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    New naphthalene compounds, a process for their preparation and pharmaceutical compositions containing them
    1.
    发明专利
    New naphthalene compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2007203045A1

    公开(公告)日：2008-01-17

    申请号：AU2007203045

    申请日：2007-06-29

    Applicant: SERVIER LAB

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

    IPC: C07C15/24 ,  A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/24 ,  C07C43/20 ,  C07C215/20 ,  C07C233/08 ,  C07C233/18 ,  C07C255/33

    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.

    Naphthalene compounds, a process for their preparation and pharmaceutical compositions containing them
    2.
    发明专利
    Naphthalene compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：ZA200704957B

    公开(公告)日：2008-08-27

    申请号：ZA200704957

    申请日：2007-06-26

    Applicant: SERVIER LAB

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

    IPC: A61K20090101 ,  A61P20090101 ,  C07C20090101

    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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