Abstract

Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[ a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin ( 8p), was chosen for clinical development. Its X-ray structure in complex with the enzyme and early efficacy data in animal models of type 2 diabetes are also presented.

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