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    DERIVADOS DE BENZOTIADIAZEPINAS USADOS COMO MODULADORES DE LOS RECEPTORES AMPA Y NMDA.
    41.
    发明专利
    DERIVADOS DE BENZOTIADIAZEPINAS USADOS COMO MODULADORES DE LOS RECEPTORES AMPA Y NMDA. 未知

    公开(公告)号：MX2011009638A

    公开(公告)日：2011-09-28

    申请号：MX2011009638

    申请日：2010-03-18

    Applicant: SERVIER LAB

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

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

    Abstract: Compuestos de fórmula (1): (ver fórmula (I)) donde R1 y R2, son idénticos o diferentes, representan cada uno un átomo de hidrógeno o de halógeno, o un grupo alquilo, alcoxi, alquiltio, acilo, alcoxicarbonilo, carboxi, hidroxi, hidroxialquilo, ciano, nitro, amino, aminocarbonilo sustituido o no sustituido, aminosulfonilo, alquilsulfonilaminoalquilo, N-hidroxicarboximidami da o benciloxi, R3 representa un átomo de hidrógeno o un grupo alquilo, cicloalquilo o cicloalquilalquilo, R4 representa un átomo de hidrógeno o un grupo alquilo sustituido o no sustituido; la invención también se refiere al uso de los mismos como moduladores alostéricos positivos de receptores AMPA y agonistas de receptores NMDA.

    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    49.
    发明专利
    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：HRP20100622T1

    公开(公告)日：2010-12-31

    申请号：HRP20100622

    申请日：2010-11-17

    Applicant: SERVIER LAB

    Inventor： FRANCOTTE PIERRE ,  TULLIO PASCAL DE ,  PIROTTE BERNARD ,  DANOBER LAURENCE ,  LESTAGE PIERRE ,  CAIGNARD DANIEL-HENRI

    IPC: C07D285/28 ,  A61K31/549 ,  A61P25/00

    Abstract: Cycloalkyl benzothiadiazine derivatives (I) and their enantiomers, diastereoisomers, acid or base addition salts, are new. Cycloalkyl benzothiadiazine derivatives of formula (I) and their enantiomers, diastereoisomers, acid or base addition salts, are new. RCy : 3-8C cycloalkyl (optionally substituted by 1-6C alkyl (optionally substituted), halo, 1-6C alkoxy, hydroxy, or amino (optionally substituted by 1-6C alkyl)), or 1-6C-alkyl-(3-8C)cycloalkyl (optionally substituted on the cyclic part by 1-6C alkyl (optionally substituted by halo), 1-6C alkoxy, OH or amino (optionally substituted by 1-6C alkyl)); and R 1-R 4H, halo, nitro, CN, OH, thio, 1-6C alkyl (optionally substituted by halo), 1-6C alkoxy (optionally substituted by halo), 1-6C alkylthio, carboxy, 1-6C alkoxycarbonyl, 1-6C acyl, amino (optionally substituted by 1-6C alkyl or 1-6C acyl), aminocarbonyl (optionally substituted by 1-6C alkyl), aminosulfonyl (optionally substituted by 1-6C alkyl), or 1-6C alkylsulfonylamino. Provided that (I) is not 6-chloro-4-cyclohexyl-3,4-dihydro-7-sulfonamido-2H-1,2,4-benzothiadiazine-1,1-dioxide. Independent claims are included for: (1) the preparations of (I); (2) a composition comprising (I) in combination with inert, non-toxic vehicle; and (3) a benzo[1,2,4]thiadiazine-1,1-dioxide compound of formula (VI). [Image] [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Antiparkinsonian; Cerebroprotective; Anticonvulsant; Antialcoholic; Neuroleptic; Vasotropic. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor modulator. The AMPA receptor modulatory activity of (I) was tested in embryonic rat neurons, where the results were calculated as EC(2X) i.e. concentration of product that doubles the potential membrane induced by AMPA. The results showed that 6,7-dichloro-4-cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxyde exhibited an EC(2X) value of 1 mu M.

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