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    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    24.
    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.

    30.
    发明专利
    未知

    公开(公告)号：DE602007002591D1

    公开(公告)日：2009-11-12

    申请号：DE602007002591

    申请日：2007-06-29

    Applicant: SERVIER LAB

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

    IPC: C07C233/18 ,  A61K31/165 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  A61P37/02

    Abstract: N-[3-Hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide (I), its enantiomers and base addition salts, are new. N-[3-Hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide 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 N-[3-hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide exhibited an inhibition constant value of 1.4 nM and 3.2 nM to bind with melatonin receptors MT 1 and MT 2, respectively.

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