Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
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.
Shi
Yan
Y
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. yan.shi@bms.com
Zhang
Jing
J
Stein
Philip D
PD
Shi
Mengxiao
M
O'Connor
Stephen P
SP
Bisaha
Sharon N
SN
Li
Chi
C
Atwal
Karnail S
KS
Bisacchi
Gregory S
GS
Sitkoff
Doree
D
Pudzianowski
Andrew T
AT
Liu
Eddie C
EC
Hartl
Karen S
KS
Seiler
Steven M
SM
Youssef
Sonia
S
Steinbacher
Thomas E
TE
Schumacher
William A
WA
Rendina
Alan R
AR
Bozarth
Jeffrey M
JM
Peterson
Tara L
TL
Zhang
Ge
G
Zahler
Robert
R
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
D005030:Ethylenes; D065427:Factor Xa Inhibitors; D007659:Ketones; D007769:Lactams; C008223:ketene