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    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    2.
    发明专利
    NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：HRP20100622T8

    公开(公告)日：2011-01-31

    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.

    DERIVADOS DE BENZOTIADIAZINAS CICLOALQUILADAS SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    3.
    发明专利
    DERIVADOS DE BENZOTIADIAZINAS CICLOALQUILADAS SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：AR072486A1

    公开(公告)日：2010-09-01

    申请号：ARP090102578

    申请日：2009-07-08

    Applicant: SERVIER LAB

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

    IPC: C07D285/24 ,  A61K31/549 ,  A61P25/00

    Abstract: Medicamentos, y uso de los mismos como moduladores del receptor AMPA. Reivindicacion 1: Compuestos de formula (1): en la que: Rcy representa: un grupo cicloalquilo C3-8 no sustituido o sustituido con uno o varios grupos, idénticos o diferentes, elegidos entre alquilo C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno alcoxi C1-6 lineal o ramificado ; hidroxi; y amino no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado; o un grupo cicloalquilo C3-8 alquilo C1-6 lineal o ramificado no sustituido o sustituido sobre la parte cíclica con uno o varios grupos, idénticos o diferentes, elegidos entre alquilo C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno; alcoxi C1-6 lineal o ramificado; hidroxi; y amino no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado; R1, R2, R3 y R4, idénticos o diferentes, representan cada uno un átomo de hidrogeno o de halogeno o un grupo nitro; ciano; hidroxi; tio; alquilo C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno; cianoalquilo C1-6 lineal o ramificado ; hidroxialquilo C1-6 lineal o ramificado; 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; ariloxicarbonilo acilo C1-6 lineal o ramificado; amino no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado o con un grupo acilo C1-6 lineal o ramificado; aminocarbonilo no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado; arilaminocarbonilo; o alquilsulfonilamino C1-6 lineal o ramificado; sus enantiomeros y sus diastereoisomeros cuando existen, así como sus sales de adicion con un ácido o una base farmacéuticamente aceptable, se entiende por ½arilo , el grupo fenilo no sustituido o sustituido con uno o varios grupos, idénticos o diferentes, elegidos entre alquilo C1-6 lineal o ramificado no sustituido o sustituido con uno o varios átomos de halogeno; alcoxi C1-6 lineal o ramificado; hidroxi y amino no sustituido o sustituido con uno o dos grupos alquilo C1-6 lineal o ramificado.

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

    公开(公告)号：AU2009202704A1

    公开(公告)日：2010-01-28

    申请号：AU2009202704

    申请日：2009-07-03

    Applicant: SERVIER LAB

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

    IPC: C07D285/24 ,  A61K31/549 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28

    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.

    5.
    发明专利
    未知

    公开(公告)号：FR2865474B1

    公开(公告)日：2008-06-13

    申请号：FR0400689

    申请日：2004-01-26

    Applicant: SERVIER LAB

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

    IPC: C07D285/24 ,  A61K31/5415 ,  A61K31/549 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07B53/00 ,  C07D285/22

    Abstract: 4-(Fluorinated alkyl or fluorinated cycloalkylalkyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide derivatives (I) are new. Benzothiadiazine derivatives of formula (I) (including optical isomers where appropriate) and their acid or base addition salts are new. R fmono- or polyfluoroalkyl or mono- or polyfluoro-cycloalkylalkyl; R 1H, alkylaminocarbonyl or alkyl (optionally substituted by one or more halo); R 2H, halo, cycloalkyl or alkyl (optionally substituted by one or more halo); R 3 - R 6H, halo, NO 2, CN, alkylsulfonyl, OH, alkoxy, alkyl (optionally substituted by one or more halo) or NH 2 (optionally substituted by 1 or 2 alkyl); Alkyl moieties have 1-6C and cycloalkyl moieties 3-7C; provided that R 3 = H when R 6 is other than H. Independent claims are also included for: (A) new benzothiadiazine derivatives of formula (VI); and (B) the preparation of (I). [Image] [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Antiparkinsonian; Anticonvulsant; Neuroleptic. In object recognition tests in 17 month old rats, 7-chloro-4-(2-fluoroethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide (Ia) at oral doses of 0.1 mg/kg significant reduced age-associated loss of memory. MECHANISM OF ACTION : alpha -Amino-5-methyl-4-isoxazole-propionic acid (AMPA) receptor modulator. In tests in Xenopus ovocytes, (Ia) strongly potentiated the excitative effect of AMPA, showing EC2X and EC5X values of 6.7 mu M and 14.5 mu M respectively for increasing the AMPA-inducedionic current.

    9.
    发明专利
    未知

    公开(公告)号：FR2854634A1

    公开(公告)日：2004-11-12

    申请号：FR0305448

    申请日：2003-05-05

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

    Abstract: Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR' and SO2NHR' wherein R' represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.

    NOUVEAUX DERIVES DE THIADIAZINE, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
    10.
    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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