Pyridine and pyrimidine derivatives as mglur2 antagonists

FIELD: medicine, pharmaceutics.

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

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

104 cl, 465 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula (I)
,
where either one of X and Y represents N and the other represents CH, or each of X and Y represents N;
And represents aryl, predstavljajushej a phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl, each of which may substituted With1-6-alkyl;
In represents H, cyano or
represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
nitro,
C1-6-alkyl, possibly substituted by hydroxy,
NRaRbwhere Raand Rbindependently represent H, C1-6-alkyl or -(CO)-C1-6-alkyl,
-S-C1-6-alkyl,
-(SO2)-OH,
-(SO2)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-Alki is, possibly substituted by hydroxy,
C1-6-halogenoalkane,
C1-6-alkoxy,
-(CO)C1-6-alkyl, possibly substituted C1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogen or C1-6-alkoxy,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1,
5 - or 6-membered heteroseksualci, with one oxygen atom in the cycle,
-(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5-, or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxy, C1-6-alkyl, C1-6-alkoxy, which is substituted by hydroxy, and 5 - or 6-membered, heteroaromatic containing as the heteroatom nitrogen,
NHSO2-C1-6-alkyl and
NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl, -(CO)O-C1-6-alkyl, or Rhand Ritogether with the nitrogen atom to which is neither attached, form morpholinyl;
R1represents H, a halogen atom, a C1-6-alkyl, possibly substituted by hydroxy, C1-6-alkoxy, C1-6-halogenoalkane,3-6-cycloalkyl;
R2represents H, cyano, halogen atom, With1-6-halogenoalkane, C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl or C3-6-cycloalkyl;
R3represents a halogen atom, H, C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl, C3-6-cycloalkyl, C1-6-halogenoalkane;
R4represents H or halogeno;
and its pharmaceutically acceptable salts, provided that 6-methyl-2,4-diphenylpyridine, 2,4-diphenylpyridine, 2,4-diphenylpyridine, 6-phenyl-2,2'-bipyridine, 6,6'-dimethyl-(4-methoxyphenyl)-2,2'-bipyridine, 6,6'-dimethyl-(4,4'-diphenyl)-2,2'-bipyridine, 6,6'-dimethyl-4,4'-bis[4-were]-2,2'-bipyridine, 2,6-diphenyl-4-triptorelin, 2-(4-chlorophenyl)-6-phenyl-4-triptorelin, 2-(4-methoxyphenyl)-6-phenyl-4-triptorelin, 2-(4-were)-6-phenyl-4-triptorelin, 2,6-diphenylpyridine, 4-methyl-2,6-diphenylpyridine, 2,6-diphenylpyridine, 6-phenyl-2-thiophene-2-yl-pyrimidine, 6-phenyl-2-pyridin-2-yl-pyrimidine, 6-phenyl-2-(2-methylthiazole-4-yl)-pyrimidine, 4-butyl-2,6-diphenylpyridine and 4-cyclohexyl-2,6-diphenylpyridine excluded.

2. The compound according to claim 1 of formula (I), where In is a N or cyan is.

3. The compound according to claim 1 of formula (I), where
Represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
nitro,
C1-6-alkyl, possibly substituted by hydroxy,
NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6-alkyl,
-S-C1-6-alkyl,
-(SO2)-OH,
-(SO2)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy,
C1-6-halogenoalkane,
With1-6-alkoxy,
-(CO)C1-6-alkyl, possibly substituted C1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogen or C1-6-alkoxy,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1,
5 - or 6-membered heteroseksualci, with one oxygen atom in the cycle,
-(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5 - or 6-membered geteroseksualnoe ring, prob is tenderly containing an additional heteroatom, selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxy, C1-6-alkyl, C1-6-alkoxy, which is substituted by hydroxy, and 5 - or 6-membered, heteroaromatic containing as the heteroatom nitrogen;
NHSO2-C1-6-alkyl and
NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl,
-(CO)O-C1-6-alkyl, or Rhand Ritogether with the nitrogen atom to which they are attached, form morpholinyl.

4. The compound according to claim 1, having the following General formula:
,
where either one of X and Y represents N and the other represents CH, or each of X and Y represents N;
And represents aryl represents phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl;
In represents H or possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where estately selected from the group consisting of
With1-6-alkyl,
-NRaRbwhere Raand Rbindependently represent H, C1-6-alkyl, -(CO)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H, C1-6-alkyl, -(CO)-C1-6-alkyl;
R1represents H, a halogen atom, a C1-6-alkyl, C1-6-alkoxy, C1-6-halogenoalkane,3-6-cycloalkyl;
R2represents H, a halogen atom, a C1-6-halogenoalkane, C1-6-alkyl or C3-6-cycloalkyl;
R3represents a halogen atom, H, C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl, C3-6-cycloalkyl,1-6-halogenoalkane,
as well as its pharmaceutically acceptable salt.

5. Compounds according to claim 1 of formula (I)having the following General formula (Ia):
,
where a, b, R1, R2, R3and R4are as defined in claim 1.

6. Compounds according to claim 5 of formula (Ia), where
And represents aryl represents phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl, each of which may substituted C1-6-alkyl;
In represents the or cyano;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or With1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

7. Compounds according to claim 5 of formula (Ia), where
And represents aryl, predstavljajushej a phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl;
Represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
With1-6-alkyl, possibly substituted by hydroxy,
NRaRbwhere Raand Rbindependently represent H or -(CO)1-6-alkyl,
-(SO2)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy,
-(CO)1-6the alkyl may someseni the C 1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1,
-(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxyl or C1-6-alkyl,
NHSO2-C1-6-alkyl and
NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or C1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

8. Compounds according to claim 5 of formula (Ia)having the following formula (Ia1):
,
where, R1, R2, R3and R4are as defined in claim 5.

9. The compound of claim 8 of formula (Ia1), where
In represents H or cyano;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or C1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

10. The compound of claim 8 of formula (Ia1), where
Represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
C1-6-alkyl, possibly substituted by hydroxy,
NRaRbwhere Raand Rbindependently represent H,
-(SO2)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy,
NHSO2-C1-6-alkyl and
NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl;
R1represents a C1-6-alkyl or the 1-6-halogenoalkane;
R2represents a halogen atom or With1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

11. Compounds according to any one of p or 10 of formula (1A1), where a is an unsubstituted aryl selected from phenyl, or unsubstituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur.

12. Compounds according to claim 11 of formula (Ia1), where these compounds selected from the group consisting of
2-(3-Pyridin-3-yl-phenyl)-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
4-(4-Chloro-phenyl)-2-(3-pyridin-3-yl-phenyl)-6-trifluoromethyl-pyrimidine and
4-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,3']bipyridinyl.

13. Compounds according to any one of p or 10 of formula (Ia1), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of C1-6-alkyl, possibly substituted by hydroxy.

14. Connection 13 of formula (Ia1), where these compounds selected from the group consisting of
2-[3-(2,6-is imethyl-pyridin-4-yl)-phenyl]-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine and
{3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-4-yl}-methanol.

15. Compounds according to any one of p or 10 of formula (Ia1), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of NRaRbwhere Raand Rbindependently represent N.

16. Connections § 15 of the formula (1A1), where these compounds selected from the group consisting of
5-{3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-f the Nile}-pyrimidine-2-ylamine;
5-{3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-4-ylamine;
5-{3-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[4-Methyl-6-(3-methyl-4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-(3-{4-[3-(2,2,2-Cryptor-ethoxy)-4-trifluoromethyl-phenyl]-6-trifluoromethyl-pyrimidine-2-yl}-phenyl)-pyridine-2-ylamine;
5-(3-{4-[3-(2,2,2-Cryptor-ethoxy)-4-trifluoromethyl-phenyl]-6-trifluoromethyl-pyrimidine-2-yl}-phenyl)-pyrimidine-2-ylamine;
5-{3-[4-Trifluoromethyl-6-(3-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2'-yl]-phenyl}-pyridine-2-ylamine;
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-ylamine and
5-{3-[4-(4-Chloro-3-methyl-phenyl)-6-methyl-pyrimidine-2-yl]-phenyl}-pyridine-2-ylamine.

17. Compounds according to any one of p or 10 of formula (Ia1), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of -(SO2)-C1-6-alkyl or -(SO2)-NRcRdwhere Rcand Rd independently represent N or C1-6-alkyl, possibly substituted by hydroxyl.

18. Connection 17 of formula (Ia1), where these compounds selected from the group consisting of
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid tert-butylamide;
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid tert-butylamide;
3'-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2'-yl]-biphenyl-3-sulfonic acid amide;
3'-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid tert-butylamide;
5-{3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
5-{3-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
3'-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(3,4-Dichloro-phenyl)-methyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
2-(3'-Methanesulfonyl-biphenyl-3-yl)-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
3'-[4-(4-Chloro-3-methyl-phenyl)-6-methyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(4-Chloro-3-methyl-phenyl)-6-methyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
5-{3-[4-(3,4-Debtor-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid (2-hydroxy-ethyl)-amide;
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid bis-(2-hydroxy-ethyl)-amide;
3'-[4-(3,4-Debtor-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
3'-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-(2,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-su is honowai acid amide;
5-{3-[4-(2,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-(2-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-(2-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-Methyl-6-(3-methyl-4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-Methyl-6-(3-methyl-4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide;
3'-[4-(3-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-biphenyl-3-sulfonic acid amide and
5-{3-[4-(3-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide.

19. Compounds according to any one of p or 10 of formula (Ia1), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are NHSO2-C1-6-alkyl.

20. Compounds according to claim 19 of the formula (Ia1), where the specified connection is {3'-[4 - Trifluoromethyl-6-(4-trift rmeil-phenyl)-pyrimidine-2-yl]-biphenyl-3-yl}-methanesulfonamide.

21. Compounds according to any one of p or 10 of formula (Ia1), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl.

22. Connection item 21 of formula (Ia1), where these compounds selected from the group consisting of N-{3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-yl}-sulphonamide and N-{3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-biphenyl-3-yl}-N',N'-dimethyl-sulphonamide.

23. Compounds according to claim 5 of formula (Ia)having the following formula (Ia2):

where, R1, R2,R3and R4are as defined in claim 5, and 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen or sulfur, can be selected from the group consisting of imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl.

24. Compounds according to item 23 of formula (Ia2), where
In represents H or cyano;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or C1-6-halogenoalkane, R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

25. Compounds according to any one of p and 24 of formula (Ia2), where In is an N.

26. Connection A.25 formula (Ia2), where these compounds selected from the group consisting of
4-(4-Chloro-phenyl)-2-imidazol-1-yl-6-trifluoromethyl-pyrimidine;
2-Imidazol-1-yl-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
2-Pyrrol-1-yl-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
4-(4-Chloro-phenyl)-2-pyrrol-1-yl-6-trifluoromethyl-pyrimidine;
2-Pyridin-3-yl-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
4-Deformity-2-pyridin-4-yl-6-(4-trifluoromethyl-phenyl)-pyrimidine and
2-Pyridin-4-yl-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine.

27. Compounds according to item 23 of formula (Ia2), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
C1-6-alkyl, possibly substituted by hydroxy,
NRaRbwhere Raand Rbindependently represent H or -(CO)1-6-alkyl,
-(SO2)-C1-6-alkyl,
-(S 2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy,
-(CO)1-6-alkyl, possibly substituted C1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1, and
-(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxy or C1-6-alkyl;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or C1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

28. Connection item 27 of formula Ia2), where In represents an unsubstituted aryl selected from phenyl, or unsubstituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur.

29. Connection p formula (Ia2), where these compounds selected from the group consisting of
2-(4-Pyridin-3-yl-imidazol-1-yl)-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
4-(4-Chloro-phenyl)-2-(4-pyridin-3-yl-imidazol-1-yl)-6-trifluoromethyl-pyrimidine;
4-(4-Chloro-phenyl)-2-(4-pyridin-4-yl-imidazol-1-yl)-6-trifluoromethyl-pyrimidine;
4-(4-Chloro-phenyl)-2-(3-pyridin-4-yl-[1,2,4]oxadiazol-5-yl)-6-trifluoromethyl-pyrimidine;
4-(4-Chloro-phenyl)-2-(3-pyridin-3-yl-[1,2,4]oxadiazol-5-yl)-6-trifluoromethyl-pyrimidine;
4-(4-Chloro-phenyl)-6-methyl-2-(4-pyridin-3-yl-imidazol-1-yl)-pyrimidine;
4-Methyl-2-(4-pyridin-3-yl-imidazol-1-yl)-6-(4-trifluoromethyl-phenyl)-pyrimidine;
4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[2,3']bipyridinyl;
4-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,4']bipyridinyl;
2-(3-Pyridin-4-yl-[1,2,4]triazole-1-yl)-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
2-(3-Pyridin-3-yl-[1,2,4]triazole-1-yl)-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine.

30. Connection item 27 of formula (Ia2), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle, the selected Isetta, oxygen or sulfur, where the Deputy represents NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6-alkyl.

31. Compounds according to article 30 of the formula (Ia2), where these compounds selected from the group consisting of
4-{5-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{5-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
4-{5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-pyrazole-4-yl}-pyridine-2-ylamine;
5-{5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyrimidine-2-ylamine;
5-{3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-5-yl}-pyridine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-5-yl}-pyridine-2-ylamine;
4-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[2,3']piperidin the l-6'-ylamine;
5-{1-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{5-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine,
5-{1-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{1-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{1-[4-(4-Chloro-phenyl)-6-cyclopropyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(4-Chloro-phenyl)-6-cyclopropyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{1-[4-(4-Chloro-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Trifluoromethyl-6-(3-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
4-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{5-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
4-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{1-[4-(3-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridin-ylamine;
N-(5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-yl)-ndimethylacetamide;
5-{5-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-pyridine-2-ylamine;
5-{1-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
4-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{1-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{5-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
4-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
4-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-phenylamine;
4-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
4-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{1-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
4-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{1-[4-Methyl-6-(3-methyl-4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Methyl-6-(3-methyl-4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidin-ylamine;
5-{1-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{5-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{5-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
4-[4-Methyl-6-(3-methyl-4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-(1-{4-[3-(2,2,2-Cryptor-ethoxy)-4-trifluoromethyl-phenyl]-6-trifluoromethyl-pyrimidine-2-yl}-1H-imidazol-4-yl)-pyridine-2-ylamine;
4-{4-[3-(2,2,2-Cryptor-ethoxy)-4-trifluoromethyl-phenyl]-6-trifluoromethyl-pyrimidine-2-yl}-[2,3']bipyridinyl-6'-ylamine;
5-{5-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{1-[4-Trifluoromethyl-6-(3-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
4-[4-Trifluoromethyl-6-(3-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{2-Methyl-1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{2-Methyl-1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
4-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-[2,3']bipyridinyl-6'-ylamine;
5-{2-Methyl-1-[4-methyl--(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-[1,2,4]triazole-3-yl}-pyridine-2-ylamine;
5-{1-[4-Isopropyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Isopropyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{5-Methyl-1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(3-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(3-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
5-{1-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-(4-Chloro-3-methyl-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine and
5-{1-[4-(3,4-Debtor-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine.

32. Connection item 27 of formula (Ia2), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a -(SO2)-C1-6-alkyl.

33. Connection p formula (Ia2), where these compounds selected from the group consisting of
4-(4-Chloro-phenyl)-2-[4-(3-methanesulfonyl-phenyl)-imidazol-1-yl]-6-methyl-pyrimidine;
4-(3,4-Dichloro-phenyl)-2-[4-(3-methanesulfonyl-phenyl)-imida the ol-1-yl]-6-methyl-pyrimidine;
2-[4-(3-Methanesulfonyl-phenyl)-imidazol-1-yl]-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine and
2-[2-(3-Methanesulfonyl-phenyl)-pyridin-4-yl]-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine.

34. Connection item 27 of formula (Ia2), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a -(SO2)-NRcRdwhere Rcand Rdindependently represent H, C1-6-alkyl, possibly substituted by hydroxy, -(CO)1-6-alkyl, possibly substituted C1-6-alkoxy, -(CH2CH2O)nCHRewhere Rerepresents N or CH2HE and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, -(CH2)m-aryl, where m has a value of 1 or 2, or -(CH2)p-C3-6-cycloalkyl, where p is 0 or 1.

35. The connection 34 of the formula (Ia2), where these compounds selected from the group consisting of
3-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-5-yl}-benzosulfimide;
3-{3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-5-yl}-benzosulfimide;
4-{5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-Trifluoromethyl-6-(4-tripto the methyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
4-{5-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
5-{3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-5-yl}-thiophene-2-sulfonic acid amide;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-5-yl}-thiophene-2-sulfonic acid amide;
4-{5-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
4-{5-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
4-{5-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
4-{5-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
4-{5-[4-(3-Methyl-4-trifluoromethyl-phenyl)6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
3-{5-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
4-{5-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
N-tert-Butyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
3-{4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
4-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
5-{4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid tert-butylamide;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
5-{4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
5-{1-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
4-{1-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-(4-Chloro-phenyl)-6-methyl-pyrimi the Jn-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{4-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
4-{1-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
2-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
2-{1-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
4-{1-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-(3-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
5-{1-[4-(3-Chloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{1-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
5-{1-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
5-{4-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-Piri is in-2-yl}-thiophene-2-sulfonic acid amide;
5-{4-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
4-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
2-{1-[4-(4-Chloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
2-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
3-{4-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
5-{1-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
5-{1-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
4-{1-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide,
4-{1-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-(3-Methyl-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide,
3-{1-[4-(3,4-Dichloro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
5-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-tiop is n-2-sulfonic acid amide;
3-{1-[4-(4-Chloro-3-methyl-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
5-{1-[4-(4-Chloro-3-methyl-phenyl)-6-methyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
N-tert-Butyl-3-{6-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide,
3-{6-[4-Trifluoromethyl-6-(4-triptoreline)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N,N-Bis-(2-{2-[2-(2-methoxy-ethoxy)-ethoxy]-ethoxy}-ethyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N,N-Bis-(2-hydroxy-ethyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-(2-{2-[2-(2-Methoxy-ethoxy)-ethoxy]-ethoxy}-ethyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Propionyl 3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid propionyl amide;
N-(2-Hydroxy-ethyl)-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-(2-Hydroxy-1,1-dimethyl-ethyl)-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N,N-Bis-(2-hydroxy-ethyl)-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{1-[4-(3,4-is iftar-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
5-{1-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
3-{1-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-{1-[4-(3,4-Debtor-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
5-{4-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(3,4-Debtor-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-(3,4-Debtor-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide,
N,N-Dimethyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Methyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Isobutyl-N-methyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Methyl-N-propyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Benzyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Phenethyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Cyclopropylmethyl-3-{4-[4-trifluoromethyl-6-(4-three is tormentil-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-Cyclopropyl-3-{4-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-(4-Chloro-3-methyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-tert-Butyl-3-{6-[4-methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide,
3-{6-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
N-tert-Butyl-3-{6-[4-(4-cyano-phenyl)-6-methyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
3-{6-[4-(4-Cyano-phenyl)-6-methyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
3-(4-{4-[3-(2,2,2-Cryptor-ethoxy)-4-trifluoromethyl-phenyl]-6-trifluoromethyl-pyrimidine-2-yl}-pyridine-2-yl)-benzosulfimide;
3-{4-[4-Trifluoromethyl-6-(3-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
3-{4-[4-(2-Fluoro-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(2-Fluoro-4-trifluoromethyl-phenyl)-6-trifloromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide;
5-{4-[4-(3-Ethoxy-4-trifluoromethyl-phenyl)-6-trifluoromethyl-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide;
3-{4-[4-Deformity-6-(4-cryptomite is-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzosulfimide and
5-{4-[4-Deformity-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-thiophene-2-sulfonic acid amide.

36. Connection item 27 of formula (Ia2), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a -(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by hydroxy or C1-6-alkyl.

37. Connection p formula (Ia2), where these compounds selected from the group consisting of
4-(3-{4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzazolyl)-the research;
2-{2-[3-(4-Methyl-piperazine-1-sulfonyl)-phenyl]-pyridin-4-yl}-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine;
2-{2-[3-(Pyrrolidin-1-sulfonyl)-phenyl]-pyridin-4-yl}-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine and
(RS)-1-(3-{4-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyrimidine-2-yl]-pyridine-2-yl}-benzazolyl)-pyrrolidin-3-ol.

38. Compounds according to claim 1 of formula (I) having the following General formula (I-b):

where a, b, R1, R2, R3and R4are as defined in claim 1.

39. Connections § 38 of the formula (IB), where
And represents aryl represents phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl, each of which may substituted C1-6-alkyl;
In represents H or cyano;
R1represents H, a halogen atom, a C1-6-alkyl, possibly substituted by hydroxy, C1-6-alkoxy, C1-6-halogenoalkane,3-6-cycloalkyl;
R2represents H, cyano, halogen atom, With1-6-halogenoalkane,1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl or C3-6-cycloalkyl;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl or C1-6-halogenoalkane;
or R2and R3together can form dioxo-bridge,
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

40. Connections § 38 of the formula (IB), where
And represents aryl represents phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle,selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl, each of which may substituted C1-6-alkyl;
Represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
nitro,
C1-6-alkyl,
NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6- -S-C1-6-alkyl, -(SO2)-OH, -(SO2)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy,
C1-6-halogenoalkane,
C1-6-alkoxy,
-(CO)1-6-alkyl, possibly substituted C1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogen or1-6-alkoxy,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1,
5 - or 6-membered heteroseksualci, with one oxygen atom in the cycle, -(SO2)-NRfRgwhere Rfand Rgthe place with the nitrogen atom, to which they are attached, form
4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxy, C1-6-alkyl, C1-6-alkoxy, which is substituted by hydroxy, and 5 - or 6-membered, heteroaromatic containing as the heteroatom nitrogen,
NHSO2-C1-6-alkyl and
NHSO2-NRhRiwhere Rhand Ri independently represent H, C1-6-alkyl or -(CO)O-C1-6-alkyl;
R1represents H, a halogen atom, a C1-6-alkyl, possibly substituted by hydroxy, C1-6-alkoxy, C1-6-halogenoalkane,3-6-cycloalkyl;
R2represents H, cyano, halogen atom, With1-6-halogenoalkane, C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl or C3-6-cycloalkyl;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl or C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

41. Connections § 38 of the formula (IB)having the following formula (B):
,
where, R1, R2,R3and R4are such as defined in § 38.

42. Compounds according to paragraph 41 of the formula (B), where a is an unsubstituted aryl selected from phenyl, or unsubstituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur.

43. Connections § 42 of the formula (B), where these compounds selected from the group consisting of
2-Methyl-6-(3-pyridin-3-yl-phenyl)-4-(4-trifluoromethyl-phenyl)-pyridine;
2-Cyclopropyl-6-(3-pyridin-3-yl-phenyl)-4-(4-trifluoromethyl-phenyl)-pyridine and
2-Methyl-6-(3-pyridin-4-yl-phenyl)-4-(4-trifluoromethyl-phenyl)-pyridine.

44. Compounds according to paragraph 41 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy represents cyano.

45. Connection item 44 of the formula (B), where the specified connection is a 3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-benzonitrile.

46. Compounds according to paragraph 41, of the formula (161) where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a C1-6-alkyl.

47. The is begins on p.46 of the formula (B), where the specified connection is a 2-Methyl-6-[3-(4-methyl-imidazol-1-yl)-phenyl]-4-(4-trifluoromethyl-phenyl)-pyridine.

48. Compounds according to paragraph 41, of the formula (B) where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy represents NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6-alkyl.

49. Connection p formula (B), where these compounds are
5-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[6-Cyclopropyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-methyl-pyridine-2-yl]-phenyl}-pyrimidine-2-ylamine,
5-{3-[4-(4-Chloro-phenyl)-6-methyl-pyridine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl}-pyridine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyridin-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[4-(4-Chloro-phenyl)-6-trifluoromethyl-pyridin-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3,4-Dichloro-phenyl)-6-methyl-pyridine-2-yl]-phenyl}-pyridine-2-ylamine;
5-{3-[4-(3,4-Dichloro-Fe who yl)-6-methyl-pyridine-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[6-Ethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyrimidine-2-ylamine;
5-{3-[6-Ethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-2-ylamine;
5-[3-(4-Benzo[1,3]dioxol-5-yl-6-methyl-pyridine-2-yl)-phenyl]-pyridin-2-ylamine and
4-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-thiazole-2-ylamine.

50. Compounds according to paragraph 41 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a -(SO2)-C1-6-alkyl.

51. Connection item 50 of the formula (B), where the specified connection is a 2-(3'-Methanesulfonyl-biphenyl-3-yl)-6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine.

52. Compounds according to paragraph 41 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy -(SO2)-NRcRdwhere Rcand Rdindependently represent H, C1-6-alkyl, possibly substituted by hydroxy, C1-6-halogenoalkane,1-6-alkoxy, -(CO)1-6-alkyl, possibly substituted C1-6-alkoxy, -(CH2CH2O)nCHRewhere Rerepresents N or CH2The h and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, -(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogen or1-6-alkoxy, -(CH2)p-C3-6-cycloalkyl, where p is 0 or 1, or 5-or 6-membered heteroseksualci, with one atom of oxygen in the loop.

53. Compounds according to paragraph 52 of the formula (B), where these compounds selected from the group consisting of
3'-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-3-sulfonic acid amide;
5-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-3-sulfonic acid amide;
5-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-3-sulfonic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
3'-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid methoxy-amide;
3'-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide;
3'-[6-Ethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid tert-butylamide;
3'-[6-Ethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid amide;
4,6-Debtor-3'-[6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-thiophene-2-sulfo the OIC acid amide;
3'-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid amide and
N-(tert-Butoxycarbonyl)-N'-(4-{3-[6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-thiazole-2-yl)-sulphonamide.

54. Compounds according to paragraph 41 of the formula (B)having the following formula (I-b):
,
where, R1, R2, R3and R4are as defined in paragraph 41.

55. Connections § 38 of the formula (16), having the following formula (B):
,
where, R1, R2,R3and R4are such as defined in § 38, and 5 - or 6-membered heteroaryl group containing 1-3 heteroatoms in the cycle selected from nitrogen, oxygen or sulfur, can be selected from the group consisting of imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl.

56. Connections § 55 of the formula (I62), where
In represents H or cyano, preferably H;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or With1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

57 Connection p formula (B), where these connections are selected from the group consisting of
2-Imidazol-1-yl-6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine;
4-(3,4-Dichloro-phenyl)-2-imidazol-1-yl-6-methyl-pyridine and
2-Methyl-6-thiazol-2-yl-4-(4-trifluoromethyl-phenyl)-pyridine.

58. Connections § 55 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
nitro,
C1-6-alkyl, possibly substituted by hydroxy,
NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6-alkyl,
-S-C1-6-alkyl,
NHSO2-C1-6-alkyl,
NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl or -(CO)O-C1-6-alkyl,
-(SO2)-C1-6-alkyl,
-(SO2)-OH, -(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy,
-(CO)1-6-alkyl, possibly substituted C1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogeno the I 1-6-alkoxy,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1,
5 - or 6-membered heteroseksualci with one oxygen atom in the cycle and is(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxy, C1-6-alkyl, C1-6-alkoxy, possibly substituted by hydroxy, or heteroaromatic containing as the heteroatom nitrogen;
R1represents a C1-6-alkyl or C1-6-halogenoalkane;
R2represents a halogen atom or With1-6-halogenoalkane;
R3represents H, a halogen atom, a C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl and C1-6-halogenoalkane;
R4represents H or halogeno;
and their pharmaceutically acceptable salts.

59. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen the ode or sulfur, where the Deputy is a nitro.

60. Connection p formula (B), where these compounds selected from the group consisting of 6-Methyl-2'-(3-nitro-phenyl)-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl and 4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-2-(3-nitro-phenyl)-pyrimidine.

61. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy represents NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6-alkyl.

62. Connection p formula (B), where these compounds selected from the group consisting of
5-{1-[6-Cyclopropyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,3',5',3"]terpyridine-6"-ylamine;
5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,3']bipyridinyl-5'-yl]-pyrimidine-2-ylamine;
6-Cyclopropyl-4-(4-trifluoromethyl-phenyl)-[2,3',5',3"]terpyridine-6"-ylamine;
6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,2';6',3"]terpyridine-6"-ylamine;
5-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-pyrimidine-2-ylamine;
6-Methyl-4-(4-trifluoromethyl-phenyl-[2,4'; 2',3"]terpyridine-6"-ylamine;
5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-pyrimidine-2-ylamine;
6-Cyclopropyl-4-(4-trifluoromethyl-phenyl)-[2,4';2',3"]terpyridine-6"-ylamine;
5-[6-Cyclopropyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-pyrimidine-2-ylamine;
5-{1-[4-(4-Chloro-phenyl)-6-methyl-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
4-(4-Chloro-phenyl)-6-methyl-[2,3';5',3"]terpyridine-6"-ylamine;
5-{2-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiazol-4-yl}-pyridine-2-ylamine;
5-{2-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiazol-4-yl}-pyrimidine-2-ylamine,
5-{5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-[1,2,4]oxadiazol-3-yl}-pyridine-2-ylamine;
5-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-pyridine-2-ylamine;
4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-[2,5']bipyridinyl-2'-ylamine;
5-{2-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-4-yl}-pyridine-2-ylamine;
5-{1-[4-(3,4-Dichloro-phenyl)-6-methyl-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiophene-2-yl}-pyridine-2-ylamine;
5-{5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiophene-2-yl}-pyrimidine-2-ylamine;
5-{5-[4-(3,4-Dichloro-phenyl)-6-methyl-pyridine-2-yl]-thiophene-2-yl}-pyridine-2-ylamine;
5-{5-[4-(3,4-Dichloro-FeNi is)-6-methyl-pyridine-2-yl]-thiophene-2-yl}-pyrimidine-2-ylamine;
5-{5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiophene-3-yl}-pyridine-2-ylamine;
3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-phenylamine;
3-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-phenylamine;
3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenylamine;
N-(3-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-phenyl)-ndimethylacetamide;
N-{3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenyl}-ndimethylacetamide;
6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,2';6',4"]terpyridine-2"-ylamine;
4-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-pyridine-2-ylamine and
3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-phenylamine.

63. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a-S-C1-6-alkyl.

64. Connection p formula (B), where the specified connection is a 6-Methyl-6'-(3-methylsulfanyl-phenyl)-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl.

65. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the CEC is e, selected from nitrogen, oxygen or sulfur, where the Deputy represents S(O)2-C1-6-alkyl.

66. Connection p formula (B), where these compounds selected from the group consisting of
2-(3-Methanesulfonyl-phenyl)-4-[6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine and
6'-(3-Methanesulfonyl-phenyl)-6-methyl-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl.

67. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a -(SO2)-NRcRdwhere Rcand Rdindependently represent H, C1-6-alkyl, possibly substituted by a hydroxyl or halogen, -(CO)1-6-alkyl, possibly substituted C1-6-alkoxy, -(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, -(CH2)m-aryl, possibly substituted, halogen or C1-6-alkoxy, where m has a value of 1 or 2 and the aryl possibly substituted, halogeno, C1-6-alkoxy, or -(CH2)p-C3-6-cycloalkyl, where p is 0 or 1, and 5 - or 6-membered heteroseksualci with one atom of oxygen in the loop.

68. Connection p formula (B), where the decree of the connections selected from the group consisting of
4-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-{5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
N-tert-Butyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-tert-Butyl-3-{4-[6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-benzosulfimide;
N-tert-Butyl-3-{2-[6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiazol-4-yl}-benzosulfimide;
3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-benzosulfimide;
3-{2-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiazol-4-yl}-benzosulfimide;
N-tert-Butyl-3-[6-methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
N-tert-Butyl-3-[6-methyl-4-(4-trifluoromethyl-phenyl)-[2,3']bipyridinyl-5'-yl]-benzosulfimide;
3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
N-tert-Butyl-3-{1-[6-trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,3']bipyridinyl-5'-yl]-benzosulfimide;
3-{1-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
4-Methyl-2-{1-[6-trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-they are the azole-4-yl}-thiazole-5-sulfonic acid tert-butylamide;
5-{1-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid tert-butylamide;
2-{1-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid tert-butylamide;
5-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-thiophene-2-sulfonic acid tert-butylamide;
5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid tert-butylamide;
5-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-thiophene-2-sulfonic acid tert-butylamide;
4-Methyl-2-{1-[6-trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
2-{1-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
5-{1-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
5-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-thiophene-2-sulfonic acid amide;
5-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid amide;
5-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-thiophene-2-sulfonic acid amide;
5-{2-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-thiazol-4-yl}-thiophene-2-sulfonic acid tert-butylamide;
5-{2-[6-Methyl-4-(4-trifluoromethyl-phenyl-pyridine-2-yl]-thiazol-4-yl}-thiophene-2-sulfonic acid amide,
4-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-benzosulfimide;
4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
N-tert-Butyl-3-[4-(3-methoxy-4-trifluoromethyl-phenyl)-6-methyl-[2,4']bipyridinyl-2'-yl]-benzosulfimide.;
5-[4-(3-Methoxy-4-trifluoromethyl-phenyl)-6-methyl-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid tert-butylamide;
3-[4-(3-Methoxy-4-trifluoromethyl-phenyl)-6-methyl-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
5-[4-(3-Methoxy-4-trifluoromethyl-phenyl)-6-methyl-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid amide;
N-(2-Hydroxy-ethyl)-3-[6-methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
N-(2-Hydroxy-1,1-dimethyl-ethyl)-3-[6-methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-N-propionyl benzosulfimide;
N-(2-Hydroxy-ethyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-(2-Hydroxy-1,1-dimethyl-ethyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-(2-Methoxy-ethyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-[2-(2-Hydroxy-ethoxy)-ethyl]-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-[2-(2-Methoxy-ethoxy)-ethyl]-3-[6'-methyl-4'-(4-trift rmeil-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-{2-[2-(2-Methoxy-ethoxy)-ethoxy]-ethyl}-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Methyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N,N-Dimethyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Cyclopropyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Cyclopropyl-N-methyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Benzyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-(4-Methoxy-benzyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-(4-Fluoro-benzyl)-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-tert-Butyl-3-[6'-methyl-4'-(4-triptoreline-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-[6'-Methyl-4'-(4-triptoreline-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-tert-Butyl-3-[6'-methyl-4'-(3-methyl-4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-[6'-Hydroxymethyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-[6'-Methyl-4'-(3-methyl-4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Acetyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-[6 who-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-N-(tetrahydro-Piran-4-yl)-benzosulfimide;
3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-N-(2,2,2-Cryptor-ethyl)-benzosulfimide;
N-Ethyl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
N-Butyryl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide and
N-Isobutyryl-3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2')bipyridinyl-6-yl]-benzosulfimide.

69. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a NHSO2-C1-6-alkyl.

70. Connection p formula (B), where these compounds selected from the group consisting of
N-{3-[6-Methyl-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-phenyl}-methanesulfonamide;
N-(3-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-phenyl)-methanesulfonamide and
N-{3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenyl}-methanesulfonamide.

71. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy represents-SO2-OH.

72. Obedinenie on p formula (B), where the specified connection is a 3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide acid.

73. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the Deputy is a NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl or -(CO)O-C1-6-alkyl.

74. Connection p formula (B), where these compounds selected from the group consisting of
N-(tert-Butoxycarbonyl)-N'-{3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenyl}-sulphonamide;
N-(tert-Butoxycarbonyl)-N'-(3-{4-[6-methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-phenyl)-sulphonamide;
N-{3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenyl}-sulphonamide;
N-(3-{4-[6-Methyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-phenyl)-sulphonamide and
N,N-(Dimethyl)-N'-{3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenyl}-sulphonamide.

75. Connections § 58 of the formula (B), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, color is Yes or sulfur, where the Deputy is a -(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form a 4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of hydroxy, C1-6-alkyl, C1-6-alkoxy, possibly substituted by hydroxy, and heteroaromatic containing as the heteroatom nitrogen.

76. Connection item 75 of the formula (B), where these compounds selected from the group consisting of
6-Methyl-2'-[3-(morpholine-4-sulfonyl)-phenyl]-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl;
6-Methyl-2'-[3-(thiomorpholine-4-sulfonyl)-phenyl]-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl;
6-Methyl-2'-[3-(4-methyl-piperazine-1-sulfonyl)-phenyl]-4-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl;
Morpholine-4-sulfonic acid {3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-phenyl}-amide;
6'-[3-(1,1-Dioxo-1-thiomorpholine-4-sulfonyl)-phenyl]-6-methyl-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl;
6-Methyl-6'-[3-(pyrrolidin-1-sulfonyl)-phenyl]-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl;
6-Methyl-6'-[3-(4-methyl-piperazine-1-sulfonyl)-phenyl]-4-(4-trifluoromethyl-phenyl)-[2,2']BIP is reinila;
6-Methyl-6'-[3-(morpholine-4-sulfonyl)-phenyl]-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl;
6'-[3-(Azetidin-1-sulfonyl-phenyl]-6-methyl-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl;
1-{3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzazolyl}-piperidine-4-ol;
1-{3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzazolyl}-azetidin-3-ol;
6'-[3-(4-Methoxy-piperidine-1-sulfonyl)-phenyl]-6-methyl-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl;
2-(1-{3-[6'-Methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzazolyl}-piperidine-4-yloxy)-ethanol;
6-Methyl-6'-{3-[4-(pyridine-4-yloxy)-piperidine-1-sulfonyl]-phenyl}-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl and
6-Methyl-6'-{3-[4-(pyrimidine-2-yloxy)-piperidine-1-sulfonyl]-phenyl}-4-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl.

77. Compounds according to claim 1 of formula (I)having the following General formula (I-b):
,
where a, b, R1, R2, R3and R4are as defined in claim 1.

78. Connection p formula (IB), where
And represents aryl, predstavljajushej a phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl, each of which may samisens 1-6-alkyl;
In represents H or cyano;
R1represents a halogen atom, a C1-6-alkyl, possibly substituted by hydroxy, C1-6-alkoxy, C1-6-halogenoalkane,3-6-cycloalkyl;
R2represents a halogen atom, a C1-6-halogenoalkane,1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl or C3-6-cycloalkyl;
R3represents a halogen atom, H, C1-6-alkoxy, C1-6-halogenoalkane,1-6-alkyl, C3-6-cycloalkyl, C1-6-halogenoalkane;
and their pharmaceutically acceptable salts.

79. Connection p formula (IB), where
And represents aryl, predstavljajushej a phenyl or 5 - or 6-membered heteroaryl containing 1-3 atoms in the cycle, selected from nitrogen, oxygen, or sulfur selected from imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl, each of which may substituted With1-6-alkyl;
Represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents selected from the group consisting of
nitro,
C1-6-alkyl, possible substituted hydroxy,
NRaRbwhere Raand RbNezavisimosty a N, C1-6-alkyl or -(CO)-C1-6-alkyl,
-S-C1-6-alkyl,
-(SO2)-OH,
-(SO2)-C1-6-alkyl,
-(SO2)-NRcRdwhere Rcand Rdindependently represent H,
C1-6-alkyl, possibly substituted by hydroxy, C1-6-halogenoalkane, C1-6-alkoxy,
-(CO)1-6-alkyl, possibly substituted C1-6-alkoxy,
-(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10,
-(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogen or C1-6-alkoxy,
-(CH2)p-C3-6-cycloalkyl, where p is 0 or 1,
5 - or 6-membered heteroseksualci, with one oxygen atom in the cycle, -(SO2)-NRfRgwhere Rfand Rgtogether with the nitrogen atom to which they are attached, form
4-, 5 - or 6-membered geteroseksualnoe ring may contain an additional heteroatom selected from nitrogen atom, oxygen atom, sulfur atom, or a group of SO2where the specified 4-, 5 - or 6-membered geteroseksualnoe ring possibly substituted by the Deputy selected from the group consisting of
hydroxy, C1-6-alkyl, C1-6-alkoxy, which is substituted by hydroxy, and 5 - or 6-membered, heteroaromatic containing as the heteroatom nitrogen,
HSO 2-C1-6-alkyl and
NHSO2-NRhRiwhere Rhand Riindependently represent H, C1-6-alkyl, -(CO)O-C1-6-alkyl, or Rhand Ritogether with the nitrogen atom to which they are attached, form morpholinyl;
R1represents a halogen atom, a C1-6-alkyl, possibly substituted by hydroxy, C1-6-alkoxy, C1-6-halogenoalkane,3-6-cycloalkyl;
R2represents a halogen atom, a C1-6-halogenoalkane, C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl or C3-6-cycloalkyl;
R3represents a halogen atom, H, C1-6-alkoxy, C1-6-halogenoalkane, C1-6-alkyl, C3-6-cycloalkyl, C1-6-halogenoalkane,
and their pharmaceutically acceptable salts.

80. Connection p formula (IB)having the following General formula (V):
,
where, R1, R2,R3and R4are as defined in p.

81. Connection item 80 of the formula (V), where a is an unsubstituted aryl selected from phenyl, or unsubstituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur.

82. Connection p formula (V), where the specified connection is a 2-(3-Pyridin-3-yl-phenyl)-4-trifluoromethyl-6-(4-trifluoromethyl-f the Nile)-pyridine.

83. Connection item 80 of the formula (V), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are NRaRbwhere Raand Rbindependently represent H or -(CO)-C1-6-alkyl.

84. Connection item 80 of the formula (V), where these compounds selected from the group consisting of 5-{3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-2-ylamine and 5-{3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-pyridine-3-sulfonic acid amide.

85. Connection item 80 of the formula (V), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are -(SO2)-NRcRdwhere Rcand Rdindependently represent H, C1-6-alkyl, possibly substituted by hydroxy, C1-6-halogenoalkane, C1-6-alkoxy, -(CO)C1-6-alkyl, possibly substituted C1-6-alkoxy, -(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, -(CH2)m-aryl, where m has a value of 1 or and aryl possibly substituted, halogen or1-6-alkoxy, or -(CH2)p-C3-6-cycloalkyl, where p is 0 or 1, or 5 - or 6-membered heteroseksualci, with one atom of oxygen in the loop.

86. Connection p formula (V), where these compounds selected from the group consisting of
3'-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid amide;
5-{3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-thiophene-2-sulfonic acid tert-butylamide;
5-{3-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-phenyl}-thiophene-2-sulfonic acid amide and
3'-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-biphenyl-3-sulfonic acid amide.

87. Connection item 80 of the formula (V), having the following General formula (V):
,
where, R1, R2,R3and R4are as defined in item 80.

88. Connection p formula (IB)having the following General formula (V):

where, R1, R2,R3and R4are as defined in p, and 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen, or sulfur selected from the group consisting of imidazolyl, [1,2,4]oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4]triazolyl, thiazolyl and pyrimidinyl.

89. Connection p is ormula (V), where In represents an unsubstituted aryl selected from phenyl, or unsubstituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur.

90. Connection p formula (V), where the specified connection is a 2-(4-Chloro-phenyl)-6-(4-pyridin-3-yl-imidazol-1-yl)-4-trifluoromethyl-pyridine.

91. Connection p, formula (V), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are C1-6-alkyl.

92. Connection p formula (V), where these compounds selected from the group consisting of
4-Methyl-2-{1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid tert-butylamide and
4-Methyl-2-{1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide.

93. Connection p formula (1B2), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are NRaRbwhere Raand Rbindependently represent H or -(CO)-C1 -C6-alkyl.

94. Connection p formula (V), where these compounds selected from the group consisting of
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-pyrimidine-2-ylamine;
4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-[2,4',2',3"]terpyridine-6"-ylamine;
5-{1-[6-(4-Chloro-phenyl)-4-trifluoromethyl-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-2-ylamine and
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-[1,2,4]triazole-3-yl}-pyridine-2-ylamine.

95. Connection p formula (V), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl containing 1-3 heteroatom in the cycle selected from nitrogen, oxygen or sulfur, where the substituents are -(SO2)-C1-C6-alkyl.

96. Connection p formula (V), where these compounds selected from the group consisting of
2-{1-[6-Trifluoromethyl-4-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide and
2-[4-(3-Methanesulfonyl-phenyl)-imidazol-1-yl]-4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine.

97. Connection p formula (V), where represents a possibly substituted aryl selected from phenyl, or substituted 5 - or 6-membered heteroaryl, content is the seer 1-3 heteroatoms in the cycle, selected from nitrogen, oxygen or sulfur, where the substituents are -(SO2)-NRcRdwhere Rcand Rdindependently represent H, C1-6-alkyl, possibly substituted by hydroxy, C1-6-halogenoalkane,1-6-alkoxy, -(CO)1-6-alkyl, possibly substituted C1-6-alkoxy, -(CH2CH2O)nCHRewhere Rerepresents N or CH2HE, and n has a value of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, -(CH2)m-aryl, where m has a value of 1 or 2 and the aryl possibly substituted, halogen or1-6-alkoxy, -(CH2)p-C3-6- cycloalkyl, where p is 0 or 1, 5 - or 6-membered heteroseksualci, with one atom of oxygen in the loop.

98. Connection p formula (V), where these compounds selected from the group consisting of
3-{5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-[1,2,4]oxadiazol-3-yl}-benzosulfimide;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid tert-butylamide;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiophene-2-sulfonic acid amide;
N-tert-Butyl-3-{1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
2-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid tre is-butylamide;
3-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-[1,2,4]triazole-3-yl}-benzosulfimide;
3-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
2-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide,
N-tert-Butyl-3-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
3-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
5-{1-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-pyridine-3-sulfonic acid amide;
N-(2-Hydroxy-1,1-dimethyl-ethyl)-3-{1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
4-Methyl-2-{1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid tert-butylamide;
4-Methyl-2-{1-[4-trifluoromethyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-1H-imidazol-4-yl}-thiazole-5-sulfonic acid amide;
N-tert-Butyl-3-[4-metil-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
N-tert-Butyl-3-{1-[6-(4-chloro-phenyl)-4-methyl-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
N-tert-Butyl-3-[4'-methyl-6'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-{4-[4-Methyl-6-(4-trifluoromethyl-phenyl)-pyridine-2-yl]-pyrimidine-2-yl}-benzosulfimide;
3-[4-ethyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-benzosulfimide;
3-[4'-Methyl-6'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]-benzosulfimide;
3-{1-[6-(4-Chloro-phenyl)-4-methyl-pyridine-2-yl]-1H-imidazol-4-yl}-benzosulfimide;
5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid tert-butylamide;
5-[4-Methyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid tert-butylamide;
5-[4-Methyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid amide and
5-[4-Trifluoromethyl-6-(4-trifluoromethyl-phenyl)-[2,4']bipyridinyl-2'-yl]-thiophene-2-sulfonic acid amide.

99. The compound of the formula:
,
representing 3-[6'-methyl-4'-(4-trifluoromethyl-phenyl)-[2,2']bipyridinyl-6-yl]benzosulfimide.

100. The method of obtaining the compounds of formula (XIII), where a is oxadiazolyl group, including the stage of interaction of the compounds of formula (VIII)

with the compound of the formula (XI)

obtaining the compounds of formula (XIII)
,
where, R1, R2and R3and X and Y are as defined in claim 1.

101. The method of obtaining the compounds of formula (XIV), where a is oxadiazolyl group, including the stage of interaction of the compounds of formula (IV)

the compound of formula (XII)

obtaining the compounds of formula (XIV)
,
where, R1, R2and R3and X and Y are as defined in claim 1.

102. The method of obtaining the compounds of formula (XV), where a is as defined for formula (I), (I-a), (I-b) or (I-C) in any one of claims 1, 4-6, 7-8, 23, 38-39, 40-41, 54-55, 77-80 and 87-88, but differs from oxadiazole group stage of the interaction between the compounds of formula (X)

with the derived Bronevoy acid of formula-B(OH)2obtaining the compounds of formula (XV)
,
where, R1, R2and R3and X and Y are as defined in claim 1.

103. Pharmaceutical composition having the properties of an antagonist of metabotropic glutamate receptors mGluR2 containing compound according to any one of claims 1 to 99 in an effective amount.

104. The use of compounds according to any one of claims 1 to 99 in the manufacture of medicaments for treating or preventing the disease or condition, which plays a role or is involved activation of mGluR2.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I)

, where: n equals 0, 1, 2; G denotes CH2, CHR3; R1 denotes H, C1-C6-alkyl, C3-C6-alkenyl, -CH2Ph; R2, R3, R4 independently denote H, CH3, -CH2F, -CHF2, CF3; A denotes 1,4-Ph, 1,3-Ph, which can be optionally substituted with 1-4 substitutes selected from halogen, C1-C4-alkyl, C1-C4alkoxy, fluorinated C1-C4-alkyl and fluorinated C1-C4alkoxy; E denotes NR5, where R5 denotes H, C1-C3-alkyl; Ar denotes a radical of formula

and

where: Ra denotes halogen, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6-alkoxy, fluorinated C1-C6-alkoxy, phenyl sulphonyl, CN, -NR6R7, where R6 and R7, together with an N atom, form a 5- or 6-member saturated ring or denotes a 5-member saturated or unsaturated aromatic or non-aromatic heterocyclic ring containing, as ring members, 1, 2 or 3 heteroatoms selected from N, O and S, and where the heterocyclic ring can carry 1, 2 or 3 substitutes selected from halogen and C1-C6-alkyl, or denotes a 6-member saturated heterocyclic ring containing, as ring members, one N and one O atom; Rb and Rc independently denote H, halogen, CH3, OCH3, CH2F, OCH2F, CHF2, OCHF2, CF3, OCF3, CH2CH2F, OCH2CH2F, CH2CHF2, OCH2CHF2, CH2CF3 or OCH2CF3; Rd denotes Ra or a 5- or 6-member heteroaromatic ring containing, as ring members, 1, 2 or 3 heteroatoms selected from N, O and S, and where the heteroaromatic ring can carry 1 substitute selected from C1-C6-alkyl and C1-C6-alkylthio; Re denotes H or is defined as Ra; Rf is defined as Ra; k equals 0, 1, 2, 3; j equals 0, 1, 2, 3, 4; provided that Ra does not denote F, CH2F, CHF2, CF3, OCF3, if A denotes 1,4-Ph, Ar denotes a radical of formula (A) and Rb and Rc denote H, halogen; except compounds, where R1 denotes propyl, G denotes CH2, n equals 1, A denotes 1,4- Ph, E denotes NH, Ar denotes a radical of formula (F) and Rd denotes halogen, C1-C6-alkyl, C2-C6-alkenyl or a 5-member heteroaromatic ring; and physiologically acceptable acid addition salts thereof.

EFFECT: compounds exhibit 5HT6 receptor simulating activity, which allows for their use in a pharmaceutical composition.

25 cl, 6 tbl, 107 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds specified in cl. 1, and also to a pharmaceutical composition possessing binding activity with respect to Bcl proteins, to applying the declared compounds for preparing a drug for treating cancer and for treating a bcl-mediated disorder.

EFFECT: use of the compounds as Bcl protein inhibitors.

18 cl, 2 tbl, 41 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula where R1, R2 and R3 are independently selected from a group consisting of hydrogen, halogen and lower alkyl containing 1-6 carbon atoms; R4 denotes a residue given in the claim; R5 denotes hydrogen or methyl; R10 is selected from a group consisting of: (i) hydrogen; (ii) (C1-C10) alkyl; (iii) (C1-C10)alkyl, substituted with one or more substitutes independently selected from a group consisting of -N(CH3)2, morpholinyl, (C1-C4) alkoxy, hydroxyl, -CON(CH3)2 and halogen; (iv) monocyclic (C3-C8) cycloalkyl containing one N heteroatom; (v) 9-methyl-9-azabicyclo[3.3.1]nonane; (vi) phenyl; (vii) phenyl substituted with one or more (C1-C4)alkoxy; R11 is selected from a group consisting of hydrogen and (C1-C10)alkyl; or R10, R11 and a nitrogen atom with which they are bonded, together, form a nitric heterocycle or a substituted nitric heterocycle, such as given in the claim. The invention also relates to a pharmaceutical composition, having serotonin type 3 receptor modulating capacity and a method of treating a disorder which depends on serotonin type 3 receptor modulation.

EFFECT: compounds of formula II as serotonin type 3 receptor modulators.

18 cl, 1 tbl, 159 ex

FIELD: chemistry.

SUBSTANCE: invention describes a compound of formula (I): or pharmaceutically acceptable salt thereof, or stereoisomer, in which: n equals 0 or 1; X denotes CH2, C=O; R1 denotes a) -(CH2)mR3 or -CO(CH2)mR3, where m equals 0, 1; and R3 denotes a 5-10-member aryl or heteroaryl, where the heteroaryl denotes a mono- or bicyclic aromatic ring containing 5-10 ring atoms, from which at least one or two atoms are heteroatoms selected oxygen, nitrogen or sulphur, optionally substituted with one or more halogens; b) -C=YR4, where Y denotes O; and R4 denotes: (C1-C10)alkyl; (C1-C10)alkoxy; (C0-C10)alkyl-(5-10-member heteroaryl), where "heteroaryl" denotes a mono- or bicyclic aromatic ring containing 5-10 ring atoms, from which at least one or two atoms are heteroatoms selected from oxygen, nitrogen or sulphur, said heteroaryl is optionally substituted with one or more substitutes selected from halogen, oxo or 2-(C1-C6)alkyl, where Z denotes S; (C0-C10)alkyl-(5-10-member aryl), said aryl is optionally substituted with one or more substitutes selected from halogen; (C1-C6)alkoxy, which itself is optionally substituted with one or more halogens; (C1-C6)alkyl, which itself is optionally substituted with one or more halogens; or -Z-(C1-C6)alkyl, where Z denotes S or SO2, and where said (C1-C6)alkyl can be optionally substituted with one or more halogens; or (C1-C6)alkyl-CO-O-R12, where R12 denotes H or (C1-C6)alkyl; or c) -C=ZNHR6, where Z denotes O or S; and R6 denotes: (C1-C10)alkyl; (C1-C10)alkoxy; 5-10-member aryl or heteroaryl, where "heteroaryl" denotes a bicyclic aromatic ring containing 9 ring atoms, from which at least one or two atoms are oxygen atoms; optionally substituted with one or more substitutes selected from halogen; cyano; (C1-C6)alkoxy, which itself is optionally substituted with one or more halogens; (C1-C6)alkyl, which itself is optionally substituted with one or more halogens; and R2 denotes H or (C1-C6)alkyl. Also described is a pharmaceutical composition for inhibiting TNFα, based on the compound of formula I.

EFFECT: novel compounds which can regulate production of certain cytokines, including TNF-α, are obtained and described.

27 cl, 81 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (IB) or to their pharmaceutically acceptable salts:

, wherein R means formula: R1 means -C(O)NR3R4, -C(O)R3 and -C(O)OR3; each R3 and R4 independently means H, C1-10 alkyl, wherein alkyl is optionally substituted by one -OH; R3 and R4 are bound together with N atoms to form a 5-6-member heterocyclic ring which additionally contains one O heteroatom; R5 means H; R6 means CN; R7 means H; W means C. What is described is a method for producing both them and intermediate compounds of formula (1-1c): , wherein: R1 means -C(O)NR3R4; R3 and R4 are specified above.

EFFECT: compounds (IB) shows DPP-IV inhibitory activity that allows them being used in a pharmaceutical composition.

9 cl, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of general formula (I) or its pharmaceutically acceptable salts which have action of mTOR inhibitors. What is also declared is preparing a pharmaceutical composition containing a therapeutically effective amount of the compound of formula (I) and a pharmaceutically acceptable carrier or diluent; besides, what is declared is the use of the compound of formula (I) or its pharmaceutically acceptable salts for preparing the drug for ensuring anticancer action.

EFFECT: preparing the pharmaceutically acceptable salts for preparing the drug for ensuring anticancer action.

11 cl, 25 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula I wherein the substitutes A, B, B', Q and R1-R5 in formula I are specified as follows: A and B' are one of the following groups: (i) (R6)N(CH2)n, wherein n is 0 or 1; (ii) (CH2)n, wherein n is 0, 1 or 2; (iii) C(O)(CH2)n, wherein n is 0 or 1; or provided each of A and B' represents nitrogen, together they can form a bivalent radical of formula: -(CH2)s-X1-(CH2)t- (a), wherein each s and t is independently 1 or 2, and X1 represents (CH2)n, wherein n is 0 or 1; B is one of the following groups: (i) (R6)N; (ii) oxygen; (iii) C=δ, wherein δ represents oxygen or sulphur; (iv) C(R6)=C(R7); each R6 and R7 independently represent hydrogen, C1-4-alkyl; R1 is specified in the following groups: (i) phenyl group substituted by one or more substitute such as: - halogen specified in F, CI, Br or I, or alkyl1 group; aryl1 or heteroaryl group1; cyano, NH-alkyl1, N(alkyl1)(alkyl1) and amino; - NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl group, or (ii) pyridinyl group which can be substituted by one substitute, such as halogen specified in I, F, Cl or Br; alkyl1 group; aryl1 group; cyano, NH-alkyl1, N(alkyl1)(alkyl1), and amino; -NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl1 group; each R2, R3, R4 and R5 are independently specified in hydrogen or linear or branched alkyl group containing 1 to 10 carbon atoms; Q is specified in the following groups: (i) alkyl1; (ii) aryl1; (iii) heteroaryl1. The compounds of formula (I) are used for preparing a drug showing the c-kit inhibitor properties and aiming at treating a disease specified in neoplastic, allergic, inflammatory and autoimmune diseases.

EFFECT: use of oxazole derivatives as tyrosine kinase inhibitors.

13 cl, 1 tbl, 31 ex

FIELD: chemistry.

SUBSTANCE: described are novel diaminotriazole compounds of general formula

(values of radicals are given in the claim), pharmaceutically acceptable salts thereof, a pharmaceutical composition containing said compounds, a method of inhibiting JAK2 and JAK3 kinase activity and use of the novel compounds to produce a medicinal agent for treating several diseases.

EFFECT: high efficiency of the compounds.

19 cl, 3 tbl, 26 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I:

or pharmaceutically acceptable salts thereof, in which Q is a divalent or trivalent radical selected from C6-10aryl and heteroaryl; where said aryl or heteroaryl in Q is optionally substituted up to 3 times with radicals independently selected from halogen, C1-6 alkyl, C1-6 alkyl substituted with halogen, C1-6 alkoxy group, C1-6 alkoxy group substituted with halogen, -C(O)R20 and -C(O)OR20; where R20 is selected from hydrogen and C1-6 alkyl; and where optionally, the carbon atom neighbouring W2 can be bonded through CR31 or O with a carbon atom of Q to form a 5-member ring condensed with A and Q rings; where R31 is selected from hydrogen and C1-6 alkyl; W1 and W2 are independently selected from CR21 and N; where R21 is selected from hydrogen and -C(O)OR25; where R25 denotes hydrogen; ring A can contain up to 2 carbon ring atoms substituted with a group selected from -C(O)-, -C(S)- and -C(=NOR30)- and can be partially unsaturated and contain up to 2 double bonds; where R30 denotes hydrogen ; L is selected from C1-6alkylene, C2-6alkenylene, -OC(O)(CH2)n-, -NR26(CH2)n- and -O(CH2)n-; where R26 is selected from hydrogen and C1-6 alkyl; where n is selected from 0, 1, 2, 3 and 4; q is selected from 0 and 1; t1, t2, t3 and t4 are each independently selected from 0, 1 and 2; R1 is selected from -X1S(O)0-2X2R6a, -X1S(O)0-2X2OR6a, -X1S(O)0-2X2C(O)R6a, -X1S(O)0-2X2C(O)OR6a, -X1S(O)0-2X2OC(O)R6a and -X1S(O)0-2NR6aR6b; where X1 is selected from a bond, O, NR7a and C1-4alkylene; where R7a is selected from hydrogen and C1-6alkyl; X2 is selected from a bond and C1-6alkylene; R6a is selected from hydrogen, cyanogroup, halogen, C1-6alkyl, C2-6alkenyl, C6-10aryl, heteroaryl, heterocycloalkyl and C3-8cycloalkyl; where said aryl, heteroaryl, cycloalkyl and heterocycloalkyl in R6a is optionally substituted with 1-3 radicals independently selected from hydroxy group, halogen, C1-6alkyl, C1-6alkyl substituted with a cyano group, C1-6alkoxy group and C6-10aryl-C1-4alkoxy group; and R6b is selected from hydrogen and C1-6alkyl; R3 is selected from hydrogen, halogen, hydroxy group, C1-6alkyl, C1-6alkyl substituted with halogen, C1-6alkyl substituted with a hydroxy group, C1-6alkoxy group, C1-6alkoxy group substituted with halogen, -C(O)R23 and -C(O)OR23; where R23 is selected from hydrogen and C1-6alkyl; R4 is selected from R8 and -C(O)OR8; where R8 is selected from C1-6alkyl, heteroaryl, C3-8cycloalkyl and heterocycloalkyl; where said heteroaryl, cycloalkyl or heterocycloalkyl in R8 is optionally substituted with 1-3 radicals independently selected from halogen, C1-6alkyl, C3-8cycloalkyl and C1-6alkyl substituted with halogen; R5 is selected from hydrogen, C1-6alkyl substituted with a hydroxy group, and a C1-6alkoxy group; heteroaryl denotes a monocyclic or condensed bicyclic aromatic ring complex containing 5-9 carbon atoms in the ring, where one or more ring members are heteroatoms selected from nitrogen, oxygen and sulphur, and heterocycloalkyl denotes a saturated monocyclic 4-6-member ring in which one or more said carbon atoms in the ring are substituted with a group selected from -O-, -S- and -NR-, where R denotes a bond, hydrogen or C1-6alkyl. The invention also relates to pharmaceutical compositions containing said compounds, and methods of using said compounds to treat or prevent diseases or disorders associated with GPR119 activity, such as obesity, type 1 diabetes, type 2 sugar diabetes, hyperlipidemia, type 1 autopathic diabetes, latent autoimmune diabetes in adults, type 2 early diabetes, child atypical diabetes, adult diabetes in children, malnutrition-associated diabetes and diabetes in pregnant women.

EFFECT: improved properties of compounds.

27 cl

FIELD: chemistry.

SUBSTANCE: invention relates to 6-piperidinyl-substituted isoquinoline derivatives of formula (I)

, where values of radicals are given in the claim, and compositions containing said compounds.

EFFECT: said compounds and compositions can be useful in treating and preventing diseases associated with Rho-kinase and mediated by Rho-kinase through myosin light chain phosphatase phosphorylation.

31 cl, 378 ex, 12 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted cyclohexylmethyl derivatives, having serotonin, noradrenaline or opioid receptor inhibiting activity, optionally in form of cis- or trans-diastereomers or mixture thereof in form of bases or salts with physiologically compatible acids. In formula (1): R2 denotes H or OH; R1 and R2 together denote or =N-OH, R3 denotes a phenyl residue which is unsubstituted or monosubstituted with a halogen atom or a heteroaryl residue selected from a five-member sulphur-containing heteroaryl such as a thienyl residue or an unsubstituted phenyl residue bonded through a C1-C4alkyl group, R4 and R5 independently denote an unsubstituted C1-C3alkyl or R4 and R5 together denote (CH2)3-6, R8 denotes a linear saturated C1-C4 alkyl group bonded with an aryl, which is unsubstituted or monosubstituted with halogen atoms, R9 denotes a saturated C1-C8alkyl; values of radicals R1, m, n, R6, R7, R10-R13 are given in the claim. The invention also relates to methods of producing compounds of formula (I), a medicinal agent containing said compounds, use of compounds of formula (I) to prepare a medicinal agent for anaesthetic treatment during sharp, neuropathic or chronic pain and for treating depression, urinary incontinence, diarrhoea and alcoholism.

EFFECT: high efficiency of using the compounds.

32 cl, 501 ex, 21 tbl

FIELD: chemistry.

SUBSTANCE: invention describes compounds of formulae (I) and (III), as well as isomers or pharmaceutically acceptable salts thereof: where the values of radicals are given in claim 1 and 5. The invention also relates to a pharmaceutical composition based on said compounds, which has vanilloid receptor antagonist activity, use of said compounds to produce a medicinal agent for preventing or treating a condition which is associated with aberrant expression and/or aberrant activation of the vanilloid receptor. Described also is a method of producing a compound of formula III.

EFFECT: novel compounds which can be used as vanilloid receptor antagonists, for preventing or treating diseases are obtained and described.

40 cl, 281 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pyridine derivatives of formula

wherein A, R1, R2, R3, R4, R5 and R6 are presented in the description, preparing and using them as pharmaceutically active compounds as immunomodulatory agents.

EFFECT: preparing the pharmaceutical composition showing agonist activity with respect to S1P1/EDG1 receptor and using it for prevention and treatment diseases or disorders associated with activated immune system.

20 cl, 244 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to heterocyclic compounds of formula ,

wherein X2 represents residue C-Z-R2 or C-R3, wherein Z represents NH or S; R1 is selected from structures , and R2 and R3 have the values specified in cl.1 of the patent claim, or to their pharmaceutically acceptable salts. The invention also refers to a pharmaceutical composition, a series of specific compounds, application of the declared compounds and to an intermediate compound for preparing the compounds of formula (I).

EFFECT: compounds under the invention have affinity to muscarine receptors and can be used in treating, relieving and preventing diseases and conditions mediated by muscarine receptors.

13 cl, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula I wherein the substitutes A, B, B', Q and R1-R5 in formula I are specified as follows: A and B' are one of the following groups: (i) (R6)N(CH2)n, wherein n is 0 or 1; (ii) (CH2)n, wherein n is 0, 1 or 2; (iii) C(O)(CH2)n, wherein n is 0 or 1; or provided each of A and B' represents nitrogen, together they can form a bivalent radical of formula: -(CH2)s-X1-(CH2)t- (a), wherein each s and t is independently 1 or 2, and X1 represents (CH2)n, wherein n is 0 or 1; B is one of the following groups: (i) (R6)N; (ii) oxygen; (iii) C=δ, wherein δ represents oxygen or sulphur; (iv) C(R6)=C(R7); each R6 and R7 independently represent hydrogen, C1-4-alkyl; R1 is specified in the following groups: (i) phenyl group substituted by one or more substitute such as: - halogen specified in F, CI, Br or I, or alkyl1 group; aryl1 or heteroaryl group1; cyano, NH-alkyl1, N(alkyl1)(alkyl1) and amino; - NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl group, or (ii) pyridinyl group which can be substituted by one substitute, such as halogen specified in I, F, Cl or Br; alkyl1 group; aryl1 group; cyano, NH-alkyl1, N(alkyl1)(alkyl1), and amino; -NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl1 group; each R2, R3, R4 and R5 are independently specified in hydrogen or linear or branched alkyl group containing 1 to 10 carbon atoms; Q is specified in the following groups: (i) alkyl1; (ii) aryl1; (iii) heteroaryl1. The compounds of formula (I) are used for preparing a drug showing the c-kit inhibitor properties and aiming at treating a disease specified in neoplastic, allergic, inflammatory and autoimmune diseases.

EFFECT: use of oxazole derivatives as tyrosine kinase inhibitors.

13 cl, 1 tbl, 31 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula I

,

where A represents S or Se; B represents H or ; R1 represents aryl selected from the following structures:

R2 represents H or ; R3 represents H or C1-C8 alkyl; R4 and R5 independently represent H or C1-C8 alkyl; R6 represents H, C1-C8 alkyl, C2-C7 alkenyl, alkaline metal or alkaline earth metal; R11 and R12 independently represent H, C1-C8 alkyl or halogen; R21 represent H, halogen or C1-C7 alkyl; m and n independently represent integers having values 1-4; p represents an integer having a value of 1-5; q represents an integer having a value of 1-4; r represents an integer having a value of 1-3; s represents an integer having a value of 1-5; as an activator of peroxisome proliferator-activated receptor (PPAR) and its hydrate, solvate, stereoisomer and pharmaceutically acceptable salt, and to a pharmaceutical composition.

EFFECT: preparing an agent for muscle strengthening, an agent for memory improvement, a therapeutic agent for dementia and Parkinson's disease.

15 cl, 8 tbl, 348 ex

FIELD: chemistry.

SUBSTANCE: invention refers to new thiophene derivatives of formula (I) where A is represented by *-CO-CH2CH2-, *-CO-CH=CH, where the asterisks indicate the link through which the formula (I) thiophene group is bound; R1 is represented by C2-5alkyl; R2 is represented by hydrogen, methyl or ethyl; R3 is represented by hydrogen; R4 is represented by C1-4alkyl; R5 is represented by a hydroxy group, 2,3-di-hydroxypropoxygroup or -OCH2-CH(OH)-CH2-NHCOR52; R52 is represented by hydroxymethyl, and R6 is represented by C1-4alkyl; and to its salt. The invention also refers to the pharmaceutical composition that is agonistic in relation to S1P1/EDG1 receptor on the basis of the mentioned compounds.

EFFECT: new compounds and a composition based on them that may find their application in medicine as immunomodulating agents.

17 cl, 2 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: present invention refers to new compounds of formula I-9 where q is represented by 1; R11 is represented by C3-8-alkyl; C3-8-cycloalkyl or C3-8-cycloalkyl-C1-3-alkyl; A is represented by phenyl substituted by one or more substituting groups independently chosen from R12; and R12 is represented by -(CH2)-NR13R14; R13 is represented by C1-6-alkylcarbanil; and R14 is represented by hydrogen; and to the pharmaceutically acceptable salts of such compounds and to the pharmaceutical compositions based on such compounds. It has been revealed that the compounds of formula I-9 are histamine NZ-receptor antagonists and thus that they can be used in treatment of diseases connected with expression of such receptors.

EFFECT: compounds of formula I-9 can be used in treatment of diseases connected with expression of histamine NZ-receptors.

6 cl, 216 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I): where R1 and R2 represent hydrogen and a group which is hydrolysed in a physiological environment, optionally substituted lower alkanoyl or aroyl; X represents a methylene group; Y represents oxygen atom; n represents the number 0, 1, 2 or 3 and m represents the number 0 or 1; R3 represents a group of pyridine N-oxide according to formula A, B or C which is attached as shown by an unmarked linking: where R4, R5, R6 and R7 independently represent aryl, heterocycle, hydrogen, C1-C6-alkyl, C1-C6-alkylthio, C6-C12-aryloxy or C6-C12-arylthio group, C1-C6-alkylsulphonyl or C6-C12-arylsulphonyl, halogen, C1-C6-haloalkyl, trifluoromethyl, or heteroaryl group; or where two or more residues R4, R5, R6 and R7 taken together represent an aromatic ring, and where P represents a central part, preferentially chosen from regioisomers 1,3,4-oxadiazol-2,5-diyl, 1,2,4-oxadiazol-3,5-diyl, 4-methyl-4H-1,2,4-triazol-3,5-diyl, 1,3,5-triazine-2,4-diyl, 1,2,4-triazine-3,5-diyl, 2H-tetrazol-2,5-diyl, 1,2,3-thiadiazol-4,5-diyl, 1-alkyl-3-(alkoxycarbonyl)-1R-pyrrol-2,5-diyl, where alkyl is presented by methyl, thiazol-2,4-diyl, 1H-pyrazol-1,5-diyl, pyrimidine-2,4-diyl, oxazol-2,4-diyl, carbonyl, 1H-imidazol-1,5-diyl, isoxazol-3,5-diyl, furan-2,4-diyl, benzole-1,3-diyl and (Z)-1-cyanoethene-1,2-diyl, and where the regioisomers of the central part include both regioisomers produced by exchanging the nitrocatechol fragment and the -(X)n-(Y)m-R3 fragment. Also, the invention refers to a method for making a compound of formula I, as well as to a method for treating an individual suffering central and peripheral nervous system disorders, to a pharmaceutical composition based on the compounds of formula I, and also to their application for preparing the drug and as COMT inhibitor.

EFFECT: there are produced and described new compounds which show a potentially effective pharmaceutical properties in treating a number of central and peripheral nervous system disorders.

25 cl, 64 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to thiophene derivatives of formula (I) where A denotes *-CO-CN=CH-, *-CO-CH2CH2-, or where the sign * indicates the thiophene bonding site in formula (I), R1 denotes hydrogen or methyl, R2 denotes n-propyl or isobutyl, R3 denotes hydrogen, methyl, ethyl, n-propyl, isopropyl or isobutyl, R4 denotes hydrogen or methoxy, R5 denotes hydrogen, C1-C4alkyl, C1-C4alkoxy or hydrogen, R6 denotes -(CH2)k-(CHR65)p-CHR66-CONR61R62 hydroxy, hydroxy(C2-C4)alkoxy, di(hydroxy(C1-C4)alkyl)(C1-C4)alkoxy, 2,3-dihydroxypropoxy, -OCH2-(CH2)m-NHCOR64, -OCH2-CH(OH)-CH2-NR61R62, -OCH2- CH(OH)-CH2-NHCOR64 or -OCH2-CH(OH)-CH2-NHSO2R63, R61 denotes hydrogen, 2-hydroxyethyl, 2-hydroxy-1-hydroxymethylethyl, carboxymethyl or C1-C4alkylcarboxymethyl, R62 denotes hydrogen, R63 denotes methyl or ethyl, R64 denotes hydroxymethyl, methyl aminomethyl or 2-methyl aminoethyl, R65 denotes hydrogen, R66 denotes hydrogen, m equals 1 or 2, k equals 0, p equals 1, R67 denotes hydrogen, C1-C4alkyl or halogen, and to a salt thereof. The invention also relates to a pharmaceutical composition for preventing or treating diseases or disorders associated with an activated immune system based on said compounds.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine as immunodepressants.

31 cl, 2 tbl, 114 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I)

, where: n equals 0, 1, 2; G denotes CH2, CHR3; R1 denotes H, C1-C6-alkyl, C3-C6-alkenyl, -CH2Ph; R2, R3, R4 independently denote H, CH3, -CH2F, -CHF2, CF3; A denotes 1,4-Ph, 1,3-Ph, which can be optionally substituted with 1-4 substitutes selected from halogen, C1-C4-alkyl, C1-C4alkoxy, fluorinated C1-C4-alkyl and fluorinated C1-C4alkoxy; E denotes NR5, where R5 denotes H, C1-C3-alkyl; Ar denotes a radical of formula

and

where: Ra denotes halogen, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6-alkoxy, fluorinated C1-C6-alkoxy, phenyl sulphonyl, CN, -NR6R7, where R6 and R7, together with an N atom, form a 5- or 6-member saturated ring or denotes a 5-member saturated or unsaturated aromatic or non-aromatic heterocyclic ring containing, as ring members, 1, 2 or 3 heteroatoms selected from N, O and S, and where the heterocyclic ring can carry 1, 2 or 3 substitutes selected from halogen and C1-C6-alkyl, or denotes a 6-member saturated heterocyclic ring containing, as ring members, one N and one O atom; Rb and Rc independently denote H, halogen, CH3, OCH3, CH2F, OCH2F, CHF2, OCHF2, CF3, OCF3, CH2CH2F, OCH2CH2F, CH2CHF2, OCH2CHF2, CH2CF3 or OCH2CF3; Rd denotes Ra or a 5- or 6-member heteroaromatic ring containing, as ring members, 1, 2 or 3 heteroatoms selected from N, O and S, and where the heteroaromatic ring can carry 1 substitute selected from C1-C6-alkyl and C1-C6-alkylthio; Re denotes H or is defined as Ra; Rf is defined as Ra; k equals 0, 1, 2, 3; j equals 0, 1, 2, 3, 4; provided that Ra does not denote F, CH2F, CHF2, CF3, OCF3, if A denotes 1,4-Ph, Ar denotes a radical of formula (A) and Rb and Rc denote H, halogen; except compounds, where R1 denotes propyl, G denotes CH2, n equals 1, A denotes 1,4- Ph, E denotes NH, Ar denotes a radical of formula (F) and Rd denotes halogen, C1-C6-alkyl, C2-C6-alkenyl or a 5-member heteroaromatic ring; and physiologically acceptable acid addition salts thereof.

EFFECT: compounds exhibit 5HT6 receptor simulating activity, which allows for their use in a pharmaceutical composition.

25 cl, 6 tbl, 107 ex

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