New Orally Active Non-Peptide Fibrinogen Receptor (GpIIb-IIIa) Antagonists:  Identification of Ethyl 3-[N-[4-[4-[Amino[(ethoxycarbonyl)imino]methyl]phenyl]- 1,3-thiazol-2-yl]-N-[1-[(ethoxycarbonyl)methyl]piperid-4-yl]amino]propionate (SR 121787) as a Potent and Long-Acting Antithrombotic Agent

1997 ◽  
Vol 40 (21) ◽  
pp. 3393-3401 ◽  
Author(s):  
Alain Badorc ◽  
Marie-Françoise Bordes ◽  
Paul de Cointet ◽  
Pierre Savi ◽  
André Bernat ◽  
...  
Keyword(s):  
Antithrombotic Agent ◽  
Fibrinogen Receptor ◽  
Long Acting ◽  
Orally Active ◽  
Methyl Phenyl

Non-Peptide Glycoprotein IIb/IIIa Inhibitors. 17. Design and Synthesis of Orally Active, Long-Acting Non-Peptide Fibrinogen Receptor Antagonists

1997 ◽  
Vol 40 (12) ◽  
pp. 1779-1788 ◽  
Author(s):  
Benny C. Askew ◽  
Rodney A. Bednar ◽  
Bohumil Bednar ◽  
David A. Claremon ◽  
Jacquelynn J. Cook ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Design And Synthesis ◽  
Fibrinogen Receptor ◽  
Long Acting ◽  
Orally Active

Comparative Studies of an Orally-active Factor Xa Inhibitor, YM-60828, with other Antithrombotic Agents in a Rat Model of Arterial Thrombosis

1998 ◽  
Vol 79 (02) ◽  
pp. 410-416 ◽  
Author(s):  
Kazuo Sato ◽  
Yumiko Sakai ◽  
Fukushi Hirayama ◽  
Hiroyuki Koshio ◽  
Yuta Taniuchi ◽  
...  
Keyword(s):  
Electrical Stimulation ◽  
Arterial Thrombosis ◽  
Thrombus Formation ◽  
Factor Xa ◽  
Test Drug ◽  
Antithrombotic Agent ◽  
Antithrombotic Activity ◽  
Thrombosis Model ◽  
Treatment And Prevention ◽  
Orally Active

SummaryWe examined the antithrombotic activity of a novel synthetic inhibitor of factor Xa, YM-60828, in an electrically-induced carotid artery thrombosis model in rats. In the first experiment, the antithrombotic activity of YM-60828 after i.v. infusion was compared with those of heparin, darteparin and argatroban. Test drug was administered by i.v. infusion from 30 min before electrical stimulation to the end of the experiment. YM-60828 at 1 mg/kg/h significantly improved patency status, prolonged the time to occlusive thrombus formation and duration of patency. Heparin at 300 U/kg/h also improved these parameters, but were accompanied by a marked increase in systemic coagulation time. In the second experiment, the antithrombotic activity of YM-60828 after oral administration was compared with those of ticlopidine, cilostazol, aspirin, beraprost, ethyl icosapentate and warfarin. Test drug was orally administered to fasted rats 60 min before electrical stimulation. YM-60828 at 30 mg/kg p.o., but not ticlopidine, cilostazol, aspirin, beraprost, ethyl icosapentate or warfarin, significantly reduced the incidence of occlusion and improved carotid arterial patency. These results suggest that YM-60828 may be a promising antithrombotic agent for the treatment and prevention of arterial thrombosis which can be given by oral as well as intravenous administration.

Discovery of an Orally Active and Long‐Acting DPP‐IV Inhibitor through Property‐Based Optimization with an in Silico Biotransformation Prediction Tool

ChemMedChem ◽  
2020 ◽  
Vol 15 (16) ◽  
pp. 1608-1617
Author(s):  
Shaogao Zeng ◽  
Wenyuan Dou ◽  
Manna Li ◽  
Yang Zhou ◽  
Jiehuang Guo ◽  
...  
Keyword(s):  
In Silico ◽  
Prediction Tool ◽  
Dpp Iv ◽  
Long Acting ◽  
Orally Active

Design of a New Class of Orally Active Fibrinogen Receptor Antagonists

1998 ◽  
Vol 41 (14) ◽  
pp. 2492-2502 ◽  
Author(s):  
Scott I. Klein ◽  
Bruce F. Molino ◽  
Mark Czekaj ◽  
Charles J. Gardner ◽  
Valeria Chu ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
New Class ◽  
Fibrinogen Receptor ◽  
Orally Active

Discovery and Preclinical Profile of Saxagliptin (BMS-477118):  A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

2005 ◽  
Vol 48 (15) ◽  
pp. 5025-5037 ◽  
Author(s):  
David J. Augeri ◽  
Jeffrey A. Robl ◽  
David A. Betebenner ◽  
David R. Magnin ◽  
Ashish Khanna ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Long Acting ◽  
Orally Active

Enantiospecific synthesis of SB 214857, a potent, orally active, nonpeptide fibrinogen receptor antagonist

1995 ◽  
Vol 36 (52) ◽  
pp. 9433-9436 ◽  
Author(s):  
William H. Miller ◽  
Thomas W. Ku ◽  
Fadia E. Ali ◽  
William E. Bondinell ◽  
Raul R. Calvo ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Fibrinogen Receptor ◽  
Enantiospecific Synthesis ◽  
Orally Active

ChemInform Abstract: Beta-Amino Acid Derivatives as Orally Active Non-Peptide Fibrinogen Receptor Antagonists.

ChemInform ◽  
2010 ◽  
Vol 28 (29) ◽  
pp. no-no ◽  
Author(s):  
G. KOTTIRSCH ◽  
H.-G. ZERWES ◽  
N. S. COOK ◽  
C. TAPPARELLI
Keyword(s):  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Receptor Antagonists ◽  
Fibrinogen Receptor ◽  
Orally Active
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