PMID

Data

Article Title

Organization

Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.

Astellas Pharma

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

Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.

Central Pharmaceutical Research Institute

Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.

Lg Life Sciences

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

Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.

Universit£

Tetrahydro-isoquinoline-based factor Xa inhibitors.

Boehringer Mannheim

Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.

Corvas International

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.

Peking University

Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.

Merck Research Laboratories

Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.

Merck

P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.

Eli Lilly

Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.

Merck

Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.

Merck Research Laboratories

Structure-based design of novel potent nonpeptide thrombin inhibitors.

Boehringer Ingelheim Pharma

Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.

Axys Pharmaceuticals

Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.

Axys Pharmaceuticals

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

Dupont Pharmaceuticals

The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.

Roche Discover Welwyn

Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.

Dupont Pharmaceuticals

In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.

3-Dimensional Pharmaceuticals

Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.

Biotech Research Institute

1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.

Northwestern University Medical School

Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.

Collegeville