PMID

Data

Article Title

Organization

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

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

Wyeth Research

4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.

Wyeth Research

N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.

Nih

Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts.

Universitat De Barcelona