Imidazopyrazines as protein kinase inhibitors
    96.
    发明授权
    Imidazopyrazines as protein kinase inhibitors 失效
    咪唑吡嗪作为蛋白激酶抑制剂

    公开(公告)号:US07557104B2

    公开(公告)日:2009-07-07

    申请号:US11758243

    申请日:2007-06-05

    IPC分类号: A61K31/497

    CPC分类号: C07D487/04

    摘要: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

    摘要翻译: 在其许多实施方案中,本发明提供了一类新颖的咪唑并吡嗪化合物作为蛋白质和/或检查点激酶的抑制剂,制备此类化合物的方法,包含一种或多种此类化合物的药物组合物,制备药物制剂的方法,包括一种或多种 化合物,以及使用这些化合物或药物组合物治疗,预防,抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
    99.
    发明授权
    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
    碳链取代的哌啶及其衍生物可用作组胺H3拮抗剂

    公开(公告)号:US07408066B2

    公开(公告)日:2008-08-05

    申请号:US11455873

    申请日:2006-06-19

    摘要: Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.

    摘要翻译: 公开了下式的化合物或其药学上可接受的盐,其中:M 1和M 3是CH或N; M 2是CH,CF或N; Y是-C(-O) - , - C(-S) - , - (CH 2 CH 2)q - , - C(-NOR 7) / SO 2 - ) - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H,烷基,烯基或任选取代的环烷基,芳基,杂芳基,杂环烷基或下式的基团:其中环A是单杂芳基环; R 2是任选取代的烷基,烯基,芳基,杂芳基,环烷基或杂环烷基; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应,充血,肥胖,代谢综合征非酒精性脂肪性肝病,肝脂肪变性,非酒精性脂肪性肝炎,肝硬化,肝细胞癌或认知缺陷障碍的组合物和方法。