626 articles for thisTarget
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Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Novartis Pharma
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
Novartis Institutes For Biomedical Research
An efficient anticoagulant candidate: Characterization, synthesis and in vivo study of a fondaparinux analogue Rrt1.17.
Nankai University
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
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.
Bristol-Myers Squibb Research and Development
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.
Bristol-Myers Squibb Research & Development
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Bristol-Myers Squibb R & D
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
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Merck Research Laboratories
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.
Aurigene Discovery Technologies
Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Development of a novel class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores.
Bayer Healthcare
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.
Southeast University
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.
Institute For Infection Research
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Rempex Pharmaceuticals
Rapid development of two factor IXa inhibitors from hit to lead.
Merck Research Laboratories
Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.
Shenyang Pharmaceutical University
Identification of anthranilamide derivatives as potential factor Xa inhibitors: drug design, synthesis and biological evaluation.
China Pharmaceutical University
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
Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.
Chang Gung University
Design, synthesis and evaluation of isoxazolo[5,4-d]pyrimidin-4(5H)-one derivatives as antithrombotic agents.
Southeast University
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
A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.
Virginia Commonwealth University
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.
Astellas Pharma
Neutrophil elastase inhibitors as potential anti-inflammatory therapies.
Therachem Research Medilab (India)
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Bristol-Myers Squibb
How aß-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties.
Consiglio Nazionale Delle Ricerche
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
Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy.
Aurigene Discovery Technologies
Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.
Aventis Pharma Deutschland
Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.
Universidad De Buenos Aires
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.
Astrazeneca
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.
Bristol-Myers Squibb R & D
Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.
Aurigene Discovery Technologies
Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.
Universidade De Lisboa
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
Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.
University of Bari &Quot;Aldo Moro&Quot
Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.
Bristol-Myers Squibb 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
Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase.
Universit£
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design.
Asubio Pharma
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores.
University of Ljubljana
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Bristol-Myers Squibb
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.
Bristol-Myers Squibb R & D
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.
University of Ljubljana
Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.
University of Florida
Torsion angle preferences in druglike chemical space: a comprehensive guide.
University of Hamburg
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
Local structural changes, global data views: graphical substructure-activity relationship trailing.
Rheinische Friedrich-Wilhelms-Universita£T
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Celera Genomics
Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase.
Syntex Research
Inhibition of human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin by elasnin and other 4-hydroxy-2-pyrones.
TBA
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.
Berlex Biosciences
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
Aarhus University
Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.
Virginia Commonwealth University
Polysulfated xanthones: multipathway development of a new generation of dual anticoagulant/antiplatelet agents.
Universidade Do Porto (Cequimed-Up)
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
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.
Virginia Commonwealth University
N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.
University of Lisbon
A new strategy for the development of highly potent and selective plasmin inhibitors.
Philipps University Marburg
Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.
Trigen
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
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Merck Research Laboratories
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Bristol-Myers Squibb Research and Development
X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives.
Wichita State University
Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations.
Albert-Ludwigs-University of Freiburg
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
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.
Glaxosmithkline
Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.
Daiichi Sankyo
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.
Takeda Pharmaceutical
Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.
Universidade De Lisboa
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
Cephalon
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bristol-Myers Squibb Research and Development
Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.
Imperial College
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
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.
Daiichi Asubio Medical Research Laboratories
Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.
Central Pharmaceutical Research Institute
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
Berlex Biosciences
Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.
Central Pharmaceutical Research Institute
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
Merck Research Laboratories
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
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.
Pharmacia
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
Development of orally active nonpeptidic inhibitors of human neutrophil elastase.
Cortech
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
GRID/CPCA: a new computational tool to design selective ligands.
Boehringer Ingelheim Pharma
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Rh£Ne-Poulenc Rorer
New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.
Rh£Ne-Poulenc Rorer
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.
Dupont Pharmaceuticals
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
Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.
Zeneca Pharmaceuticals
Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones.
Marion Merrell Dow Research Institute
2,6-Disubstituted aryl carboxylic acids, leaving groups"par excellence" for benzisothiazolone inhibitors of human leukocyte elastase.
Sterling Winthrop Pharmaceutical Research Division
Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.
Georgia Institute of Technology
Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones.
Boehringer Ingelheim Pharmaceuticals
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
Merck Research Laboratories
Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.
Thrombosis Research Institute
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Maxim Pharmaceuticals
Exploring new non-sugar sulfated molecules as activators of antithrombin.
Virginia Commonwealth University
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.
Pharmacia
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.
Life Science R & D, Lgci
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.
Corvas International
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.
Glaxowellcome Medicines Research Centre
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
Glaxowellcome Medicines Research Centre
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.
Dupont Pharmaceuticals
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.
Boehringer Ingelheim 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
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.
Research and Development
Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.
Rh£Ne-Poulenc Rorer
Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.
Palatin Technologies
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.
University of Ljubljana
Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.
Sanofi Pharmaceuticals
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.
Universit£T Bielefeld
Orally active zwitterionic factor Xa inhibitors with long duration of action.
Daiichi Sankyo
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.
Astellas Pharma
HLE-inhibitory alkaloids with a polyketide skeleton from the marine-derived fungus Coniothyrium cereale.
University of Bonn
Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.
Universit£
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.
Philipps University Marburg
Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.
Technical University of Denmark
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors.
Daiichi Sankyo
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.
Glaxosmithkline
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
Boehringer Ingelheim (Canada)
New furin inhibitors based on weakly basic amidinohydrazones.
Philipps University Marburg
2-Azetidinone--a new profile of various pharmacological activities.
Barkatullah University
Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.
Wichita State University
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Merck Research Laboratories
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
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
Endotis Pharma
Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats.
Chang Gung University
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 beta-tryptase and human leukocyte elastase based on the MCoTI-II scaffold.
Imperial College
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
Merck Frosst Canada
Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.
Trigen
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.
Glaxosmithkline
Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa.
Korea Research Institute of Bioscience and Biotechnology
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Philipps University Marburg
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.
National Human Genome Research Institute
4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.
University of Lisbon
Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.
Activx Biosciences
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Bristol-Myers Squibb
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.
F. Hoffmann-La Roche
Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor.
University of Montpellier
Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation.
University of Bari
Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.
TBA
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
Inhibition of human cytomegalovirus protease by benzoxazinones and evidence of antiviral activity in cell culture
TBA
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates
TBA
Synthesis of 7α-methoxy-2-(1,3-dithiolan-2-ylidene)cephem sulphones. A new series of human leukocyte elastase inhibitors
TBA
A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase
TBA
Tricyclic cephems as inhibitors of human leukocyte elastase. thieno[3,4-c]cepham sulfones and pyrrolo[3,4-c]cepham sulfones
TBA
Inhibitors of human leukocyte elastase. 3.1 inhibition by tetrahydrobenzisothiazolinylmethyl aryl carboxylates
TBA
Inhibitors of human leukocyte elastase. 2.1 synthesis and sar of benzisothiazolinylmethyl aryl ethers
TBA
Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase
TBA
Alkoxy substituted benzisothiazolone (BIT) derivatives: potent inhibitors of human leukocyte elastase
TBA
Synthesis and porcine pancreatic elastase inhibitory evaluation of 6α-(sulfonyl)oxy-and 6α-chloropenicillanate sulfone esters and 3α-(acyloxy)methyl-6α-chloropenam sulfones
TBA
1,3-Oxazino[4,5-b]indole-2,4-(1H,9H)-diones and 5,6-dimethylpyrrolo-[2,3-d]-1,3-oxazin-2,4-(1H,7H)-diones as serine protease inhi...
TBA
Synthesis of new thiazinoindole derivatives and their evaluation as inhibitors of human leukocyte elastase and other related serine proteases
TBA
Examination of peptidic α′,β-diamino-α,α-difluoroketones as inhibitors of human leukocyte elastase
TBA
A benzisothiazolone class of potent, selective mechanism-based inhibitors of human leukocyte elastase
TBA
elastase inhibitors containing conformationally restricted lactams as P3-P2 dipeptide replacements
TBA
Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted β-lactam antibiotics
TBA
Inhibition of human leukocyte elastase. 5. Inhibition by 6-alkyl substituted penem benzyl esters.
TBA
Cephem sulfones as inactivators of human leukocyte elastase. II. Keto-enol tautomerish in cephem-4-ketones.
TBA
The effect of N-acyl substituents on the stability of monocyclic β-lactam inhibitors of human leukocyte elastase
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)
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Pfizer
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
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Bristol-Myers Squibb
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.
Curacyte Discovery
3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.
University of Ljubljana
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
University of Leipzig
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors.
Daiichi Sankyo
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.
Chugai Pharmaceutical
Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.
Kissei Pharmaceutical
Synthesis and evaluation of acylguanidine FXa inhibitors.
Bristol-Myers Squibb Research and Development
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Bristol-Myers Squibb
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.
Takeda Pharmaceutical
Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.
University of Ljubljana
Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.
National University of Singapore
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
Johnson & Johnson Pharmaceutical Research and Development
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.
Glaxosmithkline
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.
Pfizer
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.
Daiichi Pharmaceutical
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.
Curacyte Discovery
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Glaxosmithkline
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.
Daiichi Asubio Pharma
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.
Astellas Pharma
Contemporary developments in the discovery of selective factor Xa inhibitors: A review.
The Maharaja Sayajirao University of Baroda
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Gilead Sciences
Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7.
University of Florida
Covalent Small Molecule Immunomodulators Targeting the Protease Active Site.
National Cancer Institute
Synthesis of pyrrolo[3,2-d]pyrimidineone derivatives as novel FXa inhibitors.
Nanjing Zhongrui Pharmaceutical Co.
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.
Astellas Pharma
Discovery and development of plasma kallikrein inhibitors for multiple diseases.
Hefei University of Technology
Recent developments of small molecules with anti-inflammatory activities for the treatment of acute lung injury.
Zhejiang University
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.
University of Antwerp
Advances in research of spirodienone and its derivatives: Biological activities and synthesis methods.
Sichuan University
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
Celera
Chemical synthesis and pharmacological properties of heparin pentasaccharide analogues.
Chinese Academy of Sciences
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.
Mochida Pharmaceutical
Design, synthesis and biological evaluation of P2-modified proline analogues targeting the HtrA serine protease in Chlamydia.
University of Otago
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.
Johnson & Johnson Pharmaceutical Research and Development
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Celera
Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Janssen Research & 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
Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.
Northwest University
Improving the selectivity of 3-amidinophenylalanine-derived matriptase inhibitors.
Philipps University
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
Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands.
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie
Boron-Containing heterocycles as promising pharmacological agents.
Long Island University
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.
Boehringer Ingelheim (Canada)
1,5,6,7-Tetrahydro-4H-indazol-4-ones as human neutrophil elastase (HNE) inhibitors.
University of Florence
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Targeting the S2 Subsite Enables the Structure-Based Discovery of Novel Highly Selective Factor XIa Inhibitors.
Hefei University of Technology
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.
Daiichi Pharmaceutical
Potent Cyclic Peptide Inhibitors of FXIIa Discovered by mRNA Display with Genetic Code Reprogramming.
The University of Sydney
Elastase Inhibitor Cyclotheonellazole A: Total Synthesis and In Vivo Biological Evaluation for Acute Lung Injury.
Nankai University
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.
Aventis Pharma Deutschland
Macrocyclic Inhibitors of HGF-Activating Serine Proteases Overcome Resistance to Receptor Tyrosine Kinase Inhibitors and Block Lung Cancer Progression.
Washington University School of Medicine
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.
University of Ljubljana
A novel series of potent and selective small molecule inhibitors of the complement component C1s.
3-Dimensional Pharmaceuticals
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.
Daiichi Pharmaceutical
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
Optimization of peptide-based inhibitors targeting the HtrA serine protease in Chlamydia: Design, synthesis and biological evaluation of pyridone-based and N-Capping group-modified analogues.
University of Otago
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
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment.
Shenyang Pharmaceutical University
Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations.
Yale University
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.
Pharmacia
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.
Merck
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.
University of Ljubljana
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
Pharmacia
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
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.
Bristol-Myers Squibb
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.
Ajinomoto
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.
3-Dimensional Pharmaceuticals
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.
Aventis Pharma Deutschland
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.
Millennium Pharmaceuticals
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.
Millennium Pharmaceuticals
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
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.
Millennium Pharmaceuticals
Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.
The Oxford Centre For Molecular Sciences and The Dyson Perrins Laboratory
Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.
Mrl Rome
Design and synthesis of factor Xa inhibitors and their prodrugs.
Millennium Pharmaceuticals
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
Currently Naeja Pharmaceutical
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides.
National Institutes of Health (Nih) National Center of Excellence For Computational Drug Abuse Research
P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.
Bristol-Myers Squibb Pharmaceutical Research Institute
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry.
Minase Research Institute
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.
Millennium Pharmaceuticals
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
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Pfizer
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
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.
Philipps University
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
Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors.
Shire Biochem
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.
Protherics Molecular Design
Design and synthesis of peptide-based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase.
Dainippon Pharmaceutical
Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors.
University of Florence
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
Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?
Centre D'Etude Des Pathologies Respiratoires and Universit£
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
Facile Synthesis of Aminomethyl Phosphinate Esters as Serine Protease Inhibitors with Primed Site Interaction.
Ku Leuven
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Merck
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
Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.
Ineti
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-?-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
Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.
Aventis Pharma
Design and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.
Colorado State University
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
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
Shionogi
Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors.
Peking University
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.
Pfizer
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.
Corvas International
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Roche Pharma Research and Early Development
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.
Dupont Pharmaceuticals
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 benzimidazole based factor Xa inhibitors.
Berlex Biosciences
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.
Berlex Biosciences
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
2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.
University of Leipzig
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.
Berlex Biosciences
Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.
3-Dimensional Pharmaceuticals
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.
University of Wollongong
Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence.
Cor Therapeutics
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
Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).
School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.
Glaxowellcome Medicines Research Centre
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.
RhôNe-Poulenc Rorer
Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities.
Peking University
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.
Washington University
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Glaxosmithkline
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.
Fujisawa Pharmaceutical
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
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.
Glaxosmithkline R&D
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.
Berlex Biosciences
Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.
Università
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
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
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.
China Pharmaceutical University
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
Universit£T Bonn
Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.
The University of Queensland
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.
Corvas International
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
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.
Glaxo Wellcome Research and Development
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.
Boehringer Ingelheim (Canada)
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
Boron in drug design: Recent advances in the development of new therapeutic agents.
S£O Paulo State University
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.
Berlex Biosciences
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.
Berlex Biosciences
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.
3-Dimensional Pharmaceuticals
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.
Boehringer Ingelheim (Canada)
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.
Dupont Pharmaceuticals
Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.
Cinc
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
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.
Dupont Pharmaceuticals
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.
Institut Jacques Monod (Umr Cnrs 7592/UniversitéS Paris Vi and Vii)
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
Glaxowellcome Medicines Research Centre
Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues.
Universidade Federal De Pernambuco
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.
Novartis Pharma
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
Berlex Biosciences
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.
Berlex Biosciences
Ahp-Cyclodepsipeptide Inhibitors of Elastase: Lyngbyastatin 7 Stability, Scalable Synthesis, and Focused Library Analysis.
University of Florida
Modulating Heparanase Activity: Tuning Sulfation Pattern and Glycosidic Linkage of Oligosaccharides.
Wayne State University
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.
Boehringer Ingelheim (Canada)
Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones.
Hoechst Marion Roussel
Novel thieno[2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase.
University of Leipzig
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
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Merck Research Laboratories
7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase.
Southern Methodist University
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.
RhôNe-Poulenc Rorer
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.
The University of Queensland
Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.
Institut De Recherche Servier
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
Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25.
Montana State 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
Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.
Corvas International
Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.
The University of Queensland
Nonpeptidic inhibitors of human neutrophil elastase. 7. Design, synthesis, and in vitro activity of a series of pyridopyrimidine trifluoromethyl ketones.
Zeneca Pharmaceuticals
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 orally active, non-peptidic inhibitors of human leukocyte elastase.
Zeneca Pharmaceuticals Group
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.
Daiichi Pharmaceutical
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.
Bristol-Myers Squibb Pharmaceutical Research Institute
Cephem sulfones as inactivators of human leukocyte elastase. 5. 7 alpha-Methoxy- and 7 alpha-chloro-1,1-dioxocephem 4-ketones.
Pharmacia-Farmitalia Carlo Erba
Nonpeptidic inhibitors of human leukocyte elastase. 3. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenylpyridin-2-one trifluoromethyl ketones.
Zeneca Pharmaceuticals Group
Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, synthesis, and in vitro activity of a series of 3-amino-6-arylopyridin-2-one trifluoromethyl ketones.
Zeneca Pharmaceuticals Group
Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors.
Zeneca
Orally bioavailable benzisothiazolone inhibitors of human leukocyte elastase.
Sterling Winthrop
Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones.
Zeneca Pharmaceuticals
Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.
Zeneca Pharmaceuticals
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency.
Zeneca Pharmaceuticals
Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone.
Zeneca Pharmaceuticals
Inhibition of human neutrophil elastase. 3. An orally active enol acetate prodrug.
Marion Merrell Dow Research Institute
Phosphonates and phosphinates: novel leaving groups for benzisothiazolone inhibitors of human leukocyte elastase.
Sterling Winthrop Pharmaceuticals Research Division
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.
Thrombosis Research Institute
Orally active beta-lactam inhibitors of human leukocyte elastase. 3. Stereospecific synthesis and structure-activity relationships for 3,3-dialkylazetidin-2-ones.
Merck Research Laboratories
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.
Zeneca Pharmaceuticals
A novel class of cyclic beta-dicarbonyl leaving groups and their use in the design of benzisothiazolone human leukocyte elastase inhibitors.
Sterling Winthrop Pharmaceuticals Research Division
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.
Eli Lilly
On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients.
Virginia Commonwealth University
Three-dimensional quantitative structure-activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices analysis to elucidate selectivity differences of inhibitors binding to trypsin, thrombin, and factor Xa.
University of Marburg
Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases.
TBA
Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase.
TBA
1H-pyrrolo[2,3-b]pyridine: A new scaffold for human neutrophil elastase (HNE) inhibitors.
University of Florence
Semisynthesis of ent-norstrobane diterpenoids as potential inhibitor for factor Xa.
Guangdong-Macau Traditional Chinese Medicine Technology Industrial Park Development
A BODIPY-Tagged Phosphono Peptide as Activity-Based Probe for Human Leukocyte Elastase.
University of Bonn
Druggability Assessment of Targets Used in Kinetic Target-Guided Synthesis.
University of Groningen
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.
University of Nottingham
Characterizing hydration sites in protein-ligand complexes towards the design of novel ligands.
Sanofi-Aventis Deutschland
(Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase.
Searle Research and Development
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
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.
Hefei University of Technology
Probing the Antiallergic and Anti-inflammatory Activity of Biflavonoids and Dihydroflavonols from Dietes bicolor.
Ain Shams University
Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.
Merck Sharp and Dohme Research Laboratories
Potential Anti-inflammatory Effects of the Fruits of Paulownia tomentosa.
Korea Research Institute of Bioscience and Biotechnology
Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G.
Merrell Dow Research Institute
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
Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors.
China Pharmaceutical 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
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity.
Shenyang Pharmaceutical University
Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.
Boehringer Ingelheim Pharmaceuticals
Neutral macrocyclic factor VIIa inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.
Mochida Pharmaceutical
Synthesis, antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines.
Giresun University
Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.
Bristol-Myers Squibb
Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-ß-lactam inhibitor of human leukocyte elastase.
University of Lisbon
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.
Pfizer
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: exploration of 6-6 fused rings as alternative S1 moieties.
Daiichi Sankyo
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: exploration of 5-6 fused rings as alternative S1 moieties.
Daiichi Sankyo
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Bristol-Myers Squibb
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.
Dainippon Sumitomo Pharma
Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores.
Biocryst Pharmaceuticals
Design, Structure-Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors.
Bristol-Myers Squibb
Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.
Curacyte Chemistry
N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.
Montana State University
Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
University of Namur
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
Bristol-Myers Squibb
Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa.
Bristol-Myers Squibb
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Bristol-Myers Squibb
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.
Gsk
Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors.
Boehringer Ingelheim Pharma
Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa.
Berlex
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.
Berlex
Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors
Berlex Biosciences
Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
Aventis Pharma Deutschland
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Aventis Pharma Deutschland
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
Genentech
Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors.
Pharmacia
Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
Pharmacia
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.
Pharmacia
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
Celera
Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.
Celera
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.
Axys Pharmaceutical
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.
Axys Pharmaceutical
A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.
Axys Pharmaceuticals
Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.
Aventis Pharma Deutschland
Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.
Aventis Pharma Deutschland
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
F. Hoffmann-La Roche
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
F. Hoffmann-La Roche
Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.
F. Hoffmann-La Roche
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.
Rhone-Poulenc Rorer
Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor.
Bayer Healthcare
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.
Daiichi Asubio Medical Research Laboratories
Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.
Bristol-Myers Squibb
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bristol-Myers Squibb
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Bristol-Myers Squibb Pharmaceutical Research Institute
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
Bristol-Myers Squibb
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.
Aventis Pharma
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.
Glaxosmithkline
Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors.
Glaxosmithkline
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.
Glaxosmithkline