MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMSAND PROCESS

摘要

The present invention provides a novel antagonist or partial agonists/ant agonist 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)cyclohex yl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, the reof, having an unexpected combination of desirable pharmacological characte ristics. Crystalline forms of the present invention are also provided. Pharm aceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, met abolic, cancer and/or cardiovascular diseases is also an objective of this i nvention. The present disclosure also provides a process for preparing compo unds of Formula (I), including N-((lR,2S,5R)-5-(tert-butylamino)-2-((S)-2-ox o-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)ace tamide: wherein R1, R8, R9, R10, and "HET" are as described herein. Compound s that are useful intermediates of the process are also provided herein.