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Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors

Bioorganic & medicinal chemistry letters, 2023-05, Vol.88, p.129304, Article 129304

2023

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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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Inhibition of factor XIa as a new approach to anticoagulation

Arteriosclerosis, thrombosis, and vascular biology, 2010-03, Vol.30 (3), p.388

2010

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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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Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (21), p.127474-127474, Article 127474

2020

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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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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 phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (21), p.127495-127495, Article 127495

2020

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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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Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2018-04, Vol.28 (6), p.987-992

2018

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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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Macrocyclic factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2017-09, Vol.27 (17), p.4056-4060

2017

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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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Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency

Bioorganic & medicinal chemistry letters, 2017-08, Vol.27 (16), p.3833-3839

2017

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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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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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Pyridine and pyridinone-based factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2015-02, Vol.25 (4), p.925-930

2015

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Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)‑one as the P2′ Moiety

ACS medicinal chemistry letters, 2015-05, Vol.6 (5), p.590-595

2015

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Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs

Drug metabolism and disposition, 2008-02, Vol.36 (2), p.303

2008

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Design, structure–activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors

Bioorganic & medicinal chemistry, 2007-12, Vol.17 (23), p.6481-6488

2007

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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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Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors

Factor XIa Inhibitors as New Anticoagulants

Inhibition of factor XIa as a new approach to anticoagulation

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

Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors

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

Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors

Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies

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

Pyridazine and pyridazinone 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

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

Macrocyclic factor XIa inhibitors

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

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency

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

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

Novel phenylalanine derived diamides as Factor XIa inhibitors

Pyridine and pyridinone-based factor XIa inhibitors

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)‑one as the P2′ Moiety

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

Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs

Design, structure–activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors

1-[3-Aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-( R)-hydroxy- N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4- c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa

Phenyltriazolinones as potent factor Xa inhibitors

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