title: Efforts toward oral bioavailability in factor VIIa inhibitors.
abstract: Efforts toward developing orally bioavailable factor VIIa inhibitors starting from parenteral lead compound 1 are described. SAR resulted in improved physicochemical properties, leading to enhanced oral absorption in rat.
authors.affiliation: Celera, 180 Kimball Way, South San Francisco, CA 94979, USA. dvijayku@hotmail.com
authors.forename: Dange
authors.initials: D
authors.lastname: Vijaykumar
authors.forename: Roopa
authors.initials: R
authors.lastname: Rai
authors.forename: Michael
authors.initials: M
authors.lastname: Shaghafi
authors.forename: Tony
authors.initials: T
authors.lastname: Ton
authors.forename: Steve
authors.initials: S
authors.lastname: Torkelson
authors.forename: Ellen M
authors.initials: EM
authors.lastname: Leahy
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Riggs
authors.forename: Huiyong
authors.initials: H
authors.lastname: Hu
authors.forename: Paul A
authors.initials: PA
authors.lastname: Sprengeler
authors.forename: William D
authors.initials: WD
authors.lastname: Shrader
authors.forename: Colin
authors.initials: C
authors.lastname: O'Bryan
authors.forename: Ronnell
authors.initials: R
authors.lastname: Cabuslay
authors.forename: Ellen
authors.initials: E
authors.lastname: Sanford
authors.forename: Erik
authors.initials: E
authors.lastname: Gjerstadt
authors.forename: Liang
authors.initials: L
authors.lastname: Liu
authors.forename: Juthamas
authors.initials: J
authors.lastname: Sukbuntherng
authors.forename: Wendy B
authors.initials: WB
authors.lastname: Young
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001682:Biological Availability; D015942:Factor VIIa / Q000037:antagonists & inhibitors*; D051381:Rats; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors; D013927:Thrombosis / Q000188:drug therapy*
chemical_list: D000925:Anticoagulants; D015942:Factor VIIa; D013917:Thrombin