PYRAZOLO[1,5-a]PYRIMIDINES, USED AS PROTEIN KINASE INHIBITORS Russian patent published in 2011 - IPC C07D487/04 A61K31/519 A61P35/00 

Abstract RU 2417996 C2

FIELD: chemistry.

SUBSTANCE: in formula I' , R denotes -(C=Q)R2a, CN or Y; Y denotes phenyl, or ; Q denotes O; R2a denotes phenyl, OR5 or N(R5)2; R1 denotes H; Z denotes a bond; R3 and R4 denotes H, halogen, C1-6alkoxy, N(R5)2 or Um-V, where m equals 0 or 1; V denotes H, phenyl, 5-6-member heteroaryl containing up to two nitrogen atoms, 5-6-member heterocyclyl containing up to two heteroatoms selected from N or O, or C1-6aliphatic group; U denotes a C1-6alkylidene chain, where up to two methylene links of the chain may be substituted with -CO2-, -C(O)-, -C(O)NH-, -C(O)NR5; R5 denotes H, C0-6alkykphenyl or C1-6aliphatic group, or two R5 groups, taken together with an atom to which they are bonded are optionally bonded to form a 5-7-member heterocyclic ring containing 1-2 heteroatoms selected from N, O or S; JY is selected from N(R9)2, SR9, OR9, halogen, CN, COOR9, -X-OH, phenyl, -X-phenyl, 5-6-member heteroaryl containing up to two nitrogen atoms, -X-(5-6-member heteroaryl containing up to two nitrogen atoms) or X; X denotes a C1-12aliphatic group; R9 denotes H, C1-6aliphatic group, phenyl, C3-6cycloaliphatic group, 4-6-member heterocyclyl containing up to 2 nitrogen atoms. Invention also relates to a pharmaceutical composition and a method of inhibiting Tec or c-Met kinase activity.

EFFECT: high inhibiting activity towards Tec or c-Met kinase.

16 cl, 11 tbl, 20 ex

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RU 2 417 996 C2

Authors

Khimenes Khuan-Migel'

Negtel Ronal'D

Sharr'Er Zhan-Dam'En

Stamos Din

Li Pan'

Kam Dzhon R.

Aronov Aleks

Dates

2011-05-10Published

2005-11-04Filed