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    1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
    4.
    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。

    1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives
    5.
    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。

    4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives
    8.
    发明授权
    4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives 失效
    4-苯基-6-取代 - 嘧啶-2-甲腈衍生物

    公开(公告)号：US07326715B2

    公开(公告)日：2008-02-05

    申请号：US11524841

    申请日：2006-09-21

    申请人： Zoran Rankovic ,  Jiaqiang Cai

    发明人： Zoran Rankovic ,  Jiaqiang Cai

    IPC分类号： C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  A61K31/505 ,  A61P9/10 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00

    CPC分类号： C07D239/42 ,  C07D239/34 ,  C07D239/38 ,  C07D403/12

    摘要： Disclosed herein are 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims; or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives and use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.

    摘要翻译： 本文公开了具有式I的4-苯基-6-取代 - 嘧啶-2-甲腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义; 或其药学上可接受的盐。 还公开了包含这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物的药物组合物和这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物用于治疗组织蛋白酶K和组织蛋白酶S相关病症 ，例如 骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛。

    4-phenyl-pyrimidine-2-carbonitrile derivatives
    9.
    发明授权
    4-phenyl-pyrimidine-2-carbonitrile derivatives 失效
    4-苯基 - 嘧啶-2-甲腈衍生物

    公开(公告)号：US07589095B2

    公开(公告)日：2009-09-15

    申请号：US11628623

    申请日：2005-06-09

    申请人： Jiaqiang Cai ,  Zoran Rankovic ,  Jennifer Helen Moir

    发明人： Jiaqiang Cai ,  Zoran Rankovic ,  Jennifer Helen Moir

    IPC分类号： C07D239/28 ,  A61K31/505 ,  A61P9/10 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00

    CPC分类号： C07D239/28

    摘要： The invention relates to 4-phenyl-pyrimidine-2-carbonitrile derivatives having the general formula I wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising the derivatives as well as to the use thereof in the treatment of osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

    摘要翻译： 本发明涉及具有通式I的4-苯基 - 嘧啶-2-甲腈衍生物，其中每个取代基被给出如说明书和权利要求书中所述的定义，或其药学上可接受的盐。 本发明还涉及包含衍生物的药物组合物以及其在治疗骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛如神经性疼痛中的用途。

    4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives
    10.
    发明申请
    4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives 失效
    4-苯基-6-取代 - 嘧啶-2-甲腈衍生物

    公开(公告)号：US20070111992A1

    公开(公告)日：2007-05-17

    申请号：US11524841

    申请日：2006-09-21

    申请人： Zoran Rankovic ,  Jiaqiang Cai

    发明人： Zoran Rankovic ,  Jiaqiang Cai

    IPC分类号： A61K31/551 ,  A61K31/5377 ,  A61K31/513 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D239/42 ,  C07D239/34 ,  C07D239/38 ,  C07D403/12

    摘要： Disclosed herein are 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims; or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives and use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.

    摘要翻译： 本文公开了具有式I的4-苯基-6-取代 - 嘧啶-2-甲腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义; 或其药学上可接受的盐。 还公开了包含这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物的药物组合物和这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物用于治疗组织蛋白酶K和组织蛋白酶S相关病症 ，例如 骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛。