PMID

Data

Article Title

Organization

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

Bristol-Myers Squibb

Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.

Bristol-Myers Squibb R & D

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

Bristol-Myers Squibb R & D

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

Bristol-Myers Squibb

Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.

Merck Research Laboratories

Novel phenylalanine derived diamides as Factor XIa inhibitors.

Bristol-Myers Squibb

Development of a novel tricyclic class of potent and selective FIXa inhibitors.

Merck Research Laboratories

Development of a novel class of potent and selective FIXa inhibitors.

Merck Research Laboratories

Pyridine and pyridinone-based factor XIa inhibitors.

Bristol-Myers Squibb

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.

TBA

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

Bristol-Myers Squibb

Rapid development of two factor IXa inhibitors from hit to lead.

Merck Research Laboratories

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

Bristol-Myers Squibb

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

Bristol-Myers Squibb

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

Bristol-Myers Squibb

Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.

Chinese Academy Of Sciences

Development of new cyclic plasmin inhibitors with excellent potency and selectivity.

Philipps University Marburg

Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.

Celera Genomics

Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.

Virginia Commonwealth University

Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.

Trigen

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

Bristol-Myers Squibb Research And Development

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).

Pharmaceutical Research Institute

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.

Dupont Pharmaceuticals

Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.

F. Hoffmann-La Roche

Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.

Takeda Pharmaceutical

Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.

Trigen

Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.

Chugai Pharmaceutical

Discovery of novel hydroxy pyrazole based factor IXa inhibitor.

Celera Genomics

Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of hydroxy pyrimidine Factor IXa inhibitors.

Merck

Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.

Merck

Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.

Novartis Institutes For Biomedical Research

Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.

The University Of Queensland

Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.

Astrazeneca

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

Bristol-Myers Squibb

Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.

China Pharmaceutical University

Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.

The University Of Queensland

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

Bristol-Myers Squibb

Discovery of novel, potent, isosteviol-based antithrombotic agents.

Peking University

Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.

University Of Nottingham

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

Bristol-Myers Squibb

Precise structures of fucosylated glycosaminoglycan and its oligosaccharides as novel intrinsic factor Xase inhibitors.

Chinese Academy Of Sciences

Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.

Virginia Commonwealth University

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

Bristol-Myers Squibb

Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.

Mochida Pharmaceutical

Synthesis, characterization and biological evaluation of novel chalcone sulfonamide hybrids as potent intestinal alkaline phosphatase inhibitors.

Comsats Institute Of Information Technology

GR127935: a potent and selective 5-HT1D receptor antagonist.

Glaxo Research And Development

5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity.

Wyeth Research

Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.

Abbott Laboratories

Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.

Northern Kentucky University

Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.

Gsk