We describe the development of the structure-activity relationships in a series of lactam-conjugated tri-substituted cyclohexanes as CCR2 antagonists.  This work culminated in the discovery of BMS-741672 as a potent, selective, and orally bioavailable CCR2 antagonist that was moved into clinical development.

Discovery of BMS-741672, a potent, selective, and orally bioavailable antagonist of CC Chemokine Receptor 2 (CCR2)

245th National Meeting (2013)

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