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    21.
    发明专利
    未知

    公开(公告)号：NO327257B1

    公开(公告)日：2009-05-25

    申请号：NO20043188

    申请日：2004-07-27

    Applicant: SERVIER LAB

    Inventor： LECLERC VERONIQUE ,  RENARD PIERRE ,  CAIGNARD DANIEL-HENRI ,  CARATO PASCAL ,  PAILLOUX SYLVIE ,  INTROVIGNE CARINE ,  LEBEGUE NICOLAS ,  BERTHELOT PASCAL ,  DACQUET CATHRINE ,  BOUTIN JEAN ALBERT

    IPC: C07D235/26 ,  C07D277/68 ,  A61K31/426 ,  A61K31/427 ,  A61P1/04 ,  A61P1/18 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/04 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/04 ,  A61P25/28 ,  A61P27/02 ,  A61P35/00 ,  C07D235/12 ,  C07D417/10 ,  C07D417/12

    Abstract: Benzoxazole, benzothiazole or indole oxime derivatives (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine) are new. Benzoxazole, benzothiazole or indole oxime derivatives of formula (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine), and their enantiomers, diastereomers and salts are new. [Image] X : O, S, CH 2 or CHR' 2>; R 1>, R 2>H, alkyl, aryl, aralkyl, aryloxy, aralkoxy, alkoxy, OH, NH 2 or mono- or dialkylamino; or R 1> + R 2>=O, =S or =NH; R' 2>group forming an additional bond with R 2>; A : 1-6C alkylene (optionally having one CH 2 replaced by O, S, NRa', phenylene or naphthylene); Ra' : H or alkyl; R 3>, R 4>H, halo, R, OR or NRR'; or R 3> + R 4>group forming an ortho-fused 5- or 6-membered ring (optionally containing an O, S or N heteroatom); R, R', R 5>, R 6>H, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, cycloalkyl, cycloalkylalkyl or polyhaloalkyl; D : benzene ring (in which case X is other than CHR' 2>); or a pyridine, pyrazine, pyrimidine or pyridazine ring; B : alkyl or alkenyl, both substituted by -CHR 7>R 8> or by R 9>; or -CHR 7>R 8> or R 9>; R 7>-C(Z)OR, -C(Z)NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; Z : O or S; R 8>aryl, aralkyl, heteroaryl, heteroaralkyl, CN, tetrazole, OR, NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; R 9>CN, tetrazole, -N(R)C(Z)R', -N(R)C(Z)OR' or -O(CH 2) n-CR 1> 0>R 1> 1>-COOR; n : 0-6; R 1> 0>, R 1> 1>H or alkyl, but not both H; aryl moieties : phenyl, naphthyl or biphenyl (all optionally partially hydrogenated and optionally substituted by 1-3 alkyl, polyhaloalkyl, alkoxy, OH, COOH, CHO, NRaRb, ester, amido, NO 2, CN or halo groups); heteroaryl moieties : 5-10 membered mono- or bicyclic aryl (where one ring is optionally partially hydrogenated in the case of bicyclic systems) containing 1-3 O, S and/or N heteroatom(s) and optionally substituted as for aryl; Rb, Rc : H, alkyl, aryl or heteroaryl; the oxime group -C(R 6>)=NOR 5> has E- or Z-configuration; alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) preparation method of (I); and (2) new ketone intermediates of formula (V). [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiant; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Nootropic; Osteopathic; Antiinflammatory; Antiarteriosclerotic; Anorectic; Cytostatic. In tests in ob/ob mice, oral administration of 10 mg/kg of methyl 3-(4-(2-(6-((methoxyimino)-(phenyl)-methyl)-2-oxo-1,3-benzothiazol-3(2H)-yl)-ethoxy)-phenyl)-2-(2,2,2-trifluoroethoxy)-propanoate (Ia) twice per day for 4 days reduced blood sugar levels by 51% and reduced the weight gain by 80% in comparison with controls, whereas analogous administration of rosiglitazone reduced blood sugar levels by 61% but increased the weight gain by 33% in comparison with controls. MECHANISM OF ACTION : Aldose Reductase Inhibitor; Angiogenesis Inhibitor.

    DERIVADOS TETRACICLICOS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    26.
    发明专利
    DERIVADOS TETRACICLICOS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：AR061835A1

    公开(公告)日：2008-09-24

    申请号：ARP070103012

    申请日：2007-07-06

    Applicant: SERVIER LAB

    Inventor： DACQUET CATHERINE ,  LECLERC VERONIQUE ,  L HELGOUAL CH JEAN-MARTIAL ,  LE NAOUR MORGAN ,  BERTHELOT PASCAL ,  LEBEGUE NICOLAS ,  CARATO PASCAL ,  KTORZA ALAIN ,  CAIGNARD DANIEL-HENRI

    IPC: C07D277/68 ,  A61K31/428 ,  A61P3/04

    Abstract: Reivindicacion 1: Compuestos de formula (1) en la que: R1 representa un átomo de hidrogeno y R2 y R3 forman junto con los 2 átomos de carbono adyacentes a los que están unidos un ciclo de formula (2) en el que R6 representa un átomo de hidrogeno o de halogeno, o un grupo alquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, amino, alquilamino C1-6 lineal o ramificado, o dialquilamino C1-6 lineal o ramificado, X representa un átomo de oxígeno o un grupo N-OR7 en el que R7 representa un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado, arilo, o arilalquilo C1-6 lineal o ramificado, o R3 representa un átomo de hidrogeno y R1 y R2 forman junto con los 2 átomos de carbono adyacentes a los que están unidos un ciclo de formula (2) tal como se ha definido anteriormente, R4 y R5, idénticos o diferentes, representan un átomo de hidrogeno o de halogeno, o un grupo alquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, amino, alquilamino C1-6 lineal o ramificado, o dialquilamino C1-6 lineal o ramificado, A representa una cadena alquileno C1-6 en la que un grupo CH2 puede reemplazarse por un heteroátomo elegido entre oxígeno o azufre, o por un grupo NRa (en el que Ra representa un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado), B representa un grupo alquilo C1-6) lineal o ramificado, o alquenilo C2-6 lineal o ramificado, estando sustituidos estos grupos con un grupo de formula (3) en la que R8 representa un grupo - COOR y R9 representa un grupo -OR' en el que R y R', idénticos o diferentes, representan cada uno un átomo de hidrogeno, o un grupo alquilo C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno, entendiéndose que: la oxima =N-OR7 puede tener configuracion Z o E, por arilo se entiende un grupo fenilo, naftilo o bifenilo, pudiendo estar estos grupos parcialmente hidrogenados, por heteroarilo se entiende cualquier grupo aromático mono o bicíclico que contiene 5 a 10 eslabones, pudiendo estar parcialmente hidrogenado en uno de los ciclos en el caso de los heteroarilos bicíclicos, y que contiene 1 a 3 heteroátomos elegidos entre oxigeno, nitrogeno y azufre, pudiendo estar sustituidos los grupos arilo y heteroarilo así definidos con 1 a 3 grupos elegidos entre alquilo C1-6 lineal o ramificado, polihalogenoalquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, hidroxi carboxi, formilo, NRbRc (en el que Rb, y Rc, idénticos o diferentes, representan un átomo de hidrogeno, un grupo alquilo C1-6 lineal o ramificado, arilo o heteroarilo), éster, amido, nitro, ciano, o átomos de halogeno, sus enantiomeros y diastereoisomeros así como sus sales de adicion a un ácido o a una base farmacéuticamente aceptables.

    27.
    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
    28.
    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
    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：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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