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    New 1-acylaminomethyl-indan or -tetralin derivatives, are melatonin receptor ligands useful e.g. for treating sleeping disorders, anxiety, depression, jet lag or appetite disorders
    1.
    发明专利
    New 1-acylaminomethyl-indan or -tetralin derivatives, are melatonin receptor ligands useful e.g. for treating sleeping disorders, anxiety, depression, jet lag or appetite disorders 未知

    公开(公告)号：FR2857010A1

    公开(公告)日：2005-01-07

    申请号：FR0307949

    申请日：2003-07-01

    Applicant: SERVIER LAB

    Inventor： LANGLOIS MICHEL ,  MATHE ALLAINMAT MONIQUE ,  CHAHED MONCEF AMINE ,  BOUTIN JEAN ALBERT ,  AUDINOT VALERIE ,  BENNEJEAN CAROLINE ,  DELAGRANGE PHILIPPE ,  RENARD PIERRE

    IPC: A61P25/00 ,  A61P35/00 ,  C07C233/05 ,  A61K31/165

    Abstract: 1-Acylaminomethyl-4-alkyl-indan or 1-acylaminomethyl-5-alkyl-1,2,3,4-tetrahydronaphthalene derivatives (I) are new. Indane or tetralin derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. [Image] R 1>alkyl; R 2>alkyl (optionally substituted by one or more halo), 2-6C alkenyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; n : 1 or 2; aryl moieties : phenyl, naphthyl or biphenylyl (all optionally substituted by 1-3 of alkyl, alkoxy, OH, COOH, CHO, CN, polyhaloalkyl, alkoxycarbonyl or halo); heteroaryl moieties : mono- or bicyclic aromatic group containing 1-3 of O, S and/or N as heteroatoms (optionally substituted as for aryl); and the alkyl moieties have 1-6C and cycloalkyl moieties 3-8C. An independent claim is included for the preparation of (I). ACTIVITY : Tranquilizer; hypnotic; antidepressant; cardiant; neuroleptic; CNS-Gen.; anorectic; eating disorders-Gen.; anticonvulsant; antidiabetic; antiparkinsonian; nootropic; antimigraine; neuroprotective; cerebroprotective; endocrine-Gen.; vasotropic; cytostatic; antifertility; contraceptive; immunomodulator; analgesic. MECHANISM OF ACTION : Melatonin receptor ligand. (I) have IC 50 values in receptor binding assays for one of the melatoninergic bonding sites (i.e. MT 1, MT 2 or MT 3 receptors); no specific values for individual compounds are given in the source material.

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