1,3-DIOXO-2,3-DIHYDRO-1H-PYRROLO[3,4-C]QUINOLINES (VARIANTS), PHARMACEUTICAL COMPOSITIONS (VARIANTS), METHOD FOR THEIR PREPARING (VARIANTS) AND METHOD FOR TREATMENT (VARIANTS) Russian patent published in 2005 - IPC

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new substituted 1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines of the general formula (1)

that are effective inhibitors if caspase-3 that can be used for preparing medicinal agents and for experimental (in vitro, in vivo) investigation of apoptosis processes as "pharmacological tools". Also, invention proposes pharmaceutical composition and a method for their preparing and applying. In the general formula (1) radicals R¹, R², R³ and R⁸ represent independently of one another hydrogen atom, halogen atom, CF₃, CN, inert substitute, optionally substituted hydroxyl group, optionally substituted carboxy-(C₁-C₆)-alkyl group, optionally substituted carbamoyl group; R⁴ represents hydrogen atom, halogen atom, inert substitute, optionally substituted amino-group, substituted hydroxyl group; R⁵ represents hydrogen atom, inert substitute, optionally substituted hydroxy-(C₁-C₅)-alkyl, optionally substituted amino-(C₁-C₇)-alkyl, optionally substituted amino-group, optionally substituted hydroxyl group; R⁶ and R⁷ represent independently of one another hydrogen atom, inert substitute, optionally substituted amino-(C₁-C₇)-alkyl, optionally substituted amino-group, optionally substituted hydroxyl group; or R⁶ and R⁷ in common with nitrogen atom to which they are bound represent optionally substituted and optionally additionally including heteroatom taken among group: oxygen, nitrogen or sulfur, 3-10-membered cycle; or R⁶ and R⁷ in common with nitrogen atom to which they are bound represent condensed heterocycle being optionally substituted and optionally additionally including heteroatom taken among group: oxygen, nitrogen or sulfur.

EFFECT: improved preparing method and treatment.

9 cl, 19 sch, 7 tbl, 25 ex