Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
Phillips
G B
GB
Discovery Research, Berlex Biosciences, 15049 San Pablo Avenue, P.O. Box 4099, Richmond, California 94804-0099, USA.
Buckman
B O
BO
Davey
D D
DD
Eagen
K A
KA
Guilford
W J
WJ
Hinchman
J
J
Ho
E
E
Koovakkat
S
S
Liang
A
A
Light
D R
DR
Mohan
R
R
Ng
H P
HP
Post
J M
JM
Shaw
K J
KJ
Smith
D
D
Subramanyam
B
B
Sullivan
M E
ME
Trinh
L
L
Vergona
R
R
Walters
J
J
White
K
K
Whitlow
M
M
Wu
S
S
Xu
W
W
Morrissey
M M
MM
D000284:Administration, Oral; D000578:Amidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D000925:Anticoagulants / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001597:Benzylidene Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001665:Binding Sites; D001682:Biological Availability; D002417:Cattle; D018360:Crystallography, X-Ray; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D065427:Factor Xa Inhibitors; D006801:Humans; D007275:Injections, Intravenous; D008252:Macaca fascicularis; D008958:Models, Molecular; D008968:Molecular Conformation; D010215:Papio; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
D000578:Amidines; D000925:Anticoagulants; D001597:Benzylidene Compounds; D065427:Factor Xa Inhibitors; D011725:Pyridines; D015842:Serine Proteinase Inhibitors; D014361:Trypsin Inhibitors; C114591:ZK 805412; C114592:Fidexaban; D013917:Thrombin