DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVES Russian patent published in 2011 - IPC C07D487/04 A61K31/519 A61P35/00 A61P43/00 

FIELD: chemistry.

SUBSTANCE: invention describes a compound of general formula where A¹ is selected from the following formula R^1c denotes a hydrogen atom, a lower alkenyl group or a -Q³-A³(R^1d)R^1e group; A³ denotes a methane or lower alkyl group; Q³ denotes a single bond; R^1d and R^1e independently denote a hydrogen atom, hydroxyl group, lower alkyl group or hydroxyl-containing lower alkyl group, or together form a lower alkylene group in which one or two or more methylene groups constituting the lower alkylene group can be independently substituted with an oxygen atom; R¹ denotes a lower alkenyl group or a lower alkynyl group; R² denotes a phenyl, pyridyl or thienyl group, which can contain a -Q⁴-A⁴(R^1g)R^1h group; A⁴ denotes a nitrogen atom, a lower alkyl group optionally substituted with a hydroxy-lower alkyl group, or a methane group optionally substituted with a halogen atom, a hydroxyl group, a lower alkyl group or a hydroxy-lower alkyl group; Q denotes a single bond or a lower alkylene group in which one or two or more methylene groups constituting the lower alkylene group can be independently substituted with an oxygen atom; R^1g and R^1h independently denote a hydrogen atom, a lower alkyl group or a lower alkylsulphonyl group; R⁵ and R⁶ independently denote a hydrogen atom, a lower alkyl group or a hydroxyl-containing lower alkyl group, or a pharmaceutically acceptable salt thereof. The invention also describes a pharmaceutical composition based on compounds of formula I, having anti-cancer activity, an anticancer agent, a codrug, as well as an exposure sensitising agent containing the pharmaceutical composition.

EFFECT: novel compounds are obtained and described, having excellent Well-kinase inhibitory action and can therefore be used in medicine, especially when treating different malignant tumours.

13 cl, 21 ex