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    MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS
    1.
    发明公开
    MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 有权
    趋化因子受体活性调节剂，结晶形式和过程

    公开(公告)号：EP2046779A2

    公开(公告)日：2009-04-15

    申请号：EP07813363.4

    申请日：2007-07-26

    申请人： Bristol-Myers Squibb Company

    发明人： CARTER, Percy, H. ,  DUNCIA, John, V. ,  MUDRYK, Boguslaw, M. ,  RANDAZZO, Michael, E. ,  XIAO, Zili ,  YANG, Michael, G. ,  ZHAO, Rulin

    IPC分类号： C07D403/12 ,  C07D207/273 ,  A61K31/4025

    CPC分类号： C07D403/12 ,  C07D207/273 ,  C07D317/72

    摘要： The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-(tert-butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((lR,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.

    摘要翻译： N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-2-氧代-3 - （6-（三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺，或其药学上可接受的盐，溶剂化物或前药，其具有理想药理学特性的意想不到的组合。 还提供了本发明的晶体形式。 含有其的药物组合物及其作为治疗炎性疾病，变应性疾病，自身免疫疾病，代谢疾病，癌症和/或心血管疾病的药物的方法也是本发明的目的。 本发明还提供了制备式（I）化合物的方法，其包括N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-2-氧代-3- （三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺：其中R 1，R 8，R 9，R 10和'HET'如本文所述。 本文还提供了作为该方法的有用中间体的化合物。

    MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS
    3.
    发明授权
    MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 有权
    趋化因子受体，晶体形式和过程的调节剂

    公开(公告)号：EP2046779B1

    公开(公告)日：2011-05-18

    申请号：EP07813363.4

    申请日：2007-07-26

    申请人： Bristol-Myers Squibb Company

    发明人： CARTER, Percy, H. ,  DUNCIA, John, V. ,  MUDRYK, Boguslaw, M. ,  RANDAZZO, Michael, E. ,  XIAO, Zili ,  YANG, Michael, G. ,  ZHAO, Rulin

    IPC分类号： C07D403/12 ,  C07D207/273 ,  A61K31/4025

    CPC分类号： C07D403/12 ,  C07D207/273 ,  C07D317/72

    摘要： The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-(tert-butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((lR,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.