Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.
We describe the structure-based design and synthesis of highly potent, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the coagulation cascade by selective inhibition of the extrinsic pathway.
Zbinden
Katrin Groebke
KG
F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. katrin.groebke_zbinden@roche.com
Obst-Sander
Ulrike
U
Hilpert
Kurt
K
Kühne
Holger
H
Banner
David W
DW
Böhm
Hans-Joachim
HJ
Stahl
Martin
M
Ackermann
Jean
J
Alig
Leo
L
Weber
Lutz
L
Wessel
Hans Peter
HP
Riederer
Markus A
MA
Tschopp
Thomas B
TB
Lavé
Thierry
T
D000284:Administration, Oral; D000818:Animals; D000925:Anticoagulants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001682:Biological Availability; D018360:Crystallography, X-Ray; D015195:Drug Design; D015942:Factor VIIa / Q000037:antagonists & inhibitors*; D005998:Glycine / Q000031:analogs & derivatives / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013925:Thromboplastin / Q000037:antagonists & inhibitors*
D000925:Anticoagulants; D015842:Serine Proteinase Inhibitors; C008852:2-phenylglycine; D013925:Thromboplastin; D015942:Factor VIIa; D005998:Glycine