ANDROGEN RECEPTOR SELECTIVE DESTROYING (SARD) LIGANDS AND METHODS OF THEIR USE Russian patent published in 2023 - IPC C07D213/56 C07D231/10 C07D207/14 A61K31/415 A61K31/40 A61K31/4164 A61K31/4196 A61P35/00 C07D401/12 

Abstract RU 2795431 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound represented by the structure of formula I, where T represents OH; R1 is CH3; Y is H, CF3, F, I, Br, Cl or CN; Z is H, NO2, CN, halide, COOH, COR, NHCOR or CONHR; X is CH or N; R represents H, C1-C6 alkyl or CH2Cl; A is R2; R2 is a pyrazole, imidazole or triazole ring unsubstituted or substituted with at least one of Q1, Q2, Q3 or Q4 each independently selected from hydrogen, linear or branched C1-C6 alkyl, C1-C6 haloalkyl, phenyl, F, Cl, Br, I, CN, NO2, OR, benzyl, NHCOOR, N(R)2, NHCOR, CONHR, COOR or COR; where the specified phenyl is not substituted or substituted by halogen; or its optical isomer or pharmaceutically acceptable salt. The invention relates to a pharmaceutical composition having selective androgen receptor disruption (SARD) activity, containing a therapeutically effective amount of a SARD compound of the invention, or an optical isomer or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

EFFECT: compounds that selectively destroy androgen receptors (SARD) based on pyrazole, imidazole, triazole for use in the treatment of prostate cancer, prostate cancer resistant to enzalutamide and abiratrenone, cancer sensitive to androgen receptors (AR).

23 cl, 4 tbl, 49 dwg, 10 ex

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RU 2 795 431 C2

Authors

Narayanan, Ramesh

Miller, Duejn

Ponnusami, Tamaraj

Khvan, Don-Dzhin

Khe, Yali

Dates

2023-05-03Published

2017-06-12Filed