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9 条记录 (耗时 0.053 秒)

    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
    1.
    发明申请
    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors 失效
    用作PDE4抑制剂的取代的2-喹啉基 - 恶唑

    公开(公告)号：US20060106062A1

    公开(公告)日：2006-05-18

    申请号：US11130359

    申请日：2005-05-16

    申请人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

    发明人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

    IPC分类号： A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

    摘要翻译： 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ，-CH 2 F，-CHF 2，-CF 3， -C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟烷基或-C（O）O烷基; R 5和R 6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH 2 F 2，-CHF 2， -CF 3，-C（O）OH或-C（O）O烷基; R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 - C（O）-O-烷基; 和R 8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部被取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8和它们所连接的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
    5.
    发明申请
    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：US20070010513A1

    公开(公告)日：2007-01-11

    申请号：US11455873

    申请日：2006-06-19

    申请人： Robert Aslanian ,  Michael Berlin ,  Ying Huang ,  Kevin McCormick ,  Mwangi Mutahi ,  Neng-Yang Shih ,  Pauline Ting ,  Wing Tom ,  Junying Zheng

    发明人： Robert Aslanian ,  Michael Berlin ,  Ying Huang ,  Kevin McCormick ,  Mwangi Mutahi ,  Neng-Yang Shih ,  Pauline Ting ,  Wing Tom ,  Junying Zheng

    IPC分类号： A61K31/538 ,  A61K31/4709 ,  A61K31/4704 ,  C07D265/12

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

    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; R1 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 1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。