- BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate
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BMS-813160 (compound 3) was identified as a potent and selective CCR2/5 dual antagonist. Compound 3 displayed good permeability at pH = 7.4 in PAMPA experiments and demonstrated excellent human liver microsome stability. Pharmacokinetic studies established that 3 had excellent oral bioavailability and exhibited low clearance in dog and cyno. Compound 3 was also studied in the mouse thioglycollate-induced peritonitis model, which confirmed its ability to inhibit the migration of inflammatory monocytes and macrophages. As a result of this profile, compound 3 was selected as a clinical candidate.
- Anjanappa, Prakash,Barrish, Joel C.,Batt, Douglas G.,Brown, Gregory D.,Carter, Percy H.,Chen, Jing,Cherney, Robert J.,Cvijic, Mary Ellen,Mandlekar, Sandhya,Mathur, Arvind,Paidi, Venkatram Reddy,Pang, Jian,Rose, Anne V.,Selvakumar, Kumaravel,Tebben, Andrew J.,Vuppugalla, Ragini,Xu, Songmei,Yarde, Melissa,Zhao, Qihong
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supporting information
p. 1753 - 1758
(2021/11/01)
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- 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
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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, there
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Page/Page column 20
(2011/04/25)
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