PIPERIDINE DERIVATIVE, A METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL USE THEREOF Russian patent published in 2020 - IPC C07D217/14 C07D217/16 C07D401/10 C07D405/12 C07D413/10 C07D417/10 C07D471/04 C07D491/48 C07D491/56 C07D495/04 A61K31/4355 A61K31/4741 A61K31/4743 A61K31/5377 A61P3/00 A61P7/00 A61P9/00 A61P15/00 A61P25/00 A61P25/18 A61P29/00 A61P35/00 A61P35/02 A61P37/00 A61P43/00 

Abstract RU 2730508 C2

FIELD: organic chemistry.

SUBSTANCE: invention relates to a heterocyclic compound of formula (I), an enantiomer thereof or a pharmaceutically acceptable salt thereof, wherein ring A is selected from a group consisting of structures given in the claim; R is a hydrogen atom; each R1 is identical to the other or different from it and each is selected from a hydrogen atom and a halogen atom; R2 is selected from C1-6-alkyl and C3-6-cycloalkyl, where each said C1-6-alkyl is optionally substituted with 1 group, selected from halogen atom; R3 is selected from C1-6-alkyl; each R4 is identical to the other or different from it and each is independently selected from a hydrogen atom, C3-6-cycloalkyl, a halogen atom, cyano, C2-6-alkynyl, heterocyclyl, C6-aryl, heteroaryl, -OR5, -NHC(O)OR5 and -NHC(O)NR6R7, where each said C2-6-alkynyl, heterocyclyl, C6-aryl and heteroaryl is optionally substituted with 1–2 groups selected from Rc, C1-6-alkyl, halogen-C1-6-alkyl, hydroxy-C1-6-alkyl, amino, oxo, C3-6-cycloalkyl or heterocyclyl; Rc is heteroaryl, where said heteroaryl is optionally substituted with 1 group selected from C1-6-alkyl; R5 is selected from a hydrogen atom, C1-6-alkyl and heterocyclyl, wherein said C1-6-alkyl is optionally substituted with 1 group selected from cyano and -C(O)NR6R7; R6 and R7 are identical or different from each other and each is selected from a hydrogen atom, C1-6-alkyl and C3-6-cycloalkyl; Ra and Rb are identical or different from each other and are each selected from hydrogen atom and C1-6-alkyl; m is 0, 1 or 2; n equals 0, 1 or 2; wherein C6-aryl ring may be fused with 5–6 membered heteroaryl; said heterocyclyl is 5–6 membered saturated monocyclic hydrocarbon group having one or two heteroatoms selected from nitrogen and oxygen, or said heterocyclyl ring can be condensed with pyridine; and said heteroaryl is 5–6-membered heteroaromatic system having from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, or said heteroaryl ring can be condensed with phenyl or pyridine. Invention also relates to an intermediate compound of formula (V), a method of producing the desired compound from a compound of formula (V), a pharmaceutical composition based on the compound of formula (I), use of a compound of formula (I) or a composition based thereon, as well as a method of treating a estrogen receptor mediated disease.

EFFECT: novel condensed piperidine derivatives useful as an estrogen receptor modulator in the treatment of estrogen receptor-mediated or estrogen-dependent diseases or conditions are obtained.

21 cl, 3 tbl, 103 ex

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RU 2 730 508 C2

Authors

Yuj Shankhaj

Yan Fanlun

Chen Lej

Yan Tszintszin

Chzhan Sitsyan

Se Chzhichao

Chen Linsyan

Khe Minsyun

Dates

2020-08-24Published

2016-05-27Filed