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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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Apixaban metabolism and pharmacokinetics after oral administration to humans

Drug metabolism and disposition, 2009-01, Vol.37 (1), p.74-81

2009

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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.302-310

2010

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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.780-782

2009

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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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Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding

Science translational medicine, 2017-01, Vol.9 (371)

2017

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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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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 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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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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In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure

Circulation. Heart failure, 2021-03, Vol.14 (3), p.e007351-e007351

2021

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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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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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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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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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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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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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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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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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Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity

Journal of medicinal chemistry, 2014-12, Vol.57 (23), p.9915-9932

2014

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Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa–Tissue Factor Complex

Journal of medicinal chemistry, 2016-08, Vol.59 (15), p.7125-7137

2016

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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

Apixaban metabolism and pharmacokinetics after oral administration to humans

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

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

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

Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding

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

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

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

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

In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure

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

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors

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

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

Atropisomer Control in Macrocyclic Factor VIIa Inhibitors

Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors

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

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

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

New advances in treating thrombotic diseases

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

Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity

Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa–Tissue Factor Complex

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