title: Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.
abstract: 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.
authors.affiliation: F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. katrin.groebke_zbinden@roche.com
authors.forename: Katrin Groebke
authors.initials: KG
authors.lastname: Zbinden
authors.forename: Ulrike
authors.initials: U
authors.lastname: Obst-Sander
authors.forename: Kurt
authors.initials: K
authors.lastname: Hilpert
authors.forename: Holger
authors.initials: H
authors.lastname: Kühne
authors.forename: David W
authors.initials: DW
authors.lastname: Banner
authors.forename: Hans-Joachim
authors.initials: HJ
authors.lastname: Böhm
authors.forename: Martin
authors.initials: M
authors.lastname: Stahl
authors.forename: Jean
authors.initials: J
authors.lastname: Ackermann
authors.forename: Leo
authors.initials: L
authors.lastname: Alig
authors.forename: Lutz
authors.initials: L
authors.lastname: Weber
authors.forename: Hans Peter
authors.initials: HP
authors.lastname: Wessel
authors.forename: Markus A
authors.initials: MA
authors.lastname: Riederer
authors.forename: Thomas B
authors.initials: TB
authors.lastname: Tschopp
authors.forename: Thierry
authors.initials: T
authors.lastname: Lavé
mesh_terms: 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*
chemical_list: D000925:Anticoagulants; D015842:Serine Proteinase Inhibitors; C008852:2-phenylglycine; D013925:Thromboplastin; D015942:Factor VIIa; D005998:Glycine