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    New benzothiadiazine compounds, a process for their preparation and pharmaceutical compositions containing them
    51.
    发明专利
    New benzothiadiazine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2005229698A1

    公开(公告)日：2006-05-18

    申请号：AU2005229698

    申请日：2005-11-03

    Applicant: SERVIER LAB

    Inventor： LESTAGE PIERRE ,  CORDI ALEXIS ,  DESOS PATRICE

    IPC: C07D285/24 ,  A61K31/549 ,  A61P25/08 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28

    Abstract: Benzothiadiazine compounds (I) and their enantiomers, diastereoisomers and addition salts with an acid or base are new. Benzothiadiazine compounds of formula (I) and their enantiomers, diastereoisomers and addition salts with an acid or base are new. R 11-6C alkyl substituted by halo(s); R 2H, halo or OH; R 3aryl (optionally substituted by 1-6C alkyl(s)), 1-6C polyhaloalkyl, halo, 1-6C alkoxy-carbonyl, 1-6C alkylthio, carboxy, 1-6C acyl, 1-6C (polyhalo)alkoxy, OH, CN, nitro, amidino (optionally substituted by 1 or 2 1-6C alkyl, OH, 1-6C alkoxy or -O-(C(=O))-R 12), amino (optionally substituted by 1 or 2 1-6C alkyl), aminocarbonyl (optionally substituted by 1 or 2 1-6C alkyl), benzyloxy, 1-6C alkylsulfonylamino (optionally substituted on the N by 1-6C alkyl), trifluoromethylsulfonylamino, heterocyclic or 1-6C alkyl (substituted by halo, 1-6C alkyl, NR 4R 5, S(O) nR 6, OR 7, amidino (optionally substituted by 1 or 2 1-6C alkyl, OH, 1-6C alkoxy or -O-(C=O)-R 12) and/or heterocyclic); R 4H, 1-6C alkyl, S(O) pR 8, COR 9 or P(O)(OR 10)(OR 11); and R 5H or 1-6C alkyl; or NR 4R 5heterocyclic; R 6, R 8-R 12H, 1-6C alkyl (optionally substituted by halo(s)), aryl-(1-6C alkyl) or aryl; R 71-6C alkyl or 1-6C acyl; and n, p : 0-2. [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Cerebroprotective; Anticonvulsant; Neuroleptic; Vasotropic. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) modulator. The ability of (I) to modulate AMPA was assessed using rats. The results showed that N-(4-{[4-(2-bromoethyl)-1,1-dioxido-3,4-dihydro-2H-1,2,4-benzothiadiazin-7-yl]oxy}benzyl)methanesulfonamide exhibited an EC2X value of 0.04 mu M.

    NUEVOS DERIVADOS DIHIDROBENZOXATIAZEPINAS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    58.
    发明专利
    NUEVOS DERIVADOS DIHIDROBENZOXATIAZEPINAS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：PE20131342A1

    公开(公告)日：2013-11-28

    申请号：PE2013000377

    申请日：2011-09-15

    Applicant: SERVIER LAB

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

    IPC: A61K31/551 ,  A61P25/00 ,  C07D291/08

    Abstract: SE REFIERE A COMPUESTOS DERIVADOS DE DIHIDROBENZOXATIAZEPINA DE FORMULA (I) DONDE R1 ES H, CN, ALCOXICARBONILO(C1-C6), ALQUIL(C1-C6)SULFONILAMINOALQUILO(C1-C6), N-HIDROXICARBOXIMIDAMIDA O UN HETEROCICLICO TAL COMO PIRAZOLILO, TIAZOLILO, OXADIAZOLILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 8-[3-(5-METIL-1,2,4-OXADIAZOL-3-IL)FENOXI]-3,4-DIHIDRO-2H-5,1,2-BENZOXATIAZEPINA 1,1-DIOXIDO; 8-[3-(3-METIL-1,2,4-OXADIAZOL-5-IL)FENOXI]-3,4-DIHIDRO-2H-5,1,2-BENZOXATIAZEPINA 1,1-DIOXIDO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LOS RECEPTORES AMPA (ACIDO ALFA-AMINO-3-HIDROXI-5-METIL-4-ISOXAZOL-PROPIONICO) SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS MNEMOCOGNITIVOS ASOCIADOS A LA EDAD, A LAS ENFERMEDADES NEURODEGENERATIVAS PROGRESIVAS, A LA ENFERMEDAD DE ALZHEIMER

    DERIVATIVES OF DIHYDROBENZOXATHIAZEPINE, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS WELL AS THEIR USES AS MODULATORS OF AMPA RECEPTORS
    59.
    发明专利
    DERIVATIVES OF DIHYDROBENZOXATHIAZEPINE, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS WELL AS THEIR USES AS MODULATORS OF AMPA RECEPTORS 未知

    公开(公告)号：RS52835B

    公开(公告)日：2013-10-31

    申请号：RSP20130274

    申请日：2011-09-15

    Applicant: SERVIER LAB

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

    IPC: C07D291/08 ,  A61K31/551 ,  A61P25/00

    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.

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