3,4-SUBSTITUTED 1H-PIRAZOLE COMPOUNDS AND THEIR APPLICATION AS CYCLIN-DEPENDANT KINASES (CDK) AND MODULATORS OF GLYCOGEN SYNTHASE KINASE-3 (GSK-3) Russian patent published in 2011 - IPC C07D231/38 C07D231/40 C07D231/12 C07D401/12 C07D401/14 C07D231/42 C07D403/04 C07D403/12 C07D405/12 C07D405/14 C07D409/12 C07D413/12 A61K31/415 A61K31/4155 A61K31/454 A61K31/422 A61K31/5377 A61P35/00 A61P31/10 A61P31/12 A61P37/00 A61P25/28 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (Ia) or their pharmaceutically acceptable salts, tautomers, or N-oxides, for use in prevention or treatment of unhealthy conditions or diseases, mediated with cyclin-dependent kinase and glycogen synthase-kinase-3, such as cancerous diseases. In formula (Ia) X stands for group R¹-A-NR⁴; A stands for link, C=O, or NR^g(C=O, where R⁸ stands for hydrogen or C_1-3 alkyl; Y stands for link or alkylene chain, made of 1, 2 or 3 atoms of carbon; R¹ stands for carbocyclic or heterocyclic group, containing from 3 to 12 circular units; or saturated C_1-8hydrocarbyl group, optionally substituted with one or more substituents selected from halogen (for instance, fluorine), hydroxygroups, C₁.₄alkoxygroups, and carbocyclic or heterocyclic groups, and where 1 or 2 atoms of hydrocarbyl group carbon may be optionally substituted with atom or group selected from O, S, NH, SO, SO₂; R² stands for hydrogen or methyl; R³ is selected from hydrogen and carbocyclic or heterocyclic groups, containing from 3 to 6 circular units; and R⁴ stands for hydrogen or methyl. Specified carbocyclic and heterocyclic groups are determined in formula of invention and may be optionally substituted with groups specified in invention formula. Objects of invention are also a pharmaceutical composition based on proposed compounds, their application to produce medicinal agents and methods of their application.

EFFECT: production of pharmaceutical composition based on proposed compounds for use in prevention or treatment of unhealthy conditions or diseases, mediated with cyclin-dependent kinase and glycogen synthase-kinase-3, such as cancerous diseases.

48 cl, 6 tbl, 254 ex