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    Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands
    1.
    发明申请
    Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands 审中-公开
    杂芳基稠合吡啶，吡嗪和嘧啶作为CRF1受体配体

    公开(公告)号：US20060199823A1

    公开(公告)日：2006-09-07

    申请号：US11389646

    申请日：2006-03-24

    申请人： Ping Ge ,  Raymond Horvath ,  Lu Zhang ,  Yasuchika Yamaguchi ,  Bernd Kaiser ,  Xuechun Zhang ,  Suoming Zhang ,  He Zhao

    发明人： Ping Ge ,  Raymond Horvath ,  Lu Zhang ,  Yasuchika Yamaguchi ,  Bernd Kaiser ,  Xuechun Zhang ,  Suoming Zhang ,  He Zhao

    IPC分类号： A61K31/498 ,  C07D487/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

    摘要翻译： 提供了作为CRF 1受体的选择性调节剂的取代的杂芳基稠合的吡啶，吡嗪和嘧啶化合物。 这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗这种疾病以及包装的药物组合物的方法。 本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。

    Amino methyl imidazoles and related compounds as C5a receptor modulators
    5.
    发明申请
    Amino methyl imidazoles and related compounds as C5a receptor modulators 失效
    氨基甲基咪唑和相关化合物作为C5a受体调节剂

    公开(公告)号：US20070212297A1

    公开(公告)日：2007-09-13

    申请号：US11615054

    申请日：2006-12-22

    申请人： Andrew Thurkauf ,  He Zhao ,  Suoming Zhang ,  Yang Gao

    发明人： Andrew Thurkauf ,  He Zhao ,  Suoming Zhang ,  Yang Gao

    IPC分类号： A61K51/00

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

    摘要： Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.

    摘要翻译： 提供式I的氨基甲基咪唑：其中R 1，R 2，R 2，R 3，R 4， >，R 5和R 6在本文中定义。 这些化合物是C5a受体的配体。 优选的式I化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。 本发明还涉及包含这些化合物的药物组合物。 它还涉及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。 此外，本发明提供标记的氨基甲基咪唑化合物，其可用作C5a受体定位的探针。

    Amino methyl imidazoles and related compounds as C5a receptor modulators
    6.
    发明授权
    Amino methyl imidazoles and related compounds as C5a receptor modulators 失效
    氨基甲基咪唑和相关化合物作为C5a受体调节剂

    公开(公告)号：US08007767B2

    公开(公告)日：2011-08-30

    申请号：US11615054

    申请日：2006-12-22

    申请人： Andrew Thurkauf ,  He Zhao ,  Suoming Zhang ,  Yang Gao

    发明人： Andrew Thurkauf ,  He Zhao ,  Suoming Zhang ,  Yang Gao

    IPC分类号： A61K51/00

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

    摘要： Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.

    摘要翻译： 提供式I的氨基甲基咪唑：其中R，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。 这些化合物是C5a受体的配体。 优选的式I化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。 本发明还涉及包含这些化合物的药物组合物。 它还涉及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。 此外，本发明提供标记的氨基甲基咪唑化合物，其可用作C5a受体定位的探针。

    Amino methyl imidazoles as C5a receptor modulators
    8.
    发明授权
    Amino methyl imidazoles as C5a receptor modulators 失效
    氨基甲基咪唑作为C5a受体调节剂

    公开(公告)号：US07169775B2

    公开(公告)日：2007-01-30

    申请号：US10647191

    申请日：2003-08-21

    申请人： Andrew Thurkauf ,  He Zhao ,  Suoming Zhang ,  Yang Gao

    发明人： Andrew Thurkauf ,  He Zhao ,  Suoming Zhang ,  Yang Gao

    IPC分类号： A61K31/541 ,  C07D517/02

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

    摘要： Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.

    摘要翻译： 提供式I的氨基甲基咪唑：其中R 1，R 2，R 2，R 3，R 4， R 5，R 6和R 6在本文中定义。 这些化合物是C5a受体的配体。 优选的式I化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。 本发明还涉及包含这些化合物的药物组合物。 它还涉及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。 此外，本发明提供标记的氨基甲基咪唑化合物，其可用作C5a受体定位的探针。

    THIAZOLE COMPOUNDS AND METHODS OF USE
    10.
    发明申请
    THIAZOLE COMPOUNDS AND METHODS OF USE 审中-公开
    噻唑化合物及其使用方法

    公开(公告)号：US20120108576A1

    公开(公告)日：2012-05-03

    申请号：US13307761

    申请日：2011-11-30

    申请人： Suoming Zhang ,  Avinash Phadke ,  Cuixian Liu ,  Xiangzhu Wang ,  Jesse Quinn ,  Dawei Chen ,  Venkat Gadhachanda ,  Shouming Li ,  Milind Deshpande

    发明人： Suoming Zhang ,  Avinash Phadke ,  Cuixian Liu ,  Xiangzhu Wang ,  Jesse Quinn ,  Dawei Chen ,  Venkat Gadhachanda ,  Shouming Li ,  Milind Deshpande

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/498 ,  A61K31/501 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/506 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/429 ,  A61K31/426 ,  A61K31/427 ,  C07D239/02 ,  C07D513/14 ,  C07D471/04 ,  C07D417/04 ,  C07D513/04 ,  C07D417/14 ,  C07D277/38 ,  A61K31/538

    CPC分类号： C07D487/04 ,  C07D277/38 ,  C07D277/42 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    摘要： The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

    摘要翻译： 本发明提供式I的化合物，盐和水合物，其中变量Ar1，R2，R3，R4，r，q和t在本文中定义。 某些本文所述的式I化合物具有有效的抗病毒活性。 本发明还提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式I化合物。 本文所述的某些化合物抑制HCV复制复合物的组装。 本发明还提供含有一种或多种式I化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。 本发明还包括通过向这些患者施用一定量的有效降低疾病体征或症状的式I化合物来治疗患有某些感染性疾病的患者的方法。 这些传染病包括病毒感染，特别是HCV感染。 本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。 治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。