- 专利标题: Compounds having activity at 5ht2c receptor and uses thereof
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申请号: US10548118申请日: 2004-02-24
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公开(公告)号: US20060205788A1公开(公告)日: 2006-09-14
- 发明人: Federica Damiani , Dieter Hamprecht , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco
- 申请人: Federica Damiani , Dieter Hamprecht , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco
- 优先权: GB0305024.2 20030305
- 国际申请: PCT/EP04/01843 WO 20040224
- 主分类号: A61K31/454
- IPC分类号: A61K31/454 ; C07D403/02
摘要:
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ═ is a double bond and m is 1 when ═ is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is —(CH2—CH2)—, —(CH═CH)—, —(CH2)3—, —C(CH3)2—, —(CH═CH—CH2)—, —(CH2-CH═CH)— or a group —(CHR5)— wherein R5 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R3 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio or COOR6, CONR7R8 or COR9 wherein R6, R7, R8 and R9 are independently hydrogen or C1-6alkyl; p is 0, 1 or 2 or 3; R4 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, —CH2— or NR10 wherein R10 is hydrogen or C1-6alkyl; D is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is —NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and anxiety, are also disclosed.
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