ESTROGEN RECEPTOR MODULATORS Russian patent published in 2020 - IPC C07D471/04 C07D471/14 C07D209/14 C07D209/18 C07C57/04 C07C61/13 A61K31/437 A61K31/438 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) having structure

,

or a pharmaceutically acceptable salt thereof, wherein A¹ denotes phenyl, optionally substituted with two -F; R¹ is C_4-5 cycloalkyl, optionally substituted with one or two -F, -CF₃; each of R² and R³ is independently selected from a group consisting of hydrogen, halogen, C_1-6 alkyl and C_1-6 haloalkyl; or R² and R³ together with a carbon atom to which R² and R³ are bonded, form C₃ cycloalkyl or C_4-6 heterocyclyl containing one heteroatom selected from O; each of R⁴ and R⁵ is independently selected from a group consisting of hydrogen, C_1-6 alkyl; each of R⁶, R⁷, R⁸ and R⁹ is hydrogen; R¹⁰ is hydrogen; R¹¹ is hydrogen or C_1-6 alkyl; and R¹² is hydrogen or C_1-3 alkyl, which are estrogen receptor alpha modulators. Such compounds, as well as their pharmaceutically acceptable salts and compositions can be used for treating diseases or conditions, which are alpha-dependent estrogen receptor and/or are mediated by estrogen alpha receptor, including conditions characterized by excessive cell proliferation, such as breast cancer.

EFFECT: modulators of estrogen receptors are proposed.

30 cl, 4 tbl, 26 ex