Proceso para la preparacion de n-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo(1,5-a)(1,3,5)triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)acetamida, un modulador dual de la actividad del receptor de quimiocinas. (divisional sol. 924-2012)

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.