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    22.
    发明专利
    未知

    公开(公告)号：FR2918370B1

    公开(公告)日：2009-08-28

    申请号：FR0704748

    申请日：2007-07-02

    Applicant: SERVIER LAB

    Inventor： YOUS SAID ,  ETTAOUSSI MOHAMED ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL HENRI ,  MILLAN MARK

    IPC: C07C233/22 ,  A61K31/165 ,  A61P1/00 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  C07C231/14

    Abstract: Substituted naphthalene derivatives (I) and their enantiomers, diastereoisomers, or acid or base addition salts, are new. Substituted naphthalene derivatives of formula (I) and their enantiomers, diastereoisomers, or acid or base addition salts, are new. R 11-6C (halo)alkyl, 1-6C alkenyl, polyhalo1-6C alkyl, 3-8C cycloalkyl, cyclo(3-8C)alkyl(1-6C)alkyl, (hetero)aryl or 1-6C (hetero)arylalkyl, where aryl is phenyl, naphthyl or biphenyl, heteroaryl is mono or bicyclic aromatic group containing 1-3 heteroatom of O, S or N, and (hetero)aryl is optionally substituted by 1-3 group comprising 1-6C alkyl, 1-6C alkoxy, OH, carboxy, formyl, nitro, CN, halo(1-6C)alkyl, polyhalo1-6C alkyl, alkyloxycarbonyl or halo; and R 2F or 1-6C alkyl (substituted by one or more F), preferably F or fluoromethyl. Independent claims are included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; CNS-Gen; Muscular-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Cytostatic; Dermatological; Vasotropic; Immunomodulator; Contraceptive; Analgesic. MECHANISM OF ACTION : Melatonin 1 receptor binder; Melatonin 2 receptor binder; 5-Hydroxytryptamine 2c receptor binder. The ability of (I) to bind melatonin 1 receptor was tested using 2-[ 125>I]-iodomelatonin radioligand. The result showed that inhibitory constant of N-[3-fluoro-2-(7-methoxy-1-naphthyl) propyl]acetamide was 0.1 nM.

    NUEVOS DERIVADOS DE ISOQUINOLEINA, SU PROCEDIMIENTO DE PREPARACION Y SU UTILIZACION PARA TRATAR TRASTORNOS DEL SISTEMA MELATONINERGICO.
    27.
    发明专利
    NUEVOS DERIVADOS DE ISOQUINOLEINA, SU PROCEDIMIENTO DE PREPARACION Y SU UTILIZACION PARA TRATAR TRASTORNOS DEL SISTEMA MELATONINERGICO. 未知

    公开(公告)号：ES2295794T3

    公开(公告)日：2008-04-16

    申请号：ES04290918

    申请日：2004-04-07

    Applicant: SERVIER LAB

    Inventor： POISSONNIER-DURIEUX SOPHIE ,  WALLEZ VALERIE ,  GASNEREAU ANNE ,  YOUS SAID ,  LESIEUR DANIEL ,  DELAGRANGE PHILIPPE

    IPC: A61K31/472 ,  C07D217/14 ,  A61P1/00 ,  A61P3/02 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D217/16 ,  C07D217/24

    Abstract: Compuesto de fórmula (I):** ver fórmula** donde: * n vale 1, 2 ó 3, - A representa un grupo o un grupo en los cuales: * Z representa un átomo de azufre o de oxígeno, * R y R", idénticos o diferentes, representan ambos un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado, y * R'''' representa un grupo alquilo(C1-C6) lineal o ramificado, alquenilo (C2-C6) lineal o ramificado, alquinilo(C2-C6) lineal o ramificado, cicloalquilo(C3-C8), cicloalquil(C3-C8)alquilo(C1-C6) donde la parte alquilo es lineal o ramificada, arilo, arilalquilo(C1-C6) con la parte alquilo lineal o ramificada, heteroarilo o heteroarilalquilo(C1-C6) con la parte alquilo lineal o ramificada, * X representa un átomo de nitrógeno o un grupo N-R1, donde R1 representa un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado, cicloalquilo(C3-C8), cicloalquil(C3-C8)alquilo(C1-C6) lineal o ramificado, arilo, aroílo o arilalquilo(C1-C6) con la parte alquilo lineal o ramificada, heteroarilo, heteroaroílo o heteroarilalquilo(C1-C6) con la parte alquilo lineal o ramificada, * R2 representa un grupo alcoxi(C1-C6) lineal o ramificado, cicloalcoxi(C3-C8) o cicloalquil(C3-C8)alquiloxi(C1-C6) lineal o ramificado, * la representación ----- indica que el enlace es sencillo o doble, entendiéndose que se respecta la valencia de los átomos, entendiéndose que: * por "arilo" se entiende un grupo fenilo o naftilo, estando estos grupos no sustituidos o sustituidos con uno a tres grupos, idénticos o diferentes, seleccionados de entre alquilo(C1-C6) lineal o ramificado, alcoxi(C1-C6) lineal o ramificado, OH, COOH, alcoxicarbonilo con la parte alcoxi lineal o ramificada, formilo, nitro, ciano, hidroximetilo, amino (eventualmente sustituido con uno o dos grupos alquilo(C1-C6) lineales o ramificados) o con átomos de halógeno, * por "heteroarilo" se entiende todo grupo mono- o bicíclico de 5 a 10 eslabones y que puede contener de 1 a 3 heteroátomos seleccionados de entre oxígeno, azufre o nitrógeno, por ejemplo los grupos furano, tiofeno, pirrol, imidazolino, piridina, quinoleína, isoquinoleína, cromano, indol, benzotiofeno o benzofurano, pudiendo estos grupos estar parcialmente hidrogenados, no sustituidos o sustituidos con uno a tres grupos, idénticos o diferentes, seleccionados de entre alquilo(C1-C6) lineal o ramificado, alcoxi(C1-C6) lineal o ramificado, OH, COOH, alcoxicarbonilo con la parte alcoxi lineal o ramificada, formilo, nitro, ciano, amino (eventualmente sustituido con uno o dos grupos alquilo(C1-C6) lineales o ramificados) hidroximetilo o con átomos de halógeno, sus enantiómeros y diastereoisómeros, así como sus sales de adición de un ácido o de una base farmacéuticamente aceptables.

    28.
    发明专利
    未知

    公开(公告)号：BRPI0702769A

    公开(公告)日：2008-02-19

    申请号：BRPI0702769

    申请日：2007-06-29

    Applicant: SERVIER LAB

    Inventor： YOUS SAID ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  CAIGNARD DANIEL HENRI ,  PERES BASILE ,  SABAOUNI AHMED ,  DELAGRANGE PHILIPPE ,  MILLAN MARK

    IPC: C07C233/22 ,  A61K31/165 ,  A61P25/00 ,  C07C231/06

    Abstract: 2-Fluoro-N-[3-hydroxy-2-(7-methoxy-naphthalen-1-yl)-propyl]-acetamide (I), its enantiomers and base addition salts, are new. 2-Fluoro-N-[3-hydroxy-2-(7-methoxy-naphthalen-1-yl)-propyl]-acetamide of formula (I), its enantiomers and base addition salts, are new. 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; Cerebroprotective; Contraceptive; Endocrine-Gen; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The ability of (I) to bind with melatonin was tested. The results showed that 2-fluoro-N-[3-hydroxy-2-(7-methoxy-1-naphthyl)propyl]acetamide exhibited an inhibition constant value of 7.7 nM and 0.5 nM to bind with melatonin receptors MT 1and MT 2, respectively.

    NEW NAPHTHALENE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    29.
    发明专利
    NEW NAPHTHALENE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：SG138590A1

    公开(公告)日：2008-01-28

    申请号：SG2007047889

    申请日：2007-06-26

    Applicant: SERVIER LAB

    Inventor： YOUS SAID ,  PERES BASILE ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL-HENRI ,  MILLAN MARK

    Abstract: 2-Fluoro-N-[3-hydroxy-2-(7-methoxy-naphthalen-1-yl)-propyl]-acetamide (I), its enantiomers and base addition salts, are new. 2-Fluoro-N-[3-hydroxy-2-(7-methoxy-naphthalen-1-yl)-propyl]-acetamide of formula (I), its enantiomers and base addition salts, are new. 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; Cerebroprotective; Contraceptive; Endocrine-Gen; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The ability of (I) to bind with melatonin was tested. The results showed that 2-fluoro-N-[3-hydroxy-2-(7-methoxy-1-naphthyl)propyl]acetamide exhibited an inhibition constant value of 7.7 nM and 0.5 nM to bind with melatonin receptors MT 1and MT 2, respectively.

    New naphthalene compounds, a process for their preparation and pharmaceutical compositions containing them
    30.
    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.

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