D. Pinto

发表

Factor Xa inhibitors: next-generation antithrombotic agents.

D. Cheney, R. Knabb, R. Wexler, 2010, Journal of medicinal chemistry.

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

Chong-Hwan Chang, P. Lam, D. Cheney, 2008, Bioorganic & medicinal chemistry letters.

Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.

J. Wityak, S. Mousa, R. Olson, 1997, Journal of medicinal chemistry.

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

R. Copeland, R. Magolda, J. Trzăskos, 1996 .

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

R. Knabb, D. Pinto, Jennifer X. Qiao, 2012, Expert opinion on therapeutic patents.

N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations.

P. Lam, K. He, T. Olah, 2008, Journal of pharmaceutical sciences.

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

S. Sheriff, D. Seiffert, J. Bozarth, 2017, Journal of medicinal chemistry.

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.

P. Lam, K. He, R. Knabb, 2006, Bioorganic & medicinal chemistry letters.

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

P. Lam, K. He, R. Knabb, 2006, Bioorganic & medicinal chemistry letters.

Nonpeptide Factor Xa Inhibitors III: Effects of DPC423, an Orally-Active Pyrazole Antithrombotic Agent, on Arterial Thrombosis in Rabbits

P. Lam, R. Knabb, R. Wexler, 2002, Journal of Pharmacology and Experimental Therapeutics.

A double antibody radioimmunoassay for the determination of XV459, the active hydrolysis metabolite of roxifiban, in human plasma.

H. Pieniaszek, R. Olson, Y. Barrett, 2003, Journal of pharmaceutical and biomedical analysis.

Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists.

W. DeGrado, J. Wityak, S. Mousa, 1997, Journal of medicinal chemistry.

Vinylogous hydroxamic acids: 5-lipoxygenase inhibitors

S. Wright, R. Magolda, D. Pinto, 1992 .

Chapter Nine - Case History: Eliquis™ (Apixaban), a Potent and Selective Inhibitor of Coagulation Factor Xa for the Prevention and Treatment of Thrombotic Diseases

R. Knabb, R. Wexler, D. Pinto, 2012 .

Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.

J. Wityak, S. Mousa, R. Olson, 1997, Journal of medicinal chemistry.

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

Michael A. Galella, S. Sheriff, A. Mathur, 2021, Journal of medicinal chemistry.

Novel phenylalanine derived diamides as Factor XIa inhibitors.

P. Lam, P. Morin, D. Seiffert, 2016, Bioorganic & medicinal chemistry letters.

Comparative effects of selective cyclooxygenase 1 and cyclooxygenase 2 inhibitors on myeloperoxidase and 3 alpha-hydroxysteroid dehydrogenase.

R. Copeland, J. Williams, J. Trzăskos, 1996, Journal of enzyme inhibition.

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

P. Lam, K. He, R. Knabb, 2014, Bioorganic & medicinal chemistry letters.

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

P. Lam, K. He, R. Knabb, 2011, European Journal of Drug Metabolism and Pharmacokinetics.

Phenyltriazolinones as potent factor Xa inhibitors.

K. Kish, S. Sheriff, P. Morin, 2010, Bioorganic & medicinal chemistry letters.

Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.

J. Wityak, P. Anderson, S. Mousa, 1999, Journal of medicinal chemistry.

Nonpeptide factor Xa inhibitors: DPC423, a highly potent and orally bioavailable pyrazole antithrombotic agent.

R. Knabb, D. Pinto, P. Wong, 2006, Cardiovascular drug reviews.

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.

P. Lam, R. Knabb, R. Alexander, 2001, Journal of medicinal chemistry.

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.

P. Lam, R. Knabb, R. Alexander, 2005, Journal of medicinal chemistry.

Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).

P. Lam, R. Knabb, R. Alexander, 2003, Journal of medicinal chemistry.

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.

Angela Smallwood, Stephanie Koch, P. Lam, 2007, Journal of medicinal chemistry.

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

Daniel L Cheney, P. Lam, D. Cheney, 2007, Bioorganic & medicinal chemistry letters.

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

R. Knabb, S. Wang, R. Wexler, 2001, Bioorganic & medicinal chemistry letters.

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

P. Lam, S. Sheriff, A. Mathur, 2017, Journal of medicinal chemistry.

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

D. Pinto, Donglu Zhang, P. Wong, 2011, Journal of Thrombosis and Thrombolysis.

Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies

P. Lam, R. Knabb, B. Xin, 2008, Journal of thrombosis and haemostasis : JTH.

Isoxazolines and isoxazoles as factor Xa inhibitors.

R. Knabb, R. Wexler, D. Pinto, 2000, Bioorganic & Medicinal Chemistry Letters.

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

K. He, R. Knabb, A. Rendina, 2011, Journal of enzyme inhibition and medicinal chemistry.

Metabolism resistant isothiazolone inhibitors of cartilage breakdown.

S. Wright, J. Petraitis, D. Pinto, 1995, Bioorganic & medicinal chemistry.

Synthesis of chiral dibenzo-1,8-diaza-14-crown-4, dibenzo-1,9-diaza-16-crown-4, and dibenzo-1,10-diaza-18-crown-4 ethers by aromatic nucleophilic substitution. Application to the preparation of bicyclic chiral crown-lithium iodide complexes

D. Pinto, M. Welch, R. Kullnig, 1988 .

Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase.

R. Copeland, J. Williams, J. Trzăskos, 1994, Proceedings of the National Academy of Sciences of the United States of America.

A nitrone-based approach to the synthesis of cis-3-amido azetidinones

D. Pinto, J. Tufariello, 1987 .

Synthesis of Chiral Dibenzo-1,8-diaza-14-crown-4, Dibenzo-1,9-diaza-16-crown-4, and Dibenzo-1,10-diaza-18-crown-4 Ethers by Aromatic Nucleophilic Substitution. Application to the Preparation of Bicyclic Chiral Crown-LiI Complexes.

D. Pinto, M. Welch, R. Kullnig, 1988 .

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

P. Lam, S. Sheriff, A. Mathur, 2019, Journal of medicinal chemistry.

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

S. Sheriff, D. Seiffert, A. Rendina, 2016, Bioorganic & medicinal chemistry.

Apixaban Metabolism and Pharmacokinetics after Oral Administration to Humans

W. Humphreys, K. He, C. Frost, 2009, Drug Metabolism and Disposition.

A convenient route to azetidine-2,3-diones and cis-3β-amido azetidinones

D. Pinto, J. Tufariello, A. S. Milowsky, 1987 .

Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis.

S. Wright, R. Collins, D. Pinto, 1992, Journal of medicinal chemistry.

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

P. Lam, K. He, R. Knabb, 2008, Bioorganic & medicinal chemistry letters.

Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.

P. Lam, K. He, R. Knabb, 2003, Journal of medicinal chemistry.

Sulfation of O-Demethyl Apixaban: Enzyme Identification and Species Comparison

Nirmala Raghavan, Donglu Zhang, W Griffith Humphreys, 2009, Drug Metabolism and Disposition.

Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.

R. Copeland, B. Jaffee, W. Pitts, 1998, Bioorganic & medicinal chemistry letters.

Immunosuppressive structure-activity relationships of Brequinar and related cinchoninic acid derivatives

R. Copeland, B. Jaffee, W. Pitts, 1995 .

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

S. Sheriff, P. Morin, D. Seiffert, 2015, Bioorganic & medicinal chemistry letters.

Factor XIa Inhibitors as New Anticoagulants.

D. Seiffert, W. R. Ewing, R. Wexler, 2018, Journal of medicinal chemistry.

Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.

R. Copeland, R. Magolda, J. Trzăskos, 1999, Bioorganic & medicinal chemistry letters.

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

David S Nirschl, P. Lam, S. Sheriff, 2019, Bioorganic & medicinal chemistry letters.

Faculty Opinions recommendation of Adenovirus-associated virus vector-mediated gene transfer in hemophilia B.

D. Pinto, 2011 .

Faculty Opinions recommendation of Direct C-H arylation of electron-deficient heterocycles with arylboronic acids.

D. Pinto, 2010 .

Disposition of 1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'- (methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)- 1H-pyrazole-5-carboxamide (DPC 423) by novel metabolic pathways. Characterization of unusual metabolites by liquid chromatography/mass spectrometry and NMR.

Liang-Shang Gan, A. Mutlib, J. Shockcor, 2002, Chemical research in toxicology.