6,7¿DIHYDRO¿5H¿BENZO[7]ANNULENE DERIVATIVES AS ESTROGEN RECEPTOR MODULATORS

6,7¿DIHYDRO¿5H¿BENZO[7]ANNULENE DERIVATIVES AS ESTROGEN RECEPTOR MODULATORS

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)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a -OH group; wherein at least o...

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Hauptverfasser: TABART, Michel, SCHIO, Laurent, CERTAL, Victor, BOUABOULA, Monsif, THOMPSON, Fabienne, EL¿AHMAD, Youssef, BROLLO, Maurice, TERRIER, Corinne, FILOCHE¿ROMMÉ, Bruno, MCCORT, Gary, HALLEY, Frank
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creator TABART, Michel
SCHIO, Laurent
CERTAL, Victor
BOUABOULA, Monsif
THOMPSON, Fabienne
EL¿AHMAD, Youssef
BROLLO, Maurice
TERRIER, Corinne
FILOCHE¿ROMMÉ, Bruno
MCCORT, Gary
HALLEY, Frank
description 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)2 group; R4 represents a hydrogen atom or a fluorine 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)2 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 (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.
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title 6,7¿DIHYDRO¿5H¿BENZO[7]ANNULENE DERIVATIVES AS ESTROGEN RECEPTOR MODULATORS
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