首页> 外国专利> New benzothiazine and benzothiadiazine derivatives useful as Alpha amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) modulators, for preventing and treating e.g. memory disorders, anxiety and depression

New benzothiazine and benzothiadiazine derivatives useful as Alpha amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) modulators, for preventing and treating e.g. memory disorders, anxiety and depression

机译:新的苯并噻嗪和苯并噻二嗪衍生物可用作预防和治疗例如α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)调节剂。记忆障碍,焦虑和抑郁

摘要

Benzothiazine and benzothiadiazine derivatives (I) their isomers and salts are new. Benzothiazine and benzothiadiazine derivatives (I) their isomers and salts are new; R1 = aryl or heteroaryl; R2 = H, halogen, or OH; A = CR4R5 or NR4, or it is N and forms with the group -CHR3 a ring of formula (i); m = 1, 2, or 3; R3 = H, 1-6C alkyl or 3-7C cycloalkyl; R4 = H or 1-6C alkyl; R5 = H or halogen; Ra, Rb = H or alkyl. Provided that: (1) aryl groups are mono or bicyclic, at least one ring of which is aromatic, and may be substituted by one or more groups selected from halogens, alkyl (optionally substituted by OH), alkoxy, perhaloalkyl, perhaloalkoxy, alkoxycarbonyl, alkylthio, carboxy, acyl, OH, CN, NO2, NH2, mono- or dialkylamino, mono- or di-acylamino, aminocarbonyl, alkylaminocarbonyl, aminosulfonyl, alkylaminosulfonyl, mono- or dialkylsulfoylamino, mono- or di-(trifluoromethylsulfonyl) amino, PO(ORa)(ORb), benzyloxy, or phenyl (optionally substituted by one or more halogen, alkyl, perhaloalkyl, hydroxy or alkoxy groups); and (2) heteroaryl groups may have up to three heteroatoms (O, N, S), may be mono or bicyclic, at least one ring being aromatic, optionally substituted by one or more groups selected from halogens, alkyl, alkoxy, perhaloalkyl, alkoxycarbonyl, carboxy, acyl, perhaloalkoxy, OH, CN, NO2, NH2, mono- or dialkylamino, aminosulfonyl, alkylaminosulfonyl, and alkylsulfonylamino. An Independent claim is also included for the preparation of (I).
机译:苯并噻嗪和苯并噻二嗪衍生物(I)的异构体和盐是新的。苯并噻嗪和苯并噻二嗪衍生物(I)的异构体和盐是新的; R1 =芳基或杂芳基; R 2 = H,卤素或OH; A = CR4R5或NR4,或为N,与-CHR3基团形成式(i)的环; m = 1、2或3; R3 = H,1-6C烷基或3-7C环烷基; R4 = H或1-6C烷基; R5 = H或卤素; Ra,Rb = H或烷基。前提是:(1)芳基是单环或双环,其至少一个环是芳族的,并且可以被选自卤素,烷基(任选被OH取代),烷氧基,全卤代烷基,全卤代烷氧基,烷氧基羰基中的一个或多个基团取代。 ,烷硫基,羧基,酰基,OH,CN,NO 2,NH 2,单或二烷基氨基,单或二酰基氨基,氨基羰基,烷基氨基羰基,氨基磺酰基,烷基氨基磺酰基,单或二烷基磺酰基氨基,单或二(三氟甲基磺酰基)氨基, PO(ORa)(ORb),苄氧基或苯基(可选地被一个或多个卤素,烷基,全卤代烷基,羟基或烷氧基取代); (2)杂芳基可具有至多三个杂原子(O,N,S),可为单环或双环,至少一个环为芳族,可选地被一个或多个选自卤素,烷基,烷氧基,全卤代烷基的基团取代,烷氧基羰基,羧基,酰基,全卤代烷氧基,OH,CN,NO 2,NH 2,单或二烷基氨基,氨基磺酰基,烷基氨基磺酰基和烷基磺酰基氨基。独立索赔也包括在准备(I)中。

著录项

  • 公开/公告号NO20042978L

    专利类型

  • 公开/公告日2004-07-14

    原文格式PDF

  • 申请/专利权人 LES LABORATOIRES SERVIER;

    申请/专利号NO20040002978

  • 发明设计人 CORDI ALEX;DESOS PATRICE;LESTAGE PIERRE;

    申请日2004-07-14

  • 分类号C07D279/02;C07D513/04;A61K31/5415;A61K31/549;A61P25/00;A61P25/28;

  • 国家 NO

  • 入库时间 2022-08-21 23:09:27

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