SELECTIVE ESTROGEN RECEPTOR INHIBITORS AND USE THEREOF Russian patent published in 2020 - IPC A61K31/473 C07D471/04 C07D471/14 C07D491/48 C07D491/147 C07D495/04 C07D495/14 A61K31/436 A61K31/4365 A61K31/437 A61K31/4375 A61K31/4355 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention refers to compounds of formulas (I) and (II) and their pharmaceutically acceptable salts possessing properties of selective estrogen receptor inhibitors. In formula (I) A is -CH= or -N= depending on valence; W is -NH- or -O-; a is equal to 1; n is 1, 2, 3 or 4; each R¹ independently represents hydrogen, F, Cl, unsubstituted C_1-6 alkyl, -CF₃, -OR^A or -CN; R² denotes hydrogen, unsubstituted C_1-6 alkyl or CF₃; R³ denotes hydrogen, halogen or unsubstituted C_1-6 alkyl; R⁴ is hydrogen, halogen or unsubstituted C_1-6 alkyl; R⁵ denotes chlorine; R⁶ denotes fluorine or chlorine; R⁷ is -CH₂F; R^A is hydrogen or unsubstituted C_1-6 alkyl. In formula (II) A is -CH= or -N= depending on valence; W is -NH-, -O- or -S-; a is equal to 1; each R¹ independently represents hydrogen, F, Cl, -CF₃, unsubstituted C_1-6 alkyl, -OR^A or -CN; R² denotes hydrogen, unsubstituted C_1-6 alkyl or -CF₃; R³ denotes hydrogen, F or unsubstituted C_1-6 alkyl; R⁴ is hydrogen, F or unsubstituted C_1-6 alkyl, or R³ and R⁴ taken together with intermediate atoms form unsubstituted cyclopropyl; R⁸ represents hydrogen, halogen or methyl; R^A1 represents unsubstituted C_1-6 alkyl, chloro or fluoro; R^A2 is unsubstituted C_1-6 alkyl, chlorine or fluorine; wherein: (i) R^A1 or R^A2 is chlorine or (ii) both R^A1 and R^A2 are chlorine; R^A is hydrogen or unsubstituted C_1-6 alkyl. Invention also relates to pharmaceutical composition, containing an effective amount of compounds of formulas (I) or (II) or their pharmaceutically acceptable salts and a pharmaceutically acceptable excipient. Described also is a method of treating a proliferative disease associated with estrogen receptor activity, comprising administering to a subject in need of treatment, effective amount of the pharmaceutical composition of the invention.

EFFECT: presented are selective estrogen receptor inhibitors and their application.

18 cl, 3 dwg, 8 tbl, 14 ex