发明授权
EP2046779B1 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
- 专利标题: MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS
- 专利标题(中): 趋化因子受体,晶体形式和过程的调节剂
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申请号: EP07813363.4申请日: 2007-07-26
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公开(公告)号: EP2046779B1公开(公告)日: 2011-05-18
- 发明人: CARTER, Percy, H. , DUNCIA, John, V. , MUDRYK, Boguslaw, M. , RANDAZZO, Michael, E. , XIAO, Zili , YANG, Michael, G. , ZHAO, Rulin
- 申请人: Bristol-Myers Squibb Company
- 申请人地址: Route 206 and Province Line Road P.O. Box 4000 Princeton NJ 08543-4000 US
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 当前专利权人地址: Route 206 and Province Line Road P.O. Box 4000 Princeton NJ 08543-4000 US
- 代理机构: Beacham, Annabel Rose
- 优先权: US834235P 20060728; US896026P 20070321; US782742 20070725
- 国际公布: WO2008014360 20080131
- 主分类号: C07D403/12
- IPC分类号: C07D403/12 ; C07D207/273 ; A61K31/4025
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.
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