P. Lam

发表

Rational design of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors.

PatrickY.-S. Lam, P. Lam, P. Jadhav, 1994, Science.

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.

Reductive Isoxazole Ring Opening of the Anticoagulant Razaxaban Is the Major Metabolic Clearance Pathway in Rats and Dogs

P. Lam, K. He, R. Knabb, 2008, Drug Metabolism and Disposition.

Discovery of a first-in-class inhibitor of sulfide:quinone oxidoreductase that protects against adverse cardiac remodeling and heart failure.

M. Jackson, P. Lam, B. Polyak, 2021, Cardiovascular research.

Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450.

J L Meek, Chong-Hwan Chang, PatrickY.-S. Lam, 1996, Chemistry & biology.

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

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

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.

Copper(ii)-catalyzed Chan-Lam cross-coupling: chemoselective N-arylation of aminophenols.

P. Lam, P. Bharatam, Chaitanya K Jaladanki, 2017, Organic & biomolecular chemistry.

Copper-catalyzed general CN and CO bond cross-coupling with arylboronic acid

P. Lam, P. Jadhav, G. Vincent, 2001 .

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.

P. Lam, Hong Shen, A. Mathur, 2014, Bioorganic & medicinal chemistry letters.

Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.

P. Lam, Hong Shen, R. Rehfuss, 2014, Journal of medicinal chemistry.

Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.

P. Lam, R. Rehfuss, D. Seiffert, 2013, Bioorganic & medicinal chemistry letters.

2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.

P. Lam, Hong Shen, R. Rehfuss, 2014, Bioorganic & medicinal chemistry letters.

Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.

P. Lam, S. Sheriff, A. Mathur, 2020, Journal of medicinal chemistry.

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

P. Lam, S. Sheriff, D. Seiffert, 2017, Bioorganic & medicinal chemistry letters.

Novel phenylalanine derived diamides as Factor XIa inhibitors.

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

Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.

P. Lam, D. Cheney, K. He, 2007, Bioorganic & medicinal chemistry letters.

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.

Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.

Steven A. Spronk, P. Lam, D. Schnur, 2013, Journal of medicinal chemistry.

Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.

P. Lam, R. Rehfuss, R. Ruel, 2013, Bioorganic & medicinal chemistry letters.

2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.

P. Lam, R. Rehfuss, Christine S. Huang, 2013, Bioorganic & medicinal chemistry letters.

New azole antagonists with high affinity for the P2Y(1) receptor.

P. Lam, R. Rehfuss, R. Ruel, 2013, Bioorganic & medicinal chemistry letters.

Razaxaban, a direct factor Xa inhibitor, in combination with aspirin and/or clopidogrel improves low-dose antithrombotic activity without enhancing bleeding liability in rabbits

P. Lam, R. Knabb, R. Wexler, 2007, Journal of Thrombosis and Thrombolysis.

Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.

P. Lam, J. Macor, E. Liu, 2007, Bioorganic & medicinal chemistry letters.

calculation of the stabilities of the oxetenyl anion and cation

P. Lam, L. E. Friedrich, 1980 .

Advances in Carbon–Element Bond Construction under Chan–Lam Cross-Coupling Conditions: A Second Decade

P. Lam, K. Radhakrishnan, Parthasarathi Das, 2020, Synthesis.

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.

SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.

Chong-Hwan Chang, Daniel L Cheney, Chong-Hwan Chang, 2007, Bioorganic & medicinal chemistry letters.

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

P. Lam, R. Knabb, R. Wexler, 2006, Bioorganic & Medicinal Chemistry Letters.

Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.

P. Lam, K. He, R. Knabb, 2009, Bioorganic & medicinal chemistry letters.

Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.

P. Lam, D. Cheney, K. He, 2008, Bioorganic & medicinal chemistry letters.

Sulfonamidolactam inhibitors of coagulation factor Xa.

P. Lam, R. Knabb, A. Rendina, 2008, Bioorganic & medicinal chemistry letters.

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

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

Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.

P. Lam, R. Knabb, R. Alexander, 2003, 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.

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.

Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.

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

Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.

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

Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.

P. Lam, R. Knabb, R. Wexler, 1997, Bioorganic & medicinal chemistry letters.

Copper-Promoted Carbon-HeteroatomBond Cross-Coupling with Boronic Acids and Derivatives

P. Lam, Jennifer X. Qiao, Patrick Y.S. Lam, 2011 .

New aryl/heteroaryl CN bond cross-coupling reactions via arylboronic acid/cupric acetate arylation

Simon Saubern, P. Lam, A. Combs, 1998 .

Copper-promoted CN bond cross-coupling with phenylstannane

P. Lam, G. Vincent, D. Bonne, 2002 .

α-Nitrogen activating effect in the room temperature copper-promoted N-arylation of heteroarylcarboxamides with phenyl siloxane or p-toluylboronic acid

P. Lam, E. Hauptman, C. Clark, 2001 .

Recent Advances in Chan–Lam Coupling Reaction: Copper‐Promoted C–Heteroatom Bond Cross‐Coupling Reactions with Boronic Acids and Derivatives

P. Lam, Jennifer X. Qiao, 2011 .

Copper-promoted/catalyzed CN and CO bond cross-coupling with vinylboronic acid and its utilities

P. Lam, G. Vincent, D. Bonne, 2003 .

Copper promoted CN and CO bond cross-coupling with phenyl and pyridylboronates

P. Lam, Renhua Li, D. Bonne, 2003 .

Stereoselective synthesis of an analog of podophyllotoxin by an intramolecular Diels-Alder reaction

P. Lam, M. Jung, L. M. Speltz, 1985 .

Solid supported CN cross-coupling reactions

P. Lam, M. Rafalski, A. Combs, 1999 .

Copper-Promoted C−N Bond Cross-Coupling with Hypervalent Aryl Siloxanes and Room-Temperature N-Arylation with Aryl Iodide

P. Lam, Mingyang He, Renhua Li, 2000 .

Chapter 7:Chan–Lam Coupling Reaction: Copper-promoted C–Element Bond Oxidative Coupling Reaction with Boronic Acids

P. Lam, 2016 .

DE NOVO DESIGN, DISCOVERY AND DEVELOPMENT OF CYCLIC UREA HIV PROTEASE INHIBITORS

P. Lam, Patrick Y.S. Lam, G. V. De Lucca, 1998 .

Copper-Promoted Carbon—Heteroatom Bond Cross-Coupling with Boronic Acids and Derivatives

P. Lam, Jennifer X. Qiao, 2011 .

SOLID SUPPORTED ARYL/HETEROARYL C-N CROSS-COUPLING REACTIONS

P. Lam, M. Rafalski, A. Combs, 1999 .

Host-guest complexation-37

Donald J. Cram, P. Lam, D. Cram, 1986 .

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa

P. Lam, S. Sheriff, D. Seiffert, 2020 .

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.

P. Lam, S. Sheriff, D. Seiffert, 2020, Bioorganic & medicinal chemistry letters.

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.

New Aryl/Heteroaryl C—N Bond Cross-Coupling Reactions via Arylboronic Acid/Cupric Acetate Arylation.

Simon Saubern, P. Lam, A. Combs, 1998 .

N-Arylation of α-aminoesters with p-tolylboronic acid promoted by copper(II) acetate

P. Lam, A. Combs, G. Vincent, 2003 .

A transacylase partial mimic

P. Lam, D. Cram, S. Ho, 1986 .

Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.

Chong-Hwan Chang, P. Lam, P. Jadhav, 1996, Journal of medicinal chemistry.

Transformation of anionically activated trifluoromethyl groups to heterocycles under mild aqueous conditions.

P. Lam, R. Wexler, Jianqing Li, 2011, Organic letters.

Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.

P. Lam, R. Knabb, R. Wexler, 2003, Bioorganic & medicinal chemistry letters.

De novo design and discovery of cyclic HIV protease inhibitors capable of displacing the active-site structural water molecule.

PatrickY.-S. Lam, P. Lam, P. Jadhav, 2002 .

Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development.

P. Lam, W. Humphreys, A. Mathur, 2015, The Journal of organic chemistry.

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

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

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

P. Lam, K. He, R. Knabb, 2007, Bioorganic & medicinal chemistry letters.

Preparation of 1‐(4‐Methoxyphenyl)‐1H‐pyrazolo[4,3‐d]pyrimidin‐7(6H)‐ones as Potent, Selective and Bioavailable Inhibitors of Coagulation Factor Xa.

P. Lam, R. Knabb, R. Wexler, 2006 .

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.

In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor

P. Lam, L. Bacheler, M. Otto, 1993, Antimicrobial Agents and Chemotherapy.

Synthesis of (+)-biotin derivatives as HIV-1 protease inhibitors

P. Lam, L. Bacheler, M. Rayner, 1996 .

Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.

J L Meek, P. Lam, P. Jadhav, 1998, Journal of medicinal chemistry.

DMP 323, a nonpeptide cyclic urea inhibitor of human immunodeficiency virus (HIV) protease, specifically and persistently blocks intracellular processing of HIV gag polyprotein

P. Lam, P. Jadhav, Y. Ru, 1994, Antimicrobial Agents and Chemotherapy.

Counteracting HIV-1 protease drug resistance: structural analysis of mutant proteases complexed with XV638 and SD146, cyclic urea amides with broad specificities.

P. Lam, P. Jadhav, C. Chang, 1998, Biochemistry.

Molecular basis of HIV-1 protease drug resistance: structural analysis of mutant proteases complexed with cyclic urea inhibitors.

P. Lam, C. Hodge, C. Chang, 1997, Biochemistry.

Recent Advances in Copper‐Promoted C–Heteroatom Bond Cross‐Coupling Reactions with Boronic Acids and Derivatives

P. Lam, D. M. Chan, 2006 .

Copper-Promoted C—N and C—O Bond Cross-Coupling with Phenyl and Pyridylboronates.

P. Lam, Renhua Li, D. Bonne, 2003 .

Oral delivery of highly lipophilic poorly water-soluble drugs: spray-dried dispersions to improve oral absorption and enable high-dose toxicology studies of a P2Y1 antagonist.

P. Lam, Christine S. Huang, M. Hageman, 2014, Journal of pharmaceutical sciences.

Correction to "Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development".

P. Lam, W. Humphreys, A. Mathur, 2015, Journal of Organic Chemistry.

Copper‐Catalyzed General C—N and C—O Bond Cross‐Coupling with Arylboronic Acid.

P. Lam, P. Jadhav, G. Vincent, 2001 .

Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.

P. Lam, P. Jadhav, Y. Ru, 1998, Journal of medicinal chemistry.

4‐Benzothiazole‐7‐hydroxyindolinyl Diaryl Ureas Are Potent P2Y1 Antagonists with Favorable Pharmacokinetics: Low Clearance and Small Volume of Distribution

Steven A. Spronk, P. Lam, Hong Shen, 2014, ChemMedChem.

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.