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    Oxazole derivatives as histamine H3 receptor agents, preparation and therapeutic uses
    1.
    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。

    Histamine H3 receptor inhibitors, preparation and therapeutic uses
    6.
    发明授权
    Histamine H3 receptor inhibitors, preparation and therapeutic uses 有权
    组胺H3受体抑制剂，制剂和治疗用途

    公开(公告)号：US07846950B2

    公开(公告)日：2010-12-07

    申请号：US11577388

    申请日：2005-10-11

    申请人： Cynthia Darshini Jesudason ,  Freddie Craig Stevens

    发明人： Cynthia Darshini Jesudason ,  Freddie Craig Stevens

    IPC分类号： A61K31/422 ,  A61K31/4025 ,  A61K31/4245 ,  C07D417/12 ,  C07D405/12 ,  A61P25/00

    CPC分类号： C07D417/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    摘要： The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiences, narcolepsy, and other histamine H3 receptor-related diseases.

    摘要翻译： 本发明提供具有组胺H3受体拮抗剂或反向激动剂活性的新型化合物。 特别地，本发明提供式I化合物或其药学上可接受的盐，包含该化合物的药物组合物，使用这些化合物和组合物的治疗方法，以及制备这些化合物的中间体和方法。 本发明提供了使用化合物和药物组合物治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。