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

Synthesis applications of cationic aza-Cope rearrangements. 24. The aza-Cope-Mannich approach to Strychnos alkaloids. Short stereocontrolled total syntheses of (.+-.)-dehydrotubifoline and (.+-.)-akuammicine

Steven R. Angle, John M. Fevig, Steven D. Knight, +2

Journal of the American Chemical Society

Cationic Aza-cope RearrangementsEngineeringBiochemistryNatural SciencesAltmetric Attention Score +10

New approach to Strychnos alkaloids. Stereocontrolled total synthesis of (.+-.)-dehydrotubifoline

John M. Fevig, Robert W. Marquis, Larry E. Overman

Journal of the American Chemical Society

Bioorganic ChemistryEngineeringBiochemistryNatural SciencesTotal Synthesis +11

Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa

John M. Fevig, Joseph Cacciola, Joseph Buriak, +7

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceBiochemistryMedicineNatural Sciences +9

An enolate claisen route to c-pyranosides

Steven D. Burke, David M. Armistead, Frank J. Schoenen, +1

Tetrahedron

Enolate Claisen RouteStereoselective SynthesisPharmacologyEnantioselective SynthesisNatural Product Synthesis

Rational design of boropeptide thrombin inhibitors: β,β-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile

John M. Fevig, Joseph Buriak, Joseph Cacciola, +6

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryRational DesignMedicineNatural Sciences +9

Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (<i>Sa</i>)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5<i>H</i>-pyrrolo[3,4-<i>b</i>]pyridin-6(7<i>H</i>)-yl)-<i>N</i>,<i>N</i>-dimethylacetamide (BMS-767778)

Pratik Devasthale, Ying Wang, Wei Wang, +18

Journal of Medicinal Chemistry

Combinatorial ChemistryPharmaceutical ScienceOrganic ChemistryClinical CandidatePharmacotherapy +21

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

Design and synthesis of ring-constrained boropeptide thrombin inhibitors

John M. Fevig, Matthew M. Abelman, David R. Brittelli, +3

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryMedicineNon-peptide LigandPharmacology +2