Hydrazinocarbonyl-thieno[2,3-c]pyrazoles, their preparation, compositions containing them and their use as inhibitors of protein kinases.

Abstract

Title compds. I [R1 = independently NHCOR2, NHCONHR2, NHCOOR2; R2 = H, (un)substituted cyclo/alkyl, hetero/aryl, etc.; R3-R5 = independently H, (un)substituted alkyl, alkyl/aryl, alkyl/heteroaryl; or NR3R4 = (un)substituted heterocyclyl; etc.] were prepd. as inhibitors of protein kinases, particularly Aurora 2 kinase (data) for treating cancer (no data). E.g., a 7-step synthesis starting from 3,4,5-tribromopyrazole was given for thienopyrazole II. II inhibited Aurora 1, Aurora 2, CDK2 and Tie2 with IC50 of 8 nM, 8 nM, 177 nM, and 117 nM, resp. I are useful for treating neoplasm, psoriasis, glaucoma, leukemias, inflammations, etc. [on SciFinder(R)]