) thiepin-1,1-dioxides and their additive salts with acids of the formula I, in which R1is methyl, ethyl, propyl, butyl; R2- H, HE; R3a balance of amino acids, the remainder of diaminoanisole, and the balance of amino acids, the remainder of diaminoanisole in case you need one - or multi-substituted aminoadenine group; R4is methyl, ethyl, propyl, butyl; R5is methyl, ethyl, propyl, butyl; Z is a covalent bond

The invention relates to the group's derivative aminomethylpropanol acid represented by the following formula:

< / BR>
where R1represents a hydrogen atom, a lower alkyl group or aracelio group; R2represents a hydrogen atom or a halogen atom; the carbon atom marked with (R) denotes the carbon atom in (R)-configuration; the carbon atom marked with (S) means a carbon atom in (S)-configuration, or their pharmaceutically acceptable salts, pharmaceutical compositions, a stimulating effect on2and3-adrenoceptor, comprising as an active ingredient derived aminomethylpropanol acid, a means to soothe the pain and how calm the pain
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The invention relates to substituted derivatives of benzo (b) thiepin-1,1-dioxides and their additive salts with acids of the formula I, in which R1is methyl, ethyl, propyl, butyl; R2- H, HE; R3a balance of amino acids, the remainder of diaminoanisole, and the balance of amino acids, the remainder of diaminoanisole in case you need one - or multi-substituted aminoadenine group; R4is methyl, ethyl, propyl, butyl; R5is methyl, ethyl, propyl, butyl; Z is a covalent bond

The invention relates to new N-phenylamine and N-pyridylamine derivative of the formula I

< / BR>
in which X denotes O or S;

R1and R2which may be identical or different, denote hydrogen, (C1-C6)alkyl or (C3-C8)cycloalkyl or R1and R2together with the carbon atom to which they are attached, form a (C3-C8)cycloalkyl;

R3means (C6-C12)aryl, optionally substituted by one or more radicals Y, which may be the same or different;

Y represents halogen;

R4and R5represent hydrogen;

Ar denotes one of the following groups or WITH:

< / BR>
T represents hydrogen or (C1-C6)alkyl;

T3and T4which may be identical or different, denote (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)allylthiourea;

R6and R7each denotes hydrogen or R6and R7together represent a bond;

Z denotes either (I) the divalent group-CHR9- in which the R11-, in which R10and R11together they form a bond that Z represents the group-CH=CH-, or R10and R11that may be the same or different, have the meanings indicated above for R9or (III) a divalent group-CHR12-CHR13-CH2-, in which R12and R13together they form a bond, Z represents-CH=CH-CH2-, or R12and R13that may be the same or different, have the meanings indicated above for R9,

as well as their additive salts with pharmaceutically acceptable acids or bases, and method of production thereof, pharmaceutical compositions and drug manifesting gipolipedimecescoe and antiatherosclerotic action based on them

The invention relates to trilateralization formula (I) in which R1 means a hydrogen atom, halogen atom or lower alkyl radical, R2, R3 and R4 independently denote a hydrogen atom or a lower alkyl radical, Az means a nitrogen-containing aromatic N-methylseleninic the five-membered heterocycle containing one to three nitrogen atoms, with analgesic activity

The invention relates to tricyclic condensed heterocyclic compounds of the formula I, X is, for example, CH, CH2, СНR (where R means a lower alkyl group or a substituted lower alkyl group) or CRR' (where R and R' have the values specified above for R); Y means, for example, CH, CH2or C=O; z means, for example, S, S=O=; U denotes C; R1-R4independent means, for example, a hydrogen atom, SR (where R has the above values), phenyl group, substituted phenyl group, follow group, thienyl group, benzofuran or benzothiazyl at least one element of R5and R8means, for example, HE and the rest of the elements of R5and R8independent means, for example, a hydrogen atom; and their optical isomers, conjugates, and pharmaceutically acceptable salts

The invention relates to new indole derivative of the formula I

< / BR>
where R1- H, halogen, CN; R2and R3the same or different is H, C1-C4alkyl, halogen; R4- H, C1-C4alkyl; And means cyanoaniline, aminosulphonylphenyl, aminopyridine, aminopyrimidine, halogenopyrimidines or cianciarulo group, provided that if all R1, R2and R3- N, when both R2and R3- N or when ring A - aminosulphonylphenyl group and both R1and R2the halogen atoms is excluded; and, in addition, when the ring a represents cyanophenyl group, 2-amino-5-pyridyloxy group or 2-halogen-5-pyridyloxy group, and R1represents a cyano or halogen group, at least one of R2and R3must not be a hydrogen atom

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The invention relates to novim retinoid compounds of General formula I, II, III, IV with retinoid negative hormone biological activity and/or activity of antagonist retinoids, compositions based on them, a method of determining the retinoid antagonists hormones,the method of treating a pathological state in a mammal, vospriimchivosti to treatment with retinoid antagonist or negative hormone by injection of compound I or II

The invention relates to new derivatives of balkanov General formula (A)

< / BR>
where Ar is phenyl which may be unsubstituted or substituted one, two or three substituents independently chosen among Cl, Br, F, -OMe, NO2, CF3C1-4lower alkyl, -NMe2, -NEt2, -SCH3, -NHCOCH3; 2-thienyl, 2-furyl; 3-pyridyl; 4-pyridyl or 3-indolyl; R-OCH2R1where R1choose from a number of-CH= CME2The CME=CH2-The CCH; provided that when Ar is a phenyl,4-alkylphenyl, 4-methoxyphenyl or 3,4-acid, R can be any except 3-methyl-2-butenyloxy

FIELD: organic synthesis.

SUBSTANCE: invention provides compounds of general formula I:

, where R1 represents -CO-Ra, -SO2-Rb, or aryl optionally substituted by lower alkoxy, wherein Ra represents cycloalkyl, cycloalkyl(lower)alkyl, cycloalkyloxy, aryl, aryloxy, aryl(lower)alkyl, aryl(lower)alkoxy, aryloxy(lower)alkyl, aryl-S-(lower)alkyl, aryl(lower)alkenyl, provided that aryl group can be optionally substituted by halogen, lower alkyl, hydroxy, nitro, cyano, lower alkoxy, phenyl, CF3, cyano(lower)alkyl, lower alkyl-C(O)NH, lower alkyl-CO, and lower alkyl-S; heteroaryl, heteroaryl(lower)alkyl, or heteroaryl(lower)alkoxy, provided that heteroaryl group is 5- or 6-membered ring or bicyclic aromatic group constituted by two 5- or 6-membered rings including 1-3 heteroatoms selected from oxygen, nitrogen, and sulfur and that heteroaryl group can be optionally substituted by lower alkoxy; Rb represents aryl, aryl(lower)alkyl, or heteroaryl, aryl group optionally substituted by halogen, cyano, or lower alkyl-C(O)NH; R2 and R3 represent hydrogen atoms; R4 representshydrogen or lower alkyl; R5 represents hydrogen, lower alkyl, cycloalkyl, benzodioxyl, or aryl optionally substituted by lower alkyl, halogen, lower alkoxy, hydroxy, or (lower)alkyl-C(O)O; n is 1 or 2; and pharmaceutically acceptable salts thereof and/or pharmaceutically acceptable esters thereof. Invention also provides a pharmaceutical composition exhibiting inhibitory activity with regard to cysteine proteases of the cathepsin family, which composition comprises compound of formula I, pharmaceutically acceptable recipient, and/or adjuvant.

EFFECT: increased choice of cysteine protease inhibitors.

34 cl, 1 tbl, 13 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a new compound of the general formula (2) and a method for its preparing wherein R1 represents hydrogen atom or salt-forming metal; R2 represent a direct or branched (C1-C7)-halogenalkyl group; m represents a whole number from 2 to 14; n represents a whole number from 2 to 7; A represents a group taken among the following formulae: (3) , (4) ,

(5) ,

(6) ,

(17) , (18) , (19) , (20) , (23) , (25) and (26) wherein R3 in formula (6) represents a direct or branched group (C1-C5)-alkyl group; R8 in formulae (18) and (20) represents a direct or branched (C1-C5)-alkyl group, a direct or branched (C2-C5)-alkenyl group or a direct or branched (C2-C5)-alkynyl group; in formula (23) each R21, R22, R23 and R24 represents independently hydrogen atom, a direct or branched (C1-C5)-alkyl group, a direct or branched (C1-C7)-halogenalkyl group, halogen atom or acyl group; in formulae (25) and (26) X represents halogen atom; or enantiomers of compound, or hydrates, or pharmaceutically acceptable salts of compound, or its enantiomers. Also, invention relates to a pharmaceutical composition containing indicated compound as an active component and to a therapeutic agent used against breast cancer based on thereof.

EFFECT: valuable medicinal properties of compounds.

10 cl, 2 tbl, 39 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new biphenylsulfonylcyanamides of the formula (I): wherein R1 means: 1. (C1-C8)-alkyl; 4. -CnH2n-nn-Y wherein nn = 0 or 2 and n = 0-4, and n is not 0 or 1 if nn = 2; 5. CnH2n-nn-Y wherein nn = 0 or 2 and n = 1-4, and n is not 1 if nn = 2, and 1 hydrogen atom in bivalent residue CnH2n-nn is substituted with amino-group or NR(22)R(23); R2 means: 2. (C1-C)-alkyl; 4. (C2-C12)-alkenyl; 5. (C2-C8)-alkynyl; 6. -CnH2n-nn-Z wherein nn = 0 or 2; n = 0-4, and n is not or 1 if nn = 2; 7. -CnH2n-nn-Z wherein nn = 0 or 2; n = 1-4, and n is not 1 if nn = 2, and 1 hydrogen atom in bivalent residue CnH2n-nn is substituted with a residue taken among a series: 1. phenyl; 3. NR(22)R(23); 5. COOR(16); R3 and R4 mean hydrogen atom; R5, R6 and R7 mean independently of one another hydrogen atom (H), (C1-C8)-alkyl; SO2-(C1-C4)-alkyl, F, Cl, Br, J, OR(10) wherein R(10) means hydrogen atom, (C1-C4)-alkyl that is substituted if necessary with methoxy- or ethoxy-group; R(9) means OR(13) wherein R(13) means hydrogen atom, H,(C1-C8)-alkyl;X means carbonyl group, -CO-CO- or sulfonyl group; Y and Z mean independently of one another: 1. phenyl, 1-naphthyl, 2-naphthyl; 2. one of residues determined in cl. 1 substituted with 1-5 similar or different residues taken among a series: phenyl, F, Cl, Br, J, CF3, SOqR(18), OR(16), NR(19)R(20), -CN, NO2, COR(9), or two residues form methylenedioxy-group; 3. furyl, thienyl, pyridyl, benzimidazolyl, indolyl, benzothiophenyl, dihydroquinazolinyl; 5. (C3-C10)-cycloalkyl wherein cyclopropyl, cyclopentyl, cyclohexyl and indalyl are preferable; 6. one of residues determined in cl. 5 substituted with phenyl; R(16) means: 1. hydrogen atom; 2. (C1-C4)-alkyl; 3. (C1-C4)-alkyl substituted with (C1-C4)-alkoxy-group; R(19) and R(20) mean independently: hydrogen atom (H), (C1-C4)-alkyl; R(22) and R(23) mean independently of one another hydrogen atom (H) or CO-OR(24) wherein R924) means -CnH2n-phenyl wherein n = 1-4; q = 2; and their physiologically acceptable salts. Compound of the formula (I) inhibit sodium-dependent chloride-bicarbonate exchange "NCBE".

EFFECT: improved preparing method, valuable medicinal properties of compounds.

4 cl, 2 tbl, 568 ex

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