Organic compounds

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I), wherein V is specified in -O- or a single bond; W is specified in -N(R5)C(O)-, -S(O)t- and -C(O)O-; X is specified in C(H) or N; Y is specified in S, N(H) or N(CH3); p means 0 or 2; t means 1 or 2; R1 is specified in a group consisting of hydrogen, C1-6alkyl optionally substituted by 1 or 2 halogroups, C3-7cycloalkylC1-6alkyl, 2,3-dihydro-1H-indenyl, C6arC1-6alkyl optionally substituted by one or two halogroups and heteroarylC1-6alkyl, wherein a heteroaryl fragment of the heteroarylalkyl group means 5-6-member monocyclic heteroaryl containing 1 or 2 heteroatoms independently specified in a group consisting of nitrogen optionally oxidated, oxygen and sulphur, or a heteroaryl fragment of the heteroarylalkyl group means 9-member bicyclic heteroaryl containing 1 or 2 heteroatoms independently specified in a group consisting of nitrogen, oxygen and sulphur, wherein monocyclic heteroaryl of the heteroarylalkyl group may be optionally substituted by one or two substitutes independently specified in a group consisting a halogroup, a cyanogroup, C1-6alkyl, haloC1-6alkyl and C1-6alkyl-O-C(O)-; R2 is specified in a group consisting of hydrogen, C1-6alkyl optionally substituted by phenoxy, hydroxy C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl, phenyl optionally substituted by a halogroup, haloC1-6alkyl, C6arC1-6alkyl (optionally substituted by a halogroup, haloC1-6alkyl or haloC1-6alkoxygroup), 2-oxo-imidazolidinyl, heterocyclylC1-6alkyl and heteroarylC1-6alkyl, wherein heterocyclyl of heterocyclylalkyl means 5- or 6-member monocycle containing oxygen, and wherein a heteroaryl fragment of the heteroarylalkyl group means 5-6-member monocycle containing 1-3 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, or a heteroaryl fragment of the heteroarylalkyl group means 9- or 10-member bicycle containing 1 to 2 heteroatoms specified in a group consisting of nitrogen and sulphur, wherein monocyclic heteroaryl of the heteroaryl alkyl group may be optionally substituted by 1 or 2 substitutes independently specified in a group consisting of a halogroup, C1-6alkyl, haloC1-6alkyl and phenyl optionally substituted by a halogroup; R3 is specified in a group consisting of hydrogen and alkyl; two adjacent R4 groups together with carbon atoms whereto attached can form phenyl; R5 means hydrogen; or a pharmaceutically acceptable salt thereof.

EFFECT: preparing the heterocyclic derivatives which modulate activity of stearoyl CoA desaturase, methods of using the above derivatives for modulating activity of stearoyl CoA desaturase and pharmaceutical compositions containing the above derivatives.

26 cl, 1 tbl, 153 ex

 

The text descriptions are listed faxing

11.1. The compound of formula (I):
,
where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)-, -S(O)tand-C(O)O-;
X is chosen from C(H) or N;
Y is chosen from S, N(H) or N(CH3);
p represents 0 or 2;
t represents 1 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography,3-7cycloalkyl1-6alkyl, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms independently selected is from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, which is optionally substituted, phenoxy, hydroxy, C1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl (which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup), 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected the data from the group including holograph, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl;
two adjacent R4group together with the carbon atoms to which they are attached may form a phenyl;
R5denotes hydrogen;
or its pharmaceutically acceptable salt.

2. The compound according to claim 1, or its pharmaceutically acceptable salt, where X denotes S(N) and Y represents S.

3. The compound according to claim 1, or its pharmaceutically acceptable salt, where X represents N and Y represents S.

4. The compound according to claim 1, or its pharmaceutically acceptable salt, where X represents N and Y represents N(H) or N(CH3).

5. The compound according to claim 1, or its pharmaceutically acceptable salt, where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
X is chosen from C(H) or N;
Y is chosen from S, N(H) or N(CH3);
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group including the surrounding nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl(which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup), 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing from 1 to heteroatoms, selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl; and
R5denotes hydrogen.

6. The compound according to claim 2, or its pharmaceutically acceptable salt, where
V is selected from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroarylboronic the group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl (which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup), 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group including hydrogen and al the sludge; and
R5denotes hydrogen.

7. The compound according to claim 3, or its pharmaceutically acceptable salt, where
V is selected from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl;
two adjacent R4group together with the carbon atoms to which they are attached may form a phenyl; and
R5denotes hydrogen.

8. The connection according to claim 7, or its pharmaceutically acceptable salt, where
V denotes a simple link;
W represents-N(R5)C(O)-;
p represents 0 or 2;
R1selected from the group comprising hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl(which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup), 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6/sub> alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl;
two adjacent R4group together with the carbon atoms to which they are attached may form a phenyl; and
R5denotes hydrogen.

9. The connection according to claim 7, or its pharmaceutically acceptable salt, where
V represents-O-;
W represents-N(R5)C(O)-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where GE is ereally fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl, containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment GE is erourolliou group denotes a 9 - or 10-membered Bicycle, containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl;
two adjacent R4group together with the carbon atoms to which they are attached may form a phenyl; and R5denotes hydrogen.
The compound according to claim 4, or pharmaceutically acceptable salt,
where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatom, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, the independent is selected from the group including holograph, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl;
two adjacent R4group together with the carbon atoms to which they are attached may form a phenyl; and
R5denotes hydrogen.

11. The compound according to claim 1, or its pharmaceutically acceptable salt,
where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
X is chosen from C(H) or N;
Y is chosen from S, N(H) or N(CH3);
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group can be neo is Astelin substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and ALK is l; and
R5denotes hydrogen.

12. The compound according to claim 2, or its pharmaceutically acceptable salt,
where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is th optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl; and
R5denotes hydrogen.

13. The compound according to claim 3, or its pharmaceutically acceptable salt,
where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-Digi the ro-1H-indenyl, With6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, which is optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle, sod is Rashi oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group including nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl; and
R5denotes hydrogen.

14. The compound according to claim 4, or pharmaceutically acceptable salt,
where V is chosen from-O - or a simple link;
W is selected from-N(R5)C(O)- or-C(O)O-;
p represents 0 or 2;
R1selected from the group including hydrogen, C1-6alkyl, which is optionally substituted 1 or 2 holography, 2,3-dihydro-1H-indenyl,6ARS1-6alkyl, which is optionally substituted by one or two holography, and heteroaryl1-6alkyl, where the heteroaryl fragment heteroallyl group denotes a 5-6-membered monocyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, to the verge optionally oxidized, oxygen and sulfur, or heteroaryl fragment heteroallyl group refers to 9-membered bicyclic heteroaryl containing 1 or 2 heteroatoms, independently selected from the group comprising nitrogen, oxygen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by one or two substituents, independently selected from the group comprising halogroup, cyano, C1-6alkyl, Gialos1-6alkyl and C1-6alkyl-O-C(O)-;
R2selected from the group including hydrogen, C1-6alkyl, hydroxys1-6alkyl, C3-7cycloalkyl,3-7cycloalkyl1-6alkyl, phenyl, which is optionally substituted by holography, Gialos1-6alkyl, C6ARS1-6alkyl, which is optionally substituted by holography, Gialos1-6the alkyl or Gialos1-6alkoxygroup, 2-oxo-imidazolidinyl, heterocyclic1-6alkyl and heteroaryl1-6alkyl, where heterocyclyl of geterotsiklicheskikh denotes a 5 - or 6-membered monocycle containing oxygen, and where heteroaryl fragment heteroallyl group denotes a 5-6-membered monocycle containing from 1-3 heteroatoms selected from the group comprising nitrogen, oxygen and sulfur, or heteroaryl fragment heteroallyl group denotes a 9 - or 10-membered Bicycle containing 1 to 2 heteroatoms selected from the group is s, including the nitrogen and sulfur, where the monocyclic heteroaryl heteroallyl group may be optionally substituted by 1 or 2 substituents, independently selected from the group comprising halogroup, C1-6alkyl, Gialos1-6alkyl and phenyl, which is optionally substituted by holography;
R3selected from the group comprising hydrogen and alkyl; and
R5denotes hydrogen.

15. The compound is chosen from the group including:
N-benzyl-4-methyl-2-(2-oxo-4-phenylpyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-2-(5-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-(4-chlorophenyl)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-(cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-methoxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-(4-terbisil)-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-(2-cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
2-(4-amino-2-oxopyridine-1(2H)-yl)-N-benzyl-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxopyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(phenylcarbamoyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-2-(3-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxym is d;
N-benzyl-2-(3-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-3-(phenylcarbamoyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-5-(phenylcarbamoyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
2-(4-benzamido-2-oxopyridine-1(2H)-yl)-N-benzyl-4-methylthiazole-5-carboxamide;
N-(4-terbisil)-4-methyl-2-(2-oxopyridine-1(2H)-yl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-N-(4-terbisil)-4-methylthiazole-5-carboxamide;
2-(4-(2-cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-N-(4-terbisil)-4-methylthiazole-5-carboxamide;
2-(4-(2-cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(pyridine-3-ylethoxy)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-2-(5-hydroxy-1-oxoethyl-2(1H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(6-hydroxy-1-exogenesis-1(2H)yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(6-(benzyloxy)-2-oxoindole-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(5-(benzyloxy)-l-exogenesis-2(1H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-1H-imidazol-5-carboxamide;
N-benzyl-5-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-3-methylthiophene-2-carboxamide;
N-benzyl-5-(4-hydroxy-2-oxopyridine-1(2H)-yl)-3-methylthiophene-2-carboxamide;
N-benzyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-1,4-dimethyl-1H-imidazol-5-to Roxane;
N-benzyl-5-(4-(2-cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-3-methylthiophene-2-carboxamide;
ethyl-4-methyl-2-(2-oxo-4-phenylpyridine-1(2H)-yl)thiazole-5-carboxylate;
ethyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylate;
ethyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-1H-imidazole-5-carboxylate;
ethyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-1,4-dimethyl-1H-imidazole-5-carboxylate;
4-methyl-2-(2-oxo-4-phenylpyridine-1(2H)-yl)thiazole-5-carboxylic acid;
4-methyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)thiazole-5-carboxylic acid;
2-(4-(cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylic acid;
2-(4-(2-cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylic acid;
2-(4-methoxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylic acid;
2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylic acid;
ethyl-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylate;
ethyl-2-(4-(cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylate;
ethyl-2-(4-methoxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylate;
ethyl-2-(4-(2-cyclopropylmethoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxylate;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-1H-imidazole-5-carboxylic acid;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-1,4-dimethyl-1H-imidazole-5-carboxylic acid;
2-(4-(benzyloxy)-2-oxopyridine-N)-yl)-4-methyl-N-(pyridine-3-ylmethyl)-1H-imidazol-5-carboxamide;
N-benzyl-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-5-(trifluoromethyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-3-(trifluoromethyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(trifluoromethyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(pyridine-2-ylethoxy)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-3-methyl-5-(2-oxo-4-(4-(trifluoromethyl)benzyloxy)pyridine-1(2H)-yl)thiophene-2-carboxamide;
N-benzyl-5-(4-(4-forbindelse)-2-oxopyridine-1(2H)-yl)-3-methylthiophene-2-carboxamide;
N-benzyl-5-(4-(4-(deformedarse)benzyloxy)-2-oxopyridine-1(2H)-yl)-3-methylthiophene-2-carboxamide;
N-benzyl-3-methyl-5-(2-oxo-4-pentoxifyllin-1(2H)-yl)thiophene-2-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-((5-(trifluoromethyl)furan-2-yl)methoxy)pyridin-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-2-(4-(4-forbindelse)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(4-(trifluoromethyl)benzyloxy)pyridine-1(2H)-yl)thiazole-5-carboxamide;
2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methyl-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
N-(3-terbisil)-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-(cyclopropylmethyl)-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-CT is the oksamid;
4-methyl-2-(2-oxopyridine-1(2H)-yl)-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
N-(2-cyclopropylethyl)-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-(4-florfenicol)-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-peneteneries-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-phenoxypyridine-1(2H)-yl)thiazole-5-carboxamide;
4-methyl-2-(2-oxo-4-(trifluoromethyl)pyridine-1(2H)-yl)-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
N-(3,4-diferensial)-2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(2-Oxymetazoline-1-yl)pyridine-1(2H)-yl)-thiazole-5-carboxamide;
2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methyl-N-(pyridine-4-ylmethyl)thiazole-5-carboxamide;
2-(4-(4-(deformedarse)benzyloxy)-2-oxopyridine-1(2H)-yl)-N-(4-terbisil)-4-methylthiazole-5-carboxamide;
2-(4-methoxy-2-oxopyridine-1(2H)-yl)-4-methyl-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
4-methyl-2-(2-oxo-4-((5-(trifluoromethyl)furan-2-yl)methoxy)pyridin-1(2H)-yl)-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
2-(4-(4-forbindelse)-2-oxopyridine-1(2H)-yl)-4-methyl-N-(pyridine-3-ylmethyl)thiazole-5-carboxamide;
N-(4-terbisil)-2-(4-(4-forbindelse)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-(cyclopentyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-(3,4-diferensial)-2-(4-methoxy-2-occupied is -1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(phenoxymethyl)pyridine-1(2H)-yl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-N-(3,4-diferensial)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-((tetrahydrofuran-2-yl)methoxy)pyridin-1(2H)-yl)thiazole-5-carboxamide;
3-((2-(4-methoxy-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamido)methyl)pyridine-1-oxide;
N-benzyl-4-methyl-2-(2-oxo-4-((5-phenyl-1,3,4-oxadiazol-2-yl)methoxy)pyridin-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-2-(4-((5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-((4-chloro-2-(trifluoromethyl)quinoline-6-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-((6-(trifluoromethyl)pyridin-3-yl)methoxy)pyridin-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-(thiazol-4-ylethoxy)pyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(2-oxo-4-((tetrahydro-2H-Piran-2-yl)methoxy)pyridin-1(2H)-yl)thiazole-5-carboxamide;
N-(benzo[b]thiophene-2-ylmethyl)-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((3-methylthiophene-2-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-N-(2,3-dihydro-N-inden-2-yl)-4-methylthiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((5-methylpyridin-2-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy-2-oxopyridine-1(2H)-yl)-4-methyl-N-(oxazol-2-ylmethyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((5-methyl-2-(trifluoromethyl)furan-3-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-(thiazol-2-ylmethyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((5-methylthiophene-2-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((4-methylthiophene-2-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-N-((1,5-dimethyl-N-pyrrol-2-yl)methyl)-4-methylthiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((1-methyl-1H-imidazol-5-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((1-methyl-1H-pyrazole-4-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((2-methylthiazole-4-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-N-((5-cianfuran-2-yl)methyl)-4-methylthiazole-5-carboxamide;
N-(benzo[d]oxazol-2-ylmethyl)-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
ethyl-5-((2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamido)methyl)furan-2-carboxylate;
N-((1H-indol-2-yl)methyl)-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-(benzo[d]thiazol-2-ylmethyl)-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-((1H-pyrazole-3-yl)methyl)-2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carb is camid;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-N-((6-chloropyridin-3-yl)methyl)-4-methylthiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)thiazole-5-carboxamide;
2-(4-(benzyloxy)-2-oxopyridine-1(2H)-yl)-4-methyl-N-((5-methylfuran-2-yl)methyl)thiazole-5-carboxamide;
N-benzyl-4-methyl-2-(4-((5-methylisoxazol-3-yl)methoxy)-2-oxopyridine-1(2H)-yl)thiazole-5-carboxamide;
N-benzyl-2-(4-((5-chlorothiophene-2-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-((5-chlorothiophene-2-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-((2-isopropylthiazole-4-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-((6-chloropyridin-3-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
N-benzyl-4-methyl-2-(4-((2-methylthiazole-4-yl)methoxy)-2-oxopyridine-1(2H)-yl)thiazole-5-carboxamide;
2-(4-((1,2,4-oxadiazol-3-yl)methoxy)-2-oxopyridine-1(2H)-yl)-N-benzyl-4-methylthiazole-5-carboxamide;
N-benzyl-2-(4-((3,5-dimethylisoxazol-4-yl)methoxy)-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide;
2-(4-hydroxy-2-oxopyridine-1(2H)-yl)-4-methyl-N-(oxazol-2-ylmethyl)thiazole-5-carboxamide; and
N-benzyl-2-(4-cyclopropyl-2-oxopyridine-1(2H)-yl)-4-methylthiazole-5-carboxamide, or its pharmaceutically acceptable salt.

16. Pharmaceutical composition for inhibiting the activity of stearoyl-SOA of desaturase, who with a compound of formula (I) according to any one of claims 1 to 15 or its pharmaceutically acceptable salt, and pharmaceutically acceptable excipient or carrier.

17. A method of inhibiting the activity of human stearoyl-SOA of desaturase (hSCD), which consists in contacting the source of hSCD with a compound according to any one of claims 1 to 15 or its pharmaceutically acceptable salt.

18. The use of the compounds of formula (I) according to any one of claims 1 to 15 or its pharmaceutically acceptable salt to obtain a pharmaceutical composition for the treatment of illness or disease in a subject mediated inhibition of stearoyl-SOA of desaturase.

19. Use p, where the disease or condition is metabolic syndrome, syndrome X, diabetes, insulin resistance, decreased glucose tolerance, non-insulin-dependent diabetes mellitus, type II diabetes, type I diabetes, diabetic complications, disorders of body weight, loss weight, body mass index, or leptin related diseases.

20. The application of claim 19, where the metabolic syndrome is dyslipidemia, obesity, insulin resistance, hypertension, microalbuminemia, hyperuricemia or hypercoagulable.

21. Use p, where the disease body mass refers to obesity, overweight, cachexia or anorexia.

22. Use p where disease or disease is a skin disease.

23. The application of article 22, where the skin disease is one the Xia eczema, acne, psoriasis, or education, or prevention of keloid scars.

24. The compound of formula (I) according to any one of claims 1 to 15 for use as a medicinal product with the activity of stearoyl-SOA of desaturase.

25. Pharmaceutical composition comprising a compound of formula (I) according to any one of claims 1 to 15 or its pharmaceutically acceptable salt, pharmaceutically acceptable excipient or carrier, for use as a medicinal product with the activity of stearoyl-SOA of desaturase.

26. The use of the pharmaceutical composition according to item 16 or 25 to obtain drugs for the treatment of illness or disease in a subject mediated inhibition of stearoyl-SOA of desaturase.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a 2H-chromen compound or a derivative thereof having action of a S1P1 agonist. The above may be used for preventing and/or treating a disease caused by undesired lymphocyte filtration, or a disease caused by abnormal cell proliferation or accumulation.

EFFECT: preparing the compounds for preventing and/or treating the disease caused by undesired lymphocyte filtration, or the disease caused by abnormal cell proliferation or accumulation.

8 cl, 131 tbl, 156 ex

FIELD: biotechnologies.

SUBSTANCE: invention relates to derivatives of aminopyrazol with the formula of , where A, E, R1 and R2 have values specified in the invention claims, and to their pharmaceutically acceptable salts. Compounds of the formula (I) are agonists of the ALX receptor. Besides, the invention relates to a pharmaceutical composition on the basis of the compound of the formula (I) or its pharmaceutically acceptable salt and to application of these compounds for production of a medicinal agent for prevention or treatment of a disease selected from inflammatory diseases, wheezing diseases, allergic states, HIV-mediated retrovirus infections, cardiovascular diseases, neuroinflammations, neurological disorders, pain, prion-mediated diseases and amiloid-mediated diseases; and for modulation of immune responses.

EFFECT: higher efficiency of compound application.

23 cl, 1 tbl, 466 ex

FIELD: chemistry.

SUBSTANCE: invention provides to a high degree a safe pharmaceutical drug which is effective for diseases caused by MMP-2 and/or MMP-9. The pharmaceutical drug contains, as an active ingredient, at least one member selected from a group which consists of thiazole derivatives of formula (1): where R1 is a phenyl group which can have 1-3 lower alkoxy groups as substitutes in the phenyl ring, and R2 is a pyridyl group which can have 1-3 carboxyl groups as substitutes in the pyridine ring, or salts thereof.

EFFECT: high activity and use when treating diseases such as fibrosis and pulmonary emphysema.

4 cl, 4 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I), stereoisomers, trans- and cis-isomers, racemates or pharmaceutically acceptable salts thereof, having modulating activity on histamine H3-receptors. In formula (I) m equals 0; one of R1 and R2 is selected from a group which includes hydrogen, C1-10alkoxycarbonyl, amido-, carboxy-, C3-8cycloalkyl, halogen, -NRARB, (NRARB)carbonyl, or a group of formula -L2-R6; the other of R1 and R2 is selected from a group which includes hydrogen, halogen; each of R3a and R3b is independently selected from a group which includes hydrogen; each of R4 and R5 is independently selected from a group which includes C1-10alkyl and C1-10hydroxyalkyl; or R4 and R5, taken together with a nitrogen atom to which each is bonded, form a heteroaromatic ring of the type (a) or (b), where Q1 is O or C; Q2 is -N(R20)-; R20 is selected from a group which includes hydrogen and C1-10alkoxycarbonyl; each of p1 and p2 is independently equal to 1, 2 or 3; each of q1, q2, q3, q4 and q5 are independently equal to 0, 1 or 2; and wherein each carbon atom in the ring is substituted with hydrogen or 0, 1 or 2 substitutes, independently selected from a group which includes hydrogen, hydroxy group, fluorine, C1-10alkyl, C1-10hydroxyalkyl and C1-10fluoroalkyl; R6 is a phenyl, heterocycle or heterocycloC1-4alkyl, wherein the heterocycle is a 4-6-member aromatic or non-aromatic ring which contains 1 or 2 heteroatoms independently selected from N, O and S, optionally condensed with a benzene ring, wherein the phenyl or heterocycle can be unsubstituted or optionally substituted with one or more substitutes independently selected from a group which includes C1-4alkoxy, C1-4alkyl, cyano, halogen and oxo-; L is a bond or C1-4alkylene; L2 is a bond, C1-4alkylene, -C(=O)-, -SO2N(R14a)-, -N(R14a)SO2-, -C(O)N(R14a)-, -N(Rl4a)C(O)- or -N(R15)-; R10 is selected from a group which includes hydrogen; R14a is selected from a group which includes hydrogen; R15 is selected from a group which includes hydrogen; and RA and RB are independently selected from a group which includes hydrogen, C1-10alkyl, C1-10acyl, C1-4halogenalkyl, C1-10alkoxycarbonyl, C3-8cycloalkyl and C3-8cycloalkylcarbonyl. The invention also relates to a pharmaceutical composition which contains compounds of formula (I), a method for selective modulation of effects of histamine H3-receptors, use of said compounds in producing a medicament for treating a condition or disorder modulated by histamine H3-receptors, as well as specific compounds of formula (I).

EFFECT: improved properties of compounds.

18 cl, 2 tbl, 154 ex

FIELD: chemistry.

SUBSTANCE: described are novel chiral cis-imidazolines selected from a group which includes 2-{4-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyrimidin-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazin-1-yl}-acetamide, [(4S,5R)-2-(2-tert-butyl-4-ethoxypyrimidin-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazol-1-yl]-[4-(1,1-dioxohexahydrothiopyran-4-yl)-piperazin-1-yl]-methanone, [(4S,5R)-2-(2-tert-butyl-4-ethoxypyrimidin-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazol-1-yl]-[4-(3-methanesulphonylpropyl)-piperazin-1-yl]-methanone, 2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridin-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazin-1-yl}-N,N-bis-(2-methoxyethyl)-acetamide. 2-{1-[(48;5K)-2-(6-tert-butyl-4-ethoxypyridin-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidin-4-yl}-acetamide and others described by the general structural formula (I), and pharmaceutical composition containing said compounds.

EFFECT: compounds can be used as anti-cancer agents, particularly as agents for treating solid tumours.

8 cl, 217 ex

FIELD: chemistry.

SUBSTANCE: invention relates to an amide derivative of formula (I), where A is benzene or pyridine, where the benzene or pyridine optionally contain 1 or 2 or 3 identical or different substitutes selected from an alkyl containing 1-6 carbon atoms, a cycloalkyl containing 3-6 carbon atoms, an alkoxy containing 1-6 carbon atoms, a halogen atom, nitro, cyano, alkylsulphonyl containing1-6 carbon atoms, amino, cyclic amine selected from 1,1-di-oxoisothiazolidinyl, 2-oxooxazolidinyl, oxopyrrolidinyl, 1,1-dioxothiazinyl and 2-oxoimidazolidinyl optionally having a substitute selected from an alkyl containing 1-6 carbon atoms and an alkylcarbonyl containing a total of 2-7 carbon atoms, acylamino containing a total of 2-7 carbon atoms, and an alkylsulphonyl amino containing 1-6 carbon atoms, wherein the right-side bond is linked to the carbonyl and the left-side bond is linked to the nitrogen atom, R1 and R2 are identical or different and each is a hydrogen, an alkyl containing 1-6 carbon atoms and optionally containing 3 halogen atoms as substitutes, a cycloalkyl containing 3-6 carbon atoms, a phenyl, a halogen atom or a cyano group and R1 and R2 are not a hydrogen atom at the same time, R3 is a hydrogen atom, an alkyl containing 1-6 carbon atoms, an alkenyl containing 2-6 carbon atoms, a cycloalkyl containing 3-6 carbon atoms, or a halogen, R4a, R4b and R4c are each independently a hydrogen atom, an alkyl containing 1-6 carbon atoms, or an oxo, R5a, R5b and R5c are identical or different and each is a hydrogen atom, an alkyl containing 1-6 carbon atoms and optionally containing substitute(s) selected from phenyl, an alkoxy group containing 1-6 carbon atoms, optionally substituted with an alkoxy group containing 1-6 carbon atoms, a phyenylcarbonyloxy group and a hydroxy group, or a phenyl, X is a carbon atom (any of R4a, R4b and R4c can be bonded to a carbon atom, but the carbon atom is not substituted with oxo) or a nitrogen atom (if Y is a single bond, the nitrogen atom can be oxidised to form an N oxide), Y is a single bond, a carbonyl or an oxygen atom, Z1 and Z2 are each independently a carbon atom (substitute R3 is optionally bonded to a carbon atom) or a nitrogen atom, and m equals 1 or 2, a pharmacologically acceptable salt thereof. The amide derivative is used as a preventive/therapeutic drug for treating autoimmune diseases, inflammatory bowel diseases or osteoarthritis.

EFFECT: amide derivative which suppresses production of inductive type MMP-9.

14 cl, 4 tbl, 581 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: application describes prodrugs being 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)-phenyl]pyridine-3,5-dicarbonitryl derivatives, and a method for preparing them.

EFFECT: invention can find application in treating and/or preventing cardiovascular diseases.

8 cl, 4 tbl, 18 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing substituted pyrimidin-5-yl carboxylic acids of formula I and can be used in organic chemistry. The method is realised by reacting N-substituted guanidines and hetarylamidines with ethoxymethylene derivatives of 1,3-ketoesters according to a scheme given below (where the substitutes are as defined in the claim).

EFFECT: improved method of producing substituted pyrimidin-5-yl carboxylic acids of formula I.

2 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: invention relates to isoxazole-pyridine derivatives of formula , where X; R1; R2, R3, R4, R5 and R6 are as described in claim 1 of the invention and a pharmaceutically acceptable salt thereof. The invention also relates to a medicinal agent for treating diseases associated with the binding site of the GABA A α5 receptor based on compounds of formula I and use of said compounds in preparing a medicinal agent.

EFFECT: novel compounds are active towards the binding site of said receptor and are useful in treating cognitive disorders such as Alzheimer's disease.

22 cl, 372 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I , wherein R2 means methyl, Y means carbon or nitrogen, and R1, R3 and R4 have the value specified in the patent claim. Also, the invention refers to a pharmaceutical composition for the use as a pharmaceutical drug having activity of a phosphatidylinositol-3-kinase inhibitor, to the use of the compounds of formula I for preparing the pharmaceutical drug for treating a disease mediated by phosphatidylinositol 3-kinase and to a method for preparing the compounds of formula I .

EFFECT: preparing the compounds of formula I possessing activity of the phosphatidylinositol-3-kinase inhibitor.

10 cl, 5 tbl, 51 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of formula (I) or pharmaceutically acceptable salts thereof wherein A, R1, R2, R3 and m are specified in the patent claim. The present invention also refers to the number of specific compounds, and to a pharmaceutical composition containing the above compounds effective for inhibition of kinases, such as glycogen synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus kinase (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

EFFECT: preparing the specific compounds and pharmaceutical composition containing the above compounds effective for kinase inhibition.

18 cl, 393 ex

FIELD: chemistry.

SUBSTANCE: invention provides to a high degree a safe pharmaceutical drug which is effective for diseases caused by MMP-2 and/or MMP-9. The pharmaceutical drug contains, as an active ingredient, at least one member selected from a group which consists of thiazole derivatives of formula (1): where R1 is a phenyl group which can have 1-3 lower alkoxy groups as substitutes in the phenyl ring, and R2 is a pyridyl group which can have 1-3 carboxyl groups as substitutes in the pyridine ring, or salts thereof.

EFFECT: high activity and use when treating diseases such as fibrosis and pulmonary emphysema.

4 cl, 4 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I), stereoisomers, trans- and cis-isomers, racemates or pharmaceutically acceptable salts thereof, having modulating activity on histamine H3-receptors. In formula (I) m equals 0; one of R1 and R2 is selected from a group which includes hydrogen, C1-10alkoxycarbonyl, amido-, carboxy-, C3-8cycloalkyl, halogen, -NRARB, (NRARB)carbonyl, or a group of formula -L2-R6; the other of R1 and R2 is selected from a group which includes hydrogen, halogen; each of R3a and R3b is independently selected from a group which includes hydrogen; each of R4 and R5 is independently selected from a group which includes C1-10alkyl and C1-10hydroxyalkyl; or R4 and R5, taken together with a nitrogen atom to which each is bonded, form a heteroaromatic ring of the type (a) or (b), where Q1 is O or C; Q2 is -N(R20)-; R20 is selected from a group which includes hydrogen and C1-10alkoxycarbonyl; each of p1 and p2 is independently equal to 1, 2 or 3; each of q1, q2, q3, q4 and q5 are independently equal to 0, 1 or 2; and wherein each carbon atom in the ring is substituted with hydrogen or 0, 1 or 2 substitutes, independently selected from a group which includes hydrogen, hydroxy group, fluorine, C1-10alkyl, C1-10hydroxyalkyl and C1-10fluoroalkyl; R6 is a phenyl, heterocycle or heterocycloC1-4alkyl, wherein the heterocycle is a 4-6-member aromatic or non-aromatic ring which contains 1 or 2 heteroatoms independently selected from N, O and S, optionally condensed with a benzene ring, wherein the phenyl or heterocycle can be unsubstituted or optionally substituted with one or more substitutes independently selected from a group which includes C1-4alkoxy, C1-4alkyl, cyano, halogen and oxo-; L is a bond or C1-4alkylene; L2 is a bond, C1-4alkylene, -C(=O)-, -SO2N(R14a)-, -N(R14a)SO2-, -C(O)N(R14a)-, -N(Rl4a)C(O)- or -N(R15)-; R10 is selected from a group which includes hydrogen; R14a is selected from a group which includes hydrogen; R15 is selected from a group which includes hydrogen; and RA and RB are independently selected from a group which includes hydrogen, C1-10alkyl, C1-10acyl, C1-4halogenalkyl, C1-10alkoxycarbonyl, C3-8cycloalkyl and C3-8cycloalkylcarbonyl. The invention also relates to a pharmaceutical composition which contains compounds of formula (I), a method for selective modulation of effects of histamine H3-receptors, use of said compounds in producing a medicament for treating a condition or disorder modulated by histamine H3-receptors, as well as specific compounds of formula (I).

EFFECT: improved properties of compounds.

18 cl, 2 tbl, 154 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention relates to methods of synthesis and to intermediate products of compounds of formula (XVII) and salts thereof.

EFFECT: preparing the hepatitis C virus protease inhibitor.

32 cl, 13 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I , wherein R2 means methyl, Y means carbon or nitrogen, and R1, R3 and R4 have the value specified in the patent claim. Also, the invention refers to a pharmaceutical composition for the use as a pharmaceutical drug having activity of a phosphatidylinositol-3-kinase inhibitor, to the use of the compounds of formula I for preparing the pharmaceutical drug for treating a disease mediated by phosphatidylinositol 3-kinase and to a method for preparing the compounds of formula I .

EFFECT: preparing the compounds of formula I possessing activity of the phosphatidylinositol-3-kinase inhibitor.

10 cl, 5 tbl, 51 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new indole compounds of formula:

wherein A means 5-member heteroaryl or heterocyclyl each of which has 1 to 3 heteroatoms specified in N, O and S, R1 means R5 -X-B-X'-, R2 means -(CR8 R9 )p-Y-R7, R3 means hydrogen, C1-C6-alkyl or -(CH2)q-C3-C6-cycloalkyl, R4 means C3-C6-cycloalkyl (the other radical values are presented in cl.1 of the patent claim), their pharmaceutically acceptable salts or isomers which may be used for preventing or treating cell necrosis and necrosis-related diseases.

EFFECT: preparing the compounds to be used for preventing or treating cell necrosis and necrosis-related diseases.

34 cl, 2 tbl, 263 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented nitrogen-containing heterocyclic compounds presented by the following formula wherein the radical values are specified in the description. These compounds or their pharmaceutically acceptable salts possess strong EP1 activity if introduced in a human or an animal; they are used as an effective component of a pharmaceutical agent, e.g. for preventing and/or treating overactive bladder.

EFFECT: compounds are used as an effective component of the pharmaceutical agent for preventing and/or treating the symptoms including frequent urination, heavy urination demand accompanied by fear of involuntary urination, and urinary incontinence.

24 cl, 145 ex, 5 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to (aza)indole derivatives of formula

wherein the values T, X1-X3, R1, Q, Y, J are presented in clause 1 of the patent claim.

EFFECT: compounds possess xanthine oxidase inhibitory action that enables using it in a pharmaceutical composition for treating a disease specified in a group consisting of hyperuricemia, gouty tophus, gouty arthritis, renal diseases associated with hyperuricemia and nephrolithiasis.

19 cl, 62 tbl, 332 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 7-substituted indoles of formula I:

or their pharmaceutically acceptable salts wherein the values A1, B1, C1, D1, E1, F1, G1, L are presented in cl. 1 of the patent claim.

EFFECT: compounds inhibit activity of anti-apoptotic protein Mc1-1 that enables using them in pharmaceutical compositions.

5 cl, 7 dwg, 2 tbl, 609 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof: where: each of R1, R2, R3, R4 is independently selected from a group consisting of a hydrogen atom, a halogen atom, an aryl, a C5-6 heteroaryl having 1-3 heteroatoms in the ring which are selected from O, S and N, -OR5, -NR5R6, and -NR5COR6, where said aryl or C5-6 heteroaryl, having 1-3 heteroatoms in the ring selected from O, S and N, is unsubstituted or additionally substituted with one or more groups selected from a group consisting of alkyl, alkoxyl and halogen, each of R5 and R6 is independently selected from a group consisting of a hydrogen atom or an alkyl, where said alkyl is unsubstituted or additionally substituted with one or more groups selected from a group consisting of an aryl, haloaryl, hydroxyl and alkoxyl. The invention also relates to a pharmaceutical composition which inhibits protein kinase and contains a compound of formula I, a method of producing the compound of formula I, use of said compounds to produce a medicinal agent for treating disorders associated with protein kinase, and a method of modulating catalytic activity of protein kinase.

EFFECT: improved method.

10 cl, 24 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a dye which contains a binding group in its molecular structure, wherein said binding group provides covalent bonding of said dye to a surface, and said binding group is represented by formula 1 , in which the binding site of said binding group inside said molecular structure of said dye is located at the terminal carbon atom marked with an asterisk in said formula. G is selected from -COOH, -SO3H, -PO3H2, -BO2H2 -SH, -OH, -NH2, A is selected from a group consisting of H, -CN, -NO2, -COOR, -COSR, -COR, -CSR, -NCS, -CF3, -CONR2, -OCF3, C6H5.mFm, in which m=1-5, R is H or any linear or branched alkyl chain of general formula -CnH2n+1 n=0-12, preferably 0-4, or any substituted or unsubstituted phenyl or biphenyl, where said dye is represented by formula (2) or formula (4), where said chromophore is a squarylium dye derivative or a croconium dye derivative, which is capable of absorbing light with a wavelength in the visible and/or infrared range, preferably in the range from 300 to 1200 nm or part thereof, wherein each derivative of said squarylium dye and said croconium dye has aromatic ring systems Ar1 and Ar2, that are bonded to the squarylium dye or croconium dye derivatives. The invention also relates to methods of producing chromophore which is part of a dye and is a dye itself, as well as devices using said dye and applications thereof as a sensitising agent and a sensor.

EFFECT: disclosed dyes are also capable of absorbing light in the long-wave spectral range.

32 cl, 23 ex, 20 dwg

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