BISPHENOL DERIVATIVES AND THEIR USE AS ACTIVITY MODULATORS OF ANDROGEN RECEPTOR Russian patent published in 2022 - IPC C07C317/16 C07C317/22 C07C43/23 C07D233/60 C07D295/88 A61K31/09 A61K31/10 A61K31/165 A61K31/222 A61K31/4164 A61K31/5375 A61P35/00 C07C69/35 

Abstract RU 2767257 C2

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to a compound having the structure (I)

I

or to its pharmaceutically acceptable salt or to stereoisomer, as well as to individual compounds with the capability of inhibiting an androgen receptor, to a pharmaceutical composition containing these compounds and to a method for inhibiting activity of an androgen receptor. In the compound I, X is -S(O)n- or -C(R8R9)-; R1 is hydroxyl or -OC(=O)R13; R2 is hydroxyl or -OC(=O)R13; R3 is -NH2, -NHC(=O)R13, -NHS(O)nR5, -S(O)nR5, 5-element heteroaryl containing two nitrogens, or 6-element heterocycle containing one nitrogen heteroatom or one oxygen heteroatom; R5 is C1-C6 alkyl; each of R8 and R9 is independently C1-C6 alkyl; each of R11a, R11b, R11c and R11d is independently H or Cl; R13 is C1-C6 alkyl; and n is equal to 2, wherein at least one of R11a, R11b, R11c or R11d is Cl.

EFFECT: obtaining compounds for inhibiting activity of an androgen receptor.

31 cl, 6 dwg, 6 tbl, 30 ex

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RU 2 767 257 C2

Authors

Andersen, Raymond

Sadar, Marianne Dorothy

Jlan, Kunzhong

Mawjl, Nasrin R.

Wang, Jun

Banuelos, Carmen Adriana

Yang, Yu-Chi

Dates

2022-03-17Published

2017-04-18Filed