J. Luettgen

发表

Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.

C. Dominguez, R. Knabb, P. Stouten, 2000, 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.

Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.

Wen Jiang, R. Knabb, A. Rendina, 2013, Bioorganic & medicinal chemistry letters.

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.

Pyridine and pyridinone-based factor XIa inhibitors.

P. Morin, D. Seiffert, A. Rendina, 2015, Bioorganic & medicinal chemistry letters.

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.

P. Morin, D. Seiffert, A. Rendina, 2014, Journal of medicinal chemistry.

Inhibition of Factor XIa as a New Approach to Anticoagulation

D. Seiffert, J. Luettgen, M. Quan, 2010, Arteriosclerosis, thrombosis, and vascular biology.

Inhibition of Factor Xa Reduces Ischemic Brain Damage After Thromboembolic Stroke in Rats

M. Chopp, G. Feuerstein, R. Knabb, 2003, Stroke.

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.

Inhibitory Effect of Apixaban Compared With Rivaroxaban and Dabigatran on Thrombin Generation Assay

Andrew A. White, P. Wong, J. Luettgen, 2013, Hospital practice.

Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.

D. Cheney, C. Weigelt, R. Wexler, 2015, Bioorganic & medicinal chemistry letters.

Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.

D. Cheney, C. Weigelt, Yan Zou, 2013, Bioorganic & medicinal chemistry letters.

Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro

P. Wong, J. Luettgen, W. Schumacher, 2009, Thrombosis and Haemostasis.

Neutral macrocyclic factor VIIa inhibitors.

Brandon L. Parkhurst, Wen Jiang, D. Cheney, 2017, Bioorganic & medicinal chemistry letters.

Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.

Brandon L. Parkhurst, Wen Jiang, D. Cheney, 2016, ACS medicinal chemistry letters.

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa

D. Seiffert, A. Rendina, M. Harpel, 2015, Journal of Thrombosis and Thrombolysis.

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

S. Sheriff, D. Seiffert, J. Bozarth, 2015, ACS Medicinal Chemistry Letters.

Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.

Wen Jiang, D. Cheney, Yan Zou, 2016, Bioorganic & medicinal chemistry letters.

Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits

K. He, B. Xin, Donglu Zhang, 2009, Journal of Thrombosis and Thrombolysis.

Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.

Jinglan Zhou, R. Knabb, R. Stanton, 2013, Bioorganic & medicinal chemistry letters.

Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.

Brandon L. Parkhurst, Wen Jiang, D. Cheney, 2016, Journal of medicinal chemistry.

Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.

Wen Jiang, D. Cheney, Yan Zou, 2014, ACS medicinal chemistry letters.

First‐in‐human study of milvexian, an oral, direct, small molecule factor XIa inhibitor

M. Cerra, D. Seiffert, J. Luettgen, 2021, Clinical and translational science.

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.

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.

Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.

S. Sheriff, D. Seiffert, J. Bozarth, 2018, Bioorganic & medicinal chemistry letters.

First‐in‐human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS‐962212, a direct, reversible, small molecule factor XIa inhibitor in non‐Japanese and Japanese healthy subjects

C. Russo, D. Seiffert, R. Knabb, 2018, British journal of clinical pharmacology.

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.

Phenyltriazolinones as potent factor Xa inhibitors.

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

BMS-593214, an active site-directed factor VIIa inhibitor: Enzyme kinetics, antithrombotic and antihaemostatic studies

R. Knabb, A. Rendina, B. Xin, 2010, Thrombosis and Haemostasis.

5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.

P. Jadhav, R. Knabb, D. Modi, 2005, Bioorganic & medicinal chemistry letters.

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.

D. Cheney, A. Rendina, R. Wexler, 2015, Journal of medicinal chemistry.

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.

SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.

P. Jadhav, R. Knabb, R. Alexander, 2004, Bioorganic & medicinal chemistry letters.

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.

Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.

D. Cheney, D. Seiffert, A. Rendina, 2017, ACS medicinal chemistry letters.

5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.

P. Jadhav, R. Knabb, D. Modi, 2004, Bioorganic & medicinal chemistry letters.

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.

Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.

A. Mathur, P. Morin, D. Seiffert, 2014, 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.

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.

Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.

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

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.

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.

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.

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.

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

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

Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits

D. Gordon, W. R. Ewing, J. Bozarth, 2021, Journal of thrombosis and haemostasis : JTH.

Antithrombotic Effects of Combined PAR (Protease-Activated Receptor)-4 Antagonism and Factor Xa Inhibition

D. Newby, Simon J. Wilson, M. Meah, 2020, Arteriosclerosis, thrombosis, and vascular biology.

Plasma biomarkers associated with adverse outcomes in patients with calcific aortic stenosis

Jason W. Moore, M. Hyman, J. Maranville, 2021, European journal of heart failure.

Preclinical metabolism and disposition of an orally bioavailable macrocyclic FXIa inhibitor

Y. Shu, W. R. Ewing, J. Luettgen, 2021, Xenobiotica; the fate of foreign compounds in biological systems.

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.

Macrocyclic factor XIa inhibitors.

S. Sheriff, D. Seiffert, J. Bozarth, 2017, 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.

BMS-593214, an active site-directed factor VIIa inhibitor: Enzyme kinetics, antithrombotic and antihaemostatic studies

R. Knabb, A. Rendina, B. Xin, 2017 .

Inhibition of Factor XIa as a New Approach to Anticoagulation

D. Seiffert, J. Luettgen, M. Quan, 2010, Arteriosclerosis, thrombosis, and vascular biology.

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

S. Sheriff, D. Seiffert, J. Bozarth, 2015, ACS medicinal chemistry letters.