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    1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
    3.
    发明申请
    1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES 有权
    1H- [1,2,3]三唑[4,5-c]吡啶-4-羰基衍生物

    公开(公告)号：US20120283239A1

    公开(公告)日：2012-11-08

    申请号：US13519924

    申请日：2011-01-13

    申请人： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

    发明人： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

    IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/54 ,  A61P25/00 ,  A61P19/10 ,  A61P9/10 ,  A61P29/00 ,  A61P37/00 ,  A61P17/06 ,  A61K31/437 ,  A61K31/551

    CPC分类号： C07D471/04

    摘要： The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.

    摘要翻译： 本发明涉及式（I）的1H- [1,2,3]三唑并[4,5-c]吡啶-4-腈衍生的组织蛋白酶S抑制剂，其中R 1是H或（C 1-3）烷基; R 2是卤素或任选被一个或多个卤素取代的（C 1-4）烷基; n为1-3; X是O或CH2; U，V和W是CH; 或U，V和W之一为N; Y是能够与Sn相互作用的组。 。 。 组织蛋白酶S活性位点的S2位点; 或其药学上可接受的盐用于包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿病的药物中的用途 关节炎，牛皮癣，癌症和慢性疼痛，如神经性疼痛。

    Aminoisoquinoline thrombin inhibitor with improved bioavailability
    4.
    发明授权
    Aminoisoquinoline thrombin inhibitor with improved bioavailability 失效
    具有改善生物利用度的氨基异喹啉凝血酶抑制剂

    公开(公告)号：US08299091B2

    公开(公告)日：2012-10-30

    申请号：US12376529

    申请日：2007-08-06

    申请人： Robert Gilfillan ,  David Jonathan Bennett

    发明人： Robert Gilfillan ,  David Jonathan Bennett

    IPC分类号： A61K31/47 ,  C07D217/14

    CPC分类号： C07D401/12 ,  A61K38/05 ,  C07K5/0202

    摘要： The invention relates to the compound N-(2-oxo-2-propoxyethyl)-β-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.

    摘要翻译： 本发明涉及化合物N-（2-氧代-2-丙氧基乙基） - 苯基-D-苯基 - 丙氨酰-N - [（1-氨基-6-异喹啉基）甲基] -L-脯氨酰胺或 其药学上可接受的盐，包含所述化合物的药物组合物，以及该化合物在制备用于治疗或预防凝血酶介导的疾病的药物中的用途。

    1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives
    8.
    发明授权
    1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives 有权
    1H- [1,2,3]三唑并[4,5-c]吡啶-4-甲腈衍生物

    公开(公告)号：US09115126B2

    公开(公告)日：2015-08-25

    申请号：US13519924

    申请日：2011-01-13

    申请人： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

    发明人： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

    IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/54 ,  A61K31/437 ,  A61K31/551

    CPC分类号： C07D471/04

    摘要： The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.

    摘要翻译： 本发明涉及式（I）的1H- [1,2,3]三唑并[4,5-c]吡啶-4-腈衍生的组织蛋白酶S抑制剂，其中R 1是H或（C 1-3）烷基; R2是卤素或任选被一个或多个卤素取代的（C 1-4）烷基; n为1-3; X是O或CH2; U，V和W是CH; 或U，V和W之一为N; Y是能够与Sn相互作用的组。 。 。 组织蛋白酶S活性位点的S2位点; 或其药学上可接受的盐用于包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿病的药物中的用途 关节炎，牛皮癣，癌症和慢性疼痛，如神经性疼痛。