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    93.
    发明专利
    未知

    公开(公告)号：FR2907451B1

    公开(公告)日：2008-12-12

    申请号：FR0609113

    申请日：2006-10-18

    Applicant: SERVIER LAB

    Inventor： MARCHAND PASCAL ,  BABONNEAU VINCENT ,  PIESSARD SYLVIE ,  DUFLOS SYLVIE ,  BOUTIN JEAN ALBERT ,  AUDINOT VALERIE ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL HENRI

    IPC: C07D209/32 ,  A61K31/454 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00

    Abstract: Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably alkyl; NR 2R 35-8 membered heterocycle, preferably piperidinyl; and n : 2-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.

    100.
    发明专利
    未知

    公开(公告)号：BRPI0702983A

    公开(公告)日：2008-02-19

    申请号：BRPI0702983

    申请日：2007-06-29

    Applicant: SERVIER LAB

    Inventor： YOUS SAID ,  PERES BASILE ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL HENRI ,  DESROSES MATTHIEU ,  BOUTIN JEAN-ALBERT ,  AUDINOT VALERIE

    IPC: C07C233/60 ,  A61K31/165 ,  A61K31/18 ,  A61P25/22 ,  C07C217/60 ,  C07C231/06 ,  C07C247/06 ,  C07C255/33 ,  C07C275/24 ,  C07C309/66 ,  C07D295/10

    Abstract: Naphthalenic derivatives (I) and their enantiomers, diastereoisomer or additive salts of acid or base, are new. Naphthalenic derivatives of formula (I) and their enantiomers, diastereoisomer or additive salts of acid or base, are new. R 1R 4or NHR 4; R 41-6C (halo)alkyl, 1-6C alkenyl, polyhalo(1-6C)alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl or heteroaryl(1-6C)alkyl; R 21-6C alkyl substituted 1-6C alkoxy, OH, OSO 2CH 3, N 3, NRR1a, NHCOR1b or NHSO 2R1b; either R, R1a : H or 1-6C alkyl, 3-8C cycloalkyl, aryl or aryl(1-6C)alkyl; or NRR1a : 5-6 membered ring having another heteroatom e.g. N, O or S; R1b : R; and R 3H, halo, 1-6C alkyl or 1-6C alkenyl. Provided that: when R 1is methyl and R 2is hydroxymethyl, then R 3is not hydrogen; the aryl is phenyl, naphthyl or biphenyl; and the heteroaryl is mono or bicyclic heteroaryl with 1-3 heteroatoms e.g. oxygen, sulfur and nitrogen. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Muscular-Gen; CNS-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Dermatological; Antimigraine; Neuroprotective; Cytostatic; Cerebroprotective; Endocrine-Gen.; Contraceptive. MECHANISM OF ACTION : Melatoninergic receptor agonist. The melatoninergic receptor inhibiting activity of N-[3-methoxy-2-(7-methoxy-1-naphtyl)propyl]acetamide was tested. The result showed that the compound had an inhibition constant (Ki) value of 4.9 mu M.

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