127 articles for thisTarget
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Article Title
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Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.
Bristol-Myers Squibb
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
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
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
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
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.
Bristol-Myers Squibb Research & Development
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
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
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
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
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
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 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
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
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Merck Research Laboratories
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
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
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.
National Human Genome Research Institute
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
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
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
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.
Takeda Pharmaceutical
Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.
Pedagogical University
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
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
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.
Merck Research Laboratories
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Abbott Laboratories
Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.
Wyeth Research
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
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 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
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
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
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
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
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
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
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
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.
RhôNe-Poulenc Rorer
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.
Molecumetics
Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.
Institut FüR Biochemie
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
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
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
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
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.
Eli Lilly
Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.
Abdulaziz University For Health Sciences
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
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
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
3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.
Jilin University