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

Donald Pinto, Michael J. Orwat, Stephanie C. Koch, +11

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryPrimary AnilinePharmaceutical ScienceBiochemistry +13

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

Donald Pinto, Michael J. Orwat, Shuaige Wang, +15

Journal of Medicinal Chemistry

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

Patrick Y. S. Lam, Charles G. Clark, Renhua Li, +15

Journal of Medicinal Chemistry

Pharmaceutical ScienceOral BioavailabilityPharmacotherapyChemical BiologyNovel Guanidine/benzamidine Mimics +16

Discovery of an Orally Active Series of Isoxazoline Glycoprotein IIb/IIIa Antagonists

Chu‐Biao Xue, John Wityak, Thais M. Sielecki, +26

Journal of Medicinal Chemistry

Pharmaceutical ScienceOrally Active SeriesGlycobiologyPharmacotherapyPharmaceutical Chemistry +15

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

Donald Pinto, Michael J. Orwat, Mimi L. Quan, +19

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryPharmaceutical ScienceMedicineImmunology +9

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

Donald Pinto, Michael J. Orwat, Leon M. Smith, +26

Journal of Medicinal Chemistry

Enantioselective synthesis of the α,α-dimethyl-β-hydroxy

Andrew S. Kende, Kuniaki Kawamura, Michael J. Orwat

Tetrahedron Letters

Organic ChemistryStereoselective SynthesisChemistryAsymmetric CatalysisEnantioselective Synthesis

Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core

John M. Fevig, Donald Pinto, Qi Han, +11

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryHeterocyclicVicinally-substituted Heterocyclic CoreNatural SciencesMedicine +7

Chemistry and pharmacokinetics of diarylthiophenes and terphenyls as selective COX-2 inhibitors

Donald Pinto, Robert A. Copeland, Maryanne Covington, +10

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryEngineeringMedicineSelective Cox-2 InhibitorsPharmacological Agent +9

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

Jeffrey Varnes, Dean A. Wacker, Donald Pinto, +10

Bioorganic & Medicinal Chemistry Letters

Structure–activity RelationshipBiochemistryMedicineMechanism Of ActionPharmacotherapy +5