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    Oxazole derivatives as histamine H3 receptor agents, preparation and therapeutic uses
    8.
    发明授权
    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

    公开(公告)号：US07666871B2

    公开(公告)日：2010-02-23

    申请号：US11572283

    申请日：2005-07-14

    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

    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

    IPC分类号： A61K31/501 ,  C07D403/14

    CPC分类号： C07D413/14 ,  C07D263/32 ,  C07D413/06 ,  C07D417/14

    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.

    摘要翻译： 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）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原子形成氮杂环丁烷基环，吡咯烷基环或哌啶基环，其中进一步 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; R6各自独立地为-H， - 卤素或-CH 3。