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    Pyrazolone derivatives as MCP-1 antagonists
    1.
    发明授权
    Pyrazolone derivatives as MCP-1 antagonists 失效
    吡唑酮衍生物作为MCP-1拮抗剂

    公开(公告)号：US06011052A

    公开(公告)日：2000-01-04

    申请号：US845729

    申请日：1997-04-25

    申请人： Janak Khimchand Padia ,  Bruce David Roth ,  John Edward Strode ,  Bharat Kalidas Trivedi

    发明人： Janak Khimchand Padia ,  Bruce David Roth ,  John Edward Strode ,  Bharat Kalidas Trivedi

    IPC分类号： C07D231/46 ,  C07D231/50 ,  C07D471/04 ,  A61K31/415 ,  C07D231/06 ,  C07D231/14 ,  C07D231/16

    CPC分类号： C07D471/04 ,  C07D231/46 ,  C07D231/50

    摘要： Pyrazolone derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammatory diseases or conditions, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## where: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 can be independently H,C.sub.1-20 alkyl,C.sub.5-7 cycloalkyl,--(CH.sub.2).sub.n NR.sub.6 R.sub.7--(CH.sub.2).sub.0-6 CONR.sub.6 R.sub.7,--(CH.sub.2).sub.n OH or--(CH.sub.2).sub.0-6 CO.sub.2 R.sub.11,biphenyl,aryl of from 6 to 10 carbon atoms, oraryl of from 6 to 10 carbon atoms substituted up to 3 times by halogen, --CN, lower alkyl of from 1-4 carbon atoms, --OH, nitro, --SO.sub.2 H, SO.sub.2 lower alkyl,--SO.sub.2 NR.sub.6 R.sub.7 lower alkoxy--C0.sub.2 R.sub.11,--CONR.sub.6 R.sub.7,--NR.sub.6 R.sub.7 or CH.sub.2 OH.

    摘要翻译： 式I的吡唑酮衍生物或其药学上可接受的盐是MCP-1拮抗剂，因此可用于治疗炎性疾病或病症，动脉粥样硬化，再狭窄和免疫疾病如关节炎和移植排斥反应，其中：R1，R2，R3， R4，R5可以独立地是H，C1-20烷基，C5-7环烷​​基， - （CH2）nNR6R7 - （CH2）0-6CONR6R7， - （CH2）nOH或 - （CH2）0-6CO2R11， 6至10个碳原子，或6至10个碳原子的芳基被卤素取代3次，-CN，1-4个碳原子的低级烷基，-OH，硝基，-SO 2 H，SO 2低级烷基，-SO 2 NR 6 R 7 低级烷氧基-C02R11，-CONR6R7，-NR6R7或CH2OH。

    Chemokine receptor antagonists
    7.
    发明授权
    Chemokine receptor antagonists 有权
    趋化因子受体拮抗剂

    公开(公告)号：US06316449B1

    公开(公告)日：2001-11-13

    申请号：US09558267

    申请日：2000-04-25

    申请人： Larry Don Bratton ,  Steven Robert Miller ,  Bruce David Roth ,  Bharat Kalidas Trivedi ,  Paul Charles Unangst

    发明人： Larry Don Bratton ,  Steven Robert Miller ,  Bruce David Roth ,  Bharat Kalidas Trivedi ,  Paul Charles Unangst

    IPC分类号： A61K31150

    CPC分类号： C07D471/14

    摘要： The instant invention is a series of compounds which are MCP-1 receptor antagonists of Formula I Also included in the invention are intermediates and processes for the preparation of the compounds as well as methods of using the compounds as agents for the treatment of atherosclerosis, chronic and acute inflammatory disease, chronic and acute immune disorders and transplant rejection as well as for preventing infection by HIV, treating infection by HIV, delaying the onset of AIDS, or treating AIDS.

    摘要翻译： 本发明是一系列化合物，其是本发明中包括的式IAl的MCP-1受体拮抗剂，其是中间体和化合物的制备方法，以及使用该化合物作为治疗动脉粥样硬化，慢性和 急性炎症性疾病，慢性和急性免疫疾病和移植排斥以及预防艾滋病毒感染，治疗艾滋病毒感染，延迟艾滋病发作或治疗艾滋病。