Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.
The selective inhibition of coagulation factor Xa has emerged as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe highly potent benzamidine factor Xa inhibitors based on a vicinally-substituted heterocyclic core.
DuPont Pharmaceuticals Company, Wilmington, DE 19880-0500, USA. john.m.fevig@dupontpharma.com
J M
JM
Fevig
D J
DJ
Pinto
Q
Q
Han
M L
ML
Quan
J R
JR
Pruitt
I C
IC
Jacobson
R A
RA
Galemmo
S
S
Wang
M J
MJ
Orwat
L L
LL
Bostrom
R M
RM
Knabb
P C
PC
Wong
Lam PYS
R R
RR
Wexler
D000818:Animals; D001550:Benzamidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D065427:Factor Xa Inhibitors; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D011817:Rabbits; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001550:Benzamidines; D065427:Factor Xa Inhibitors; D006571:Heterocyclic Compounds; D015842:Serine Proteinase Inhibitors