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

Systematic variations of the xanthine scaffold in BI 1356 leading to the potent DPP-4 inhibitor 12-( R) are reported. 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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-06, Vol.18 (11), p.3158-3162
Hauptverfasser:	Eckhardt, Matthias, Hauel, Norbert, Himmelsbach, Frank, Langkopf, Elke, Nar, Herbert, Mark, Michael, Tadayyon, Moh, Thomas, Leo, Guth, Brian, Lotz, Ralf
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Combinatorial Chemistry Techniques Dipeptidyl peptidase 4 Dipeptidyl-Peptidase IV Inhibitors DPP-4 General and cellular metabolism. Vitamins Humans Imidazopyridazinones Linagliptin Medical sciences Molecular Structure Pharmacology. Drug treatments Purines - chemical synthesis Purines - chemistry Purines - pharmacology Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacology Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Structure-Activity Relationship
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Zusammenfassung:	Systematic variations of the xanthine scaffold in BI 1356 leading to the potent DPP-4 inhibitor 12-( R) are reported. 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.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.04.075