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6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES AS ESTROGEN RECEPTOR MODULATORS
专利权人:
SANOFI
发明人:
BOUABOULA, Monsif,BROLLO, Maurice,CERTAL, Victor,EL-AHMAD, Youssef,FILOCHE-ROMMÉ, Bruno,HALLEY, Frank,MCCORT, Gary,SCHIO, Laurent,TABART, Michel,TERRIER, Corinne,THOMPSON, Fabienne
申请号:
TN2018000285
公开号:
TN2018000285A1
申请日:
2017.02.14
申请国别(地区):
TN
年份:
2020
代理人:
摘要:
The present invention relates to compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a -COOH, a -OH or a -OPO(OH)<;sub>;2<;/sub>; group; R4 represents a hydrogen atom or afluorine atom; R5 represents a hydrogen atom or a -OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a -COOH, -OH or -OPO(OH)<;sub>;2<;/sub>; group, then R5 represents a hydrogen atom; when R5 represents a -OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl or heterocycloalkyl group.The invention also relates to the preparation and to the therapeutic uses of the compounds of formula (1) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.
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