发明名称 USE OF 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, A DUAL MODULATOR OF CHEMOKINE RECEPTORTOR ACTIVITY
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.
申请公布号 ZA201305994(B) 申请公布日期 2014.05.28
申请号 ZA20130005994 申请日期 2013.08.08
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 CARTER PERCY H;ROSSO VICTOR W;CHERNEY ROBERT J;LI JUN
分类号 A61K;A61P;C07D 主分类号 A61K
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