| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374329 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
We describe the systematic optimization, focused on the improvement of CV-TI, of a series of CCR2 antagonists. This work resulted in the identification of 10 (((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone) which possessed a low projected human dose 35–45 mg BID and a CV-TI = 3800-fold.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert O. Hughes, D.J. Rogier, Rajesh Devraj, Changsheng Zheng, Ganfeng Cao, Hao Feng, Michael Xia, Rajan Anand, Li Xing, Joseph Glenn, Ke Zhang, Maryanne Covington, Philip A. Morton, J. Matthew Hutzler, John W. Davis II, Peggy Scherle, Fred Baribaud,