发明申请
US20110105543A1 NOVEL TRIARYL DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
审中-公开
新型三肽衍生物有用作为非线性乙酰胆碱受体的调节剂
- 专利标题: NOVEL TRIARYL DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
- 专利标题(中): 新型三肽衍生物有用作为非线性乙酰胆碱受体的调节剂
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申请号: US12922007申请日: 2009-03-09
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公开(公告)号: US20110105543A1公开(公告)日: 2011-05-05
- 发明人: Antonio Nardi , Jeppe Kejser Christensen , Dan Peters
- 申请人: Antonio Nardi , Jeppe Kejser Christensen , Dan Peters
- 申请人地址: DK Ballerup
- 专利权人: NeuroSearch A/S
- 当前专利权人: NeuroSearch A/S
- 当前专利权人地址: DK Ballerup
- 优先权: DKPA200800371 20080311
- 国际申请: PCT/EP09/52733 WO 20090309
- 主分类号: A61K31/505
- IPC分类号: A61K31/505 ; C07D239/42 ; C07C217/80 ; C07C215/74 ; C07D403/10 ; C07D239/30 ; C07D405/10 ; C07D239/48 ; C07D237/20 ; C07D213/73 ; C07D401/10 ; C07D209/08 ; C07C309/01 ; A61K31/136 ; A61K31/506 ; A61K31/50 ; A61K31/44 ; A61K31/4439 ; A61K31/404 ; A61K31/185 ; A61P25/22 ; A61P25/28 ; A61P25/00 ; A61P25/16 ; A61P25/18 ; A61P25/24 ; A61P3/00 ; A61P3/04 ; A61P25/20 ; A61P25/08 ; A61P15/00 ; A61P9/12 ; A61P9/06 ; A61P43/00 ; A61P1/12 ; A61P5/00 ; A61P25/04 ; A61P25/06 ; A61P29/00 ; A61P17/00 ; A61P25/30 ; A61P25/36 ; A61P25/34
摘要:
This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R1, R2, R3, R4 and R5. independently of each other, represent hydrogen, halo, tri-fluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkoxy, alkyl, amino or sulfamoyl; or R1 and R2, together with the phenyl ring to which they are attached form an indolyl ring or a benzo-dioxolyl ring; and R3, R4 and R5 are as defined above; and R6 represents amino or nitro, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
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