The present invention provides a novel antagonist or partial
agonists/antagonist of MCP-1 receptor activity:
N-((1R,2S,5R)-5-tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quina-
zolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, ##STR00001## 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-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-trifluoromethyl)quina-
zolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: ##STR00002##
wherein R.sup.1, R.sup.8,R.sup.9, R.sup.10, and ##STR00003## are as
described herein. Compounds that are useful intermediates of the process
are also provided herein.