title: Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
abstract: N,N'-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. yan.shi@bms.com
authors.forename: Yan
authors.initials: Y
authors.lastname: Shi
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.forename: Philip D
authors.initials: PD
authors.lastname: Stein
authors.forename: Mengxiao
authors.initials: M
authors.lastname: Shi
authors.forename: Stephen P
authors.initials: SP
authors.lastname: O'Connor
authors.forename: Sharon N
authors.initials: SN
authors.lastname: Bisaha
authors.forename: Chi
authors.initials: C
authors.lastname: Li
authors.forename: Karnail S
authors.initials: KS
authors.lastname: Atwal
authors.forename: Gregory S
authors.initials: GS
authors.lastname: Bisacchi
authors.forename: Doree
authors.initials: D
authors.lastname: Sitkoff
authors.forename: Andrew T
authors.initials: AT
authors.lastname: Pudzianowski
authors.forename: Eddie C
authors.initials: EC
authors.lastname: Liu
authors.forename: Karen S
authors.initials: KS
authors.lastname: Hartl
authors.forename: Steven M
authors.initials: SM
authors.lastname: Seiler
authors.forename: Sonia
authors.initials: S
authors.lastname: Youssef
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Steinbacher
authors.forename: William A
authors.initials: WA
authors.lastname: Schumacher
authors.forename: Alan R
authors.initials: AR
authors.lastname: Rendina
authors.forename: Jeffrey M
authors.initials: JM
authors.lastname: Bozarth
authors.forename: Tara L
authors.initials: TL
authors.lastname: Peterson
authors.forename: Ge
authors.initials: G
authors.lastname: Zhang
authors.forename: Robert
authors.initials: R
authors.lastname: Zahler
mesh_terms: D000284:Administration, Oral; D005030:Ethylenes / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D065427:Factor Xa Inhibitors; D006801:Humans; D007659:Ketones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D007769:Lactams / Q000008:administration & dosage / Q000494:pharmacology*; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
chemical_list: D005030:Ethylenes; D065427:Factor Xa Inhibitors; D007659:Ketones; D007769:Lactams; C008223:ketene