| 摘要 |
The invention provides compounds of formula I,;;wherein:
R1 represents a cyclic group selected from phenyl, heteroaryl1, heterocyclyl1 and C3-6 cycloalkyl;
wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C1-6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C1-6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl1a and heterocyclyl1a;and wherein each cyclic group is optionally fused to a benzene ring or a 5- or 6-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole;and wherein heterocyclyl1 and heterocyclyl1a may additionally be substituted with ═O;X represents a bond or C1-6 alkylene (which may be straight or branched);R2 represents H or C1-6 alkyl;R3 represents H or C1-6 alkyl;Y represents a bond or C1-6 alkylene (which may be straight or branched, and optionally substituted with OH or CF3);R4 represents a cyclic group selected from phenyl, heteroaryl4, heterocyclyl4 and C3-6 cycloalkyl;
wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C1-6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C1-6 alkyl substituted with phenyl, C1-6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl4a and heterocyclyl4a;and wherein each cyclic group is optionally fused to benzene ring or a 5- or 6-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole;and wherein heterocyclyl4 and heterocyclyl4a may additionally be substituted with ═O;heteroaryl1, heteroaryl1a, heteroaryl4 and heteroaryl4a independently represent a 5- or 6-membered heteroaryl group containing from 1 to 3 heteroatoms (selected from N, O and S); andheterocyclyl1, heterocyclyl1a, heterocyclyl4 and heterocyclyl4a independently represent a 5- or 6-membered heterocyclyl group containing from 1 to 3 heteroatoms (selected from N, O and S);
and pharmaceutically acceptable salts and solvates thereof.;The compounds are useful as pharmaceuticals, particularly in the treatment of fibrotic diseases, cancer and pain. |
