SUBSTITUTED CARBONUCLEOSIDES DERIVATIVES USED AS ANTICANCER AGENTS Russian patent published in 2020 - IPC C07D239/42 C07D239/84 C07D251/18 C07D487/04 C07D491/48 C07D519/00 A61K31/519 A61K31/505 A61K31/53 A61P35/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to compounds of general formula I–IV possessing property of enzyme inhibitor PRMT5, their application, pharmaceutical composition based on them, method of treating abnormal growth of cells, including various types of cancer. In general formula I R¹ is selected from a group comprising (C₁-C₈)alkyl and N(R⁴)₂, where each R⁴ independently is A-R¹⁴, where A is absent and R¹⁴ is hydrogen; R² is hydrogen, (C₁-C₈)alkyl or N(R⁵)₂, where each R⁵ independently is hydrogen; each R³ are independently selected from hydrogen, hydroxy, (C₁-C₈)alkyl, or if D is C(R³)₂, R³ additionally selected from fluorine; each R⁹ independently is hydrogen; D is C(R³)₂, O; G is phenyl or 10–12-member heteroaryl ring system with 1 to 2 nitrogen atoms or 9–11-heterocyclic ring system with 1 to 2 heteroatoms selected from nitrogen and oxygen; each R⁸ is absent or is independently selected from a group comprising (C₁-C₈)alkyl, (C₁-C₈)haloalkyl, hydroxy, (C₁-C₈)alkoxy, 5-member heteroaryl with 2-3 heteroatoms selected from N, O and S, CN, halogen and CON(R⁴)₂, and where two R⁸ optionally combined with formation of carbonate; Q is absent; V is N or C, if Z is present, where if V forms a double bond, V is carbon or V is N or CH and forms a double bond with W, if Z is absent; W is C, where if W forms a double bond, if W is carbon; X is N, if Y is present, where if X forms a double bond, X is carbon or X is NR¹⁶, if Y is absent, where R¹⁶ is H or methyl; Y is absent, is CR¹⁰; Z is absent, is CR¹², where each R¹² independently selected from hydrogen, fluorine, chlorine, bromine.

EFFECT: substituted carbonucleosides derivatives used as anticancer agents are disclosed.

39 cl, 2 tbl, 216 ex