Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.
Bruncko
Milan
M
Cancer Research, Global Pharmaceutical R&D, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6101, USA. milan.bruncko@abbott.com
McClellan
William J
WJ
Wendt
Michael D
MD
Sauer
Daryl R
DR
Geyer
Andrew
A
Dalton
Christopher R
CR
Kaminski
Michele A
MA
Weitzberg
Moshe
M
Gong
Jane
J
Dellaria
Joseph F
JF
Mantei
Robert
R
Zhao
Xumiao
X
Nienaber
Vicki L
VL
Stewart
Kent
K
Klinghofer
Vered
V
Bouska
Jennifer
J
Rockway
Todd W
TW
Giranda
Vincent L
VL
D008958:Models, Molecular; D009281:Naphthalenes / Q000737:chemistry / Q000493:pharmacokinetics*; D015849:Plasminogen Inactivators / Q000737:chemistry / Q000493:pharmacokinetics*; D013379:Substrate Specificity; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
D009281:Naphthalenes; D015849:Plasminogen Inactivators; C018609:beta-naphthamidine; D014568:Urokinase-Type Plasminogen Activator