Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV

…, B Gerhartz, J Trappe, U Hassiepen, A Duttaroy…

Index: Namoto, Kenji; Sirockin, Finton; Ostermann, Nils; Gessier, Francois; Flohr, Stefanie; Sedrani, Richard; Gerhartz, Bernd; Trappe, Joerg; Hassiepen, Ulrich; Duttaroy, Alokesh; Ferreira, Suzie; Sutton, Jon M.; Clark, David E.; Fenton, Garry; Beswick, Mandy; Baeschlin, Daniel K. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 3 p. 731 - 736

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Abstract

Abstract The successful launches of dipeptidyl peptidase IV (DPP IV) inhibitors as oral anti- diabetics warrant and spur the further quest for additional chemical entities in this promising class of therapeutics. Numerous pharmaceutical companies have pursued their proprietary candidates towards the clinic, resulting in a large body of published chemical structures associated with DPP IV. Herein, we report the discovery of a novel chemotype for DPP IV ...