New pyrazolopyridine derivatives are p38 kinase inhibitors useful in medicaments for the treatment or prevention of e.g. cardiovascular diseases, neurodegenerative diseases and proliferative diseases

Реферат: Pyrazolopyridine derivatives (I), their salts, solvates and prodrugs are new. Pyrazolopyridine derivatives of formula (I), their salts, solvates and prodrugs are new. [Image] A : N or N +>O -> R 1>phenyl or het (optionally substituted with one or more substituents of R-a or R-b) R 2>het (optionally substituted with one or more substituents of R-a or R-b) either R 3>H, Cy (optionally substituted with one or more substituents of R-a or R-b) or R 3>1-6C alkyl (optionally substituted with one or more substituents of R-b or Cy*) Cy* : optionally substituted with one or more substituents of R-b or R-c R 4>H, R-a, halo, OR-a', OCOR-a, OSO 2R-a, OCONR-aR-a', NO 2, CN, COR-a', CO 2R-a', CONR-a'R-a', NR-a'R-a', NR-a'COR-a', NR-a'CONR-a'R-a', NR-a'CO 2R-a, NR-a'SO 2R-a, SR-a', SOR-a, SO 2Ra or SO 2NR-a'R-a' R 5> = H or R-f (where R 5> can be placed on any of the 2 N of the pyrazole ring) R-a : 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or Cy (where the groups 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl optionally substituted with one or more substituents of R-b or Cy*, and where any of the groups Cy or Cy* optionally substituted with one or more substituents of R-b or R-c) R-a' : H or R-a R-b : halo, OR-c', OCOR-c, OSO 2R-c, OCONR-cR-c', NO 2, CN, COR-c', CO 2R-c', CONR-c'R-c', CONR-c'NR-c'R-c', NR-c'R-c', NR-c'COR-c', NR-c'CONR-c'R-c', NR-c'CO 2R-c, NR-c'SO 2R-c, SR-c, SOR-c, SO 2R-c, SO 2NR-c'R-c', C(NR-c')NR-c'R-c', C(NSO 2NR-c'R-c')NR-c'R-c', C(NOR-c')R-c', C(NNR-c'R-c')R-c', NR-c'C(NR-c')NR-c'R-c' or NR-c'C(NCN)NR-c'R-c' R-c : 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or Cy (where all these groups optionally substituted with one or more substituents R-d) R-c' : H or R-c R-d : halo, R-e, OR-e', OCOR-e, OSO 2R-e, OCONR-eR-e', NO 2, CN, COR-e', CO 2R-e', CONR-e'R-e', CONR-e'NR-e'R-e', NR-e'R-e', NR-e'COR-e', NR-e'CONR-e'R-e', NR-e'CO 2R-e, NR-eSO 2R-e, SR-e', SOR-e, SO 2R-e, SO 2NR-e'R-e', C(NR-e')NR-e'R-e', C(NSO 2NR-e'R-e')NR-e'R-e', C(NOR-e')R-e', C(NNR-e'R-e')R-e', NR-e'C(NR-e')NR-e'R-e', NR-e'C(NCN)NR-e'R-e or Cy (optionally substituted with one or more substituents of halo, R-e, OR-e', OCOR-e, OSO 2R-e, OCONR-eR-e', NO 2, CN, COR-e', CO 2R-e', CONR-e'R-e', CONR-e'NR-e'R-e', NR-e'R-e', NR-e'COR-e', NR-e'CONR-e'R-e', NR-e'CO 2R-e, NR-eSO 2R-e, SR-e', SOR-e, SO 2R-e, SO 2NR-e'R-e', C(NR-e')NR-e'R-e', C(NSO 2NR-e'R-e')NR-e'R-e', C(NOR-e')R-e', C(NNR-e'R-e')R-e', NR-e'C(NR-e')NR-e'R-e' or NR-e'C(NCN)NR-e'R-e) R-e : (halo)1-6C alkyl R-e' : H or R-e R-f : 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl (all optionally substituted with one or more substituents of R-g or Cy*) or Cy (where any of the groups Cy or Cy* optionally substituted with one or more substituents of R-g or R-a) R-g : halo, OR-a', OCOR-a, OSO 2R-a, OCONR-aR-a', NO 2, CN, COR-a', CO 2R-a', CONR-a'R-a', CONR-a'NR-a'R-a', NR-aR-a', NR-a'COR-a', NR-a'CONR-a'R-a', NR-a'CO 2R-a, NR-a'SO 2R-a, SR-a', SOR-a, SO 2R-a, SO 2NR-a'R-a', C(NR-a')NR-a'R-a', C(NSO 2NR-a'R-a')NR-a'R-a', C(NOR-a')R-a', C(NNR-a'R-a')R-a', NR-a'C(NR-a')NR-a'R-a' or NR-a'C(NCN)NR-a'R-a' Het : pyridine, pyrazine, pyrimidine, pyridazine, 2(1H)-pyridone, 2(1H)-pyrazinone, 2(1H)-pyrimidinone or 2(1H)-pyridazinone and Cy or Cy* : a partially unsaturated, saturated or aromatic 3-7 membered monocyclic or 8-12 membered bicyclic carbocyclic ring (optionally contains 1-4 of N, S or O, which optionally contain 1 or 2 oxo groups when the ring is saturated or partially unsaturated, and where the ring or rings can be bonded to the rest of the molecule through a carbon or a nitrogen atom). ACTIVITY : Immunomodulator Immunosuppressive Antiinflammatory Cardiovascular-Gen. Antimicrobial Osteopathic Neuroprotective Cytostatic. MECHANISM OF ACTION : P38 kinase inhibitor.