PYRASOLBENZODIAZEPINES AS CDK2 INHIBITORS, SYNTHESIS INTERMEDIATES AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME Russian patent published in 2005 - IPC

FIELD: organic chemistry, pharmaceutical compositions.

SUBSTANCE: invention relates to novel pyrasolbenzodiazepines of formula I 1 (in formula R¹ is hydrogen, -NO₂, -CN, halogen, -OR⁵, -COOR⁷, -CONR⁸R⁹, -NR¹⁰R¹¹, NHCOR¹², NHSO₂R¹³; each R² and R⁴ independently of one another are hydrogen, halogen, -NO₂, -CF₃; R³ is hydpegen, C3-C8-cycloalkyl, aryl, in particular C6-C10-aromatic group having 1 or 2 rings, 5-10-membered heteroaryl, having 1 or 2 rings and1-3 heteroatoms, selected from N, O, and S, -COOR⁷, CN, C2-C6-alkenyl, -CONR⁸R⁹ or C1-C6-alkyl optionally substituted with OR⁹-group, F or aryl as mentioned above; R⁵ is C1-C6-alkyl; R⁷ is hydrogen or C1-C6-alkyl; each independently of one another are hydrogen or C1-C6-alkyl optionally substituted with hydroxyl or NH₂, or alternatively R⁸ and R⁹ together form morpholino group; each R¹⁰,^{R11 and R12 independently of one another are hydrogen or C1-C6-alkyl; R13 is C1-C6-alkyl optionally substituted with halogen or -NR14R15; each R14 and R15 independently of one another are hydrogen or C1-C6-alkyl optionally substituted with halogen; or alternatively -NR14R15 is morpholino group) or pharmaceutically acceptable salts thereof, as well as to certain pyrasolbenzodiazepine derivatives, thiolactam intermediates for production of compound (I) and pharmaceutical compositions containing the same. Compound and pharmaceutical composition of present invention are cycline-dependent kinase (CDK2) inhibitors and antiproliferation agents used in treatment or controlling disorders associated with cell proliferation, in particular breast, colon, lung and/or prostate tumors.}

EFFECT: new antiproliferation agents.

20 cl, 12 tbl, 8 ex