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    81.
    发明专利
    未知

    公开(公告)号：DE60221041T2

    公开(公告)日：2008-04-10

    申请号：DE60221041

    申请日：2002-12-20

    Applicant: SERVIER LAB

    Inventor： CORDI ALEX ,  DESOS PATRICE ,  LESTAGE PIERRE

    IPC: C07D279/02 ,  A61K31/5415 ,  A61K31/549 ,  A61P9/10 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07B61/00 ,  C07D285/24

    Abstract: Benzothia(dia)zine derivatives (I), their isomers and salts are new. Benzothia(dia)zine derivatives (I), their isomers and salts are new; R1 = OH or RCOO-; R2 = H, halogen, OH or R'COO-; R, R' = 1-6C alkyl or 2-6C alkenyl (both optionally substituted by aryl), 1-6C perhaloalkyl, 3-7C cycloalkyl, adamantyl, aryl, or heteroaryl; R3 = H, 1-6C alkyl, or 3-7C cycloalkyl; A = CR4R5 or NR4; R4 = H or 1-6C alkyl; R5 = H or halogen Provided that: (1) when R1 is RCOO- it is in position 5; (2) aryl groups are mono or bicyclic and may be substituted by alkyl, alkoxy, perhaloalkyl, perhaloalkoxy, OH, CN, alkyl, mono- or dialkylamino, aminosulfonyl, mono or dialkylaminosulfonyl, or optionally substituted phenyl; and (3) heteroaryl groups may have up to three heteroatoms (O, N, S), may be mono or bicyclic and may be substituted as described for aryl groups. An Independent claim is also included for the preparation of (I).

    83.
    发明专利
    未知

    公开(公告)号：DE602005003907D1

    公开(公告)日：2008-01-31

    申请号：DE602005003907

    申请日：2005-11-02

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    IPC: A61K31/5415 ,  A61P25/00 ,  C07D285/24

    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.

    COMPUESTOS POLISUSTITUIDOS 1,1-PIRIDILAMINOCICLOPROPANAMINA, COMO LIGANDOS ESPECIFICOS DE RECEPTORES NICOTINICOS ALFA4BETA2
    85.
    发明专利
    COMPUESTOS POLISUSTITUIDOS 1,1-PIRIDILAMINOCICLOPROPANAMINA, COMO LIGANDOS ESPECIFICOS DE RECEPTORES NICOTINICOS ALFA4BETA2 未知

    公开(公告)号：AR055589A1

    公开(公告)日：2007-08-29

    申请号：ARP060103248

    申请日：2006-07-27

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

    IPC: A61K31/44 ,  A61P25/00 ,  C07D213/74 ,  A61P25/28 ,  A61P25/32 ,  A61P25/34

    Abstract: Composiciones farmacéuticas que los contienen, método de preparacion y usos para tratar neuropatologías asociadas al envejecimiento cerebral. Reivindicacion 1: Compuesto formula (1) en la cual n representa un entero de 1 a 6, inclusive, R1 y R2, que pueden ser idénticos o diferentes, representan, independientemente entre sí, un átomo de H, alquilo C1-6 lineal o ramificado o arilalquilo C1-6, en el cual la parte alquilo puede ser lineal o ramificada; R3 y R4, que pueden ser idénticos o diferentes, representan, cada uno independientemente del otro, H o alquilo C1-6 lineal o ramificado; R5 y R6, que pueden ser idénticos o diferentes, representan, cada uno independientemente del otro, H o alquilo C1-6 lineal o ramificado, halogeno, hidroxi, alcoxi C1-6 lineal o ramificado, ciano, nitro, acilo C2-6 lineal o ramificado, alcoxicarbonilo C1-6 lineal o ramificado, trihaloalquilo C1-6 lineal o ramificado, o trihaloalcoxi C1-6 lineal o ramificado, o un grupo amino, opcionalmente sustituido por 1 o 2 grupos alquilo C1-6 lineal o ramificado; R7 representa H, alquilo C1-6 lineal o ramificado, o un grupo arilalquilo C1-6 en el cual la parte alquilo puede ser lineal o ramificada, se entiende por grupo arilo, un grupo fenilo, bifenilo, naftilo, dihidronaftilo, tetrahidronaftilo, indanilo o indenilo, y cada uno de esos grupos puede ser sustituido, opcionalmente, por uno o más grupos idénticos o diferentes, seleccionados entre átomos de halogeno, alquilo C1-6 lineal o ramificado, hidroxi, ciano, nitro, alcoxi C1-6 lineal o ramificado, acilo C2-7 lineal o ramificado, alcoxicarbonilo C1-6 lineal o ramificado, trihaloalquilo C1-6 lineal o ramificado, trihaloalcoxi C1-6 lineal o ramificado, y grupos amino, sustituidos, opcionalmente, por 1 o 2 grupos alquilo C1-6 lineal o ramificado.

    87.
    发明专利
    未知

    公开(公告)号：AT366245T

    公开(公告)日：2007-07-15

    申请号：AT02805407

    申请日：2002-12-20

    Applicant: SERVIER LAB

    Inventor： CORDI ALEX ,  DESOS PATRICE ,  LESTAGE PIERRE

    IPC: C07D279/02 ,  A61K31/5415 ,  A61K31/549 ,  A61P9/10 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07B61/00 ,  C07D285/24

    Abstract: Benzothia(dia)zine derivatives (I), their isomers and salts are new. Benzothia(dia)zine derivatives (I), their isomers and salts are new; R1 = OH or RCOO-; R2 = H, halogen, OH or R'COO-; R, R' = 1-6C alkyl or 2-6C alkenyl (both optionally substituted by aryl), 1-6C perhaloalkyl, 3-7C cycloalkyl, adamantyl, aryl, or heteroaryl; R3 = H, 1-6C alkyl, or 3-7C cycloalkyl; A = CR4R5 or NR4; R4 = H or 1-6C alkyl; R5 = H or halogen Provided that: (1) when R1 is RCOO- it is in position 5; (2) aryl groups are mono or bicyclic and may be substituted by alkyl, alkoxy, perhaloalkyl, perhaloalkoxy, OH, CN, alkyl, mono- or dialkylamino, aminosulfonyl, mono or dialkylaminosulfonyl, or optionally substituted phenyl; and (3) heteroaryl groups may have up to three heteroatoms (O, N, S), may be mono or bicyclic and may be substituted as described for aryl groups. An Independent claim is also included for the preparation of (I).

    88.
    发明专利
    未知

    公开(公告)号：DE602004002990T2

    公开(公告)日：2007-07-05

    申请号：DE602004002990

    申请日：2004-06-09

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEX ,  LESTAGE PIERRE

    IPC: C07D513/04 ,  A61K31/54 ,  A61K31/549 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D513/02

    Abstract: Benzothiazine or benzothiadiazine derivatives (I) are new. Benzothiazine or benzothiadiazine derivatives of formula (I) and their isomers and salts are new: [Image] R 1H, halo or 1-6C alkyl; R 1a = H or 1-6C alkyl; R 2H, halo or OH; A : NR 4or CR 4R 5; R 3H, 1-6C alkyl or 3-7C cycloalkyl; R 4H or 1-6C alkyl; R 5H or halo; R 6R 4or forms a CH 2(CH 2) mCH 2group with R 3; m : 1-3; X : NR 6R 7, SO nR 8, OR' 8or a heterocyclic group; R 6, R 7H or 1-6C alkyl, or R 6is SO pR 9, COR 9or P(O)(OR 9)(OR 10); or NR 6R 7is a heterocyclic group; R 8-R 10H, 1-6C (halo)alkyl, aralkyl or aryl; R' 81-6C alkyl or 1-6C acyl; n, p : 1 or 2. [Image] An independent claim is also included for two processes for preparing (I). ACTIVITY : Nootropic. MECHANISM OF ACTION : alpha -Amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) modulator. (3-(5,5-Dioxido-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazin-7-yloxy)phenyl)methanamine hydrochloride increased the current intensity induced by AMPA in Xenopusoocytes by a factor of 2 at 3.5 MicroM and by a factor of 5 at 9.2 MicroM.

    89.
    发明专利
    未知

    公开(公告)号：FR2885615B1

    公开(公告)日：2007-06-22

    申请号：FR0504757

    申请日：2005-05-12

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    IPC: C07D413/14 ,  A61K31/496 ,  A61P3/04 ,  A61P25/00 ,  A61P29/00 ,  C07D213/74 ,  C07D241/04 ,  C07D295/26 ,  C07D401/04

    Abstract: Phenyl pyridinyl piperazine derivatives (I), their enantiomers and diastereoisomers, acid and base addition salts are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts are new. R 1NR 3SO 2R 4; R 3H or 1-6C alkyl; R 41-6C alkyl, T or NR 5R 6; either R 5, R 6R 3, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; NR 5R 65-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphtyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist.

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