会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明申请
    • Oxazole derivatives as histamine h3 receptor agents,preparation and therapeutic uses
    • 恶唑衍生物作为组胺h3受体剂,制备和治疗用途
    • US20070197604A1
    • 2007-08-23
    • US11572283
    • 2005-07-14
    • Lisa BeaversSerge BouletTerry FinnRobert GadskiWillaim HornbackCynthia JesudasonRichard PickardFreddie StevensGrant Vaught
    • Lisa BeaversSerge BouletTerry FinnRobert GadskiWillaim HornbackCynthia JesudasonRichard PickardFreddie StevensGrant Vaught
    • A61K31/421A61K31/44C07D413/10
    • C07D413/14C07D263/32C07D413/06C07D417/14
    • 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.
    • 本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式I(I)的新型芳基恶唑化合物或其药学上可接受的盐,以及制备和使用这些化合物的方法。 在另一个实施方案中,本发明公开了包含式I化合物的药物组合物以及使用这些组合物治疗肥胖症,认知缺陷,发作性睡病和其他组胺H3受体相关疾病的方法。 式I(I)或其药学上可接受的盐,其中:m在每次出现时独立地为1,2或3,Z独立地表示碳(被氢或本文所示的任选取代基)或氮,条件是当Z为 氮,然后R6不连接到Z; R 1和R 2独立地为 - (C 1 -C 7 -C 7)烷基(任选被一至三个卤素取代),或R 1和R 2以及与它们相连的氮 形成氮杂环丁烷基环,吡咯烷基环或哌啶基环,其中如此形成的氮杂环丁烷基,吡咯烷基或哌啶基环可以任选地被R 5取代一至三次; R 6在每次出现时独立地为-H, - 卤素或-CH 3。