PMID

Data

Article Title

Organization

Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.

Emory University

Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.

Lg Life 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

Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.

Astrazeneca

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

Development of activity-based probes for trypsin-family serine proteases.

Celera Genomics

Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.

Aarhus University

Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.

Zydus Research Centre

Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.

Hokkaido University

A new strategy for the development of highly potent and selective plasmin inhibitors.

Philipps University Marburg

2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.

University Of Louisville

Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.

Takeda Pharmaceutical

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University Of Florida

Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.

Chiba University

Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.

Takeda Pharmaceutical

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Johnson & Johnson Pharmaceutical Research & Development

Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.

Takeda Pharmaceutical

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

Bristol-Myers Squibb Research And Development

Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.

University Of Antwerp

SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.

Bristol-Myers Squibb

Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.

Abbott

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 novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.

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

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: current status and future prospects.

University Of Queensland

Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.

Rh£Ne-Poulenc Rorer

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

Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.

Klinikum Der Friedrich-Schiller-Universit£T Jena

Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.

Abbott Laboratories

Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.

Universit£

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

Novartis Horsham Research Centre

 

Design and synthesis of conformationally constrained arginal thrombin inhibitors

TBA

 

DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORS

TBA

Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).

University Of Antwerp

Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.

Bristol-Myers Squibb

Identification of novel plasmin inhibitors possessing nitrile moiety as warhead.

Hiroshima International University

Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.

Philipps University Marburg

New furin inhibitors based on weakly basic amidinohydrazones.

Philipps University Marburg

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

Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.

University Of Basel

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

Takeda Pharmaceutical

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

Johnson & Johnson Pharmaceutical Research And Development

Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.

Philipps University Marburg

Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).

Berlex Biosciences

Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.

Bristol-Myers Squibb

 

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

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

 

Characterization of LY806303 as a potent and selective inhibitor of thrombin

TBA

Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.

Millennium Pharmaceuticals

Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.

Millennium Pharmaceuticals

Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.

The Medicines Company (Leipzig)

Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.

Daiichi Sankyo

Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.

Curacyte Discovery

Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.

Takeda Pharmaceutical

Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.

University Of ZüRich

Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.

Bristol-Myers Squibb

Selective and dual action orally active inhibitors of thrombin and factor Xa.

Glaxosmithkline

Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.

University Of Antwerp

Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.

Celera Genomics

Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.

Mochida Pharmaceutical

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.

Johnson & Johnson Pharmaceutical Research And Development

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

Bristol-Myers Squibb Pharmaceutical Research Institute

9-hydroxyazafluorenes and their use in thrombin inhibitors.

Merck Research Laboratories

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

Abbott Laboratories

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

Eli Lilly

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.

Pfizer

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

Abbott Laboratories

Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.

University Of Antwerp

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

Millennium Pharmaceuticals

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

Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.

Boehringer Ingelheim Pharma

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

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

Millennium Pharmaceuticals

Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Celera

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Celera

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

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

4-amidinobenzylamine-based inhibitors of urokinase.

Universitat Jena

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.

Pfizer

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.

Pfizer

Design, synthesis, and SAR of amino 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

Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Shionogi

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

Axys Pharmaceuticals

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

3-Dimensional Pharmaceuticals

Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.

Institute Of Molecular And Cell Biology

Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.

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

Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and HT29 cell lines.

Kobe Gakuin University

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

Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.

Corvas International

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

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

3-Amidinophenylalanine-based inhibitors of urokinase.

UniversitäT Jena

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

RhôNe-Poulenc Rorer

Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.

Brown University

Novel benzo-fused lactam scaffolds as factor Xa inhibitors.

Corvas International

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

Brown University

Thrombin inhibitors based on a propargylglycine template.

Biotech Research Institute

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

Corvas International

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

Dupont Pharmaceuticals

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

Corvas International

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

3-Dimensional Pharmaceuticals

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

Bristol-Myers Squibb Pharmaceutical Research Institute

Design of benzamidine-type inhibitors of factor Xa.

Institut FüR Biochemie

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

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

Highly selective tripeptide thrombin inhibitors.

Eli Lilly

Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series.

Bristol-Myers Squibb Pharmaceutical Research Institute

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

Bristol-Myers Squibb Pharmaceutical Research Institute

Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.

Thrombosis Research Institute

Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.

Eli Lilly

Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.

TBA

Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.

University Of Illinois

 

Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles

Hacettepe University

Cloning and characterization of the human galanin GALR2 receptor.

Synaptic Pharmaceutical

Muscarinic receptor binding sites of the M4 subtype in porcine lung parenchyma.

Case Western Reserve University