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Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits

Journal of thrombosis and haemostasis, 2022-02, Vol.20 (2), p.399-408

2022

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Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor

Journal of thrombosis and thrombolysis, 2011-05, Vol.31 (4), p.478-492

2011

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Calibration and validation of the rabbit model of electrolytic‐mediated arterial thrombosis against the standard‐of‐care anticoagulant apixaban

Pharmacology research & perspectives, 2022-06, Vol.10 (3), p.e00963-n/a

2022

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Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

Journal of medicinal chemistry, 2007-11, Vol.50 (22), p.5339-5356

2007

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Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212)

Journal of medicinal chemistry, 2017-12, Vol.60 (23), p.9703-9723

2017

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Improved efficacy/safety profile of factor XIa inhibitor BMS‐724296 versus factor Xa inhibitor apixaban and thrombin inhibitor dabigatran in cynomolgus monkeys

Research and practice in thrombosis and haemostasis, 2021-05, Vol.5 (4), p.e12524-n/a, Article e12524

2021

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Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro

Thrombosis and haemostasis, 2009-04, Vol.101 (4), p.780

2009

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The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys

Journal of thrombosis and thrombolysis, 2016-04, Vol.41 (3), p.514-521

2016

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In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa

Journal of thrombosis and thrombolysis, 2015-11, Vol.40 (4), p.416-423

2015

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Discovery of 1-(3‘-Aminobenzisoxazol-5‘-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2‘-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor

Journal of medicinal chemistry, 2005-03, Vol.48 (6), p.1729-1744

2005

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Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (8), p.2432-2435

2013

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Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor

European journal of drug metabolism and pharmacokinetics, 2011-09, Vol.36 (3), p.129-139

2011

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Apixaban, a direct factor Xa inhibitor, inhibits tissue-factor induced human platelet aggregation in vitro: comparison with direct inhibitors of factor VIIa, XIa and thrombin

Thrombosis and haemostasis, 2010-08, Vol.104 (2), p.302

2010

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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Journal of medicinal chemistry, 2022-02, Vol.65 (3), p.1770-1785

2022

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Clopidogrel versus prasugrel in rabbits. Effects on thrombosis, haemostasis, platelet function and response variability

Thrombosis and haemostasis, 2009-01, Vol.101 (1), p.108

2009

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Effect of the Direct Factor Xa Inhibitor Apixaban in Rat Models of Thrombosis and Hemostasis

Journal of cardiovascular pharmacology, 2010-06, Vol.55 (6), p.609-616

2010

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Biomarker optimization to track the antithrombotic and hemostatic effects of clopidogrel in rats

The Journal of pharmacology and experimental therapeutics, 2007-07, Vol.322 (1), p.369

2007

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Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors

Journal of medicinal chemistry, 2015-08, Vol.58 (15), p.6225-6236

2015

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Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.955-969

2014

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Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species

Journal of medicinal chemistry, 2020-07, Vol.63 (13), p.7226-7242

2020

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Atropisomer Control in Macrocyclic Factor VIIa Inhibitors

Journal of medicinal chemistry, 2016-04, Vol.59 (8), p.4007-4018

2016

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On the article " Drugs targeting protease-activated receptor-4 improve the anti-thrombotic therapeutic window "

Annals of translational medicine, 2018-02, Vol.6 (3), p.71-71

2018

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New advances in treating thrombotic diseases

Drug discovery today, 2014-09, Vol.19 (9), p.1433-1434

2014

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A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits

Journal of thrombosis and thrombolysis, 2011-08, Vol.32 (2), p.129-137

2011

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Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits

Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor

Calibration and validation of the rabbit model of electrolytic‐mediated arterial thrombosis against the standard‐of‐care anticoagulant apixaban

Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212)

Improved efficacy/safety profile of factor XIa inhibitor BMS‐724296 versus factor Xa inhibitor apixaban and thrombin inhibitor dabigatran in cynomolgus monkeys

Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro

The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa

Discovery of 1-(3‘-Aminobenzisoxazol-5‘-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2‘-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor

Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor

Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor

Apixaban, a direct factor Xa inhibitor, inhibits tissue-factor induced human platelet aggregation in vitro: comparison with direct inhibitors of factor VIIa, XIa and thrombin

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Clopidogrel versus prasugrel in rabbits. Effects on thrombosis, haemostasis, platelet function and response variability

Effect of the Direct Factor Xa Inhibitor Apixaban in Rat Models of Thrombosis and Hemostasis

Biomarker optimization to track the antithrombotic and hemostatic effects of clopidogrel in rats

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors

Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups

Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors

Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species

Atropisomer Control in Macrocyclic Factor VIIa Inhibitors

On the article " Drugs targeting protease-activated receptor-4 improve the anti-thrombotic therapeutic window "

New advances in treating thrombotic diseases

A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits

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