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N-((1R,2S,5R)-5-(第三-丁基胺基)-2-((S)-3-(7-第三-丁基吡唑並[1,5-A][1,3,5]三-4-基胺基)-2-氧代吡咯烷-1-基)環己基)乙醯胺,趨化激素受體活性之雙重調節劑,晶形及方法
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
CARTER, PERCY H.,CHERNEY, ROBERT J.,ROSSO, VICTOR W.,LI, JUN
申请号:
HK13101398.1
公开号:
HK1174614B
申请日:
2013.01.31
申请国别(地区):
HK
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.
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