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    DIHYDROBENZOXATHIAZEPINE COMPOUNDS,A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    34.
    发明专利
    DIHYDROBENZOXATHIAZEPINE COMPOUNDS,A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：ZA201106353B

    公开(公告)日：2012-05-30

    申请号：ZA201106353

    申请日：2011-08-30

    Applicant: SERVIER LAB

    Inventor： CORDI ALEXIS ,  DESOS PATRICE ,  LESTAGE PIERRE ,  DANOBER LAURENCE

    IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

    Abstract: Phenoxy-3,4-dihydro-2H-benzo[b][1,4,5]oxathiazepine-dioxide compounds (I) and their enantiomers and diastereoisomers, and addition salts with an acid or a base, are new. Phenoxy-3,4-dihydro-2H-benzo[b][1,4,5]oxathiazepine-dioxide compounds of formula (I) and their enantiomers and diastereoisomers, and addition salts with an acid or a base, are new. R1 = H, CN, 1-6C alkoxycarbonyl group, 1-6C alkylsulfonylamino1-6C alkyl group or N-hydroxy carboximidamide group, where the heterocyclic group is a 5-membered monocyclic aryl group containing 1-4 heteroatoms of N, O or S, the heterocyclic group is optionally substituted by one or more 1-6C alkyl or polyhalo-1-6C-alkyl group. Independent claims are included for: (1) the preparation of (I); and (2) 3,4-dihydro-2H-benzo[b][1,4,5]oxathiazepine-1,1-dioxide compound of formula (V). Hal = halo such as fluorine, chlorine or bromine. [Image] [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Antiparkinsonian; Cerebroprotective; Anticonvulsant; Antialcoholic; Neuroleptic; Vasotropic. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor modulator. Tests details are described but no results given.

    DERIVADOS DE BENZOTIADIAZINAS CICLOPROPILADAS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    36.
    发明专利
    DERIVADOS DE BENZOTIADIAZINAS CICLOPROPILADAS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：AR079848A1

    公开(公告)日：2012-02-22

    申请号：ARP110100040

    申请日：2011-01-07

    Applicant: SERVIER LAB

    Inventor： LESTAGE PIERRE ,  PIROTTE BERNARD ,  BOTEZ IULIANA ,  DE TULLIO PASCAL ,  DANOBER LAURENCE

    IPC: C07D285/24 ,  A61K31/5415 ,  A61P25/00

    Abstract: Como moduladores de los receptores AMPA. Reivindicacion 1: Compuestos de formula (1) en la que R1 y R2, idénticos o diferentes, representan cada uno un átomo de hidrogeno, halogeno, o un grupo ciano; hidroxi; tio; nitro; alquilo C1-6 lineal o ramificado sustituido opcionalmente; alcoxi C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno; alquiltio C1-6 lineal o ramificado; carboxi; alcoxicarbonilo C1-6 lineal o ramificado; aciloxi C1-6 lineal o ramificado; amino no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado, idénticos o diferentes; acilamino C1-6 lineal o ramificado no sustituido o sustituido en el átomo de nitrogeno con un grupo alquilo C1-6 lineal o ramificado; aminocarbonilo no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado, idénticos o diferentes; aminosulfonilo no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado, idénticos o diferentes; alquilsulfonilamino C1-6 lineal o ramificado no sustituido o sustituido en el átomo de nitrogeno con un grupo alquilo C1-6 lineal o ramificado; o N-hidroxicarboximidamida, entendiéndose que la expresion ôsustituido opcionalmenteö destinada al término alquilo significa que este grupo puede estar sustituido con uno o varios átomos de halogeno, o con un grupo ciano; hidroxi; tio; nitro; alcoxi C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno; alquiltio C1-6 lineal o ramificado; carboxi; alcoxicarbonilo C1-6 lineal o ramificado; aciloxi C1-6 lineal o ramificado; amino no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado, idénticos o diferentes; acilamino C1-6 lineal o ramificado no sustituido o sustituido en el átomo de nitrogeno con un grupo alquilo C1-6 lineal o ramificado; aminocarbonilo no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado, idénticos o diferentes aminosulfonilo no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado, idénticos o diferentes; alquilsulfonilamino C1-6 lineal o ramificado no sustituido o sustituido en el átomo de nitrogeno con un grupo alquilo C1-6 lineal o ramificado; o N-hidroxicarboximidamida, sus enantiomeros y sus diastereoisomeros cuando existen, así como sus sales de adicion con un ácido o una base farmacéuticamente aceptable.

    New Benzothiadiazepine compounds, a process for their preparation and pharmaceutical compositions comprising them.
    39.
    发明专利
    New Benzothiadiazepine compounds, a process for their preparation and pharmaceutical compositions comprising them. 未知

    公开(公告)号：AP2011005935A0

    公开(公告)日：2011-10-31

    申请号：AP2011005935

    申请日：2010-03-18

    Applicant: SERVIER LAB

    Inventor： DANOBER LAURENCE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    IPC: C07D285/36 ,  A61K31/554 ,  A61P25/00

    Abstract: Benzothiadiazepine derivatives (I) and their optical and positional isomers, or addition salts with an acid or base, are new. Benzothiadiazepine derivatives of formula (I) and their optical and positional isomers, or addition salts with an acid or base, are new. R 1>, R 2> : H, halo, or 1-6C alkyl (optionally substituted by one or more halo, 1-6C alkoxy, 1-6C alkylthio, 1-6C alkoxycarbonyl, carboxy group, 1-6C acyl, hydroxyl group, 1-6C hydroxyalkyl group, CN, nitro, amino group (substituted by an 1-6C acyl and optionally substituted by one or more 1-6C alkyl), aminocarbonyl group (optionally substituted by one or more 1-6C alkyl), aminosulfonyl group (optionally substituted by one or more 1-6C alkyl), alkyl(1-6C)sulfonylamino1-6C alkyl, N-hydroxycarboximidamide or benzyloxy); R 3> : H, 1-6C alkyl, 3-8C cycloalkyl, or 3-8C-cycloalkyl-1-6C alkyl; and R 4> : H or 1-6C alkyl (optionally substituted by one or more halo). Independent claims are included for: (1) the preparation of (I); and (2) 1,1-dioxo-2,3,4,5-tetrahydro-1H-benzo[f][1,2,5]thiadiazepin-8-ol (VI) as an intermediate for the synthesis of (I). [Image] ACTIVITY : Neuroprotective; Nootropic; Antiparkinsonian; Cerebroprotective; Anticonvulsant; Antialcoholic; Neuroleptic; Vasotropic; Antidepressant; Tranquilizer. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor modulator; N-methyl-D-aspartate (NMDA) receptor antagonist. The NMDA receptor antagonistic activity of (I) was tested in rats. The result showed that 8-phenoxy-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine-1,1-dioxide exhibited an IC 50value of 9 microM.

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