8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a Highly Potent, Selective, Long-acting, and Orally Bioavailable DPP-4 Inhibitor for the Treatment of Type 2 Diabetes

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2007 Dec 7

PMID 18052023

Citations 58

Authors

Matthias Eckhardt

Elke Langkopf

Michael Mark

Moh Tadayyon

Leo Thomas

Herbert Nar

Waldemar Pfrengle

Brian Guth

Ralf Lotz

Peter Sieger

Holger Fuchs

Frank Himmelsbach

Affiliations

Soon will be listed here.

Abstract

A new chemical class of potent DPP-4 inhibitors structurally derived from the xanthine scaffold for the treatment of type 2 diabetes has been discovered and evaluated. Systematic structural variations have led to 1 (BI 1356), a highly potent, selective, long-acting, and orally active DPP-4 inhibitor that shows considerable blood glucose lowering in different animal species. 1 is currently undergoing clinical phase IIb trials and holds the potential for once-daily treatment of type 2 diabetics.

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