Invention Grant
US08906920B2 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 receptor activity, crystalline forms and processes
有权
N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-3-（7-叔丁基吡唑并[1,5-A] 吡啶-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺，趋化因子受体活性的双重调节剂，结晶形式和方法
![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 receptor activity, crystalline forms and processes](/docs/US/2014-12-09/US08906920B2/abs.jpg.600x600.jpg)
- Patent Title: 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 receptor activity, crystalline forms and processes
- Patent Title (中): N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-3-（7-叔丁基吡唑并[1,5-A] 吡啶-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺，趋化因子受体活性的双重调节剂，结晶形式和方法
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Application No.: US14091388Application Date: 2013-11-27
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Publication No.: US08906920B2Publication Date: 2014-12-09
- Inventor: Percy H. Carter , Robert J. Cherney
- Applicant: Bristol-Myers Squibb Company
- Applicant Address: US NJ Princeton
- Assignee: Bristol-Myers Squibb Company
- Current Assignee: Bristol-Myers Squibb Company
- Current Assignee Address: US NJ Princeton
- Agent Elliott Korsen
- Main IPC: C07D487/04
- IPC: C07D487/04 ; A61K31/53 ; A61P13/12
![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 receptor activity, crystalline forms and processes](/abs-image/US/2014/12/09/US08906920B2/abs.jpg.150x150.jpg)
Abstract:
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)cyclohexyl)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 inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular 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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