| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373161 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
We report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl]-3-methoxytetrahydro-2H-pyran-4-amine (19). After evaluation in 28-day toxicology studies, compound 19 (INCB10820/PF-4178903) was selected as a clinical candidate.
Graphical abstractWe report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl]-3-methoxytetrahydro-2H-pyran-4-amine (INCB10820/PF-4178903). After evaluation in 28-day toxicology studies, INCB10820/PF-4178903 was selected as a clinical candidate.Figure optionsDownload full-size imageDownload as PowerPoint slide
