PMID

Data

Article Title

Organization

Synthesis of a cyanopeptide-analogue with trypsin activating properties.

Ernst-Moritz-Arndt-University

Evaluation of bisbenzamidines as inhibitors for matriptase-2.

University Of Bonn

Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.

Bristol-Myers Squibb Research & Development

Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.

Southern Research

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

Bristol-Myers Squibb

Active site-directed plasmin inhibitors: Extension on the P2 residue.

Kobe Gakuin University

Novel phenylalanine derived diamides as Factor XIa inhibitors.

Bristol-Myers Squibb

Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.

Aurigene Discovery Technologies

Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors.

Heidelberg University

Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.

Queensland University Of Technology

Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.

Southeast University

Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.

Tokyo University Of Pharmacy And Life Sciences

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

Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.

Rempex Pharmaceuticals

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

Bristol-Myers Squibb R & D

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

Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.

Astellas Pharma

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

Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.

Ecole Polytechnique F�D�Rale De Lausanne Epfl

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

Philipps University Marburg

Simple linear QSAR models based on quantum similarity measures.

Czech Academy Of Sciences

Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.

Berlex Biosciences

Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.

Astrazeneca

Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.

Brown University

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

Central Pharmaceutical Research Institute

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

Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.

Johnson & Johnson Pharmaceutical Research & Development

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 further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).

Gsk

Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.

Berlex Biosciences

Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.

University Of Parma

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£

Protease inhibitors: current status and future prospects.

University Of Queensland

GRID/CPCA: a new computational tool to design selective ligands.

Boehringer Ingelheim Pharma

Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.

Dupont Pharmaceuticals

Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.

Merck Research Laboratories

Tetrahydro-isoquinoline-based factor Xa inhibitors.

Boehringer Mannheim

Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.

Merck Research Laboratories

Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.

Merck Research Laboratories

Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia.

University Of North Carolina

Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.

The Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of potent and selective macrocyclic thrombin inhibitors.

Merck Research Laboratories

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

Corvas International

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.

Dupont Pharmaceuticals

The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.

Novartis Horsham Research Centre

1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.

Nv Organon

Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.

Nv Organon

Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.

Rh£Ne-Poulenc Rorer

Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).

Institute For Drug Research

 

L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor

TBA

 

S1 heterocyclic thrombin inhibitors

TBA

MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.

Merck Research Laboratories

 

Rational design, synthesis, and serine protease inhibitory activity of a novel P₁-argininal derivative featuring a conformationally constrained P₂–P₃ bicyclic lactam moiety

TBA

 

Synthesis and biological activity of P₂–P₄ azapeptidomimetic P₁-argininal and P₁-ketoargininamide derivatives: a novel class of serine protease inhibitors

TBA

 

Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors

TBA

 

Rational design and synthesis of a novel, selective class of thrombin inhibitors: P₁-argininal derivatives incorporating P₃---P₄ quaternary lactam dipeptide surrogates

TBA

 

Biaryl substituted alkylboronate esters as thrombin inhibitors

TBA

 

An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatran

TBA

 

Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates

TBA

 

RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P₁-ARGININOYL HETEROCYCLES

TBA

 

Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors

TBA

 

(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors

TBA

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

9-hydroxyazafluorenes and their use in thrombin inhibitors.

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

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.

Abbott Laboratories

A novel series of potent and selective small molecule inhibitors of the complement component C1s.

3-Dimensional Pharmaceuticals

Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.

The Bristol-Myers Squibb Pharmaceutical Research Institute

N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.

Millennium Pharmaceuticals

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.

Millennium Pharmaceuticals

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.

Millennium Pharmaceuticals

Thrombin inhibitors built on an azaphenylalanine scaffold.

University Of Ljubljana

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.

Millennium Pharmaceuticals

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.

Millennium Pharmaceuticals

Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.

Johnson & Johnson Pharmaceutical Research & Development

Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.

Abbott Laboratories

Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.

The Bristol-Myers Squibb Pharmaceutical Research Institute

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.

Merck Research Laboratories

Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.

Pharmacia

Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.

Boehringer Ingelheim Pharma

Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.

3-Dimensional Pharmaceuticals

3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.

Merck Research Laboratories

Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.

Bristol-Myers Squibb

Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.

Millennium Pharmaceuticals

Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.

Merck Research Laboratories

Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.

University Of Ljubljana

Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.

Senju Pharmaceutical

Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.

Aventis Pharmaceuticals

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.

Merck Research Laboratories

Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.

Bristol-Myers Squibb

Design and synthesis of factor Xa inhibitors and their prodrugs.

Millennium Pharmaceuticals

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

Merck Research Laboratories

Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.

Millennium Pharmaceuticals

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.

Aventis Pharmaceuticals

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.

Aventis Pharmaceuticals

Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.

Millennium Pharmaceuticals

Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.

Millennium Pharmaceuticals

Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.

Pfizer

Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.

Millennium Pharmaceuticals

Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.

Berlex Biosciences

Structure-based design of novel potent nonpeptide thrombin inhibitors.

Boehringer Ingelheim Pharma

Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.

Aventis Pharmaceuticals

Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.

Corvas International

4-amidinobenzylamine-based inhibitors of urokinase.

Universitat Jena

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

Axys Pharmaceuticals

Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.

Cor Therapeutics

Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.

National Cancer Institute-Frederick

Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.

Cor Therapeutics

Optimization of a screening lead for factor VIIa/TF.

Axys Pharmaceuticals

Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.

Axys Pharmaceuticals

Development of potent and selective factor Xa inhibitors.

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

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

Merck

Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.

3-Dimensional Pharmaceuticals

A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays.

Heidelberg University

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.

Qpex Biopharma

The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.

Prosthetics Molecular Design

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

Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.

Biochem Pharma

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

Dupont Pharmaceuticals

1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.

Shionogi

Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.

Pfizer

Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.

Axys Pharmaceuticals

Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.

Axys Pharmaceuticals

Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.

Corvas International

Nonbenzamidine compounds as selective factor Xa inhibitors.

Aventis Pharmaceuticals

The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.

Novartis Horsham Research Centre

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

The University Of Queensland

Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.

The Oxford Centre For Molecular Sciences

Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.

Berlex Biosciences

Trypsin inhibitors for the treatment of pancreatitis.

Novartis Pharma

Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.

Merck Research Laboratories

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

Astrazeneca

Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.

Philipps University Marburg

Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.

Corvas International

Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.

Rhone-Poulenc Rorer

Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.

Warner-Lambert

6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.

University Of Wollongong

Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.

Corvas International

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.

RhôNe-Poulenc Rorer

Novel benzo-fused lactam scaffolds as factor Xa inhibitors.

Corvas International

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.

Warner-Lambert

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.

Warner-Lambert

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

Bristol-Myers Squibb

Structure-activity analysis of peptidic Chlamydia HtrA inhibitors.

University Of Otago

4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.

Brown University

Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.

Dupont Pharmaceuticals

Thrombin inhibitors based on [5,5] trans-fused indane lactams.

Glaxo Wellcome Research And Development

Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.

Dupont Pharmaceuticals

The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.

Novartis Horsham Research Centre

Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.

Dupont Pharmaceuticals

Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.

Corvas International

Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.

Warner-Lambert

Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.

Warner-Lambert

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

China Pharmaceutical University

Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.

Nippon Steel

Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.

Corvas International

Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.

Warner-Lambert

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

Dupont Pharmaceuticals

5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.

Glaxo Wellcome Research And Development

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.

Dupont Pharmaceuticals

Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.

Corvas International

Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.

Molecumetics

C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.

Merck Research Laboratories

Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.

Merck Research Laboratories

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 LB30057, a benzamidrazone-based selective oral thrombin inhibitor.

Biotech Research Institute

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.

Merck Research Laboratories

Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.

Dupont Pharmaceuticals

Potential Anticancer Agents Characterized from Selected Tropical Plants.

The Ohio State University

Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors.

Heidelberg University

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

Bristol-Myers Squibb Pharmaceutical Research Institute

Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.

Merck Research Laboratories

Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.

Merck Research Laboratories

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

Collegeville

Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.

Dupont Pharmaceuticals

Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.

Zeneca Pharmaceuticals

Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.

The University Of Queensland

Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.

Merck Research Laboratories

3-Acyltetramic acids as a novel class of inhibitors for human kallikreins 5 and 7.

Universidade Federal Fluminense

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

Peking University

Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.

Corvas International

Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.

The University Of Queensland

Highly selective tripeptide thrombin inhibitors.

Eli Lilly

Protease inhibitors from Microcystis aeruginosa bloom material collected from the Dalton Reservoir, Israel.

Tel-Aviv University

Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.

Bristol-Myers Squibb Pharmaceutical Research Institute

Aeruginosins from a Microcystis sp. bloom material collected in Varanasi, India.

Tel-Aviv University

Metabolites from Microcystis aeruginosa bloom material collected at a water reservoir near Kibbutz Hafetz Haim, Israel.

Tel-Aviv University

New orally active serine protease inhibitors.

Minase Research Institute

Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin.

Friedrich Miescher-Institut

Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.

Zeneca Pharmaceuticals

HCV-NS3/4A protease inhibitory iridoid glucosides and dimeric foliamenthoic acid derivatives from Anarrhinum orientale.

Cairo University

Effects of flavonoids isolated from scutellariae radix on fibrinolytic system induced by trypsin in human umbilical vein endothelial cells.

Ehime University

Synthesis of fluorescent-labeled aeruginosin derivatives for high-throughput fluorescence correlation spectroscopy assays.

Graduate School Of Science And Engineering

SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.

Harvard University

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

University Of Nottingham

Structure-based drug design of 1,3,6-trisubstituted 1,4-diazepan-7-ones as selective human kallikrein 7 inhibitors.

Asubio Pharma

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

Bristol-Myers Squibb

Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity.

German Cancer Research Center (Dkfz)

6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.

University Of Wollongong

Factor XIa Inhibitors as New Anticoagulants.

Bristol-Myers Squibb

The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.

Hefei University Of Technology

Discovery and structure-activity relationship study of 1,3,6-trisubstituted 1,4-diazepane-7-ones as novel human kallikrein 7 inhibitors.

Asubio Pharma

Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1.

The University Of Queensland

Jizanpeptins, Cyanobacterial Protease Inhibitors from a Symploca sp. Cyanobacterium Collected in the Red Sea.

Oregon State University

New leupeptin analogues: synthesis and inhibition data.

University Of Arkansas

Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.

Emory University

Fragment-based discovery of novel thymidylate synthase leads by NMR screening and group epitope mapping.

University Of Washington

Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.

Bristol-Myers Squibb

Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.

Abbott Laboratories

Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors.

Durham University

5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.

Parke-Davis Pharmaceutical Research