发明授权
US07666871B2 Oxazole derivatives as histamine H3 receptor agents, preparation and therapeutic uses
有权
恶唑衍生物作为组胺H3受体剂,制备和治疗用途
- 专利标题: Oxazole derivatives as histamine H3 receptor agents, preparation and therapeutic uses
- 专利标题(中): 恶唑衍生物作为组胺H3受体剂,制备和治疗用途
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申请号: US11572283申请日: 2005-07-14
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公开(公告)号: US07666871B2公开(公告)日: 2010-02-23
- 发明人: Lisa Selsam Beavers , Serge Louis Boulet , Terry Patrick Finn , Robert Alan Gadski , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Freddie Craig Stevens , Grant Mathews Vaught
- 申请人: Lisa Selsam Beavers , Serge Louis Boulet , Terry Patrick Finn , Robert Alan Gadski , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Freddie Craig Stevens , Grant Mathews Vaught
- 申请人地址: US IN Indianapolis
- 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: US IN Indianapolis
- 代理商 Dan L. Wood
- 国际申请: PCT/US2005/024883 WO 20050714
- 国际公布: WO2006/019833 WO 20060223
- 主分类号: A61K31/501
- IPC分类号: A61K31/501 ; C07D403/14
摘要:
The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently —(C1—C7) alkyl (optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence —H, -halogen, or —CH3.
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