3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors

Matthias Eckhardt; Norbert Hauel; Frank Himmelsbach; Elke Langkopf; Herbert Nar; Michael Mark; Moh Tadayyon; Leo Thomas; Brian Guth; Ralf Lotz

doi:10.1016/j.bmcl.2008.04.075

3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3158-62. doi: 10.1016/j.bmcl.2008.04.075. Epub 2008 May 1.

Authors

Matthias Eckhardt¹, Norbert Hauel, Frank Himmelsbach, Elke Langkopf, Herbert Nar, Michael Mark, Moh Tadayyon, Leo Thomas, Brian Guth, Ralf Lotz

Affiliation

¹ Department of Chemical Research, Boehringer Ingelheim Pharma GmbH & Co. KG, 88400 Biberach, Germany. matthias.eckhardt@boehringer-ingelheim.com

PMID: 18485703
DOI: 10.1016/j.bmcl.2008.04.075

Abstract

Systematic variations of the xanthine scaffold in close analogs of development compound BI 1356 led to the class of 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones which provided, after substituent screening, a series of highly potent DPP-4 inhibitors.

MeSH terms

Combinatorial Chemistry Techniques
Dipeptidyl-Peptidase IV Inhibitors*
Humans
Linagliptin
Molecular Structure
Purines / chemical synthesis*
Purines / chemistry
Purines / pharmacology*
Pyridazines / chemical synthesis*
Pyridazines / chemistry
Pyridazines / pharmacology*
Quinazolines / chemical synthesis*
Quinazolines / chemistry
Quinazolines / pharmacology*
Structure-Activity Relationship

Substances

Dipeptidyl-Peptidase IV Inhibitors
Purines
Pyridazines
Quinazolines
Linagliptin