LOW-MOLECULAR INHIBITORS OF N-TERMINUS ACTIVATION OF ANDROGEN RECEPTOR Russian patent published in 2014 - IPC C07D207/38 C07D241/08 A61K31/4015 A61K31/495 A61P35/00 

Abstract RU 2519948 C2

FIELD: chemistry.

SUBSTANCE: invention relates to low-molecular inhibitors of N-terminus activation of androgen receptors of formula B: or pharmaceutically acceptable salts thereof, where: X denotes N; Y denotes O; R1 denotes OJ, where J denotes a linear or branched, saturated C1-10alkyl; R2 denotes a linear or branched, saturated, optionally substituted C1-10alkyl, where the optional substitute denotes one or more: F, Cl, Br and I; R3 denotes H; R4 denotes H, linear or branched, saturated C1-4alkyl, optionally substituted, where the optional substitute denotes one or more: F, Cl, Br and I; R5 denotes a linear or branched, saturated C1-10alkyl, optionally substituted, where the optional substitute denotes one or more: F, Cl, Br and I; Z denotes Bu, Pr, Et or Me; denotes a double bond; and under the condition that the compound is not: .

EFFECT: compound exhibits inhibiting activity on AR, which allows use thereof to treat various diseases, including prostate cancer.

26 cl, 9 dwg, 2 tbl, 6 ex

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RU 2 519 948 C2

Authors

Sadar Mariann D.

Mavdzhi Nasrin R.

Van Tszjun'

Andersen Rehjmond Dzh.

Uill'Jams Dehvid Eh.

Leblan Majk

Jan' Lu-Pin

Dates

2014-06-20Published

2009-08-24Filed