3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
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.
Eckhardt
Matthias
M
Department of Chemical Research, Boehringer Ingelheim Pharma GmbH & Co. KG, 88400 Biberach, Germany. matthias.eckhardt@boehringer-ingelheim.com
Hauel
Norbert
N
Himmelsbach
Frank
F
Langkopf
Elke
E
Nar
Herbert
H
Mark
Michael
M
Tadayyon
Moh
M
Thomas
Leo
L
Guth
Brian
B
Lotz
Ralf
R
D020650:Combinatorial Chemistry Techniques; D054873:Dipeptidyl-Peptidase IV Inhibitors; D006801:Humans; D000069476:Linagliptin; D015394:Molecular Structure; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D054873:Dipeptidyl-Peptidase IV Inhibitors; D011687:Purines; D011724:Pyridazines; D011799:Quinazolines; D000069476:Linagliptin