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    Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds and Their Derivatives, Processes for Their Preparation and Therapeutic Uses Thereof
    41.
    发明公开
    Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds and Their Derivatives, Processes for Their Preparation and Therapeutic Uses Thereof 审中-公开

    公开(公告)号：US20240101512A1

    公开(公告)日：2024-03-28

    申请号：US18032502

    申请日：2021-10-19

    Applicant: Sanofi

    Inventor： Patrick Bernardelli ,  Marc Bianciotto ,  Youssef El Ahmad ,  Frank Halley ,  Patrick Mougenot ,  Frédéric Petit ,  Franck Slowinski ,  Corinne Terrier

    IPC: C07D205/10 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10 ,  C07D401/06

    CPC classification number: C07D205/10 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10 ,  C07D401/06

    Abstract: The present application relates to compounds of formula (I), or pharmaceutically acceptable salts thereof: wherein R1 and R2 represent hydrogen or deuterium; R3 represents hydrogen, —COOH or —OH; R3′ and R3″ represent hydrogen, methyl, methoxy, chlorine, fluorine or cyano; R4 and R41 represent hydrogen or fluorine; R5 represents hydrogen, fluorine or (C1-C3)alkyl; R6 represents phenyl, fused phenyl, bicyclic group comprising 5 to 12 carbon atoms, heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, cycloalkyl group comprising 3 to 7 carbon atoms, (C3-C6)cycloalkyl(C1-C3)alkyl group, 3 to 8 membered-heterocycloalkyl group comprising 1 or 2 heteroatoms, (C1-C6)alkyl, and phenyl(C1-C2)alkyl group; X represents —CH2—, —O— or —S—; Y represents —CH═, —N═ or —CR″═, wherein R″ represents (C1-C3)alkyl, halogen, cyano, or (C1-C3)fluoroalkyl; R7 represents (C1-C3)alkyl, halogen atom, cyano, or (C1-C3)fluoroalkyl; R8 represents hydrogen or fluorine; R9 represents hydrogen, (C1-C3)alkyl or a cyclopropyl; n is 0, 1 or 2; and m is 0 or 1. Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.

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