OESTROGEN RECEPTOR ANTAGONIST Russian patent published in 2024 - IPC C07D209/08 C07D221/02 C07D401/14 C07D409/14 C07D471/04 A61K31/4439 A61K31/437 A61P35/00 

Abstract RU 2832735 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (II), an isomer thereof or a pharmaceutically acceptable salt thereof, (II), where X is NH; Y is selected from a group consisting of N and CR7; Y1 is CH and Y2 is N; or Y1 is N and Y2 is CH or CF; or Y1 is CH and Y2 is CH; L is or ; ring A is selected from the group consisting of phenyl, thienyl and pyridinyl; R1 is selected from the group consisting of H, halogen and C1-6 alkyl; R2 is C1-3 alkyl, optionally substituted with 1, 2 or 3 Rb; R3 is selected from the group consisting of H and C1-3 alkyl; R13 is H or ; R4 is selected from a group consisting of COOH, , , -NHCH3 and -N(CH3)2; R5 is H; each of R6, R7, R8 and R9 independently is H; each of R10, R11 and R12 is independently selected from the group consisting of H, halogen, CN, C1-3alkyl and -OC1-3 alkyl; and Rb is selected from the group consisting of H, F, Cl, Br and I, as well as to a pharmaceutical composition based thereon and use in preparing a medicament for treating oestrogen receptor-positive breast cancer.

EFFECT: novel compounds which can be used as oestrogen receptor antagonists for treating oestrogen receptor-positive breast cancer are obtained.

29 cl, 4 tbl, 31 ex

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RU 2 832 735 C2

Authors

Duan, Shuven

Lu, Tszyanyuj

Khu, Likhun

Din, Charlz Z.

Khu, Gopin

Li, Tszyan

Chen, Shukhuej

Dates

2024-12-28Published

2019-12-17Filed