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    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    1.
    发明专利
    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：RS51518B

    公开(公告)日：2011-06-30

    申请号：RSP20100540

    申请日：2009-07-08

    Applicant: SERVIER LAB

    Inventor： LESTAGE PIERRE ,  FRANCOTTE PIERRE ,  DE TULLIO PASCAL ,  PIROTTE BERNARD ,  DANOBER LAURENCE ,  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.

    3.
    发明专利
    未知

    公开(公告)号：AT481393T

    公开(公告)日：2010-10-15

    申请号：AT09290547

    申请日：2009-07-08

    Applicant: SERVIER LAB

    Inventor： FRANCOTTE PIERRE ,  DE TULLIO PASCAL ,  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.

    New thiadiazine compounds, a process for their preparation and pharmaceutical compositions containing them
    4.
    发明专利
    New thiadiazine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：NZ543214A

    公开(公告)日：2009-02-28

    申请号：NZ54321404

    申请日：2004-05-04

    Applicant: SERVIER LAB

    Inventor： GRAINDORGE EMMANUEL ,  FRANCOTTE PIERRE ,  BOVERIE STEPHANE ,  PIROTTE BERNARD ,  LESTAGE PIERRE ,  DANOBER LAURENCE ,  RENARD PIERRE ,  CAIGNARD DANIEL-HENRI ,  DE TULLIO PASCAL

    IPC: A61P25/18 ,  C07D513/04 ,  A61K31/549

    Abstract: The disclosure relates to thiadiazine derivatives and to the use thereof as positive AMPA receptor modulators. More specifically, the disclosure relates to compounds having formula (I) and a process for their preparation, wherein: A represents a thienyl, furyl, pyrrolyl, oxathiole, thiazole, isothiazole, oxazole or imidazole group as defined X; ------- represents a single bond or a double bond; R1 represents a hydrogen atom, a linear or branched (C1-C6) alkyl group which is optionally substituted by one or more halogen atoms, or a (C1-C6) alkoxy (C1-C6) alkyl group; R2 represents a hydrogen atom or a linear or branched (C=-C6) alkyl group which is optionally substituted by one or more halogen atoms; and R3 represents a hydrogen atom or a group which is selected from linear or branched (C1-C6) alkyl, CONHR' or SO2NHR', in which R' represents a linear or branched (C1-C6) alkyl group. The disclosure also relates to the enantiomers and diastereoisomers of the above-mentioned compounds as well as to the pharmaceutically-acceptable base or acid addition salts thereof. The disclosure further relates to the use of these thiadiazine derivatives in the manufacture of a medicament for treating disease requiring AMPA modulators.

    NOUVEAUX DERIVES DE THIADIAZINE, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
    7.
    发明专利
    NOUVEAUX DERIVES DE THIADIAZINE, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知

    公开(公告)号：CA2524377C

    公开(公告)日：2010-08-24

    申请号：CA2524377

    申请日：2004-05-04

    Applicant: SERVIER LAB

    Inventor： GRAINDORGE EMMANUEL ,  FRANCOTTE PIERRE ,  BOVERIE STEPHANE ,  DE TULLIO PASCAL ,  PIROTTE BERNARD ,  LESTAGE PIERRE ,  DANOBER LAURENCE ,  RENARD PIERRE ,  CAIGNARD DANIEL-HENRI

    IPC: C07D513/04 ,  A61K31/549 ,  A61P25/18

    Abstract: L'invention concerne des composés de formule (I): (voir formule 1) dans laquelle : =~ A représente un groupement thiényle, furyle, pyrrolyle, oxathiole, thiazole, isothiazole, oxazole ou imidazole, =~~ représente une liaison simple ou une liaison double, =~ R1 représente un atome d'hydrogène, un groupement alkyle (C1-C6) linéaire ou ramifié, éventuellement substitué par un ou plusieurs atomes d'halogène, ou un groupement alkoxy (C1-C6) alkyle (C1-C6), =~ R2 représente un atome d'hydrogène ou un groupement alkyle (C1-C6) linéaire ou ramifié, éventuellement substitué par un ou plusieurs atomes d'halogène, =~ R3 représente un atome d'hydrogène ou un groupement choisi parmi alkyle (C1-C6) linéaire ou ramifié, CONHR' ou SO2NHR' dans lesquels R' représente un groupement alkyle (C1-C6) linéaire ou ramifié, leurs énantiomères, diastéréoisomères ou leurs sels d'addition à un acide ou à une base pharmaceutiquement acceptable ainsi que leurs utilisations. L'invention s'étend aussi aux compositions comprenant un composé selon l'invention destiné au traitement des maladies nécessitant des modulateurs AMPA, de la schizophrénie et comme facilitateur mnémocognitifs.

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