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
Title | Year | Author | Number |
---|---|---|---|
1-SULFONYL-1,3-DIHYDROINDOLE-2-ONES, PHARMACEUTICAL COMPOSITIONS (VARIANTS), METHOD FOR THEIR PREPARING AND APPLYING | 2003 |
|
RU2259999C2 |
PHARMACEUTICAL COMPOSITION, METHODS FOR ITS PREPARING AND APPLYING | 2003 |
|
RU2248978C1 |
HETEROCYCLYLSULFINIC ACIDS AND THEIR DERIVATIVES, FOCUSED LIBRARY AND PHARMACEUTICAL COMPOSITION | 2004 |
|
RU2263666C1 |
ANELLATED CARBAMOYL AZAHETEROCYCLES, METHODS FOR THEIR PREPARING (VARIANTS), PHARMACEUTICAL COMPOSITION, FOCUSED LIBRARY | 2004 |
|
RU2266906C1 |
SUBSTITUTED 7-SULFONYL-BENZO[B][1,4]DIAZEPINES (VARIANTS), METHODS FOR THEIR PREPARING (VARIANTS), FOCUSED LIBRARY AND PHARMACEUTICAL COMPOSITION | 2004 |
|
RU2261246C1 |
SUBSTITUTED 2H-PYRANO[2,3-C]PYRIDINES, COMBINATORY AND FOCUSED LIBRARIES | 2003 |
|
RU2261251C2 |
PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING AND USING | 2006 |
|
RU2303597C1 |
SUBSTITUTED 1,2-DIHYDRO[2,7]NAPHTHIRIDINES, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING AND APPLYING | 2003 |
|
RU2243218C1 |
HETEROCYCLIC COMPOUNDS COMPRISING 2-AMINOPYRIDINE-3-SULFOMIC FRAGMENT, METHODS FOR THEIR PREPARING (VARIANTS), FOCUSED LIBRARY AND PHARMACEUTICAL COMPOSITION | 2004 |
|
RU2263667C1 |
ANELLATED CABAMOYLAZAHETEROCYCLES, FOCUSED LIBRARY, PHARMACEUTICAL COMPOSITION AND METHOD FOR ITS PREPARING | 2005 |
|
RU2281947C1 |
Authors
Dates
2005-07-27—Published
2003-08-26—Filed