240 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.
Bristol-Myers Squibb
Synthesis of a cyanopeptide-analogue with trypsin activating properties.
Ernst-Moritz-Arndt-University
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.
Global Blood Therapeutics
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
Active site-directed plasmin inhibitors: Extension on the P2 residue.
Kobe Gakuin University
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.
Aurigene Discovery Technologies
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.
Queensland University of Technology
Inhibitors of melanogenesis in B16 melanoma 4A5 cells from flower buds of Lawsonia inermis (Henna).
Kyoto Pharmaceutical University
Novel type of plasmin inhibitors: providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine.
Hiroshima International University
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Rempex Pharmaceuticals
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Bristol-Myers Squibb
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
Astrazeneca
Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.
TBA
Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin.
Hiroshima International University
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.
Sanofi-Aventis R&D
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
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
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
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.
Novartis Horsham Research Centre
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Rh£Ne-Poulenc Rorer
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
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.
University of Arkansas
Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.
Thrombosis Research Institute
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.
Abbott Laboratories
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.
University of Montreal
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.
Novartis Horsham Research Centre
Synthesis of potent and selective inhibitors of human plasma kallikrein.
The Procter & Gamble
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
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
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
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
Discovery of a Novel Series of Potent, Selective, Orally Available, and Brain-Penetrable C1s Inhibitors for Modulation of the Complement Pathway.
Takeda Pharmaceutical
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Glaxosmithkline
Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Verseon
Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives.
Hefei University of Technology
Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.
University of Nottingham
Engineering the Cyclization Loop of MCoTI-II Generates Targeted Cyclotides that Potently Inhibit Factor XIIa.
The University of Queensland
Discovery and development of plasma kallikrein inhibitors for multiple diseases.
Hefei University of Technology
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
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Kalvista Pharmaceuticals
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Abbott Laboratories
Potent Cyclic Peptide Inhibitors of FXIIa Discovered by mRNA Display with Genetic Code Reprogramming.
The University of Sydney
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Eli Lilly
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
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
A novel series of potent and selective small molecule inhibitors of the complement component C1s.
3-Dimensional Pharmaceuticals
Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE).
TBA
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.
University of Antwerp
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
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
Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation.
Sorbonne Universit£
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
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.
Philipps University
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
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
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
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
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
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
Qpex Biopharma
Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.
Institute of Molecular and Cell Biology
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Shionogi
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
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
Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.
Corvas International
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
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.
Chinese Academy of Sciences
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.
Rhone-Poulenc Rorer
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
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.
Brown University
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.
Novartis Horsham Research Centre
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.
Molecumetics
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.
Corvas International
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.
Corvas International
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.
The University of Queensland
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
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.
Philipps University Marburg
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
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, 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
Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity.
Hiroshima International University
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.
University of Antwerp (Ua)
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.
Aarhus University
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
Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis.
The University of Tokyo
Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica.
The University of Tokyo
Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
TBA
Isolation and structure determination of nostocyclopeptides A1 and A2 from the terrestrial cyanobacterium Nostoc sp. ATCC53789.
University of Hawaii At Manoa
Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.
Abdulaziz University For Health Sciences
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
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
University of Wollongong
Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold.
The University of Queensland
Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.
Virginia Commonwealth University
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Bicycle Therapeutics
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Bristol-Myers Squibb
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
Neutral macrocyclic factor VIIa inhibitors.
Bristol-Myers Squibb Research and Development
4-AMINO-3-(4-PHENOXYPHENYL)-1,3-DIHYDRO-2H-IMIDAZO[4,5-C]PYRIDIN-2-ONE DERIVATIVES AND SALTS THEREOF
Genzyme
OXA- IBOGAINE INSPIRED ANALOGUES FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
Columbia University
Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
Vtv Therapeutics
Pyrazolo[3,4-d]pyrimidine compounds, their preparation and use as sigma ligands
Laboratorios Del Dr. Esteve
Broad-spectrum allosteric inhibition of herpesvirus proteases.
University of California San Francisco
Synthesis and Biological Evaluation of 3-thiazolocoumarinyl Schiff-base Derivatives as Cholinesterase Inhibitors.
Comsats Institute of Information Technology
Cloning of the cDNA and gene for a human D2 dopamine receptor.
Oregon Health Sciences University
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1.
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines.
Wyeth-Ayerst Research