CARTER, PERCY H.,CHERNEY, ROBERT J.,ROSSO, VICTOR W.,LI, JUN
申请号:
DK10768153
公开号:
DK2488523T3
申请日:
2010.10.12
申请国别(地区):
DK
年份:
2014
代理人:
摘要:
The present invention provides a novel antagonist: N-((1R,2S,5R)-5-( tert- butylamino)-2-((S)-3-(7- tert -butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclo hexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of kidney diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-( tert -butylamino)-2-((S)-3-(7- tert -butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.