Efforts toward oral bioavailability in factor VIIa inhibitors.
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.
Vijaykumar
Dange
D
Celera, 180 Kimball Way, South San Francisco, CA 94979, USA. dvijayku@hotmail.com
Rai
Roopa
R
Shaghafi
Michael
M
Ton
Tony
T
Torkelson
Steve
S
Leahy
Ellen M
EM
Riggs
Jennifer R
JR
Hu
Huiyong
H
Sprengeler
Paul A
PA
Shrader
William D
WD
O'Bryan
Colin
C
Cabuslay
Ronnell
R
Sanford
Ellen
E
Gjerstadt
Erik
E
Liu
Liang
L
Sukbuntherng
Juthamas
J
Young
Wendy B
WB
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*
D000925:Anticoagulants; D015942:Factor VIIa; D013917:Thrombin