发明公开
- 专利标题: PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES
- 专利标题(中): 苯丙酸甲酯
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申请号: EP03784411.5申请日: 2003-07-28
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公开(公告)号: EP1546134A1公开(公告)日: 2005-06-29
- 发明人: AICHER, Thomas, Daniel , CHEN, Zhaogen , LE HUEROU, Yvan , MARTIN, Fionna MitchellEli Lilly and Company Ltd. , PINEIRO-NUNEZ, Marta, Maria , ROCCO, Vincent, Patrick , RULEY, Kevin, Michael , SCHAUS, John, Mehnert , SPINAZZE, Patrick, Gianpietro , TUPPER, David EdwardEli Lilly and Company
- 申请人: ELI LILLY AND COMPANY
- 申请人地址: Lilly Corporate Center Indianapolis, Indiana 46285 US
- 专利权人: ELI LILLY AND COMPANY
- 当前专利权人: ELI LILLY AND COMPANY
- 当前专利权人地址: Lilly Corporate Center Indianapolis, Indiana 46285 US
- 代理机构: Kingsbury, Oliver William
- 优先权: US401297P 20020805
- 国际公布: WO2004014895 20040219
- 主分类号: C07D403/04
- IPC分类号: C07D403/04 ; C07D495/04 ; C07D513/04 ; A61K31/55 ; A61P25/18
摘要:
Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or -CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, N02, CN, COR4, C(O)OR4, CONR5R6 , NR5R6, S02NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen, (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyl is unsubsituted or substituted with a phenyl; R4 is hydrogen, (C1-6 alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treament of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).
公开/授权文献
- EP1546134B1 PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES 公开/授权日:2007-05-02
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