Benzimidazole derivatives, synthesis methods thereof, use thereof as farnesoid x receptor (fxr) agonist and pharmaceutical preparations containing said derivatives

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzimidazole derivatives of formula

and pharmaceutically acceptable salts and esters thereof, where R1 denotes C1-10alkyl, lower alkoxy group-lower alkyl, lower alkoxy group-carbonyl-lower alkyl, C3-6cycloalkyl, C3-6cycloalkyl-lower alkyl, phenyl, phenyl-lower alkyl, di(phenyl)-lower alkyl, heterocyclyl, such as piperidinyl, tetrahydropyranyl, 2-oxo-pyrrolidinyl-lower alkyl, where the cycloalkyl, phenyl or heterocyclyl group is optionally substituted with 1-2 substitutes independently selected from a group comprising lower alkyl, lower alkoxy group, lower alkoxy group-carbonyl, morpholinyl, formylamino group and halogen; R2 denotes hydrogen or lower alkyl; R3 denotes lower alkyl, C3-6cycloalkyl, partially unsaturated cyclohexyl, phenyl, phenyl-lower alkyl, pyridinyl, benzodioxolyl, tetrahydropyranyl, where the phenyl group is optionally substituted with 1-2 substitutes independently selected from a group comprising a halogen, lower alkyl, lower alkoxy group, fluoro-lower alkyl, fluoro-lower alkoxy group, N(lower alkyl)2; R4 denotes: a) heteroaryl which is an aromatic 5-6-member monocyclic ring or a 9-10-member bicyclic ring containing 1 or 2 heteroatoms selected from nitrogen, oxygen and/or sulphur, which is optionally substituted with 1-2 substitutes independently selected from a group comprising lower alkyl, phenyl, lower alkoxy group, -N(lower alkyl)2, oxo group, NH2, halogen, cyano group and morpholinyl; b) unsubstituted naphthyl, naphthyl or phenyl, which are substituted with 1-3 substitutes independently selected from a group comprising halogen, hydroxy group, NH2, CN, hydroxy-lower alkyl, lower alkoxy group, lower alkyl-carbonyl, lower alkoxy group-carbonyl, sulphamoyl, di-lower alkyl-sulphamoyl, lower alkyl-sulphonyl, thiophenyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-oxopyrrolidinyl, lower alkyl, fluoro-lower alkyl, fluoro-lower alkoxy group, N(lower alkyl)2, carbamoyl, lower alkenyl, benzoyl, phenoxy group and phenyl which is optionally substituted with 1-2 substitutes independently selected from halogen and fluoro-lower alkyl; or c) if R3 denotes cycloalkyl and R1 denotes cycloalkyl, then R4 can also denote phenyl; R5, R6, R7 and R8 independently denote H, halogen, lower alkoxy group or lower alkyl, or R6 and R7, which are bonded to each other, form a 6-member aromatic carbocyclic ring together with carbon atoms to which they are bonded; provided that the compound of formula (I) is not selected from a group comprising butylamide 2-[2-(2-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid and 2-(2-benzo[1,3]dioxol-5-ylbenzoimidazol-1-yl)-N-benzyl-butyric acid amide. The invention also relates to a pharmaceutical composition based on the formula I compound.

EFFECT: novel benzimidazole derivatives which are useful as farnesoid X receptor antagonists are obtained.

30 cl, 379 ex

 

The text descriptions are given in facsimile form.

1. The compounds of formula (I)

where R 1stands With1-10alkyl, lower alkoxygroup-lower alkyl, lower alkoxygroup-carbonyl-lower alkyl, C3-6cycloalkyl,3 - 6cycloalkyl-lower alkyl, phenyl, phenyl-lower alkyl, di(phenyl)-lower alkyl, heterocyclyl, such as piperidinyl, tetrahydropyranyl, 2-oxo-pyrrolidinyl-lower alkyl, where cycloalkyl, phenyl or heterocyclyl group optionally substituted with 1-2 substituents independently selected from the group comprising lower alkyl, lower alkoxygroup, lower alkoxygroup-carbonyl, morpholinyl, formylamino and halogen;
R2denotes hydrogen or lower alkyl;
R3denotes lower alkyl, C3-6cycloalkyl, partially unsaturated cyclohexyl, phenyl, phenyl-lower alkyl, pyridinyl, benzodioxolyl, tetrahydropyranyl, where the phenyl group is optionally substituted with 1-2 substituents independently selected from the group comprising halogen, lower alkyl, lower alkoxygroup, fluoro-lower alkyl, fluoro-lower alkoxygroup, N(lower alkyl)2;
R4means;
a) heteroaryl, which represents an aromatic 5-6 membered monocyclic ring or 9-10-membered bicyclic ring containing 1 or 2 heteroatoms selected from nitrogen, oxygen and/or sulfur, which is optionally substituted with 1-2 substituents independently selected and from the group including lower alkyl, phenyl, lower alkoxygroup, -N(lower alkyl)2oxoprop, NH2, halogen, cyano and morpholinyl;
b) unsubstituted naphthyl, or naphthyl or phenyl, which is substituted by from 1 to 3 substituents, independently selected from the group comprising halogen, a hydroxy-group, NH2, CN, hydroxy-lower alkyl, lower alkoxygroup, lower alkyl-carbonyl, lower alkoxygroup-carbonyl, sulfamoyl, di-lower alkyl-sulfamoyl, lower alkyl-sulfonyl, thiophenyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-oxopyrrolidin, lower alkyl, fluoro-lower alkyl, fluoro-lower alkoxygroup, N(lower alkyl)2, carbarnoyl, lower alkenyl, benzoyl, fenoxaprop and phenyl, which is optionally substituted with 1-2 substituents independently selected from halogen and fluoro-lower alkyl; or
C) if R3denotes cycloalkyl and R1denotes cycloalkyl, R4may also represent a phenyl;
R5, R6, R7and R8independently of one another denote H, halogen, lower alkoxygroup or lower alkyl, or R6and R7connected to each other, form a 6-membered aromatic carbocyclic ring together with the carbon atoms to which they are attached;
and their pharmaceutically acceptable salts and esters;
provided that the compound f is rmula (I) is selected from the group including
butylamide 2-[2-(2-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid and
2-(2-benzo[1,3]dioxol-5-eventimages-1-yl)-N-benzylmaleimide.

2. Compounds according to claim 1, where R4does
a) heteroaryl, which optionally is substituted by 1-2 substituents independently selected from the group comprising lower alkyl, phenyl, NH2N(lower alkyl)2, lower alkoxygroup, halogen;
b) unsubstituted naphthyl, or naphthyl or phenyl, which is substituted by 1-2 substituents independently selected from the group comprising halogen, a hydroxy-group, NH2, CN, hydroxy-lower alkyl, lower alkoxygroup, lower alkyl-carbonyl, lower alkoxygroup-carbonyl, sulfamoyl, di-lower alkyl-sulfamoyl, lower alkyl-sulfonyl, thiophenyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-oxopyrrolidin, lower alkyl, fluoro-lower alkyl, fluoro-lower alkoxygroup, N(lower alkyl)2and carbarnoyl; or
C) if R3denotes cycloalkyl and R1denotes cycloalkyl, R4may also represent a phenyl.

3. Compounds according to claim 1, where R1stands With1-10alkyl, lower alkoxygroup-lower alkyl, lower alkoxygroup-carbonyl-lower alkyl, C3-6cycloalkyl,3-6cycloalkyl-lower alkyl, phenyl, phenyl-lower alkyl, di(phenyl)-lower alkyl and heterocyclyl selected and the group, including piperidinyl and 2-oxopyrrolidin,
where cycloalkyl, phenyl or heterocyclyl group optionally substituted with 1-2 substituents independently selected from the group comprising lower alkyl, lower alkoxygroup, lower alkoxygroup-carbonyl, morpholinyl and formylamino.

4. Compounds according to claim 1, where R1represents C1-10alkyl, C3-6cycloalkyl or phenyl, where phenyl is optionally substituted with 1-2 substituents independently selected from lower alkyl.

5. Compounds according to claim 1, where R1means 1,1,3,3-TETRAMETHYLBUTYL, cyclopentyl, cyclohexyl or 2.5-dimetilfenil.

6. Compounds according to claim 1, where R1denotes tetrahydropyranyl,3-6cycloalkyl, which is substituted by 1-2 halogen atoms, or phenyl which is substituted by 1-2 lower alkilani.

7. Compounds according to claim 6, where R1means tetrahydropyran-4-yl, 4,4-diverticulosis or 2,6-dimetilfenil.

8. Compounds according to claim 1, where R3denotes lower alkyl, C3-6cycloalkyl, partially unsaturated cyclohexyl, phenyl, phenyl-lower alkyl, pyridinyl, tetrahydropyran-2-yl or benzodioxolyl, where phenyl optionally substituted with 1-2 substituents independently selected from the group comprising halogen, lower alkyl, lower alkoxygroup and N(lower alkyl)2.

9. Compounds according to claim 1, where R3 stands With4-6cycloalkyl, phenyl, phenyl-lower alkyl or pyridinyl.

10. Connection p,1, where R3denotes cyclopentyl, cyclohexyl, phenyl, 3-phenylpropyl or pyridine-2-yl.

11. Compounds according to claim 1, where R3denotes lower alkyl, tetrahydropyranyl or phenyl, which is substituted by 1-2 substituents independently selected from fluoro-lower-alkyl and fluoro-lower alkoxygroup.

12. Connection of claim 8, where R3represents isobutyl, pentyl or tetrahydropyran-2-yl.

13. Compounds according to claim 1, where R4means:
a) heteroaryl selected from the group comprising thiophenyl, pyrrolyl, 2-oxo-1,2-dihydropyridine, indolyl, chinoline and 1,3-dikshithar, with heteroaryl is optionally substituted with 1-2 substituents independently selected from the group comprising lower alkyl and phenyl;
b) unsubstituted naphthyl, or naphthyl or phenyl, which is substituted by from 1 to 3 substituents, independently selected from the group comprising halogen, a hydroxy-group, NH2, CN, hydroxy-group-lower alkyl, lower alkoxygroup, lower alkyl-carbonyl, lower alkoxygroup-carbonyl, sulfamoyl, di-lower alkyl-sulfamoyl, lower alkyl-sulfonyl, thiophenyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-oxopyrrolidin; or
C) if R3denotes cycloalkyl and R1denotes cycloalkyl, 4may also represent a phenyl.

14. Compounds according to claim 1, where R4means:
a) heteroaryl selected from the group comprising thiophenyl, 2-oxo-1,2-dihydropyridine and chinoline where thiophenyl optionally substituted by phenyl; or
b) unsubstituted naphthyl, or phenyl which is substituted by 1-2 substituents independently selected from the group comprising hydroxy-lower alkyl, lower alkoxygroup, imidazolyl or tetrazolyl.

15. Compounds according to claim 1, where R4denotes 2,4-acid, naphthalene-2-yl, 4-hydroxymethylene, 4-(tetrazolyl-5-yl)phenyl, 4-(imidazol-2-yl)phenyl, 4-acetylaminophenol, 5-phenylthiophene-2-yl, 2-oxo - 1,2-dihydropyridines-4-yl or quinoline-6-yl.

16. Compounds according to claim 1, where R4means:
a) heteroaryl selected from the group including pyridinyl, pyrazolyl, isoxazolyl, benzimidazolyl, furanyl, thiophenyl, indolyl, benzo[b]thiophenyl, benzothiazolyl, benzofuranyl and honokalani, with heteroaryl is optionally substituted from 1 to 2 substituents, independently selected from the group including halogen, CN, NH2N(lower alkyl)2, lower alkyl, lower alkoxygroup and morpholinyl; or
b) unsubstituted naphthyl, or naphthyl or phenyl, which is substituted by from 1 to 3 substituents, independently selected from the group comprising carbarnoyl, halogen, lower alkyl, fluoro-lower alkyl, whom Thor-the lower alkoxygroup, lower-alkenyl, N(lower alkyl)2N(H, lower alkyl), benzoyl, fenoxaprop and phenyl, which is optionally substituted from 1 to 2 substituents, independently selected from halogen and fluoro-lower-alkyl.

17. Join on clause 16, where R4does
a) thiophenyl, substituted with halogen; or
b) phenyl, which is substituted by carbamoyl or halogen.

18. Connection 17, where R4denotes 5-chlorothiophene-2-yl, 2 - aminocarbonylmethyl or 4-chlorophenyl.

19. Compounds according to claim 1, where R5, R6, R7and R8independently of one another denote H, halogen, lower alkyl or lower alkoxygroup, or R6and R7connected to each other, forming a 6-membered aromatic carbocyclic ring together with the carbon atoms to which they are attached.

20. Compounds according to claim 1, where R5denotes hydrogen.

21. Compounds according to claim 1, where R6denotes hydrogen, fluorine or methyl.

22. Compounds according to claim 1, where R7denotes hydrogen, fluorine or chlorine.

23. Compounds according to claim 1, where R8denotes hydrogen.

24. Compounds according to claim 1, selected from the group including:
Hydrochloride 2,N-DICYCLOHEXYL-2-(2-phenylbenzimidazol-1-yl)acetamide", she
Cyclohexylamin 2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
Hydrochloride methyl ester 4-{1-[cyclohexyl-(4-(morpholine-4-infiniscale)methyl]-1H-shall benzoimidazol-2-yl}benzoic acid,
2,N-DICYCLOHEXYL-2-[5,6-dichloro-2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
Hydrochloride of 2-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-N-isopropylacrylamide,
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(4-methoxyphenyl)-benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(3-methoxyphenyl)-benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(2-methoxyphenyl)-benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-(2-naphthalene-1-eventimages-1-yl)acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(3-ethoxyphenyl)benzoimidazol-1-yl]acetamide", she
N-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-4-phenylbutyramide,
Hydrochloride, N-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-3-methylbutylamine,
Hydrochloride, N-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-3-phenylpropionamide,
Hydrochloride, N-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-2-pyridine-2-ylacetamide,
Hydrochloride, N-cyclohexyl-2-cyclopentyl-2-[2-(2,4-acid)benzoimidazol-1-yl] acetamide", she
Methyl ester of 4-{1-[cyclohexyl(cyclohexylcarbonyl)]-1H-benzoimidazol-2-yl}benzoic acid,
2,N-DICYCLOHEXYL-2-(2-naphthalene-2-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-thiophene-2-ylphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(5-phenylthiophene-2-yl)benzoimidazol-1-yl]acetamide", she
Cyclohexylamin 2-[2-(3-hydroxyphenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
Cyclohexylamin 2-[2-(4-hydroxymethylene)benzoimidazol-1-yl]-4-methylpentanoic acid,
Cyclohexylamin 2-[2-(1H-indol-5-yl)benzimidazol-1-yl]-4-methylpentanoic acid,
Cyclohexylamin 2-[2-(1H-indol-6-yl)benzimidazol-1-yl]-4-methylpentanoic acid,
Cyclohexylamin 2-[2-(4-AMINOPHENYL)benzoimidazol-1-yl]-4-methylpentanoic acid,
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-((R)-1-phenyl-ethyl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-hydroxymethylene)benzoimidazol-1-yl]acetamide", she
N-Cyclohexyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-4-phenylbutyramide,
2-[2-(3-Cyanophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[4-(1H-tetrazol-5-yl)-phenyl]benzoimidazol-1-yl}acetamide", she
Methyl ester of 3-[1-(benzylcarbamoyl)-1H-benzoimidazol-2-yl]benzoic acid
Cyclohexylamin 2-[2-(2,4-acid)benzoimidazol-1-yl]hexanoic acid,
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(3-methanesulfonyl)-benzoimidazol-1-yl]acetamide", she
N-Benzyl-2-cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(1-methylbutyl)ndimethylacetamide,
Methyl ester of 4-[1-(benzylcarbamoyl)-1H-benzoimidazol-2-yl]benzoic acid is,
Hydrochloride N-cyclopentyl-2-[2-(3-methoxyphenyl)benzoimidazol-1-yl]-4-phenylbutyramide,
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(2,4-acid)-5-methylbenzimidazole-1-yl]acetamide", she
Hydrochloride of 2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-2,N-Dicyclopentadiene,
N-Benzhydryl-2-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]acetamide", she
N-Benzyl-2-(2-naphthalene-1-eventimages-1-yl)-4-phenylbutyramide,
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(4-methoxyphenyl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-acid)-4-methylbenzimidazole-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[3-(2-oxopyrrolidin-1-yl)-phenyl]benzoimidazol-1-yl}acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-oxo-1,2-dihydropyridines-4-yl)benzoimidazol-1-yl]acetamide", she
N-Cyclopentyl-2-[2-(2-methoxyphenyl)benzoimidazol-1-yl]-4-phenylbutyramide,
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-ventilated,
The hydrochloride of N-benzyl-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-2-cyclopentylacetic,
2,N-Dicyclopentyl-2-(2-naphthalene-1-eventimages-1-yl)acetamide", she
2-[2-(3-Cyanophenyl)benzoimidazol-1-yl]-N-cyclohexyl-4-phenylbutyramide,
Hydrochloride cyclohexylamine 2-[2-(4-hydroxy-phenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
N-tert-Butyl-2-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]acetamide", she
Methyl ester of 4-[1-(1-benzylcarbamoyl-3-phenylprop the l)-1H-benzoimidazol-2-yl]benzoic acid
Methyl ester of 4-[1-(1-cyclohexylcarbonyl-3-phenylpropyl)-1H-benzoimidazol-2-yl] benzoic acid
2,N-Dicyclopentyl-2-[2-(2-methoxyphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-acid)of oil[2,3-d]imidazol-1-yl]acetamide", she
Cyclohexylamin 2-[2-(2,3-acid)benzoimidazol-1-yl]-4-methylpentanoic acid,
N-Benzyl-2-[2-(2-methoxyphenyl)benzoimidazol-1-yl]-4-phenylbutyramide,
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(3-isopropoxy-propyl)acetamide", she
2-[2-(2,4-Acid)benzoimidazol-1-yl]-N-isopropyl-4-phenylbutyramide,
N-Benzyl-2-cyclopentyl-2-(2-naphthalene-1-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3-acid)benzoimidazol-1-yl]acetamide", she
Cyclohexylamin 2-[2-(2,4-acid)benzoimidazol-1-yl]-4-methylpentanoic acid,
2-Cyclohexyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-N-isopropylacetate,
2-[2-(2,3-Acid)benzoimidazol-1-yl]-1N-isopropyl-4-phenylbutyramide,
2-[2-(4-Acetylphenyl)benzoimidazol-1-yl]-N-cyclohexyl-4-phenylbutyramide,
The hydrochloride of N-benzyl-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-4-phenylbutyramide,
Methyl ester of 4-[1-(1-isopropylaminomethyl)-1H-benzoimidazol-2-yl]benzoic acid
N-Butyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-2-phenylacetamide,
Isopropylated 2-[2-(2,3-acid)benzoimidazol-1-yl]-4-methylpentanoic acid br/> 2-Benzo[1,3]dioxol-5-yl-N-butyl-2-[2-(2,3-acid)-benzoimidazol-1-yl]acetamide", she
2-Benzo[1,3]dioxol-5-yl-N-butyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]acetamide", she
N-Butyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-2-(2-forfinal)ndimethylacetamide,
N-Cyclopentyl-2-[2-(3-hydroxyphenyl)benzoimidazol-1-yl]-4-phenylbutyramide,
Isopropylated 2-[2-(4-acetylphenyl)benzoimidazol-1-yl]hexanoic acid,
N-Butyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-2-phenylacetamide,
Cyclohexylamin 2-[2-(4-acetylphenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
N-Butyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-2-o-tolylacetate,
N-Butyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-2-(4-methoxyphenyl)acetamide", she
N-Butyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-2-(2-fluoro-phenyl)acetamide", she
N-Butyl-2-[2-(2,3-acid)benzoimidazol-1-yl]-2-(4-dimethylaminophenyl)ndimethylacetamide,
Isopropylated 2-[2-(2,3-acid)benzoimidazol-1-yl]hexanoic acid,
Methyl ester of 4-{1-[(2-forfinal)isopropylaminomethyl]-1H-benzoimidazol-2-yl}benzoic acid,
Cyclohexylamin 2-[2-(3-cyanophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
Cyclohexylamin 2-[2-(3-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
N-Butyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-2-(4-methoxyphenyl)acetamide", she
The hydrochloride of N-benzyl-2-[2-(3-methoxyphenyl)benzoimidazol-1-yl]-4-phenyl who tyramide,
2-(4-Chlorophenyl)-2-[2-(2,3-acid)benzoimidazol-1-yl]-N-isopropylacetate,
N-Butyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-2-(4-dimethylamino-phenyl)acetamide", she
2-[2-(4-Hydroxyphenyl)benzoimidazol-1-yl]-N-isopropyl-4-phenylbutyramide,
Cyclohexylamin 2-[2-(4-hydroxyphenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
2-[2-(3-Chlorophenyl)benzoimidazol-1-yl]-N-isopropyl-4-phenylbutyramide,
N-Butyl-2-(4-chlorophenyl)-2-[2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
2-[2-(3-Cyanophenyl)benzoimidazol-1-yl]-N-isopropyl-4-phenylbutyramide,
2-[2-(4-Acetylphenyl)benzoimidazol-1-yl]-N-isopropyl-2-(4-methoxyphenyl)acetamide", she
Methyl ester of 4-{1-[isopropylcarbamate-(4-methoxyphenyl)methyl]-1H-benzoimidazol-2-yl}benzoic acid,
Methyl ester of 4-[1-(isopropylaminomethyl)-1H-benzoimidazol-2-yl] benzoic acid
N-Isopropyl-2-[2-(1-methyl-1H-pyrrol-2-yl)benzoimidazol-1-yl]-4-phenylbutyramide,
Isopropylated 2-[2-(3-cyanophenyl)benzoimidazol-1-yl]hexanoic acid,
Isopropylated 2-[2-(4-hydroxyphenyl)benzoimidazol-1-yl]pentanol acid,
2-Benzo[1,3]dioxol-5-yl-N-butyl-2-[2-(1-methyl-1H-pyrrol-2-yl)benzoimidazol-1-yl]acetamide", she
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(2,6-dimethyl-phenyl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
2-Cyclohex-3-enyl-N-cyclohexyl-2-[2-(2,4-acid)-benzo is imidazol-1-yl]acetamide", she
Hydrochloride of 2-[2-(4-cyanophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-Cyclohexyl-N-cyclopentyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-acid)-5,6-differentiality-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-acid)-6-methylbenzimidazole-1-yl]acetamide", she
2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(4-sulfamoylbenzoyl)-benzoimidazol-1-yl]acetamide", she
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(1,1,3,3-TETRAMETHYLBUTYL)ndimethylacetamide,
Hydrochloride methyl ester 4-{[1-cyclopentyl(cyclopentanecarbonyl)]-1H-benzoimidazol-2-yl}benzoic acid,
Hydrochloride 2,N-DICYCLOHEXYL-2-(2-quinoline-6-eventimages-1-yl)acetamide", she
2-[2-(4-AMINOPHENYL)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Hydrochloride cyclohexylamine 2-[2-(2,4-acid)benzoimidazol-1-yl]-5-phenylpentane acid,
Methyl ester of 4-[1-(1-cyclopentanecarbonyl-3-phenylpropyl)-1H - benzoimidazol-2-yl]benzoic acid
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(4-dimethylsulphamoyl-phenyl)benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(3-sulfamoylbenzoyl)-benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[3-(1H-tetrazol-5-yl)-phenyl]benzoimidazol-1-yl}acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[4-(1H-imide is evil-2-yl)phenyl]benzoimidazol-1-yl}acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(4-imidazol-1-ylphenyl)benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(4-[1,2,4]triazole-4-yl-phenyl)benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[4-(1H-pyrazole-4-yl)phenyl]benzoimidazol-1-yl}acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(4-[1,2,3]thiadiazole-4-yl-phenyl)benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(1,3-dioxo-2,3-dihydro-1H-isoindole-5-yl)benzimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(3-tetrazol-1-ylphenyl)benzoimidazol-1-yl]acetamide", she
Hydrochloride methyl ester 4-[1-(cyclohexyl-3-methoxycarbonylpropionyl)-1H-benzoimidazol-2-yl]benzoic acid
The hydrochloride of the methyl ester of TRANS-4-(1-{cyclohexyl-[(4-methoxycarbonyl-cyclohexylmethyl)carbarnoyl]methyl}-1H-benzoimidazol-2-yl)benzoic acid
Hydrochloride ethyl ester 4-{2-cyclohexyl-2-[2-(4-methoxycarbonyl-phenyl)benzoimidazol-1-yl]acetylamino}piperidine-1-carboxylic acid,
Hydrochloride, N-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-2-phenylacetamide,
The hydrochloride of the methyl ester of 4-(1-{cyclohexyl-[3-(2-oxopyrrolidin-1-yl)-propellerblades] methyl}-1H-benzoimidazol-2-yl)benzoic acid
Hydrochloride methyl ester 4-{1-[cyclohexyl(3-methoxycarbonyl-propellerblades)methyl]-1H-benzoimidazol-2-yl}benzoic acid,
Hydrochlo the ID of the methyl ester of 4-{1-[cyclohexyl-(4-methoxycarbonylaminophenyl)methyl]-1H-benzoimidazol-2-yl}benzoic acid,
Hydrochloride methyl ester 4-{1-[cyclohexyl-(5-methoxycarbonylmethylene)methyl]-1H-benzoimidazol-2-yl}benzoic acid,
Hydrochloride of 2-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-N-methylacetamide,
2-[2-(4-Acetylaminophenol)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(3-Acetylaminophenol)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Hydrochloride methyl ester 4-{1-[cyclohexyl-(3-formelementname)methyl]-1H-benzoimidazol-2-yl}benzoic acid
N-cyclopentyl-2-(2-naphthalene-1-eventimages-1-yl)propionamide, and their pharmaceutically acceptable salts.

25. Compounds according to claim 1, selected from the group including:
Hydrochloride, N-cyclohexyl-2-[2-(2,4-acid)-benzoimidazol-1-yl]-2-pyridine-2-ylacetamide,
Hydrochloride, N-cyclohexyl-2-cyclopentyl-2-[2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-(2-naphthalene-2-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(5-phenylthiophene-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-hydroxymethylene)benzoimidazol-1-yl]acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[4-(1H-tetrazol-5-yl)phenyl]benzoimidazol-1-yl}acetamide", she
Hydrochloride 2,N-DICYCLOHEXYL-2-[2-(2,4-acid)-5-methylbenzimidazole-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-oxo-1,2-dihydropyridines-4-yl)benzoimidazol-1-yl]acetamide", she
2-Cyclohexyl-2-[2-(2,4-is methoxyphenyl)benzoimidazol-1-yl]-N-(2,6-dimetilfenil)ndimethylacetamide,
2-Cyclohexyl-]-N-cyclopentyl-2-[2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(1,1,3,3-TETRAMETHYLBUTYL)ndimethylacetamide,
Hydrochloride 2,N-DICYCLOHEXYL-2-(2-quinoline-6-eventimages-1-yl)acetamide", she
Hydrochloride cyclohexylamine 2-[2-(2,4-acid)-benzoimidazol-1-yl]-5-phenylpentane acid,
Hydrochloride 2,N-DICYCLOHEXYL-2-{2-[4-(1H-imidazol-2-yl)phenyl]benzoimidazol-1-yl}acetamide", she
Hydrochloride, N-cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-2-phenylacetamide, and
2-[2-(4-Acetylaminophenol)benzoimidazol-1-yl]-2,N-dicyclohexylamine, and their pharmaceutically acceptable salts.

26. Compounds according to claim 1, selected from the group including:
2,N-DICYCLOHEXYL-2-(2-phenylbenzimidazol-1-yl)acetamide", she
2-[1-(Cyclohexyloxycarbonyl)-1H-benzoimidazol-2-yl]benzamide,
2-[2-(5-Aminopyridine-2-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(2-ethyl-5-methyl-2H-pyrazole-3-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(5-methylisoxazol-4-yl)benzoimidazol-1-yl] acetamide", she
2,N-DICYCLOHEXYL-2-[2-(1H-pyrrol-2-yl)benzoimidazol-1-yl]acetamide", she
2-(1 N-[2,5']Dibenzonitrile-1-yl)-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-(2-furan-2-eventimages-1-yl)acetamide", she
2-[6-Bromo-2-(4-chlorophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[6-Chloro-2-(4-CHL is henyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-2,N-dicyclohexylamine,
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-2,N-dicyclohexylamine,
(S)-2,N-DICYCLOHEXYL-2-[2-(2,4-acid)benzoimidazol-1-yl]acetamide", she
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[1-(Cyclohexyloxycarbonyl)-1H-benzoimidazol-2-yl]-N-methylbenzamide,
2,N-DICYCLOHEXYL-2-(2-furan-3-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-methylfuran-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-methylisoxazol-5-yl)benzimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-(2-m-talibandominated-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-forfinal)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-forfinal)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,5-dimethylisoxazol-4-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-methylthiophene-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-vinylphenol)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3-dimetilfenil)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,4-dimetilfenil)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-ethylphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-dimetilfenil)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-ethylphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-fluoro-3-methylpentanediol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-fluoro-4-were)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,6-differenl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,5-differenl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,5-differenl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,4-differenl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3-differenl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(1H-indol-4-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(1H-indol-6-yl)benzimidazol-1-yl]acetamide", she
2-[2-(5-Chlorothiophene-2-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Acetylphenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(2-Acetylphenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(4-isopropylphenyl)benzoimidazol-1-yl]acetamide", she
2-[2-(4-Cyano-2-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(2-dimethylaminophenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-dimethylaminophenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-methoxy-3-were)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-methoxy-2-were)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-methoxy-4-were)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-ethoxyphenyl)benzoimidazol-1-yl]acetamide", she
2-[2-(6-Chloropyridin-3 is)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(2-Chloropyridin-4-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(3-fluoro-4-methoxyphenyl)benzimidazol-1-yl]acetamide", she
2-[2-(4-Chloro-3-were)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(3-Chloro-2-were)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chloro-3-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(3-Chloro-4-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(5-methyl-1H-indol-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3,4-tryptophanyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4,5-tryptophanyl)benzoimidazol-1-yl]acetamide", she
2-(2-Benzo[b]thiophene-2-eventimages-1-yl)-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(5-fluoro-1H-indol-2-yl)benzoimidazol-1-yl]acetamide", she
2-(2-Benzothiazol-6-eventimages-1-yl)-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(4-isopropoxyphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,4-acid)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,5-acid)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-deformational)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4-deformational)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-deformational)benzoimidazol-1-the l]ndimethylacetamide,
2,N-DICYCLOHEXYL-2-[2-(4-triptoreline)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,4-dichlorophenyl)benzoimidazol-1-yl]acetamide", she
2-[2-(4-Bromophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(6-methoxynaphthalene-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-trifloromethyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(7-ethoxyresorufin-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-fluoro-4-triptoreline)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(6-diethylaminomethyl-3-yl)benzoimidazol-1-yl]acetamide", she
2-[2-(2-Chloro-5-methylphenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(5-Chloro-2-were)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(2-Chloro-6-were)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-(2-cinoxacin-6-eventimages-1-yl)acetamide", she
2-[2-(5-Chloro-2-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(4-methoxy-3, 5dimethylphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3-acid)benzoimidazol-1-yl]acetamide", she
2-[2-(3-Chloro-4-methoxyphenyl)benzimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(2,5-dichlorophenyl)benzoimidazol-1-yl]acetamide", she
2-[2-(3-Chloro-2,4-differenl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(2-Chloro-4,5-differenl)benzamid the evils-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(4-diethylaminophenyl)benzoimidazol-1-yl]acetamide", she
2-[2-(4-Benzoylphenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
(S)-2-[2-(4-Cyanophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(4-phenoxyphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-phenoxyphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-phenoxyphenyl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-{2-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]benzoimidazol-1-yl}acetamide", she
2,N-DICYCLOHEXYL-2-{2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]benzoimidazol-1-yl}acetamide", she
2,N-DICYCLOHEXYL-2-{2-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]benzoimidazol-1-yl}acetamide", she
2,N-DICYCLOHEXYL-2-[2-(4'-triptorelin-4-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3',4'-dichlorobiphenyl-4-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-dichloro-5-sulfamoylbenzoyl)benzoimidazol-1-yl]acetamide", she
(S)-2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-(2-pyridin-2-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(6-methylpyridin-3-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-methylpyridin-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(6-methylpyridin-2-yl)benzoimidazol-1-yl]acetamide", she
2-[2-(2-Aminopyridine-3-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(6-Cyano-3-the l)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-[2-(2-methoxypyridine-3-yl)benzoimidazol-1-yl]acetamide", she
2-[2-(2-Chloro-6-methylpyridin-3-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(2-Chloro-6-methylpyridin-4-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-(2-quinoline-3-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-(2-quinoline-4-eventimages-1-yl)acetamide", she
2-[2-(3-Chloro-4-triptoreline)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Cyclohexylamin (S)-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
2-(4-Chlorophenyl)-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-N-cyclohexylacetate,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(4-triptoreline)ndimethylacetamide,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(3,4-dichlorophenyl)acetamide", she
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(3-methoxyphenyl)acetamide", she
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-p-tolylacetate,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(3-forfinal)ndimethylacetamide,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(4-deformational)ndimethylacetamide,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(2,5-differenl)ndimethylacetamide,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(2-fluoro-5-methoxyphenyl)acetamide", she
(S)-2-[2-(5-Chloro-2-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
(S)-2,N-DICYCLOHEXYL-2-[2-(2,3-Dimethoxyphenyl is)benzoimidazol-1-yl]acetamide", she
(S)-2-[2-(3-Chloro-4-methoxyphenyl)benzimidazol-1-yl]-2,N-dicyclohexylamine,
(S)-2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(2,6-dimetilfenil)ndimethylacetamide,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-(4,4-diverticulosis)ndimethylacetamide,
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-(4,4-diverticulosis)ndimethylacetamide,
(S)-2-[2-(2-Aminopyridine-3-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2,N-DICYCLOHEXYL-2-(6-fluoro-2-pyridin-2-eventimages-1-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,4-acid)-6-perbenzoate-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[6-fluoro-2-(4-methoxyphenyl)benzimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3-differenl)-6-perbenzoate-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2,3-acid)-6-perbenzoate-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(2-ethyl-5-methyl-2H-pyrazole-3-yl)-6-perbenzoate-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,5-dimethylisoxazol-4-yl)-6-perbenzoate-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[6-fluoro-2-(1H-pyrazole-4-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(1,5-dimethyl-1H-pyrazole-3-yl)-6-perbenzoate-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[6-fluoro-2-(3-methylisoxazol-5-yl)benzimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[6-fluoro-2-(1H-pyrrol-2-yl)benzoimidazol-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[6-fluoro-2-(3-methylthiophene-2-yl)benzoimidazol-1-yl]acetamide", she
N Be the ZIL-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-2-cyclohexylacetate,
N-Butyl-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-2-cyclohexylacetate,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
2-[5-Chloro-2-(4-chlorophenyl)-6-perbenzoate-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chlorophenyl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-(tetrahydropyran-4-yl)acetamide", she
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-cyclopropylacetic,
2,N-DICYCLOHEXYL-2-[2-(6-morpholine-4-espiridion-3-yl)benzoimidazol-1-yl]acetamide", she
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-(tetrahydropyran-4-yl)acetamide", she
(S)-2,N-DICYCLOHEXYL-2-[2-(4-methanesulfonyl)benzoimidazol-1-yl]acetamide", she
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-cyclopropylacetic,
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[2-(4-Chlorophenyl)-5,6-differentiality-1-yl]-2-dicyclohexylamine,
(S)-2-[2-(5-Chlorothiophene-2-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
(S)-2,N-DICYCLOHEXYL-2-[2-(2,3-differenl)-6-perbenzoate-1-yl]acetamide", she
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-N-cyclo is exil-2-cyclopentylacetic,
Cyclohexylamin (S)-2-[6-chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]heptane acid,
(S)-2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-cyclopentylacetic,
2-[2-(4-Chlorophenyl)-5-perbenzoate-1-yl]-2,N-dicyclohexylamine,
Methyl ester 2-[1-(cyclohexyloxycarbonyl)-5,6-debtor-1H-benzoimidazol-2-yl]benzoic acid
2,N-DICYCLOHEXYL-2-(5,6-debtor-2-pyridine-2-eventimages-1-yl)acetamide", she
2-[2-(5-Chlorothiophene-2-yl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
Methyl ester 2-[6-chloro-1-(cyclohexyloxycarbonyl)-5-fluoro-1H-benzoimidazol-2-yl]benzoic acid
2-(6-Chloro-5-fluoro-2-pyridin-2-eventimages-1-yl)-2,N-dicyclohexylamine,
2-(6-Chloro-5-fluoro-2-pyridin-3-eventimages-1-yl)-2,N-dicyclohexylamine,
2-(6-Chloro-5-fluoro-2-pyridin-4-eventimages-1-yl)-2,N-dicyclohexylamine,
2-[6-Chloro-2-(3-chlorothiophene-2-yl)-5-perbenzoate-1-yl]-2,N-dicyclohexylamine,
2-[6-Chloro-2-(5-chlorothiophene-2-yl)-5-perbenzoate-1-yl]-2,N-dicyclohexylamine,
Cyclohexylamin (S)-2-[6-chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-3-ethylpentane acid,
2-[6-Chloro-5-fluoro-2-(4-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-(1-isopropyl-2-methylpropyl " ndimethylacetamide,
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-2-cyclohex the Il-N-cyclopentylacetic,
2-[2-(4-Chlorophenyl)-5,6-differentiality-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[2-(4-Chlorophenyl)-5-perbenzoate-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chlorophenyl)-5,6-differentiality-1-yl]-2-cyclohexyl-N-(tetrahydropyran-4-yl)acetamide", she
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-2-cyclohexyl-N-(tetrahydropyran-4-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-dimethylaminophenyl)-5,6-differentiality-1-yl]acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3-dimethylaminophenyl)-6-perbenzoate-1-yl]acetamide", she
2-[2-(4-Chlorophenyl)-5,6-differentiality-1-yl]-2-cyclohexyl-N-(1-isopropyl-2-methylpropyl " ndimethylacetamide,
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-2-cyclohexyl-N-(1-isopropyl-2-methylpropyl " ndimethylacetamide,
2-[2-(3-Chlorophenyl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
2-[2-(2-Chlorophenyl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
(S)-2-[6-Chloro-5-fluoro-2-(4-forfinal)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
(S)-2-[2-(4-Chlorophenyl)-5,6-differentiality-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
2-[2-(4-Chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-2-yl)acetamide", she
2-[6-Chloro-2-(4-chlorophenyl)-5-fluoro shall benzoimidazol-1-yl]-N-cyclohexyl-2-(tetrahydropyran-2-yl)acetamide", she
(S)-2,N-DICYCLOHEXYL-2-[6-fluoro-2-(3-methylthiophene-2-yl)benzoimidazol-1-yl]acetamide", she
(S)-2-[2-(2-Chlorophenyl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
(S)-2-[2-(4-Chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(R)-tetrahydropyran-2-ylacetamide,
(S)-2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(S)-tetrahydropyran-2-ylacetamide,
2-[2-(4-Chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-2-yl)acetamide", she
2,N-DICYCLOHEXYL-2-[2-(3,4-dichlorophenyl)-6-methoxybenzimidazole-1-yl]acetamide", she
2-[2-(4-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-2,N-dicyclohexylamine,
2-[2-(5-Chlorothiophene-2-yl)-6-methoxybenzimidazole-1-yl]-2,N-dicyclohexylamine,
2-[2-(3-Chloro-4-methoxyphenyl)-6-methoxybenzimidazole-1-yl]-2,N-dicyclohexylamine,
2-[2-(4-Chloro-3-forfinal)-6-methoxybenzimidazole-1-yl]-2,N-dicyclohexylamine,
2-Cyclohexyl-N-cyclopentyl-2-[2-(3,4-dichlorophenyl)-6-methoxybenzimidazole-1-yl]acetamide", she
N-Cyclohexyl-2-cyclopentyl-2-[2-(3,4-dichlorophenyl)-6-methoxybenzimidazole-1-yl]acetamide", she
2-[2-(4-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-2-cyclohexyl-N-cyclopentylacetic,
2-[2-(3-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-N-dicyclohexylamine br/> 2,N-Dicyclopentyl-2-[2-(3,4-dichlorophenyl)-6-methoxybenzimidazole-1-yl]acetamide", she
2-[2-(4-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-N-cyclohexyl-2-cyclopentylacetic,
2-[2-(4-Chloro-3-forfinal)-6-methoxybenzimidazole-1-yl]-2-cyclohexyl-N-cyclopentylacetic,
2-[2-(3-Chloro-4-methoxyphenyl)-6-methoxybenzimidazole-1-yl]-2-cyclohexyl-N-cyclopentylacetic,
2,N-DICYCLOHEXYL-2-[2-(4-forfinal)-6-methoxybenzimidazole-1-yl]acetamide", she
2-[2-(3-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-2-cyclohexyl-N-cyclopentylacetic,
2-[2-(3-Chloro-4-methoxyphenyl)-6-methoxybenzimidazole-1-yl]-N-cyclohexyl-2-cyclopentylacetic,
2-[2-(5-Chlorothiophene-2-yl)-6-methoxybenzimidazole-1-yl]-N-cyclohexyl-2-cyclopentylacetic,
2-Cyclobutyl-N-cyclohexyl-2-[2-(3,4-dichlorophenyl)-6-methoxybenzimidazole-1-yl]acetamide", she
2-[2-(5-Chlorothiophene-2-yl)-6-methoxybenzimidazole-1-yl]-2-cyclohexyl-N-cyclopentylacetic,
2-[2-(6-Chloropyridin-3-yl)-6-methoxybenzimidazole-1-yl]-2,N-cyclohexylacetate,
2-[2-(3-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-N-cyclohexyl-2-cyclopentylacetic,
2-[2-(3-Chloro-4-methoxyphenyl)-6-methoxybenzimidazole-1-yl]-2,N-Dicyclopentadiene,
2,N-DICYCLOHEXYL-2-[6-methoxy-2-(6-triptorelin-3-yl)benzoimidazol-1-yl]acetamide", she
2-[2-(5-Chlorothiophene-2-yl)-6-methoxybenzimidazole-1-yl]-2-cyclobutyl-N-cyclohexylacetate,
2-[2-(3-Chlorophenyl)-6-methoxybenzimidazole-1-yl]-2-cyclobutyl-N-C is cogenerated, and
N-Cyclohexyl-2-cyclopentyl-2-[2-(4-forfinal)-6-methoxybenzimidazole-1-yl] ndimethylacetamide, and their pharmaceutically acceptable salts.

27. Compounds according to claim 1, selected from the group including:
2-[1-(Cyclohexyloxycarbonyl)-1H-benzoimidazol-2-yl]benzamide,
(S)-2,N-DICYCLOHEXYL-2-[2-(2,4-acid)benzoimidazol-1-yl] acetamide", she
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Cyclohexylamin (S)-2-[2-(4-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid,
2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-N-cyclohexyl-2-(4-triptoreline)ndimethylacetamide,
(S)-2-Cyclohexyl-2-[2-(2,4-acid)benzoimidazol-1-yl]-N-(2,6-dimetilfenil)ndimethylacetamide,
(S)-2-[2-(4-Chlorophenyl)benzoimidazol-1-yl]-2-cyclohexyl-N-(4,4-diverticulosis)ndimethylacetamide,
(S)-2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-4-yl)acetamide", she
(S)-2-[2-(5-Chlorothiophene-2-yl)benzoimidazol-1-yl]-2,N-dicyclohexylamine,
Cyclohexylamin (S)-2-[6-chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]heptane acid,
2-[6-Chloro-2-(4-chlorophenyl)-5-perbenzoate-1-yl]-2-cyclohexyl-N-(tetrahydropyran-4-yl)acetamide", she
2-[2-(3-Chlorophenyl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
(S)-2,N-DICYCLOHEXYL-2-[6-fluoro-2-(3-methylthiophene-2-yl)benzoimidazol-1-yl]acetamide", she
(S)-2-[2-(2-Chlorophenyl)-5,6-differentiality-1-yl]-2,N-dicyclohexylamine,
(S)-2-[2-(4-shall lorgeril)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(R)-tetrahydropyran-2-ylacetamide,
(S)-2-[2-(4-Chlorophenyl)-6-perbenzoate-1-yl]-N-cyclohexyl-2-(S)-tetrahydropyran-2-ylacetamide, and
2-[2-(4-Chlorophenyl)-5-perbenzoate-1-yl]-N-cyclohexyl-2-(tetrahydropyran-2-yl)ndimethylacetamide, and their pharmaceutically acceptable salts.

28. Compounds according to one of claims 1 to 27, for use as therapeutically active substances with activity against farnesoid-X-receptor (FXR).

29. Compounds according to one of claims 1 to 27, for use as therapeutically active substances for the treatment and/or prevention of diseases modulated by FXR agonists.

30. Pharmaceutical composition having activity against farnesoid-X-receptor, comprising an effective amount of a compound according to one of claims 1 to 27 and a pharmaceutically acceptable carrier or adjuvant.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: present invention relates to organic electroluminescent devices based on compounds of formula

where Y, Z is selected from N, P, P=O, C=O, O, S, S=O and SO2; Ar1, Ar2, Ar3 are selected from benzene, naphthaline, anthracene, phenanthrene, pyridine, pyrene or thiophene, optionally substituted with R1; Ar4, Ar5, Ar6, Ar7 are selected from benzene, naphthaline, anthracene, phenanthrene, pyridine, pyrene, thiophene, triphenylamine, diphenyl-1-naphthylamine, diphenyl-2-naphthylamine, phenyldi(1-naphthyl)amine, phenyldi(2-naphthyl)amine or spirobifluorene, optionally substituted with R1; E is a single bond, N(R1), O, S or C(R1)2; R1 denotes H, F, CN, alkyl, where the CH2 can be substituted with -R2C=CR2 -, -C=C-, -O- or -S-, and H can be substituted with F, optionally substituted aryl or heteroaryl, where R1 can form a ring with each other; R2 denotes H, aliphatic or aromatic hydrocarbon; X1, X4, X2, X3 are selected from C(R1)2, C=O, C=NR1, O, S, S=O, SO2, N(R1), P(R1), P(=O)R1, C(R1)2-C(R1)2, C(R1)2-C(R1)2-C(R1)2, C(R1)2-O and C(R1)2-O-C(R1)2; n, o, p, q, r and t are equal to 0 or 1; s = 1.

EFFECT: obtaining novel compounds - emission layer dopants, and novel electroluminescent devices based on said compounds which emit a blue colour.

18 cl, 91 ex, 6 tbl

Organic compounds // 2411239

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I, in which R1 denotes alkyl or cycloalkyl; R2 denotes phenyl-C1-C7-alkyl, di-(phenyl)- C1-C7-alkyl, naphthyl- C1-C7-alkyl, phenyl, naphthyl, pyridyl-C1-C7-alkyl, indolyl- C1-C7-alkyl, 1H-indazolyl- C1-C7-alkyl, quinolyl C1-C7-alkyl, isoquinolyl- C1-C7-alkyl, 1,2,3,4-tetrahydro-1,4-benzoxazinyl- C1-C7-alkyl, 2H-1,4-benzoxazin-3(4H)-onyl-C1-C7-alkyl, 9-xanthenyl-C1-C7-alkyl, 1-benzothiophenyl-C1-C7-alkyl, pyridyl, indolyl, 1H-indazolyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydro-1,4-benzoxazonyl, 2H-1,4-benzoxazin-3(4H)-onyl, 9-xanthenyl, 1-benzothiophenyl, 4H-benzo[1,4]thiazin-3-only, 3,4-dihydro-1H-quinolin-2-onyl or 3H-benzoxazol-2-onyl, where each phenyl, naphthyl, pyridyl, indolyl, 1H-indazolyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydro-1,4-benzoxazonyl, 2H-1,4-benzoxazin-3(4H)-onyl, 1-benzothiophenyl, 4H-benzo[1,4]thiazin-3-only, 3,4-dihydro-1H-quinolin-2-onyl or 3H-benzoxazol-2-onyl are unsubstituted or contain one or up to 3 substitutes independently selected from a group comprising C1-C7-alkyl, hydroxy-C1-C7-alkyl, C1-C7-alkoxy- C1-C7-alkyl, C1-C7-alkoxy- C1-C7-alkoxy-C1-C7-alkoxy- C1-C7-alkyl, C1-C7-alkanoyloxy- C1-C7-alkyl, amino- C1-C7-alkyl, C1-C7-alkoxy- C1-C7-alkylamino- C1-C7-alkyl, C1-C7-alkanoylamino- C1-C7-alkyl, C1-C7-alkylsulphonylamino- C1-C7-alkyl, carboxy- C1-C7-alkyl, C1-C7-alkoxycarbonyl- C1-C7-alkyl, halogen, hydroxy group, C1-C7-alkoxy group, C1-C7-alkoxy- C1-C7-alkoxy group, amino- C1-C7-alkoxy group, N-C1-C7-alkanoylamino-C1-C7-alkoxy group, carbamoyl- C1-C7-alkoxy group, N-C1-C7-alkylcarbamoyl-C1-C7-alkoxy group, C1-C7-alkanoyl, C1-C7-alkoxy-C1-C7-alkanoyl, C1-C7-alkoxy- C1-C7-alkanoyl, carboxyl, carbamoyl and N-C1-C7-alkoxy-C1-C7-alkylcarbamoyl; W denotes a fragment selected from residues of formulae IA, IB and IC, where () indicates the position in which the fragment W is bonded to the carbon atom in position 4 of the piperidine ring in formula I, and where X1, X2, X3, X4 and X5 are independently selected from a group containing carbon and oxygen, where X4 in formula IB and X1 in formula IC can assume one of these values or can be additionally selected from a group comprising S and O, where carbon and nitrogen ring atoms can include a number of hydrogen atoms or substitutes R3 or R4 if contained, taking into account limitations given below, required to bring the number of bonds of the carbon ring atom to 4 and 3 for the nitrogen ring atom; provided that in formula IA at least 2, preferably at least 3 of the atoms X1-X5 denote carbon and in formulae IB and IC at least one of X1-X4 denotes carbon, preferably 2 of the atoms X1-X4 denote carbon; y equals 0 or 1; z equals 0 or 1; R3, which can be bonded with any of the atoms X1, X2, X3 and X4, denotes hydrogen or a C1-C7-alkyloxy-C1-C7-alkyloxy group, phenyloxy-C1-C7-alkyl, phenyl, pyridinyl, phenyl- C1-C7-alkoxy group, phenyloxy group, phenyloxy-C1-C7-alkoxy group, pyridyl-C1-C7-alkoxy group, tetrahydropyranyloxy group, 2H,3H-1,4-benzodioxynyl-C1-C7-alkoxy group, phenylaminocarbonyl or phenylcarbonylamino group, where each phenyl or pyridyl is unsubstituted or contains one or up to 3 substitutes, preferably 1 or 2 substitutes independently selected from a group comprising C1-C7-alkyl, hydroxy group, C1-C7-alkoxy group, phenyl-C1-C7-alkoxy group, where phenyl is unsubstituted or substituted with a C1-C7-alkoxy group and/or halogen; carboxy- C1-C7-alkyloxy group, N-mono- or N,N-di-(C1-C7-alkyl)aminocarbonyl-C1-C7-alkyloxy group, halogen, amino group, N-mono- or N,N-di-(C1-C7-alkyl)amino group, C1-C7-alkanoylamino group, morpholino-C1-C7-alkoxy group, thiomorpholino-C1-C7-alkoxy group, pyridyl-C1-C7-alkoxy group, pyrazolyl, 4- C1-C7-alkylpiperidin-1-yl, tetrazolyl, carboxyl, N-mono- or N,N-di-(C1-C7-alkylamino)carbonyl or cyano group; or denotes 2-oxo-3-phenyltetrahydropyrazolidin-1-yl, oxetidin-3-yl-C1-C7-alkyloxy group, 3-C1-C7-alkyloxetidin-3-yl- C1-C7-alkyloxy group or 2-oxotetrahydrofuran-4-yl- C1-C7-alkyloxy group; provided that if R3 denotes hydrogen, then y and z are equal to 0; R4, if contained, denotes a hydroxy group, halogen or C1-C7-alkoxy group; T denotes carbonyl; and R11 denotes hydrogen, or pharmaceutically acceptable salts thereof. The invention also relates to use of formula I compounds, a pharmaceutical composition, as well as a method of treating diseases.

EFFECT: obtaining novel biologically active compounds having activity towards rennin.

11 cl, 338 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: this invention relates to cocrystalline form of (1S)-1,5-anhydro-1-[3-(1-benzothiene-2-ylmethyl)-4-fluorophenyl]-D-glucitol (compound A) with L-proline. Proposed cocrystalline form is a promising anti-diabetes medicine.

EFFECT: cocrystalline form of compound is characterised with constant composition, improved stability in storage, and also low hygroscopicity, and is suitable for use as crystalline medicinal substance to produce pharmaceutical preparations.

11 cl, 1 ex, 2 tbl, 10 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof, having CRP receptor antagonist activity. In formula (I) R1 denotes C3-C8 alkyl, optionally substituted with hydroxyl; phenyl optionally substituted with 1-3 substitutes selected from halogen, nitro, amino, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, optionally substituted with hydroxyl or C1-C4 alkylamino; naphthyl; C-bonded 5-6-member heteroaryl with 1-2 heteroatoms selected from S, N or O, optionally substituted with C1-C4 alkyl, C1-C4 alkoxy or acetyl; N-bonded 5-member heteroaryl with 1-2 heteroatoms selected from N, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl or phenyl; R2 denotes phenyl, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl, halogenC1-C4alkyl, C1-C4 alkoxy, halogenC1-C4alkoxy, halogen, hydroxy, di(C1-C4 alkyl)amino or di(C1-C4 alkyl)aminocarbonyl; or a heterocyclic group which is pyridyl, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl, C1-C4 alkoxy or di(C1-C4 alkyl)amino; X denotes -NR3-, where R3 denotes C1-C4 alkyl, optionally substituted with hydroxyl, carboxyl or C1-C4 alkoxycarbonyl; Y1 denotes CR3a, where R3a denotes hydrogen, halogen, cyano, hydroxy, C1-C4 alkyl, optionally substituted with hydroxyl or halogen, C1-C4 alkoxy optionally substituted with halogen; Y2 denotes CR3b, where R3b denotes hydrogen or halogen; Y3 denotes N or CR3c, where R3c denotes hydrogen; and Z denotes O or -NR4-, where R4 denotes hydrogen.

EFFECT: invention also pertains to a method of producing compounds of formula (I), a pharmaceutical composition, an inhibiting method, CRF receptor antagonists and use thereof to prepare a medicinal agent.

25 cl, 9 tbl, 163 ex

FIELD: chemistry.

SUBSTANCE: invention relates to synthesis of hydroperoxides of alkylaromatic hydrocarbons which can serve as a source of oxygen-containing organic compounds (phenol, methylphenols, acetone, cyclohexanone etc) and as an initiator of emulsion polymerisation of unsaturated hydrocarbons. The invention discloses a method for synthesis of hydroperoxides of alkylaromatic hydrocarbons through liquid-phase oxidation of these hydrocarbons with atmospheric oxygen at atmospheric pressure, process temperature of 110-130°C, for 1-3 hours in the presence of a 4-methyl-N-hydroxyphthalimide catalyst in amount of 1.0-2.0 wt %.

EFFECT: catalyst prevents use of an initiator and alkaline additives, which considerably simplifies the process, higher conversion of initial alkylaromatic hydrocarbons while preserving high selectivity of the process.

2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel 1-thio-D-glucitol compounds of formula I or to pharmaceutically acceptable salts thereof or hydrates of the compound or salts: , [where R1, R2, R3 and R4 are identical or different, and each is a hydrogen atom, C1-C6-alkyl group), A is -(CH2)n-, -CONH(CH2)n-, -O- or -(CH2)nCH=CH- (where n is an integer from 0 to 3, Ar1 is an arylene group, heteroarylene group, which is an unsaturated 5-9-member mono- or bicyclic group, containing 1-2 heteroatoms, selected from S and N, Ar2 is an aryl group or heteroaryl group which is an unsaturated 5-9-member mono- or bicyclic group containing 1-2 heteroatoms selected from O, S and N, and R5, R6, R7, R8, R9 and R10 are identical or different, and each is (i) a hydrogen atom, (ii) a halogen atom, (iii) a hydroxyl group, (iv) C1-8-alkyl group, optionally substituted with hydroxyl group(s), (v) -(CH2)m-Q {where m is an integer from 0 to 4, and Q is -CO2H, -ORc1, -CO2Ra3, -SRe1, -NHRa6 or -NRa7Ra7 (where each of Ra3, Ra6 and Ra7 is a C1-6-alkyl group, Rc1 is a C1-6-alkyl group, and Rc1 is a C1-6-alkyl group)}, (vi) -O-(CH2)m'-Q' {where m' is an integer from 1 to 4, and Q' is a hydroxyl group,-CO2H, -CO2Ra8, -CONRa10Ra10, -NRa12Ra12 (where each of Ra8, Ra10 and Ra12 is a C1-6-alkyl group)}, (vii) -ORf {where Rf is C3-7-cycloalkyl group or tetrahydropyranyl group)}, (viii) morpholine group, (ix) phenyl group, (x) pyridyl group]. The invention also relates to 1-thio-D-glucitol compounds of formulae IA, II, III, IV, to a pharmaceutical agent, to methods of obtaining 1-thio-D-glucitol compounds, as well as to compounds of formulae XIII, XIV.

EFFECT: obtaining novel biologically active compounds which are inhibitors of sodium-dependent co-transporter-2-glucose.

25 cl, 140 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns a new glucitol derivative of formula (I): wherein m represents an integer chosen from 1-3; each R1, R2, R3 and R4 are independently choose from hydrogen atom and benzyl groups; Ar1 represents a naphthyl group which can be substituted by one or more substitutes chosen from the group, consisting of C1-C6alkyl group or halogen atom; A represents 5-7-members aromatic heterocyclic group containing one or more heteroatoms independently chosen from oxygen atom and sulphur atom which can form a condensed cycle with an aromatic carbocycle or an aromatic heterocycle where A can be substituted by one or more Rb provided when A is a benzocondensed cycle containing two or more rings, the group -(CH2)m- is connected with a heterocycle in A; Each Rb is independently chosen from C1-C6alkyl group, halogen atom and C1-C6-alkoxy group; or to their pharmaceutically acceptable salts. These compounds are used as a Na+ cotransport inhibitor and exhibits ability to reduce blood sugar level.

EFFECT: invention covers a pharmaceutical composition based on these compounds and to the method for treatment and prevention of such diseases associated with hyperglycemia, as diabetes, diabetes complications and obesity.

12 cl, 4 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of formula , where R1 is -O-X, where X is -(CH2)m-(CR9R10)p-(CH2)n-Z-(CH2)q-W, where m, n and q are independently equal to zero or assume values from 1 to 5; p equals 0 or 1; R9 and R10 are independently hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy or cycloalkyl; or R9 and R10 together represent alkylene, which together with the carbon atom to which the are bonded, form an aryl; Z is a bond or O, W is aryl; R2 is hydrogen; L is a bond; R3 is hydrogen; R4 is hydrogen; R5 and R6 are independently hydrogen; R7 is hydrogen, halogen, hydroxy, trifluromethyl, lower alkyl, lower alkoxy, alkanoyl, alkyloxyalkoxy, alkanoyloxy, amino, alkylamino, dialkylamino, acylamino, carbamoyl, carboxy, alkoxycarbonyl; or R5 and R6 together represent -(CH2)1-2-; Y is -(CH2)r-, -O-(CH2)r, -(CH2)r-O-, where r equals zero or assumes values from 1 to 3; Q together with atoms to which it is bonded form an aryl, pyridyl, pyrimidinyl, thienyl, furyl, pyrroliyl or indolyl ring; or to its pharmaceutically acceptable salts. The invention also relates to a method of inhibiting rennin activity in mammals, to a pharmaceutical composition, as well as to application.

EFFECT: obtaining new biologically active compounds with inhibitory activity towards renin.

23 cl, 52 ex

FIELD: chemistry.

SUBSTANCE: invention claims compounds of the formula (I) with radicals as described in the claim, and medicine with inhibition effect on glycine absorption, based on compound of the formula (I) .

EFFECT: medicine for diseases treatment where glycine absorption inhibition can be effective.

21 cl, 1 tbl, 173 ex

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to compounds of the formula (I): wherein R1 means -lower alkyl, -CH2-aryl, -cycloalkyl, -(CH2)3, -OC(=O)CH3, -lower alcohol, -lower alkyl-R10, -CH2COOH or -CH2CH2OCH2CH3; R2 means -lower alkyl, -CH2-aryl, -lower alcohol, -CH2C(=O)-NH2 or lower alkyl-R10 wherein at least one radical among R1 or R2 means -CH3; R3 means -COOH, -lower alkyl-COOH, -lower alcohol, -CH2OCH2, -CH2NH2, -CHNHSO2R11, -C(=O)-R12, -(CH2)nNHC(=O)-R13, -(CH2)mC(=O)N-(R15)(R16), -C(=NH)-R17 or -(CH2)n-R18; R4 means hydrogen atom (-H), -lower alkoxy group, -O-C(R7R8)C(=O)-R19, -halogen atom, -SCH3, -C=CHC(=O)-R10, -CH2CH2C(=O)-R10, -O-lower alcohol, -OCH2CH(OH)CH2N=N±N-, -OCH2CH2OCH2CH2Cl, -NHC9=O)-CH2-lower alkyl, -O(CH2)n-cycloalkyl, -O-lower alkene or 5-membered unsaturated heterocyclic ring comprising one heteroatom representing sulfur (S) or oxygen (O) atom; R5 and R6 mean independently -H, -halogen atom or -lower alkoxy group; R7 and R8 mean independently -H or -CH3; R10 means 5-6-membered saturated heterocyclyl comprising 1 or 2 heteroatoms, such as N and O, and this group is bound with other moiety of molecule by a ring N atom; R11 means -CF3, -lower alkyl, -CH2Cl, -CH2CF3 or -R12; R12 means 5-6-membered saturated substituted or unsubstituted heterocyclic ring comprising 1 heteroatom, such as N, O and S wherein substituted ring represents heterocyclic ring substituted with -OH or -phenyl; R13 means -lower alkyl, -lower alkoxy group or -(CH2)nR14; R14 means 5-6-membered saturated or unsaturated heterocyclic ring comprising 1 and 2 heteroatoms, that are chosen from group comprising N and O; R15 means -H, -lower alkyl, -OH, -lower alkoxy group or -CH2COOCH2CH3; R17 means -lower alkoxy group, -NH2 or -N-lower alkyl; R18 means saturated or unsaturated 5-membered substituted or unsubstituted heterocyclic ring comprising from 1 to 4 heteroatoms, such as N, O and S wherein substituted ring represents heterocyclic ring that is substituted by one or two cyclic carbon atoms by =O, or it is substituted by cyclic N atom by -lower alcohol or -lower alkyl; R19 means -OH, -NHCH(CH3)2, -N(CH3)CH2-aryl, -N(CH3)-lower alkyl, 1-(aryl-(CH2)n-)-[1,4]-diazin-4-yl or 5-6-membered saturated heterocyclyl and optionally substituted with lower alkyl comprising 1 or 2 heteroatoms, such as N and O; m = 0, 1 or 2; n = 0 or 1, and their pharmaceutically acceptable salts and esters. Also, invention relates to a pharmaceutical composition possessing inhibitory activity with respect to GFAT and containing the effective amount of compound of the formula (I). Invention provides expanding assortment of agents possessing inhibitory activity with respect to GFAT. Proposed compounds can be used as inhibitors of GFAT, and pharmaceutical composition possessing inhibitory activity with respect to GFAT containing above said compound of the formula (I) also.

EFFECT: valuable biochemical properties of compounds and pharmaceutical composition.

25 cl, 134 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula , where R1 is a 3-7-member carbocyclic ring and n is a number ranging from 1 to 8, and the rest of the radicals are described in the claim.

EFFECT: possibility of using such compounds and compositions in therapy as metabotropic glutamate receptor modulators.

33 cl, 367 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry. Pharmaceutical compositions including, at least, one compound of formula where -X- represents, for instance, group of formula and Y represents, for instance, group of formula or its pharmaceutically acceptable salts, esters or amides, or pro-drugs and pharmaceutically acceptable carrier, which is acceptable in therapy, can be applied for modulation in vitro and in vivo processes of binding, mediated by binding of E-, P- or L- selectin.

EFFECT: obtaining novel floroglucin derivatives.

9 cl, 10 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: in formula (I) Cy1 is a 6-member heterocyclyl containing N as a heteroatom, a 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteroatoms selected from N, S and O, phenyl or phenyl condensed with a 5-member heterocycle containing O as a heteroatom, each optionally having 1-3 identical or different substituting Cy1 groups which are: (C1-C6)-acyl, cyano, carboxy, hydroxy, (C1-C6)alkylsulphonyl, (C3-C6)-cycloalkyl, a 6-member heterocyclyl containing 1-2 heteroatoms selected from O and N, phenyl, a 5-member heteroaryl containing 1-3 heteroatoms selected from N, S and O, Y1Y2N-, Y1Y2NC(=O)-, Y1Y2NSO2-, (C1-C6)-alkyl-SO2-N(R5)-C(=O)-, R6-C(=O)-N(R5)-, R7-NH-C(=O)-NH-; (C1-C6)-alkoxycarbonyl; (C1-C6)-alkyl, which optionally contains 1-3 identical or different substitutes which are halogen, carboxy, cyano, hydroxy, Y1Y2N-, Y1Y2N-C(=O)-, R6-C(=O)-N(R5)-, R8-SO2-N(R5)-C(=O)-, 5-member heterocyclyl, containing N as a heteroatom, 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; or (C1-C6)-alkoxycarbonyl; as well as (C1-C6)-alkoxy which optionally have 1-3 identical or different substitutes which are carboxy, (C1-C6)-alkoxycarbonyl, cyano, 3-member heterocyclyl containing O as a heteroatom, or 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; where phenyl or heteroaryl fragments in the substituting Cy1 groups optionally and independently have substitutes represented by hydroxy, (C1-C6)-alkyl, (C1-C6)-alkoxy, carboxy, (C1-C6)-alkoxycarbonyl or R8-SO2-N(R5)-C(=O)-; and where cycloalkyl fragments in the substituting Cy1 groups which optionally and independently have substitutes represented by (C1-C6)-alkoxy, carboxy; Cy2 is a 9-member cycloalkenyl, phenyl, 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteratoms selected from N, S and O, or phenyl condensed with a 5,6-member heterocycle containing 1-2 heteroatoms selected from N and O, each independently and optionally having 1-3 identical or different substitutes represented by (C1-C6)-alkoxy, (C1-C3)-alkyl, hydroxy, halogen, halogen-(C1-C6)-alkoxy, nitro, Y1Y2N-; L1 is an alkylene with a straight or branched chain containing 1-6 carbon atoms, optionally substituted carboxy; or L1 is -CH2-(C1-C5)halogenalkylene; L2 is a bond, -O- or -CH2-O-. Other values of radicals are given in the formula of invention.

EFFECT: novel compounds have prostaglandin D2 receptor antagonist properties, can be used in treating primarily allergic disorders such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy and other diseases.

39 cl, 1 tbl, 99 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrrole derivatives of the formula I: , where R1 and R2 independently denote Ph; mono- or disubstituted in different positions of the ring Ph, where substitute denotes -OCH3; C5-heteroaryl with one heteroatom selected from O or S; R2 denotes H, NO2, NH2, C(O)NH2; R4 denotes H, a straight or branched C1-C6-alkyl; n equals the number of methylene groups and is between 1 and 8 inclusively; X denotes O, S, NH; Y NH, -CH2-; Z denotes O, S; W denotes -OH, hydroxylamine, hydrazine, alkylhydrazine.

EFFECT: compounds can inhibit histone deacetylase, which enables their use in cancer treatment.

10 cl, 9 dwg, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new cyclopenta[b]benzofuranyl derivatives of formula wherein substitutes R1, R2, R3, R4, R5, R6 and R7 and n are specified in the patent clam. These compounds exhibit properties of NF-kB-activity and/or AP-1 inhibitor/modulator. Also, the inventive subject matter are methods for preparing intermediate compounds thereof, a pharmaceutical composition containing them, administration thereof for prevention and/or treatment of inflammatory and autoimmune diseases, neurodegenerative diseases and hyperproliferative diseases caused by NF-kB- and/or AP-1-activity, and a method for prevention and/or treatment of said diseases.

EFFECT: preparation of new cyclopenta[b]benzofuranyl derivatives.

21 cl, 3 tbl, 151 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compound described by formula where R1 represents a monocyclic nitrogen-containing heterocyclic group optionally condensed with heterocycle with the monocyclic nitrogen-containing heterocyclic group optionally condensed with heterocycle, optionally having 1 to 5 substitutes chosen from a group consisting of (1) halogen atom, (2) cyano, (3) hydroxy, (4) C1-6 alkoxy optionally having 1 to 3 halogen atoms, (5) amino, (6) mono- C1-6 alkylamino, (7) C1-6 alkoxycarbonyl and (8) C1-6 alkyl optionally having 1 to 3 halogen atoms, R2 represents (i) C6-14 aryl group optionally substituted by 1 to 5 substitutes chosen of a group consisting of (1) halogen atom, (2) cyano, (3) C1-6 alkoxy optionally having 1 to 3 halogen atoms, (4) C1-6 alkylthio optionally having 1 to 3 halogen atoms, (5) C1-6alkylcarbonyl, (6) C1-6 alkylsulphonyl, (7) C1-6 alkylthionyl, (8) C3-7 cycloalkyl, (9) C1-6 alkyl group optionally having 1 to 3 halogen atoms, and (10) C1-6 alkyl group substituted by 1 to 3 hydroxy, (ii) a thienyl group optionally substituted by 1 to 4 substitutes chosen from a group consisting of (1) cyano and (2) C1-6 alkyl group optionally having 1 to 3 halogen atoms, (iii) a pyridyl group optionally substituted by 1 to 4 substitutes chosen from a group consisting of (1) halogen atom, (2) 5-10-members aromatic heterocyclic group containing carbon atom, and 1 or 2 presentations of 1-4 heteroatoms chosen from nitrogen atom, sulphur atom and oxygen atom, and (3) C1-6 alkyl group optionally having 1 to 3 halogen atoms, or (iv) a bipyridyl group optionally substituted by 1 to 3 halogen atoms, each R3 and R4 represents hydrogen atom, or one of R3 and R4 represents hydrogen atom, and another represent a lower alkyl group, halogen atom or a cyanogroup, and R5 represents an alkyl group, or to its salt. Also, the invention refers to a pharmaceutical composition showing an acid secretion inhibitory effect enabled by the compound of formula I, to a method for treatment or prevention, besides, to application of the compound of formula I for preparing a pharmaceutical composition for treatment or prevention of a number of diseases presented in the patent claim.

EFFECT: preparation of the new compounds showing the acid secretion inhibitory effect and exhibiting antiulcerant action.

20 cl, 92 ex, 24 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a method for synthesis of novel 4-(1H-indol-3-yl)-but-3-en-2-one derivatives of general formula 3: , : which can be used in synthesis of novel preparations for pharmaceutical and agricultural purposes. The method involves mixing 2-alkyl-5-(2-amino-4-alkylphenyl)-furans 1 with aromatic and heteroaromatic aldehydes 2 in acetic acid in equimola ratio at temperature 35°C for 40 minutes in the presence of 0.01 ml hydrochloric acid.

EFFECT: improved method.

2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I: or its pharmaceutically acceptable salt or stereoisomer, where a is independently equal to 0 or 1; b is independently equal to 0 or 1; R1 is selected from aryl, heterocyclyl and NR10R11; said aryl or heterocyclyl group is optionally substituted with between one and five substitutes, each independently selected from R8; R5 is selected from C1-6alkyl, C2-6alkenyl, -C(=O)NR10R11, NHS(O)2NR10R11 and NR10R11, each alkyl, alkenyl or aryl is optionally substituted with between one and five substitutes, each independently selected from R8; R8 independently denotes (C=O)aObC1-C10alkyl, (C=O)aObaryl, (C=O)aObheterocyclyl, OH, Oa(C=O)bNR10R11 or (C=O)aCbC3-C8cycloalkyl, said alkyl, aryl, heterocyclyl are optionally substituted with one, two or three substitutes selected from R9; R9 is independently selected from (C=O)aCb(C1-C10)alkyl and N(Rb)2; R10 and R11 is independently selected from H, (C=O)Cb(C1-C10)alkyl, C1-C10alkyl, SO2Ra, said alkyl is optionally substituted with one, two or three substitutes selected from R8 or R10 and R11 can be taken together with nitrogen to which they are bonded with formation of a monocyclic heterocycle with 5 members in each ring and optionally contains one or two heteroatoms, in addition to the nitrogen, selected from N and S, said monocyclic heterocycle is optionally substituted with one, two or three substitutes selected from R9; Ra is independently selected from (C1-C6)alkyl, (C2-C6)alkenyl; and Rb is independently selected from H, (C1-C6)alkyd, as well as to a pharmaceutical composition for inhibiting receptor tyrosine kinase MET based on this compound, as well as a method of using said compound to produce a drug.

EFFECT: novel compounds which can be used to treat cell proliferative diseases, disorders associated with MET activity and for inhibiting receptor tyrosine kinase MET are obtained and described.

8 cl, 32 ex, 4 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

and pharmaceutically acceptable salts thereof, where substitutes R1-R4 are as defined in claim 1. Said compounds have 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) enzyme inhibiting activity.

EFFECT: compounds can be used in form of a pharmaceutical composition.

15 cl, 1 tbl, 94 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) and to its pharmaceutically acceptable additive salts, optionally in the form of stereochemical isomer and exhibiting anti-HIV antiviral activity, particularly having HIV inhibitor properties and applied as a drug. In formula , -a1=a2-a3=a4- represents a bivalent radical of formula -CH=CH-CH=CH-(a-1); -b1=b2-b3-b4 - represents a bivalent radical of formula -CH=CH-CH=CH- (b-1); n is equal to 0, 1, 2, 3, 4; m is equal to 0, 1, 2; each R1 independently represents hydrogen; each R2 represents hydrogen; R2a represents cyano; X1 represents -NR1-; R3 represents C1-6alkyl, substituted cyano; C2-6alkrnyl, substituted cyano; R4 represents halogen; C1-6alkyl; R5 represents 5 or 6-member completely unsaturated cyclic system where one, two or three members of the cycle represent heteroatoms, each independently specified from the group consisting of nitrogen, oxygen and sulphur and where the rest members of the cycle represent carbon atoms; and where 6-member cyclic system can be optionally annelated with a benzene cycle; and where any carbon atom in the cycle can be independently optionally substituted with a substitute specified from C1-6alkyl, amino, mono- and diC1-4alkylamino, aminocarbonyl, mono-and diC1-4alkylcarbonylamino, phenyl and Het; where Het represents pyridyl, thienyl, furanyl; Q represents hydrogen The invention also concerns a pharmaceutical composition.

EFFECT: preparation of the new anti-HIV antiviral compounds.

4 cl, 2 tbl, 22 ex

FIELD: medicine.

SUBSTANCE: compounds can be used for treating neurological conditions, more specifically for treating neurodegenerative conditions, such as Alzheimer's disease. In a compound of formula I R2 represents H or CH2NR1R4 where R1 and R4 are independently selected from H, unsubstituted C1-6alkyl, substituted or unsubstituted C3-6 cycloalkyl, R3 represents H; substituted or unsubstituted C1-4alkyl; substituted or unsubstituted C2-4alkenyl; substituted or unsubstituted 6-members aryl condensed or uncondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl, containing 1-2 nitrogen atoms in a cycle; substituted or unsubstituted saturated or unsaturated 5 or 6-members N-containing heterocycle which can additionally contain nitrogen, oxygen or the sulphur atom condensed or ucondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl containing nitrogen in a cycle; (CH2)nR6 where n is an integer from 1 to 6, and the values of R6 and the values of other radicals are specified in the patent claim.

EFFECT: increased antiamyloidogenic action.

20 cl, 20 tbl, 6 dwg, 7 ex

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