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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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Factor Xa Inhibitors: Next-Generation Antithrombotic Agents

Journal of medicinal chemistry, 2010-09, Vol.53 (17), p.6243-6274

2010

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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 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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Factor XIa Inhibitors as New Anticoagulants

Journal of medicinal chemistry, 2018-09, Vol.61 (17), p.7425-7447

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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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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Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker

Journal of medicinal chemistry, 2017-02, Vol.60 (3), p.1060-1075

2017

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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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Structure–activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors

Bioorganic & medicinal chemistry, 2008-01, Vol.18 (2), p.749-754

2008

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Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (10), p.2257-2272

2016

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Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties

Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (21), p.5584-5589

2006

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Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties

Bioorganic & medicinal chemistry letters, 2014-08, Vol.24 (15), p.3341-3345

2014

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Structure-Based Design of Novel Guanidine/Benzamidine Mimics: Potent and Orally Bioavailable Factor Xa Inhibitors as Novel Anticoagulants

Journal of medicinal chemistry, 2003-10, Vol.46 (21), p.4405-4418

2003

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Phenyltriazolinones as potent factor Xa inhibitors

Bioorganic & medicinal chemistry letters, 2010-02, Vol.20 (4), p.1373-1377

2010

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Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

Bioorganic & medicinal chemistry letters, 2008-05, Vol.18 (9), p.2845-2849

2008

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Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability

Bioorganic & medicinal chemistry letters, 2019-10, Vol.29 (19), p.126604-126604, Article 126604

2019

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Nonpeptide factor Xa inhibitors III: effects of DPC423, an orally-active pyrazole antithrombotic agent, on arterial thrombosis in rabbits

The Journal of pharmacology and experimental therapeutics, 2002-12, Vol.303 (3), p.993-1000

2002

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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (7), p.1635-1642

2015

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Novel phenylalanine derived diamides as Factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (2), p.472-478

2016

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Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues

Bioorganic & medicinal chemistry letters, 2007-03, Vol.17 (5), p.1432-1437

2007

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Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma

Journal of enzyme inhibition and medicinal chemistry, 2011-08, Vol.26 (4), p.514-526

2011

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The emergence of factor Xa inhibitors for the treatment of cardiovascular diseases: a patent review

Expert opinion on therapeutic patents, 2012-06, Vol.22 (6), p.645-661

2012

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Discovery of 1-[3-(Aminomethyl)phenyl]-N-[3-fluoro-2‘-(methylsulfonyl)- [1,1‘-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a Highly Potent, Selective, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

Journal of medicinal chemistry, 2001-02, Vol.44 (4), p.566-578

2001

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

Factor Xa Inhibitors: Next-Generation Antithrombotic Agents

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

Factor XIa Inhibitors as New Anticoagulants

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

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

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker

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

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

Structure–activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties

Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties

Structure-Based Design of Novel Guanidine/Benzamidine Mimics: Potent and Orally Bioavailable Factor Xa Inhibitors as Novel Anticoagulants

Phenyltriazolinones as potent factor Xa inhibitors

Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability

Nonpeptide factor Xa inhibitors III: effects of DPC423, an orally-active pyrazole antithrombotic agent, on arterial thrombosis in rabbits

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Novel phenylalanine derived diamides as Factor XIa inhibitors

Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues

Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma

The emergence of factor Xa inhibitors for the treatment of cardiovascular diseases: a patent review

Discovery of 1-[3-(Aminomethyl)phenyl]-N-[3-fluoro-2‘-(methylsulfonyl)- [1,1‘-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a Highly Potent, Selective, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

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