169 articles for thisTarget
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Synthesis of a cyanopeptide-analogue with trypsin activating properties.
Ernst-Moritz-Arndt-University
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
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
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
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
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
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
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
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
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogates
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
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
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
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
Design and synthesis of factor Xa inhibitors and their prodrugs.
Millennium Pharmaceuticals
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, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.
Millennium Pharmaceuticals
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.
Berlex Biosciences
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
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.
Cor Therapeutics
Design and synthesis of glycolic and mandelic 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
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.
3-Dimensional Pharmaceuticals
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.
Prosthetics Molecular Design
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
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.
Novartis Horsham Research Centre
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
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
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
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
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
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
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
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
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
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
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 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
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
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.
Bristol-Myers Squibb Pharmaceutical 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
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.
Harvard University
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1.
The University of Queensland
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
Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
Vertex Pharmaceuticals
Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals
Imidazopyrazine compounds, preparation methods and uses thereof
Dongguan Zhenxing-Beite Medicine Technology
Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
Amide derivatives as lysophosphatidic acid receptor antagonists
Takeda Pharmaceutical
Pyrazolo[3,4-d]pyrimidine compounds, their preparation and use as sigma ligands
Laboratorios Del Dr. Esteve
Design, synthesis and preliminary activity evaluation of novel 3-amino-2-hydroxyl-3-phenylpropanoic acid derivatives as aminopeptidase N/CD13 inhibitors.
Shandong University
Adenosine receptor agonists, partial agonists, and antagonists
The United States of America, As Represented By The Secretary, Department of Health and Human Services
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
Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38.
The Scripps Research Institute
Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist.
University of Occupational and Environmental Health
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
National Institutes of Health