Mitigation of hERG and CYP liabilities in the 5-oxopyrrolopyridine series via exploitation of the solvent-exposed region of the active site of DPP4 yielded BMS-767778 with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. Stucture-Activity relationships in the series as well as characterization of BMS-767778 is described.

Discovery of BMS-767778, a highly potent and selective DPP4 inhibitor for the treatment of diabetes mellitus

246th National Meeting (2013)

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