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    Oxazole derivatives as histamine h3 receptor agents,preparation and therapeutic uses
    5.
    发明申请
    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：US20070197604A1

    公开(公告)日：2007-08-23

    申请号：US11572283

    申请日：2005-07-14

    申请人： Lisa Beavers ,  Serge Boulet ,  Terry Finn ,  Robert Gadski ,  Willaim Hornback ,  Cynthia Jesudason ,  Richard Pickard ,  Freddie Stevens ,  Grant Vaught

    发明人： Lisa Beavers ,  Serge Boulet ,  Terry Finn ,  Robert Gadski ,  Willaim Hornback ,  Cynthia Jesudason ,  Richard Pickard ,  Freddie Stevens ,  Grant Vaught

    IPC分类号： A61K31/421 ,  A61K31/44 ,  C07D413/10

    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 -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。

    2-Oxo-benzimidazolyl substituted ethanolamine derivatives and their use as beta3 agonists
    7.
    发明申请
    2-Oxo-benzimidazolyl substituted ethanolamine derivatives and their use as beta3 agonists 失效
    2-氧代苯并咪唑基取代的乙醇胺衍生物及其作为β3激动剂的用途

    公开(公告)号：US20060014963A1

    公开(公告)日：2006-01-19

    申请号：US11228620

    申请日：2005-09-16

    申请人： Cynthia Jesudason ,  Don Finley

    发明人： Cynthia Jesudason ,  Don Finley

    IPC分类号： A61K31/4184 ,  C07C235/12

    CPC分类号： C07D213/82 ,  C07C235/46 ,  C07C2601/02 ,  C07C2601/08 ,  C07D235/26 ,  C07D401/12

    摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I), wherein R is C3-C8 alkyl or (C3-C7 cycloalkyl)C1-C5 alk-di-yl: R1 is H, CN, halo; C1-C6 alkyl, C1-C4 haloalkyl, C02 R6, CONR6R6, NR6COR7, NR6R6, OR6, SR6, SOR7. S02R7 or S02NR6R6; R1a is H, halo or C1-C6 aLkyl; R2 is Hi or C1-C6 alkyl; R3 and R4 are independently H or C1-C6 alkyl R5 is hydrogen, optionally substituted phenyl or optionally substituted heterocycle; X is absent or is OCH2 or SCH2; X1 is absent or C1-C5 alk-di-yl; and X2 is absent or is O, S, NH, NHS02, S02NH or CH2; or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 deabetes and/or obesity

    摘要翻译： 本发明涉及式（I）的β3 N 3肾上腺素能受体激动剂，其中R是C 3 -C 8烷基或（C C 3 -C 3 - 环烷基）C 1 -C 5烷基 - 二基：R 1 H，CN，卤素; C 1 -C 6烷基，C 1 -C 4卤代烷基，C 0 2 或者S0＆lt; 2＆lt; 6＆lt; 6＆gt; 6＆lt; 6＆gt; R 1a是H，卤素或C 1 -C 6 -C 1-4烷基; R 2是H 1或C 1 -C 6烷基; R 3和R 4独立地为H或C 1 -C 6烷基R 5， SUP>是氢，任选取代的苯基或任选取代的杂环; X不存在或是OCH 2或SCH 2; X 1不存在或C 1 -C 5烷基 - 二基; 和X 2不存在，或者是O，S，NH，NHSO 2，SO 2 NH或CH 2， ; 或其药学盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖