title: Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
abstract: Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit arteriovenous-shunt (AV) thrombosis model.
authors.affiliation: Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543, USA. james.corte@bms.com
authors.forename: James R
authors.initials: JR
authors.lastname: Corte
authors.forename: Tianan
authors.initials: T
authors.lastname: Fang
authors.forename: Donald J P
authors.initials: DJ
authors.lastname: Pinto
authors.forename: Wei
authors.initials: W
authors.lastname: Han
authors.forename: Zilun
authors.initials: Z
authors.lastname: Hu
authors.forename: Xiang-Jun
authors.initials: XJ
authors.lastname: Jiang
authors.forename: Yun-Long
authors.initials: YL
authors.lastname: Li
authors.forename: Jolicia F
authors.initials: JF
authors.lastname: Gauuan
authors.forename: Mark
authors.initials: M
authors.lastname: Hadden
authors.forename: Darren
authors.initials: D
authors.lastname: Orton
authors.forename: Alan R
authors.initials: AR
authors.lastname: Rendina
authors.forename: Joseph M
authors.initials: JM
authors.lastname: Luettgen
authors.forename: Pancras C
authors.initials: PC
authors.lastname: Wong
authors.forename: Kan
authors.initials: K
authors.lastname: He
authors.forename: Paul E
authors.initials: PE
authors.lastname: Morin
authors.forename: Chong-Hwan
authors.initials: CH
authors.lastname: Chang
authors.forename: Daniel L
authors.initials: DL
authors.lastname: Cheney
authors.forename: Robert M
authors.initials: RM
authors.lastname: Knabb
authors.forename: Ruth R
authors.initials: RR
authors.lastname: Wexler
authors.forename: Patrick Y S
authors.initials: PY
authors.lastname: Lam
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000990:Antithrombin III / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D001166:Arteriovenous Shunt, Surgical; D001665:Binding Sites; D001682:Biological Availability; D023421:Models, Animal; D010880:Piperidines / Q000737:chemistry*; D011728:Pyridones / Q000737:chemistry*; D011817:Rabbits; D015842:Serine Proteinase Inhibitors / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship; D013927:Thrombosis / Q000188:drug therapy* / Q000209:etiology; D062367:ortho-Aminobenzoates / Q000737:chemistry*
chemical_list: D010880:Piperidines; D011728:Pyridones; D015842:Serine Proteinase Inhibitors; D062367:ortho-Aminobenzoates; D000990:Antithrombin III; C000219:anthranilamide