Mudryk, Boguslaw M.,Xiao, Zili,Zhao, Rulin,Carter, Percy H.,Duncia, John V.,Yang, Michael G.,Randazzo, Michael E.
申请号：
AU2007279333
公开号：
AU2007279333B2
申请日:
2007.07.26
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
The present invention provides a novel antagonist or partial agonists/antagonistof MCP-I receptor activity: N-((lR,2S,5R)-5-(-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvateor prodrug, thereof, having an unexpected combination of desirable pharmacologicalcharacteristics. Crystalline forms of the present invention are also provided.Pharmaceutical compositions containing the same and methods of using the sameas agents for the treatment of inflammatory diseases, allergic, autoimmune,metabolic, cancer and/or cardiovascular diseases is also an objective of thisinvention. The present disclosure also provides a process for preparing compoundsof Formula (I), including N-((lR,2S,5R)-5-(-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide:wherein R, R, R, R, and "HET"are as described herein. Compounds that are useful intermediates of the processare also provided herein.
