| Structural highlights
Publication Abstract from PubMed
Optimization of a 5-oxopyrrolopyridine series based upon structure-activity relationships (SAR) developed from our previous efforts on a number of related bicyclic series yielded compound 2s (BMS-767778) with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. SAR in the series as well as characterization of 2s are described.
Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors leading to clinical candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).,Devasthale P, Wang Y, Wang W, Fevig JM, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei H, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby M, Hamann LG J Med Chem. 2013 Aug 21. PMID:23964740[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Devasthale P, Wang Y, Wang W, Fevig JM, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei H, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby M, Hamann LG. Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors leading to clinical candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778). J Med Chem. 2013 Aug 21. PMID:23964740 doi:10.1021/jm4008906
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