Cis-2,4,5-triarylimidazolines and use thereof as anticancer medicinal agents

FIELD: chemistry.

SUBSTANCE: present invention relates to novel derivatives of cis-2,4,5-triarylimidazoline of general formula I and pharmaceutically acceptable salts thereof, where X1 is selected from a group comprising lower alkoxy; X2 and X3 are independently selected from a group comprising hydrogen, halogen, cyano, lower alkyl, lower alkoxy, piperidinyl, -NX4X5, -SO2NX4X5, -C(O)NX4X5, -C(O)X6, -SOX6, -SO2X6, -NC(O)-lower alkoxy, -C≡C-X7, provided that both X2 and X3 do not denote hydrogen, lower alkyl or lower alkoxy, provided that when X2 or X3 denote hydrogen, the other does not denote lower alkyl, lower alkoxy or halogen, provided that when X2 denotes -HX4X5, X3 does not denote hydrogen, X2 and X3 together can form a ring selected from 5-7-member unsaturated rings which can contain three heteroatoms selected from S, N and O, X4 and X5 are independently selected from a group comprising hydrogen, lower alkyl, lower alkoxy, lower alkyl, substituted by a lower alkoxy, -SO2-lower alkyl, -C(O)piperazinyl-3-one; X6 is selected from a group comprising lower alkyl, morpholine, piperidine, pyrrolidine; X7 is selected from a group comprising hydrogen, lower alkyl, trifluoromethyl; Y1 and Y2 are independently selected from a group comprising halogen; R is selected from a group comprising lower alkoxy, piperidinyl substituted with a five-member heterocyclic ring which contains one nitrogen heteroatom, piperidinyl substituted with a hydroxy, -CH2OH or -C(O)NH2, piperazinyl substituted with one or two R1 [1,4]diazepanyl, substituted R1, R1 can denote one or two substitutes selected from a group comprising oxo, lower alkyl substituted with one R2, -C(O)R3, -SO2-lower alkyl, -SO2-five-memer heterocyclyl, which is selected from isoxazolyl, dimethylisoxazolyl, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolidinyl, imidazolidinyl; R2 is selected from a group comprising -SO2-lower alkyl, hydroxy, lower alkoxy, -NH-SO2-lower alkyl, -cyano, -C(O)R4; R3 is selected from a group comprising a five-member heterocyclyl which is selected from isoxazolyl, dimethylisoxazolyl, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolidinyl, imidazolidinyl, lower alkyl, lower alkenyl, lower alkyl substituted with a six-member heterocyclyl selected from piperidinyl, piperazinyl, 3-oxopiperazinyl, morpholinyl, C3-cycloalkyl; R4 is selected from a group comprising hydroxy, morpholine, piperidine, 4-acetylpiperazinyl, -NR5R6; R5 and R6 are independently selected from a group comprising hydrogen, lower alkyl, lower alkyl substituted with lower alkoxy or cyano, lower alkoxy and C3-cycloalkyl. The invention also relates to a pharmaceutical composition based on the formula I compound, use of the formula I compound in preparing a medicinal agent and a method for synthesis of the formula I compound.

EFFECT: novel derivatives of cis-2,4,5-triarylimidazoline of general formula I are obtained, which can be used to treat diseases, based on reaction of the MDM2 protein with p53-like protein, particularly as anticancer agent.

54 cl, 412 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula I:

and its pharmaceutically acceptable salts, where
X1selected from the group consisting of:
lower alkoxy;
X2and X3independently selected from the group consisting of:
hydrogen
halogen,
cyano,
lower alkyl,
lower alkoxy,
piperidinyl,
-NX4X5,
-SO2NX4X5,
-C(O)NX4X5,
-C(O)X6,
-SOX6, -SO2X6,
-NC(O)-lower alkoxy,
-C≡C-X7,
provided that X2and X3both represent hydrogen, lower alkyl or lower alkoxy,
provided that when X2or X3represents hydrogen, and the other represents lower alkyl, lower alkoxy or halogen,
provided that when X2represents-NX4X5, X3does not represent hydrogen,
X 2and X3may together form a ring selected from a 5-7-membered unsaturated rings containing three heteroatoms selected from S, N and O;
X4and X5independently selected from the group consisting of:
hydrogen
lower alkyl,
lower alkoxy,
lower alkyl, substituted lower alkoxy,
-SO2-lower alkyl,
-C(O)piperazinil-3-one;
X6selected from the group consisting of:
lower alkyl,
the research,
piperidine,
pyrrolidine;
X7selected from the group consisting of:
hydrogen
lower alkyl,
trifloromethyl;
Y1and Y2independently selected from the group consisting of:
halogen;
R is selected from the group consisting of:
lower alkoxy,
piperidinyl, substituted five-membered heterocycle containing one nitrogen heteroatom,
piperidinyl, substituted hydroxy, -CH2HE or-C(O)NH2,
the piperazinil substituted by one or two R1,
[1,4]diazepine, substituted R1,
R1can be a one or two substituent selected from the group consisting of:
oxo,
lower alkyl substituted with one R2,
-C(O)R3,
-SO2-lower alkyl,
-SO2-membered heterocyclyl selected from isoxazolyl, dimethylisoxazole, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolyl the Nile, imidazolidinyl;
R2selected from the group consisting of:
-SO2-lower alkyl, hydroxy, lower alkoxy,
-NH-SO2-lower alkyl,
is cyano,
-C(O)R4;
R3selected from the group consisting of:
five-membered heterocyclyl selected from isoxazolyl, dimethylisoxazole, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolidine, imidazolidine,
lower alkyl,
lowest alkenyl,
lower alkyl, substituted six-membered by heterocyclyl selected from piperidinyl, piperazinil, 3-oxopiperidine, morpholinyl,
With3-cycloalkyl;
R4selected from the group consisting of:
hydroxy,
the research,
piperidine,
4-acetylpiperidine,
-NR5R6;
R5and R6independently selected from the group consisting of:
hydrogen
lower alkyl,
lower alkyl, substituted lower alkoxy or cyano,
lower alkoxy and
With3-cycloalkyl.

2. The compound of formula I according to claim 1 and pharmaceutically acceptable salts, where
X1selected from the group consisting of:
lower alkoxy;
X2and X3independently selected from the group consisting of:
hydrogen
halogen,
cyano,
lower alkyl,
lower alkoxy,
-NX4X5,
-SO2NX4X5,
-C(O)NX4X5,
-C(O)X6,
-SOX6, -SO2 6,
-NC(O)-lower alkoxy,
-C≡C-X7,
provided that X2and X3both represent hydrogen, lower alkyl or lower alkoxy,
provided that when X2or X3represents hydrogen, and the other represents lower alkyl, lower alkoxy or halogen;
provided that when X2represents-NX4X5, X3does not represent hydrogen,
X2and X3may together form a ring selected from a 5-7-membered unsaturated rings containing three heteroatoms selected from S, N and O;
X4and X5independently selected from the group consisting of:
hydrogen
lower alkyl,
lower alkoxy,
lower alkyl, substituted lower alkoxy;
X6selected from the group consisting of:
lower alkyl,
the research,
piperidine,
pyrrolidine;
X7selected from the group consisting of:
hydrogen
lower alkyl,
trifloromethyl;
Y1and Y2independently selected from the group consisting of:
halogen;
R is selected from the group consisting of:
lower alkoxy,
piperidinyl, substituted five-membered heterocycle containing one nitrogen heteroatom,
piperidinyl, substituted hydroxy, -CH2HE or-C(O)NH2,
the piperazinil substituted by one or two R1,
[1,4]diazepine, substituted od what they R 1,
R1can be a one or two substituent selected from the group consisting of:
oxo,
lower alkyl substituted with one R2,
-C(O)R3,
-SO2is lower alkyl;
R2selected from the group consisting of:
-SO2-lower alkyl, hydroxy, lower alkoxy,
-NH-SO2-lower alkyl,
is cyano,
-C(O)R4;
R3selected from the group consisting of:
five-membered heterocyclyl selected from isoxazolyl, dimethylisoxazole, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolidine, imidazolidine,
lower alkyl;
R4selected from the group consisting of:
hydroxy,
the research,
piperidine,
-NR5R6;
R5and R6independently selected from the group consisting of:
hydrogen
lower alkyl,
lower alkyl, substituted lower alkoxy or cyano, and
lower alkoxy.

3. The compound according to claim 1 or 2, where two of the hydrogen atom of the imidazoline ring are in the CIS-configuration relative to each other.

4. The compound according to claim 1 or 2, where Y1and Y2selected from-Cl, or-Br.

5. The compound according to claim 4, where X1represents ethoxy or isopropoxy.

6. The compound according to claim 5, where X2represents halogen, cyano, -SO2NX4X5, -C(O)NX4X5-C(O)X6, -SO2X6or Is The C-X 7.

7. The connection according to claim 6, where X3represents-SO2NX4X5, -C(O)NX4X5or-SO2X6.

8. The connection according to claim 7, where R is a piperazinil, substituted by oxo or lower alkyl, substituted R2where R2represents-SO2-lower alkyl or-C(O)R4.

9. The compound according to claim 1, selected from the group consisting of the following compounds:
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N,N-dimethylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxybenzaldehyde;
4-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
4-{4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-[4,5-bis-(4-chlorophenyl)-1-(4-pyrrolidin-1-reparacin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
3-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbon is l)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzenesulfonamide and
3-[4,5-bis-(4-chlorophenyl)-1-(4-pyrrolidin-1-reparacin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-dimethylbenzenesulfonamide.

10. The compound according to claim 1, selected from the group consisting of the following compounds:
5-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxy-N,N-dimethylbenzenesulfonamide;
5-{4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N,N-dimethylbenzenesulfonamide;
5-{4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)-3-oxopiperidin-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-dimethylbenzenesulfonamide;
5-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2-methoxy-N,N-dimethylbenzenesulfonamide;
5-{4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-methoxy-N,N-dimethylbenzenesulfonamide;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
5-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-methoxy-N-dimethylbenzenesulfonamide;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-meanswhen later)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N,N-dimethylbenzenesulfonamide and
4-[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-it.

11. The compound according to claim 1, selected from the group consisting of the following compounds:
4-[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-he;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-dimethylacetamide;
[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-yl]-[4-(2-hydroxyethyl)piperazine-1-yl]metano;
[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-methanesulfonyl)-4,5-dihydroimidazole-1-yl]-[4-(2-hydroxyethyl)piperazine-1-yl]metano;
amide 1-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperidine-4-carboxylic acid;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol the-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile and
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-cyclopropanecarbonyl-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile.

12. The compound according to claim 1, selected from the group consisting of the following compounds:
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methylbut-2-enoyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-sulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-cyanoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methoxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-((4S,5R)-4,5-bis-(4-chlorophenyl)-1-{4-[2-(3-oxopiperidin-1-yl)acetyl]piperazine-1-carbonyl}-4,5-dihydro-1H-imidazol-2-yl)-3-ethoxybenzonitrile;
amide 1-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperidine-3-carboxylic acid;
4-[(4S,5R)-1-{4-[2-(4-acetylpiperidine-1-yl)-2-oxoethyl]piperazine-1-carbonyl}-4,5-bis-(4-chlorophenyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-methoxy-1-methylethyl)ndimethylacetamide and
4-[(4S,5R)-4,5-bis-(4-chlorphen is)-1-(4-hydroxyethylpiperazine-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile.

13. The compound according to claim 1, selected from the group consisting of the following compounds:
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-hydroxypiperidine-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-oxo-2-piperidine-1-retil)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxybenzonitrile;
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
amide 1-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperidine-4-carboxylic acid;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-dimethylbenzenesulfonamide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-cyclopropanecarbonyl-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(3-methylbut-2-enoyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-dimethylbenzenesulfonamide and
3-{4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-sulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzenesulfonamide.

3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-cyanoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methoxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-(4,5-bis-(4-chlorophenyl)-1-{4-[2-(3-oxopiperidin-1-yl)acetyl]piperazine-1-carbonyl}-4,5-dihydro-1H-imidazol-2-yl)-4-ethoxy-N,N-dimethylbenzenesulfonamide;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methylacetamide;
amide 1-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperidine-3-carboxylic acid;
3-[1-{4-[2-(4-acetylpiperidine-1-yl)-2-oxoethyl]piperazine-1-carbonyl}-4,5-bis-(4-chlorophenyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-dimethylbenzenesulfonamide;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-hydroxyethylpiperazine-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-dimethylbenzenesulfonamide;
3-[4,5-bis-(4-chlorophenyl)-1-(3-hydroxypiperidine-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-dimethylbenzenesulfonamide and
2-{4-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazo the ol-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide.

15. The compound according to claim 1, selected from the group consisting of the following compounds:
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-oxo-2-piperidine-1-retil)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-dimethylbenzenesulfonamide;
3-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(isobutylmethylxanthine)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-dimethylacetamide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide;
3-(4,5-bis-(4-chlorophenyl)-1-{4-[2-(3-oxopiperidin-1-yl)acetyl]piperazine-1-carbonyl}-4,5-dihydro-1H-imidazol-2-yl)-4-ethoxy-N-isobutyl-H-methylbenzenesulfonamide;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(isobutylmethylxanthine)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide and
3-{4,5-bis-(4-chloro who enyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide.

16. The compound according to claim 1, selected from the group consisting of the following compounds:
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(isobutylmethylxanthine)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methylacetamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-cyclopropanecarbonyl-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methoxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-isobutyl-N-methylbenzenesulfonamide;
3-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-bis-(2-methoxyethyl)benzosulfimide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-bis-(2-methoxyethyl)benzosulfimide;
2-{4-[2-{5-[bis-(2-methoxyethyl)sulfamoyl]-2-ethoxyphenyl}-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
3-(4,5-bis-(4-chlorophenyl)-1-{4-[2-(3-oxopiperidin-1-yl)acetyl]piperazine-1-carbonyl}-4,5-dihydro-1H-imidazol-2-yl)-4-ethoxy-N,N-bis-(2-methoxyethyl)benzosulfimide;
2-{4-[2-{5-[bis-(2-methoxyethyl)sulfamoyl]-2-ethoxyphenyl}-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-methoxy-1-mutilat the l)ndimethylacetamide and
2-{4-[2-{5-[bis-(2-methoxyethyl)sulfamoyl]-2-ethoxyphenyl}-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methylacetamide.

17. The compound according to claim 1, selected from the group consisting of the following compounds:
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-bis-(2-methoxyethyl)benzosulfimide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-cyclopropanecarbonyl-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-bis-(2-methoxyethyl)benzosulfimide;
4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-he;
{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-dimethylacetamide;
{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-(4-acanaloniidae-1-yl)methanon;
4-[2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-2-oxoethyl]piperazine-2-he;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-hydroxyethyl)piperazine-1-yl]metano;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methylacetamide and
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ylatason.

18. The compound according to claim 1, selected from the group consisting of the following compounds:
{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-(4-cyclopropanecarbonyl-1-yl)methanon;
3-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-methoxy-1-methylethyl)benzosulfimide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-ethoxy-N-(2-methoxy-1-methylethyl)benzosulfimide;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(2-methoxy-1-methylaminoethanol)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-dimethylacetamide;
3-[4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-(2-methoxy-1-methylethyl)benzosulfimide;
3-(4,5-bis-(4-chlorophenyl)-1-{4-[2-(3-oxopiperidin-1-yl)acetyl]piperazine-1-carbonyl}-4,5-dihydro-1H-imidazol-2-yl)-4-ethoxy-N-(2-methoxy-1-methylethyl)benzosulfimide;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(2-methoxy-1-methylaminoethanol)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)are the amide;
3-{4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-(2-methoxy-1-methylethyl)benzosulfimide;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(2-methoxy-1-methylaminoethanol)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methylacetamide and
4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it.

19. The compound according to claim 1, selected from the group consisting of the following compounds:
{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-dimethylacetamide;
4-[2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-2-oxoethyl]piperazine-2-he;
2-(4-{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
{4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-hydroxyethyl)piperazine-1-yl]metano;
5-[4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2-fluoro-N,N-dimethylbenzenesulfonamide;
5-{4,5-bis-(4-chlorophenyl)-1-[4-(2-hydroxyethyl)piperazine-1-carbon is l]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-fluoro-N,N-dimethylbenzenesulfonamide;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxy-4-forfinal)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
5-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-fluoro-N,N-dimethylbenzenesulfonamide and
4-[4,5-bis-(4-chlorophenyl)-2-(7-ethoxy-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[b][1,4,5]oxathiazin-8-yl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-it.

20. The compound according to claim 1, selected from the group consisting of the following compounds:
[4,5-bis-(4-chlorophenyl)-2-(7-ethoxy-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[b][1,4,5]oxathiazin-8-yl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
2-{4-[4,5-bis-(4-chlorophenyl)-2-(7-ethoxy-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[b][1,4,5]oxathiazin-8-yl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-1-morpholine-4-ylatason;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxy-4-forfinal)-4,5-dihydroimidazole-1-carbonyl] piperazine-1-yl}-N,N-dimethylacetamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-fluoro-N,N-dimethylbenzenesulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-fluoro-N,N-dimethylbenzenesulfonamide;
hydrochloride 4-[4,5-bis-(chlorphenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxy-N-dimethylbenzenesulfonamide;
hydrochloride 4-{4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 4-{4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride of 2-{4-[4,5-bis-(4-chlorophenyl)-2-(4-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide and
4-[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-5-methanesulfonyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-it.

21. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride [4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-5-methanesulfonyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-{4-[4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-5-methanesulfonyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-1-morpholine-4-ratanana;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-cyano-4-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-cyano-4-ethoxy-N,N-xylene is sulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-cyano-4-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-methoxybenzonitrile;
hydrochloride 5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2-methoxybenzonitrile;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-methoxybenzonitrile and
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide.

22. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-methoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzamide;
hydrochloride 3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N,N-dimethylbenzamide;
hydrochloride 3-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-occupier the Jn-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N,N-dimethylbenzamide;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(pyrrolidin-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(morpholine-4-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana.

23. The compound according to claim 1, selected from the group consisting of the following compounds:
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2-fluoro-N,N-dimethylbenzenesulfonamide;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride [(4S,5R)-2-[4-chloro-2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-{4-[(4S,5R)-2-[4-chloro-2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl] piperazine-1-yl}-1-morpholine-4-ratanana;
hydrochloride [(4S,5R)-2-[4-chloro-2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride 4-[(4S,5R)-2-[4-chloro-2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-it;
hydrochloride of 2-{4-[(4S,5R)-2-[4-chloro-2-ethoxy-5-(morpholine-4-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-1-morpholine-4-ratanana;
hydrochloride [(4S,5R)-2-[4-chloro-2-ethoxy-5-(morpholine-4-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride 4-[(4S,5R)-2-[4-chloro-2-ethoxy-5-(morpholine-4-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-it
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone.

24. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorphen is)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it;
hydrochloride of 2-{4-[(4S,5R)-2-[4-chloro-2-ethoxy-5-(pyrrolidin-1-sulfonyl)phenyl]-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-1-morpholine-4-ratanana;
hydrochloride 4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxy-N,N-dimethylbenzenesulfonamide and
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxy-N,N-dimethylbenzenesulfonamide.

25. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-dimethylsulphamoyl-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-dimethylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-tert-butylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-cyanomethyl-N-methylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-cyclopropylacetic;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-methoxyethyl)ndimethylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methoxy-N-methylacetamide;
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide and
2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(4-cyano-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-cyanoethyl)-N-methylacetamide.

26. The compound according to claim 1, selected from the group consisting of the following compounds:
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxo-[1,4]diazepan-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzonitrile;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-fter-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-he;
1-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-fluoro-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}-[1,4]diazepan-5-he;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-fluoro-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-fluoro-5-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(morpholine-4-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone.

27. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(pyrrolidin-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-CT is of IMT}piperazine-1-yl)-1-morpholine-4-ratanana;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-2,N-dimethylbenzenesulfonamide;
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2,5-diethoxybenzene;
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(5-oxo-[1,4]diazepan-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2,5-diethoxybenzene;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2,5-diethoxybenzene;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2,5-diethoxybenzene;
hydrochloride 4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)-4-piperidine-1-ylphenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-it;
hydrochloride of 1-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)-4-piperidine-1-ylphenyl]-4,5-dihydroimidazole-1-carbonyl}-[1,4]diazepan-5-it;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)-4-piperidine-1-ylphenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone and
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)-4-piperidine-1-ylphenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana.

28. The compound according to claim 1, selected from the group consisting exploring the connections:
the hydrochloride of the ethyl ester of 4,5-bis-(4-chlorophenyl)-2-(4-dimethylamino-5-dimethylsulphamoyl-2-ethoxyphenyl)-4,5-dihydroimidazole-1-carboxylic acid;
hydrochloride 5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-dimethylamino-4-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-dimethylamino-4-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(5-oxo-[1,4]diazepan-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-dimethylamino-4-ethoxy-N,N-dimethylbenzenesulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-dimethylamino-4-ethoxy-N,N-dimethylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxybenzonitrile;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-isopropyl-2-methylbenzenesulfonamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-isopropyl-2-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethylbenzenesulfonamide and
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethylbenzenesulfonamide.

29. The compound according to claim 1, selected from the group consisting of the following compounds:
[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2,N-dimethylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxybenzonitrile;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxybenzonitrile;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-dimethylamino-4-ethoxybenzonitrile;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-dimethylamino-4-ethoxybenzonitrile;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-isopropyl-2-methylbenzenesulfonamide;
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-he;
1-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]-[1,4]diazepan-5-he;
hydrochloride [(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]meth is Nona and
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-1-morpholine-4-ratanana.

30. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride 5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-N-tert-butyl-2-chloro-4-ethoxybenzaldehyde;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxybenzaldehyde;
N-tert-butyl-2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-sulfamoylbenzoyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxybenzaldehyde;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxybenzaldehyde;
2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-sulfamoylbenzoyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-sulfamoylbenzoyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxybenzaldehyde;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methansulfonate)p is perazin-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-3-ethoxybenzene and
N-tert-butyl-4-[(4S,5R)-l-(4-carbamoyltransferase-1-carbonyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxybenzene.

31. The compound according to claim 1, selected from the group consisting of the following compounds:
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-yl]metano;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ylatason;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide;
4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-2-he;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-(piperidine-1-carbonyl)phenyl]-4,5-dihydroimidazole-1-yl}-(4-acanaloniidae-1-yl)methanon;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)Pipa is Azin-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-methylbenzenesulfonamide and
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-isopropylbenzenesulfonyl.

32. The compound according to claim 1, selected from the group consisting of the following compounds:
2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-isopropylaminoethyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-isopropylaminoethyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxy-N-isopropylbenzenesulfonyl;
N-tert-butyl-2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-methylsulfinylphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxy-N-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-methylbenzenesulfonamide;
2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-methylsulfinylphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-methylsulfinylphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
5-[(4S,5R)-4,5-bis-(4-chloro who enyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxy-N-methylbenzenesulfonamide and
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-isopropylbenzenesulfonyl.

33. The compound according to claim 1, selected from the group consisting of the following compounds:
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-2-chloro-4-ethoxy-N-isopropylbenzenesulfonyl;
N-tert-butyl-2-{4-[(4S,5R)-2-(4-chloro-2-ethoxy-5-isopropylaminoethyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-2-chloro-4-ethoxy-N-isopropylbenzenesulfonyl;
N-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxyphenyl}-N-(3-oxopiperidin-1-carbonyl)methanesulfonamide;
the hydrochloride of N-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxyphenyl)methanesulfonamide;
N-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxyphenyl}-2,2-dimethylpropanamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(3-oxopiperidin-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2-ethinyl-N,N-dimethylbenzenesulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-ethinyl-,N-dimethylbenzenesulfonamide;
hydrochloride 5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2-ethinyl-N,N-dimethylbenzenesulfonamide and
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(5-dimethylsulphamoyl-2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide.

34. The compound according to claim 1, selected from the group consisting of the following compounds:
the hydrochloride of N-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxyphenyl)-2,2-dimethylpropanamide;
the hydrochloride of N-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-dimethylcarbamodithioato-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-3-ethoxyphenyl}-2,2-dimethylpropanamide;
the hydrochloride of N-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxyphenyl)-2,2-dimethylpropanamide;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-tert-butylacetamide;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methoxy-N-methylacetamide;
the hydrochloride of N-(2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ethyl)methanesulfonamide;
[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethinyl enyl)-4,5-dihydroimidazole-1-yl]-(4-acanaloniidae-1-yl)methanon;
hydrochloride [(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-yl]-[4-(2-methoxyethyl)piperazine-1-yl]methanone;
1-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}Etalon and
hydrochloride 3-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}propionitrile.

35. The compound according to claim 1, selected from the group consisting of the following compounds:
hydrochloride [(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
hydrochloride 3-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-ethynylphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}propionic acid;
4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-Cryptocom-1-initfini)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-he;
hydrochloride [(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-Cryptocom-1-initfini)-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-Cryptocom-1-initfini)-4,5-dihydroimidazole--carbonyl]piperazine-1-yl}-1-morpholine-4-ratanana;
hydrochloride of 2-{4-[(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-Cryptocom-1-initfini)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide and
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide.

36. The compound according to claim 1, selected from the group consisting of the following compounds:
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methoxy-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-cyanoethyl)-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-Sul is the IMT)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-yl]metano;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-(4-acanaloniidae-1-yl)methanon;
N-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ethyl]methanesulfonamide;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methyl-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3-methanesulfonyl)piperazine-1-yl]metano and
N-tert-butyl-2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide.

37. The compound according to claim 1, selected from the group consisting of the following compounds:
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methoxy-N-methylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-arbonyl]piperazine-1-yl}-N-(2-cyanoethyl)-N-methylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-were)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methylbenzenesulfonamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-N-tert-butyl-N-ethoxy-2-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonylaminoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methylbenzenesulfonamide and
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methylbenzenesulfonamide.

38. The compound according to claim 1, selected from the group consisting of the following compounds:
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methylbenzenesulfonamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)-4-were]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methox methylsulfonyl)-4-were]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)-4-were]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)-4-were]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methoxy-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)-4-were]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)-4-were]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-2,N-dimethylbenzenesulfonamide and
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-methoxy-2,N-dimethylbenzenesulfonamide.

39. The compound according to claim 1, selected from the group consisting of the following compounds:
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-2,N-dimethylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-2,N-dimethylbenzenesulfonamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-e is hydroxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methoxy-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-cyanoethyl)-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide and
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-yl]metano.

40. The compound according to claim 1, selected from the group consisting of the following compounds:
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-(4-acanaloniidae-1-yl)methanon;
N-[2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-labels and-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ethyl]methanesulfonamide;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3-methanesulfonyl)piperazine-1-yl]metano;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]metano;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ylatason;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methoxy-N-methylacetamide and
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide.

41. The compound according to claim 1, selected from the group consisting of the following compounds:
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(meth who climatically)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-cyanoethyl)-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-4-methoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethoxy-N-methylbenzenesulfonamide;
5-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-2,N-dimethoxy-N-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonylaminoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethoxy-N-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethoxy-N-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethoxy-N-methylbenzenesulfonamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-2,N-dimethoxy-N-methylbenzenesulfonamide;
4-[(4S,5R)-2-(4-acetyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-2-he
hydrochloride of 1-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxyphenyl)ethanone.

42. The compound according to claim 1, selected the second group, consisting of the following compounds:
hydrochloride of 2-{4-[(4S,5R)-2-(4-acetyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-1-morpholine-4-ratanana;
hydrochloride of 1-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-3-ethoxyphenyl)ethanone;
hydrochloride [(4S,5R)-4,5-bis-(4-chlorophenyl)-2-(2-ethoxy-4-Cryptocom-1-initfini)-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)piperazine-1-yl]methanone;
N-tert-butyl-2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methoxy-N-methylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-cyanoethyl)-N-methylacetamide and
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-atok iphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-(2-methoxy-1-methylethyl)ndimethylacetamide.

43. The compound according to claim 1, selected from the group consisting of the following compounds:
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxybenzaldehyde;
3-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-N-tert-butyl-4-ethoxybenzaldehyde;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonylaminoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxybenzaldehyde;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxybenzaldehyde;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxybenzaldehyde;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxybenzaldehyde;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-bis-(2-metakit the l)ndimethylacetamide and
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methoxy-N-methylacetamide.

44. The compound according to claim 1, selected from the group consisting of the following compounds:
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-cyanoethyl)-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-yl]metano;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-(4-acanaloniidae-1-yl)methanon;
N-[2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ethyl]methanesulfonamide;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(3-methanesulfonyl)piperazine-1-yl]metano;
{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methansulfonate)PI is erasin-1-yl]metano;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(piperidine-1-sulfonyl)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ylatason and
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-tert-butylacetamide.

45. The compound according to claim 1, selected from the group consisting of the following compounds:
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N,N-bis-(2-methoxyethyl)ndimethylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-methoxy-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-isopropyl-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-cyanoethyl)-N-methylacetamide;
2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[2-ethoxy-5-(methoxymethylethoxy)phenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-N-(2-methoxy-1-methylethyl)ndimethylacetamide;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3,5-dimethylisoxazol-4-carbonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl-4-ethoxy-N-methoxy-N-methylbenzenesulfonamide;
3-[(4S,5R)-4,5-bis-(4-chlorophenyl)-1-(4-acanaloniidae-1-carbonyl)-4,5-dihydro-1H-imidazol-2-yl]-4-ethoxy-N-methoxy-N-methylbenzenesulfonamide;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonylaminoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-N-methylbenzenesulfonamide and
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-N-methylbenzenesulfonamide.

46. The compound according to claim 1, selected from the group consisting of the following compounds:
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-N-methylbenzenesulfonamide;
3-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-morpholine-4-yl-2-oxoethyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-4-ethoxy-N-methoxy-N-methylbenzenesulfonamide;
hydrochloride {(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[4-(3,3-dimethylbutan-1-inyl)-2-ethoxyphenyl]-4,5-dihydroimidazole-1-yl}-[4-(2-methanesulfonyl)piperazine-1-yl]methanone;
hydrochloride of 2-(4-{(4S,5R)-4,5-bis-(4-chlorophenyl)-2-[4-(3,3-dimethylbutan-1-inyl)-2-ethoxyphenyl]-4,5-dihydroimidazole-1-carbonyl}piperazine-1-yl)-1-morpholine-4-ratanana;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-methoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
N-tert-butyl-2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-methoxyphenyl)-4,5-bis-(4-chlorphen is)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}ndimethylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-methoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-methoxy-N-methylacetamide;
2-{4-[(4S,5R)-2-(5-tert-butylsulfonyl-2-ethoxy-4-methoxyphenyl)-4,5-bis-(4-chlorophenyl)-4,5-dihydroimidazole-1-carbonyl]piperazine-1-yl}-N-isopropyl-N-methylacetamide;
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(3-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methoxybenzenesulfonamide and
5-{(4S,5R)-4,5-bis-(4-chlorophenyl)-1-[4-(2-methanesulfonyl)piperazine-1-carbonyl]-4,5-dihydro-1H-imidazol-2-yl}-N-tert-butyl-4-ethoxy-2-methoxybenzenesulfonamide.

47. The compound of formula I according to claim 1, where
X1represents ethoxy;
Y1and Y2both represent-Cl;
R represents piperazinil substituted by one or two R1;
and the remaining substituents have the meanings given in claim 1.

48. The compound according to claim 2, where
X1represents ethoxy;
Y1and Y2both represent-Cl;
R represents piperazinil substituted by one or two R1;
and the remaining substituents have the meanings given in claim 2.

49. Connection p, where
Y1and Y2both represent-Cl;
X1represents ethoxy;
X2represents halogen, cyano, -SO2NX4X5, -C(O)NX4X5-C(O)X 6, -SO2X6or-C≡C-X7;
X3represents-SO2NX4X5, -C(O)NX4X5or-SO2X6;
R represents piperazinil substituted by one or two R1;
and the remaining substituents have the meanings given in claim 2.

50. The pharmaceutical composition intended for the treatment of diseases based on the interaction of MDM2 protein with a p53-like protein, comprising at least one compound of formula I according to claim 1 or 2, together with pharmaceutically acceptable adjuvants.

51. The compound according to claim 1 or 2 for the manufacture of a medicinal product intended for the treatment of diseases based on the interaction of MDM2 protein with a p53-like protein, in particular anti-cancer drugs.

52. The use of compounds according to claim 1 or 2 for the manufacture of medicines for the treatment of cell proliferative disorders, based on the interaction of MDM2 protein with a p53-like protein, in particular solid tumors.

53. The use of the compounds according to paragraph 52, for the manufacture of medicinal products intended for the treatment of tumors of the breast, colon, lung and prostate.

54. The method of obtaining the compounds of formula I according to claim 1, where
a) compound of formula 1:

subjected to reaction with a compound of formula 2:
,
in the presence of a catalyst, in particular trimethylaluminum, obtaining the compounds of formula 3:
,
b) the compound of formula 3 is then subjected to reaction in the presence of phosgene and a base, particularly triethylamine, to obtain the racemic mixture of compounds of formula enantiomer-5A" and "enantiomer-5V":
;
C) the specified connection formula "enantiomer-5A highlights from the specified racemic mixture of chiral chromatography and then subjected to reaction in the presence of an amine, substituted by a group R as defined in claim 1, to obtain the compounds of formula I according to claim 1,
g) the compound of the formula I according to claim 1 isolated from the reaction mixture and, if necessary, converted into its pharmaceutically acceptable salt; and
R, Y1, Y2X1, X2and X3have the meanings indicated in claim 1; and Z represents lower alkyl.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I), where R1 denotes a 5- or 6-member ring of formulae

(II) or (III), respectively: R2 denotes H, C1-C7-alkyl, C3-C6-cycloalkyl or -(CH2)m,-Ra; R3 denotes aryl or heteroaryl, which can be substituted with CN, Cl, F, Br, CF3, CHF2, C3-C6-cycloalkyl or denotes heteroaryl which can be possibly substituted with C1-C7-alkyl; R4 denotes H, -OH, Cl, F, Br, CN, -CHF2, CF3, C1-C7-alkyl, C3-C6-cycloalkyl or -(CH2)m-Re; R5 denotes C1-C7-alkyl, -(CH2)n-O-Rf, or -(CH2)n-Re; Ra denotes -OH; Re denotes -OH; Rf denotes C1-C7-alkyl; m equals 1-4; n equals 2-6; and pharmaceutically acceptable salts thereof. The invention also relates to a medicinal agent containing said derivatives, use thereof in preparing medicinal agents suitable for treating diseases of the central nervous system.

EFFECT: novel compounds suitable for treating diseases of the central nervous system are obtained and described.

29 cl, 111 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel antibacterial compounds of formula (I). Compounds of formula (I) Q-NH-CO-R3, where Q stands for group of the following structure , R1 represents hydrogen, halogen, hydroxy, amino, mercapto, alkyl, heteroalkyl, alkeloxy, heteroalkyloxy, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, cycloalkyloxy, alkylcycloalkyloxy, heterocycloalkyloxy or heteroalkylcycloalkyloxy, X1, X2, X3, X4, X5 and X6 each independently on each other represent nitrogen atom or group of formula CR2, R2 represents hydrogen, halogen or hydroxy, amino, alkyl, alkenyl, alkinyl or heteroalkyl group, R3 is selected from the following groups R5 represents group of formula -B-Y, where B represents alkylene, alkenylene, alkinylene, -NH- or heteroalkylene, and Y represents aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl or heteroalkylcycloalkyl, or their pharmaceutically acceptable salt, solvate, hydrate or pharmaceutically acceptable composition, as well as to pharmaceutical composition, which possesses antibacterial activity, based on said compounds and to their application for preparation of medication, intended for treatment of bacterial infections.

EFFECT: obtained and described are compounds, which can be useful in medicine.

9 cl, 147 ex

FIELD: chemistry.

SUBSTANCE: described are novel derivatives of genera formula (1) (where A denotes an oxygen or sulphur atom, -CH2- or -NH- group; R1 denotes C1-6alkyl group, possibly substituted ; R1A denotes a hydrogen atom or a C1-6 alkyl group; or these two radicals together with a carbon atom to which they are bonded form a cyclic C3-6 alkyl group; R2 denotes a C1-6 alkyl group or a C3-6 cycloalkyl group; R3 denotes an aryl group or a heteroaryl group, which can be substituted; R4 denotes a hydrogen atom; R5 denotes C1-6 alkyl group, aryl or heteroaryl group, which can be substituted), a pharmaceutical composition containing said derivatives and intermediate compounds. Said compounds (1) can inhibit bonding between SIP and its receptor Edg-1 (SIP1).

EFFECT: possibility of use in medicine.

18 cl, 2 tbl, 28 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to new compounds of formula (1) or its pharmaceutically acceptable salts, with properties of antagonist CXCR2 of human neutrophils receptor. In formula (1) R1 represents a group selected from C1-8alkyl; where this group is possibly substituted with 1 substituent, independently selected from phenyl or 5-6-unit heteroaryl, containing 1-2 heteroatoms selected from N, S; where phenyl and heteroaryl are possibly substituted by 1, 2 or 3 substitutors, independently selected from halogeno, cyano, -OR4, -COOR7, -SO2R10, C1-6alkyl; X represents -CH2-, oxygen, sulfur; R2 represents C3-7carbocyclil, possibly substituted with 1, 2 or 3 substituents, independently selected from -OR4; or R2 represents 5-unit ring, containing 2 heteroatoms, selected from O, -NR8, and where this ring is possibly substituted with 1 substituent, independently selected from C1-3alkyl; or R2 represents group, selected from C1-8alkyla, where this group is substituted with 1, 2 or 3 substituents, independently selected from hydroxy, amino, C1-6alkoxy, C1-6alkylamino, di(C1-6alkyl)amino, N-C1-6alkylcarbamoyl, N,N-di(C1-6alkyl)carbamoyl, carboxy, -NR8COR9 and -CONR5R6; R3 represents group -NR5R6, or R3 represents phenyl, possibly condensed with 6-unit heterocyclil, containing nitrogen, naphthyl, 4-8-unit monocyclic heterocyclil, containing 1-3 heteroatoms, selected from N, O, S, possibly condensed with benzole ring or 3-unit nitrogen-containing ring, where heteroring may be non-saturated, partially or fully saturated, and one or more than one circular atom of carbon may form carbonyl group, and where each phenyl or heterocyclil group is possibly substituted with 1, 2 or 3 substituents, independently selected from halogeno, cyano, phenyl, 5-6-unit heteroaryl, containing 1-2 atoms of nitrogen, -OR4, -NR5R6, -CONR5R6, -COR7, -COR20, -COOR7, -NR8COR9, -SO2R10, -SO2NR5R6 or C1-6alkyl [possibly additionally substituted with 1, 2 or 3 substituents, independently selected from halogeno, cyano, -OR20, -COOR20, -NR18R19, -CONR18R19, phenyl or 5-6-unit of monocyclic heteroaryl, containing 1-2 heteroatoms O, N, S, or 10-unit bicyclic heteroaryl, containing 1 heteroatom O, where heteroring may be partially or fully saturated, and where each phenyl or heteroaryl is group possibly substituted with 1 or 2 substituents, independently selected from halogeno, cyano, nitro, -OR20, -NR5R6, -COOR7, -NR8COR9, 6-unit heterocyclil, containing two heteroatoms, selected from O and N, 5-unit heteroaryl, containing 3 heteroatoms N, C1-6alkyl (possibly additionally substituted with 1 substituent, independently selected from halogeno, cyano, nitro, -OR20, -COOR20; or R3 represents group, selected from C3-7carbocyclil, C1-8alkyl, where this group is possibly substituted with 1, 2 or 3 substituents, independently selected from halogeno, -OR4, -NR5R6; R4 represents hydrogen; R5 and R6 independently represent hydrogen or group, selected from C1-6alkyl and monocyclic 6-unit saturated heterocyclil containing 1 heteroatom N; where C1-6alkyl is possibly substituted with 1 substituent, independently selected from -NR15R16; or R5 and R6 together with atom of nitrogen, to which they are linked, form 4-7-unit saturated heterocyclic circukar system, possibly containing additional heteroatom, selected from oxygen, -SO(n)- (where n equals 0, 1 or 2) and atoms of nitrogen; R10 represents hydrogen or group, selected from C1-6alkyl; and each of R7, R8, R9, R15, R16, R17 independently represents hydrogen, C1-6alkyl; R18, R19 and R20 represent hydrogen or group, selected from C1-6alkyl, where this group is possibly substituted with 1 substituent, independently selected from -NR8R9, -CONR8R9.

EFFECT: production of new compounds, which may find application in production of medicinal agent for use in treatment of diseases and disorders mediated with chemokines, such as asthma, allergic rhinitis, chronic obstructive pulmonary disease, inflammatory intestine disease, irritable colon syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis or psoriasis, and also for treatment of cancer.

12 cl, 155 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: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds with common formulae I, II, IV and V: (I), (III), (IV), (V), values of radicals, such as provided in invention formula. Besides, proposed invention relates to pharmaceutical composition on the basis of above-described compounds, to their application, and also to method for treatment of repeated urination, incontinence and higher activity of urinary bladder, besides, to method to treat pain.

EFFECT: new compounds have been produced and described, which may be useful for treatment of diseases related to fatty-acid amide-hydrolase (FAAH), in particular to treat repeated urination and incontinence, higher activity of bladder and/or pain.

16 cl, 442 ex, 73 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds with common formulae I, II, IV and V: (I), (III), (IV), (V), values of radicals, such as provided in invention formula. Besides, proposed invention relates to pharmaceutical composition on the basis of above-described compounds, to their application, and also to method for treatment of repeated urination, incontinence and higher activity of urinary bladder, besides, to method to treat pain.

EFFECT: new compounds have been produced and described, which may be useful for treatment of diseases related to fatty-acid amide-hydrolase (FAAH), in particular to treat repeated urination and incontinence, higher activity of bladder and/or pain.

16 cl, 442 ex, 73 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrazine-2-carboxamide derivatives of general

formula , where R1 denote a 5- or 6-member ring, having a formula given in claim 1, R2 denotes H or C1-C7-alkyl; R3 denotes phenyl, pyridinyl or pyrimidinyl, possibly substituted with the following substitutes: Cl, F or Br; R4 denotes H, CI, F, Br, CF3 or C1-C7-alkyl; R5 denotes C1-C7-alkyl; as well as pharmaceutically acceptable salts thereof. Disclosed compounds are metabotropic glutamate receptor (mGLUR 5) antagonists. The invention also pertains to a medicinal agent based on disclosed compounds.

EFFECT: improved method.

17 cl, 23 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula I and to its pharmaceutically acceptable salts. In formula I , R1 means hydrogen or ; is specified from phenyl, and a 5-member heteroaromatic ring containing 1 to 2 heteroatoms specified inhe group consisting of sulphur and nitrogen; X is specified from lower alkylene, cyclisated lower alkylene containing 3 to 6 carbon atoms, and hydroxy(lower alkylene); R5 and R6 are independently specified in the group including hydrogen, lower alkyl, halogen and lower alkoxygroup; R3 is specified from hydrogen and -NH-R7; R4 is specified from hydrogen and -O(CH2CH2O)y-R10; R7 means lower alkyl; R10 means lower alkyl; n means an integer within 0 to 1; and y is equal to 0; provided when n is equal to 0, and R1 means hydrogen, then R3/R4 both cannot mean hydrogen. The invention also concerns a pharmaceutical composition containing a therapeutically effective amount of the compound under the invention.

EFFECT: preparation of the new compounds which show CDK1 kinase inhibiting activity and can be effective in cancer treatment, particularly breast cancer, lung cancer, colon cancer and prostate cancer treatment.

45 cl, 21 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula I and to its pharmaceutically acceptable salts. In formula I , Y means -S- or -NH-; R1 is specified from hydrogen, -C(O)O-[CH2CH2O]P-R4, -C(O)-R3 and R2-(X)n-; R3 is specified from lower alkyl, cycloalkyl containing 3 to 6 carbon atoms and ; R4 means lower alkyl; X is specified from lower alkylene and cyclisated lower alkylene; R2 means ; where is specified from phenyl, and a 5 or 6-merous heteroaromatic ring containing 1 to 2 heteroatoms specified in the group consisting of sulphur and nitrogen; R5 and R6 are independently specified in the group including hydrogen, lower alkyl, halogen, perfluor (lower alkyl) and lower alkoxygroup; n means an integer within 1 to 2; and r means 0. The invention also concerns a pharmaceutical composition containing a therapeutically effective amount of the compound under the invention.

EFFECT: preparation of the new compounds which show CDK1 kinase inhibiting activity and can be effective in cancer treatment, particularly breast cancer, lung cancer, colon cancer and prostate cancer treatment.

64 cl, 27 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel derivatives of 1H-imidazole of formula I, in which R1 represents hydrogen, halogen atom, C1-3-alkyl group, and said C1-3-alkyl groupcan include 1-3 fluorine atoms or R1 represents cyclopropyl, piano, or methylsulfanyl group, R2 represents phenyl group, which can be substituted with 1 substituent Y, selected from methoxy, chlorine, fluorine, trifluoromethyl and cyano, or R2 represents pyridyl group, on condition that R2 is not 6-methyl-2-pyridyl group, or R2 represents fully saturated 6-7-member monocyclic, condensed bicyclic ring system or benzothiazolyl, benzodioxane or thiazole group, and said groups can be substituted by 1 fluorine atom, or R2 represents group of general formula CH2-R5, in which R5 represents phenyl group or fully saturated 7-member condensed bicyclic carbocyclic ring system, or R5 represents piperidine or tetrahydrofuran ring system, which can be substituted by methyl, or R2 represents methylsulfonylamino(C3)alkyl group, R3 represents hydrogen, halogen atom, C1-6-alkylsulfonyl, cyanogroup, or R3 represents C1-8-alkyl group, and said C1-8-alkyl group can be substituted by 1-3 fluorine atoms, or R3 represents phenyl group, which is substituted by substituent Y, where Y has value, specified above, or R3 represents furanyl group, R4 represents one of subgroups (i) or (ii), where R6 represents C4-8-branched or linear alkyl group or naphtyl group, R7 represents hydrogen atom, linear C1-6-alkyl group, R8 represents C2-6-alkyl group, substituted by 1-3 fluorine atoms, or R8 represents C3-8-cycloalkyl group, piperidine group, C3-8-cycloalkyl- C1-2-alkyl group, tetrahydrofuranyl- C1-2-alkyl group, C5-10-bicycloalkyl group, C5-10-bicycloalkyl-C1-2-alkyl group, C6-10-tricycloalkyl group, C6-10-tricycloalkyl-C1-2-alkyl group, and said groups can be substituted by 1-3 substituents, selected from methyl or hydroxyl, or R8 represents phenyl group, substituted by 1-2 substituents Y, specified above, or R8 represents naphtyl, 1,2,3,4-tetrahydronaphtyl or indanyl group, and said groups can be substituted by 1 substituent Y, or R8 represents phenyl- C1-3-alkyl group, diphenyl- C1-3-alkyl group, and said groups can be substituted ob their phenyl ring by 1 substituent Y, where Y has value specified above, or R8 represents benzyl group, substituted by 2 substituents Y, or R8 represents quinilinyl, pyridinyl, benzimidazole or naphtylmethyl group which can be substituted by substituent Y, where Y has value, specified above, or R8 represents asabicyclo[3,3,0]octanyl group, on condition that R8 is neither 6-methoxybenzothiazole-2-yl group, nor [3-chlor-5-(trifluoromethyl)pyrid-2-yl]methyl group, or R7 and R8 together with nitrogen atom, to which they are bound, form saturated, non-aromatic, monocyclic or bicyclic heterocyclic group, including only one nitrogen atom, having 7-10 ring atoms, which can be subslituted by 3 C1-3-alkyl groups, or R7 and R8 together with nitrogen atom, to which they are bound, form saturated, monocyclic heterocyclic group, optionally including another N atom, having 6 ring atoms, and said heterocyclic group is substituted by C1-3-alkyl groups, on condition that R7 and R8 together with nitrogen atom, to which they are bound, do not form trimethylsubstituted asabicyclo[3,3,0]octanyl group, as well as their stereoisomers and pharmacologically acceptable salts of said formula (I) compounds and their stereoisomers Invention also relates to intermediate compounds of formula XIV, pharmaceutical composition based on formula I compound, method of obtaining such pharmaceutical composition and application of formula T compound.

EFFECT: obtained are novel derivatives of IH-imidazole, which are modulators of cannabinoid CB2-receptors.

8 cl, 1 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel amide derivatives of general formula [1] in any of versions (A) or (B), or its pharmaceutically acceptable salt, which possess properties of tyrosinkinase BCR-ABL inhibitor. Amide derivative of general formula [1] represents compound: , where according to Version (A) R1 represents any of the following groups (1)-(3): (1) -) -CH2-R11 [R11 represents saturated 4-6 member nitrogen-containing heterocyclic group, optionally containing additional nitrogen atom; saturated 5-6-member nitrogen-containing heterocyclic group, optionally containing additional nitrogen atom, which is substituted by group selected from group, consisting of oxo, -CH2-R111 (R111 represents saturated 5-member nitrogen-containing heterocyclic group), saturated 5-member nitrogen-containing heterocyclic group, aminomethyl, monoalkylaminomethyl, dialkylaminomethyl and (5-methyl-2-oxo-1,3-Dioxol-4-yl)methyl, and in addition, can be substituted by 1 or 2 similar or different substituents, selected from group, consisting of (C1-C4)alkyl, (C1-C4 alkoxycarbonyl, halogen, halogen(C1-C4)alkyl, hydroxy(C1-C4)alkyl, amino, carbamoyl], (2) -O-R12 [R12 represents saturated 4-6-member nitrogen-containing heterocyclic group]; and (3) - CH=R13 [R13 represents saturated 4-6-member nitrogen-containing heterocyclic group, which can contain additional nitrogen atom, and which can be substituted by 1-3 similar or different substituents, selected from group, consisting of oxo, (C1-C4)alkyl]; R2 represents (C1-C4)alkyl, halogen, halogen(C1-C4)alkyl, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy and carbamoyl; R3 represents hydrogen, halogen; Het1 represents any of groups with the following chemical formulae [4] and [6]: [4] [6] [19] [10] Het2 represents pyridyl or pyrimidinyl. According to Version (B) R1 represents -CH2-R14 [R14 represents saturated 4-6-member nitrogen-containing heterocyclic group, optionally containing additional nitrogen atom; saturated 5-6-member nitrogen-containing heterocyclic group, which can be substituted by 1-3 similar groups, selected from (C1-C4)alkyl] R2 represents (C1-C4)alkyl, halogen, halogen(C1-C4)alkyl, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkoxy (C1-C4)alkyl, (C1-C4)alkoxycarbonyl, (C1-C4)acyl, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, nitro, carbamoyl, mono(C1-C4)alkylcarbamoyl, di(C1-C4)alkylcarbamoyl or cyano; R3 represents hydrogen or halogen; Het1 represents any of groups with the following chemical formulas [9] and [10], Het2 represents pyridyl.

EFFECT: invention can be applied for treatment of chronic myeloleukosis, acute lymphoblastic leukosis and acute myeloblastic leukosis.

6 cl, 89 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a novel anhydrous tetomilast type A crystalline form, having powder X-ray diffraction spectrum essentially the same as the powder X-ray diffraction spectrum having characteristic peaks at 2θ = 10.5°, 13.1°, 18.4°, 21.9° and 25.8°, pharmaceutical compositions based thereon and synthesis methods thereof.

EFFECT: considerable advantages in terms of industrial production owing to significantly better filterability.

8 cl, 14 dwg, 8 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 synthetic cytoskeleton-active compounds which are from the family of natural latrunculin A or latrunculin B and have structural formulae

and described in the formula of invention. Present invention also relates to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier. The invention also pertains to a method of preventing or treating diseases and conditions associated with actin polymerisation. In one embodiment of the invention, high intraocular pressure, such as during primary open angle glaucoma, is treated using the method. The method involves administering a therapeutically effective amount of the cytoskeleton-active compound of formula I or II to a subject, where the said amount is sufficient for acting on a cytoskeleton, for example through actin polymerisation inhibition.

EFFECT: compounds are highly effective.

16 cl, 75 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: chemistry.

SUBSTANCE: invention relates to pyrrole derivatives of formula (I): , where R1 denotes hydrogen; R2 denotes adamantine which is unsubstituted or substituted with a hydroxy group or halogen; R3 denotes trifluoromethyl, pyrazole, triazole, piperidine, pyrrolidine, hydroxymethylpiperidine, benzylpiperazine, hydroxypyrrolidine, tert-butylpyrrolidine, hydroxyethylpiperazine, hydroxypiperidine or thiomorpholyl group; R4 denotes cyclopropyl, tert-butyl, -CH(CH3)2CH2OH, methyl, -CF3 or -(CH2)nCF3 group, where n equals 1 or 2; R5 denotes hydrogen or lower alkyl which is unsubstituted or substituted with a halogen, as well as pharmaceutically acceptable salts thereof.

EFFECT: compounds and pharmaceutical compositions containing said compounds can inhibit 11β-hydroxysteroid dehydrogenase of the form 1 (11-BETA-HSD-1) and can be used to treat diseases such as type II sugar diabetes type and metabolic syndrome.

17 cl, 99 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of formula I: and their pharmaceutically acceptable salts, in which R1-R4 have values, given in item 1 of invention formula. Said compounds possess inhibiting activity with respect to 11-beta-hydroxysteroid-dehydrogenase and can be applied for production of medications, intended for treatment and prevention of diabetes, especially, diabetes of II type, obesity, malnutrition and hypertension.

EFFECT: development of efficient method of obtaining formula I compounds and based on them pharmaceutical composition.

25 cl, 1 tbl, 149 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) in form of base or a pharmaceutically acceptable addition salt with an acid. The disclosed compounds have β-amyloid peptide(β-A4) formation inhibiting properties. In formula (I), R1 denotes: C1-6-alkyl or phenyl; where said phenyl groups are substituted with two substitutes selected from halogen atoms; R1 and R2' independently denote a hydrogen atom or a hydroxy group; R3 denotes C1-6-alkyl; one or another of radicals R4 and R5 is a group Z and one or another of radicals R4 and R5 is a -C(X)R6 group; G denotes a single bond; Y denotes a single bond, an oxygen atom, a sulphur atom, a C1-4-alkylene group; A and B independently denote a hydrogen atom, a halogen, trifluoromethyl, trifluoromethoxy group; provided that if Y denotes a single bond or an oxygen atom and if group Z is a type group, A does not denote a hydrogen atom; X denotes an oxygen atom; R6 denotes a C1-6alkoxy group. The invention also relates to a method for synthesis of formula (I) compounds, to a medicinal agent and a pharmaceutical composition based on said compounds, and to use of formula (I) compounds in preparing the medicinal agent.

EFFECT: increased effectiveness of using said derivatives.

6 cl, 1 tbl, 31 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula

, in which A is a counter ion, a=1-3, b=0-3, X=1-6C alkyl, R1=1-6C alkyl, one or R2 and R3 is 1-6C alkyl and the other is XN+Hb(R1)3-b, or R2 and R3 form a methylenedioxy group, one or R4 and R5 is a halogen and the other is a halogen-substituted 1-6C alkyl, or R4 and R5 are bonded to form a 6-10C aromatic ring or a substituted 6-10C aromatic ring in which the substitute is selected from 1-6C alkoxy, halogen and halogen-substituted 1-6C alkyl. The invention also relates to a method of measuring content of analysed substance capable of ensuring proportional colour change as a result of a reaction in a biological fluid, involving the following steps: ensuring availability of the disclosed tetrazolium salt as an indicator and determination of concentration of the said analysed substance in the biological fluid using the said tetrazolium salt which is used as an indicator.

EFFECT: agents are highly effective.

24 cl, 7 dwg, 1 tbl, 9 ex

FIELD: chemistry.

SUBSTANCE: described are novel derivatives of genera formula (1) (where A denotes an oxygen or sulphur atom, -CH2- or -NH- group; R1 denotes C1-6alkyl group, possibly substituted ; R1A denotes a hydrogen atom or a C1-6 alkyl group; or these two radicals together with a carbon atom to which they are bonded form a cyclic C3-6 alkyl group; R2 denotes a C1-6 alkyl group or a C3-6 cycloalkyl group; R3 denotes an aryl group or a heteroaryl group, which can be substituted; R4 denotes a hydrogen atom; R5 denotes C1-6 alkyl group, aryl or heteroaryl group, which can be substituted), a pharmaceutical composition containing said derivatives and intermediate compounds. Said compounds (1) can inhibit bonding between SIP and its receptor Edg-1 (SIP1).

EFFECT: possibility of use in medicine.

18 cl, 2 tbl, 28 ex

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