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519 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28621538 63 Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.EBI Novartis Pharma AG
28157311 11 Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.EBI Novartis Institutes for BioMedical Research
28012344 9 An efficient anticoagulant candidate: Characterization, synthesis and inávivo study of a fondaparinux analogue Rrt1.17.EBI Nankai University
28085275 53 Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.EBI Bristol-Myers Squibb Company
28197309 40 Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.EBI Global Blood Therapeutics
27994741 48 Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.EBI Bristol-Myers Squibb R&D
27663548 7 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.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
27564532 3 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.EBI Bristol-Myers Squibb Research and Development
27612545 37 Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.EBI Bristol-Myers Squibb Research& Development
27455395 66 Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.EBI Bristol-Myers Squibb R&D
27287367 36 Evaluation of bisbenzamidines as inhibitors for matriptase-2.EBI University of Bonn
27015008 51 Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.EBI Bristol-Myers Squibb Research& Development
26985294 114 Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.EBI Southern Research
27073051 71 Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.EBI Bristol-Myers Squibb Company
26871940 7 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.EBI Merck Research Laboratories
26704266 80 Novel phenylalanine derived diamides as Factor XIa inhibitors.EBI Bristol-Myers Squibb Company
26421993 44 Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.EBI Aurigene Discovery Technologies Limited
26318999 70 Development of a novel tricyclic class of potent and selective FIXa inhibitors.EBI Merck Research Laboratories
25978966 65 Development of a novel class of potent and selective FIXa inhibitors.EBI Merck Research Laboratories
26358162 27 Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores.EBI Bayer HealthCare AG
26114810 8 Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.EBI Southeast University
25592713 37 Pyridine and pyridinone-based factor XIa inhibitors.EBI Bristol-Myers Squibb Company
26151189 56 Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.EBI TBA
26005539 23 Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.EBI Bristol-Myers Squibb
25990761 66 Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.EBI Institute for Infection Research
25782055 9 Discovery of a Cyclic Boronic Acid▀-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.EBI Rempex Pharmaceuticals, Inc.
25937013 40 Rapid development of two factor IXa inhibitors from hit to lead.EBI Merck Research Laboratories
25911624 121 Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.EBI Shenyang Pharmaceutical University
25839438 19 Identification of anthranilamide derivatives as potential factor Xa inhibitors: drug design, synthesis and biological evaluation.EBI China Pharmaceutical University
25881820 62 Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.EBI Bristol-Myers Squibb R&D
25728130 79 Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI Bristol-Myers Squibb Company
25650311 76 Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.EBI Chang Gung University
25559742 6 Design, synthesis and evaluation of isoxazolo[5,4-d]pyrimidin-4(5H)-one derivatives as antithrombotic agents.EBI Southeast University
24951330 25 Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.EBI Bristol-Myers Squibb Company
25523211 18 Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.EBI Astellas Pharma Inc.
25453807 13 A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.EBI Virginia Commonwealth University
25438755 9 Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.EBI Astellas Pharma Inc.
25408826 8 Neutrophil elastase inhibitors as potential anti-inflammatory therapies.EBI Therachem Research Medilab (India) Pvt. Ltd.
25405503 109 Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.EBI Bristol-Myers Squibb
25268757 16 How a▀-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.EBI Consiglio Nazionale delle Ricerche
25179681 81 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.EBI Chinese Academy of Sciences
24794746 168 Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy.EBI Aurigene Discovery Technologies Limited
915907 6 Proteinase inhibitors. I. Inhibitors of elastase.EBI TBA
15125936 61 Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.EBI Aventis Pharma Deutschland GmbH
24556381 4 Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.EBI Universidad de Buenos Aires
24405333 69 Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.EBI Bristol-Myers Squibb Company
24461292 14 Heterocyclic core analogs of a direct thrombin inhibitor.EBI Merck Research Laboratories
24418773 61 Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.EBI AstraZeneca
24900796 42 Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.EBI Bristol-Myers Squibb R&D
24900621 48 Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.EBI Aurigene Discovery Technologies Limited
24224573 31 Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.EBI Universidade de Lisboa
24175584 35 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.EBI Sanofi-Aventis R&D
24135727 7 Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.EBI Emory University School of Medicine
24102612 105 Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.EBI University of Bari "Aldo Moro"
23845220 53 Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.EBI Bristol-Myers Squibb R&D
23927973 41 Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.EBI Bristol-Myers Squibb Research& Development
23899618 9 Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.EBI LG Life Sciences
23844670 52 Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase.EBI Universit£ degli Studi di Firenze
23478148 10 Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
23719288 41 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.EBI Asubio Pharma Co., Ltd
23644213 57 Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores.EBI University of Ljubljana
23602442 28 Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.EBI Bristol-Myers Squibb
23416003 52 Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.EBI Bristol-Myers Squibb R&D
23376251 32 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.EBI University of Ljubljana
23350733 10 Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.EBI University of Florida
23379567 2 Torsion angle preferences in druglike chemical space: a comprehensive guide.EBI University of Hamburg
23294255 114 Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI Philipps University Marburg
21443196 38 Local structural changes, global data views: graphical substructure-activity relationship trailing.EBI Rheinische Friedrich-Wilhelms-Universita£t
16644215 52 Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.EBI Celera Genomics
2299617 174 Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase.EBI Syntex Research
4068006 46 Inhibition of human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin by elasnin and other 4-hydroxy-2-pyrones.EBI TBA
12565961 177 Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.EBI Berlex Biosciences
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
22882079 26 Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.EBI Aarhus University
22788964 2 Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.EBI Virginia Commonwealth University
21732671 4 Polysulfated xanthones: multipathway development of a new generation of dual anticoagulant/antiplatelet agents.EBI Universidade do Porto (CEQUIMED-UP)
23124211 22 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.EBI Zydus Research Centre
22770607 54 Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.EBI Virginia Commonwealth University
22595175 18 N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.EBI University of Lisbon
22276953 63 A new strategy for the development of highly potent and selective plasmin inhibitors.EBI Philipps University Marburg
20503967 138 Factor Xa inhibitors: next-generation antithrombotic agents.EBI Bristol-Myers Squibb Company
20121198 63 Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.EBI Trigen Ltd.
19861238 14 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.EBI Takeda Pharmaceutical Company, Ltd
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
17535802 91 Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.EBI Merck Research Laboratories
18424044 32 Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.EBI Bristol-Myers Squibb Research and Development
18318470 1 X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives.EBI Wichita State University
18078761 2 Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations.EBI Albert-Ludwigs-Universit£t Freiburg
18164204 24 Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.EBI Takeda Pharmaceutical Co., Ltd
18329876 53 Sulfonamidolactam inhibitors of coagulation factor Xa.EBI Bristol-Myers Squibb Company
18053726 364 Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI Johnson& Johnson Pharmaceutical Research& Development
18053714 20 Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.EBI GlaxoSmithKline
18039572 22 Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.EBI Daiichi Sankyo Co., Ltd
18077174 31 Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.EBI Takeda Pharmaceutical Co., Ltd
18290604 1 Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.EBI Universidade de Lisboa
18247547 6 Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.EBI Cephalon, Inc.
18054227 45 Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.EBI Bristol-Myers Squibb Research and Development
17470393 6 Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.EBI Imperial College London
18052026 97 Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.EBI University of Antwerp
17588746 103 SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.EBI Bristol-Myers Squibb Company
16876411 17 Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.EBI Daiichi Asubio Medical Research Laboratories, LLC
16517159 45 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.EBI Abbott GmbH& Co. KG
16078825 8 Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.EBI Schering Plough Research Institute
15887966 58 Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.EBI Central Pharmaceutical Research Institute
15837303 52 Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI Berlex Biosciences
15261287 44 Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.EBI Central Pharmaceutical Research Institute
15163182 47 Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.EBI Merck Research Laboratories
14640539 112 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).EBI Pharmaceutical Research Institute
12954057 113 Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.EBI Pharmacia Corporation
12904065 30 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.EBI LG Life Sciences Ltd.
12190311 37 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).EBI GSK
12036356 234 Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.EBI Berlex Biosciences
11312926 39 Development of orally active nonpeptidic inhibitors of human neutrophil elastase.EBI Cortech, Inc.
11170646 106 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.EBI DuPont Pharmaceuticals Company
10669559 180 Protease inhibitors: current status and future prospects.EBI University of Queensland
10956211 14 GRID/CPCA: a new computational tool to design selective ligands.EBI Boehringer Ingelheim Pharma KG
10479288 141 Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI Rh£ne-Poulenc Rorer
10464012 5 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.EBI Rh£ne-Poulenc Rorer
10425086 83 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.EBI DuPont Pharmaceuticals Company
9836616 92 Tetrahydro-isoquinoline-based factor Xa inhibitors.EBI Boehringer Mannheim GmbH
9357536 47 Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.EBI Merck Research Laboratories
9301673 234 Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.EBI Klinikum der Friedrich-Schiller-Universit£t Jena
9191965 58 Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.EBI ZENECA Pharmaceuticals
7799404 22 Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones.EBI Marion Merrell Dow Research Institute
8064791 18 2,6-Disubstituted aryl carboxylic acids, leaving groups"par excellence" for benzisothiazolone inhibitors of human leukocyte elastase.EBI Sterling Winthrop Pharmaceutical Research Division
1578486 53 Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.EBI School of Chemistry and Biochemistry
1542092 38 Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones.EBI Boehringer Ingelheim Pharmaceuticals
1433188 7 Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.EBI Merck Research Laboratories
1527787 11 Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.EBI Thrombosis Research Institute
15081015 91 Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
14980679 30 Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.EBI Maxim Pharmaceuticals
12639557 7 Exploring new non-sugar sulfated molecules as activators of antithrombin.EBI Virginia Commonwealth University
12824035 39 Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.EBI Pharmacia Corporation
11909707 69 Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.EBI Life Science R&D, LGCI
11858993 60 Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.EBI Corvas International, Inc.
11294386 5 The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.EBI GlaxoWellcome Medicines Research Centre
11206469 14 Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.EBI Glaxo Wellcome Medicines Research Centre
10698459 41 The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.EBI DuPont Pharmaceuticals Company
11055335 27 Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.EBI Boehringer Ingelheim
10915051 43 The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.EBI Novartis Horsham Research Centre
10340604 22 Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.EBI Research and Development
10498204 25 Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.EBI Rh£ne-Poulenc Rorer
10360758 10 Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.EBI Palatin Technologies Inc.
 43 S1 heterocyclic thrombin inhibitorsEBI TBA
22365562 154 Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.EBI University of Ljubljana
22192588 9 Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.EBI Sanofi Pharmaceuticals
22047802 8 The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.EBI Universit£t Bielefeld
22044620 36 Orally active zwitterionic factor Xa inhibitors with long duration of action.EBI Daiichi Sankyo Co., Ltd
22041058 44 Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI Bristol-Myers Squibb Company
21995444 32 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.EBI Astellas Pharma Inc
21923104 12 HLE-inhibitory alkaloids with a polyketide skeleton from the marine-derived fungus Coniothyrium cereale.EBI University of Bonn
21741848 66 Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.EBI Universit£ degli Studi di Firenze
21741839 83 Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.EBI Philipps University Marburg
21641796 30 Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.EBI Technical University of Denmark
21345673 33 Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors.EBI Daiichi Sankyo Co, Ltd
21349711 19 The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.EBI GlaxoSmithKline
21349710 21 Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.EBI GlaxoSmithKline
21316975 23 2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor.EBI Daiichi Sankyo Co., Ltd
20823284 9 Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.EBI Boehringer Ingelheim (Canada) Ltd.
21168329 47 New furin inhibitors based on weakly basic amidinohydrazones.EBI Philipps University Marburg
20970895 4 2-Azetidinone--a new profile of various pharmacological activities.EBI Barkatullah University
20638756 1 Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.EBI Wichita State University
19841155 29 MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.EBI Merck Research Laboratories
20650636 118 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.EBI F. Hoffmann-La Roche Ltd
19805567 3 Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.EBI Endotis Pharma
20417587 14 Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats.EBI Chang Gung University
20355714 26 Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.EBI Takeda Pharmaceutical Company Ltd.
20102150 35 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.EBI Johnson& Johnson Pharmaceutical Research and Development
19772295 5 Potent inhibitors of beta-tryptase and human leukocyte elastase based on the MCoTI-II scaffold.EBI Imperial College London SW7 2AZ
19665376 48 Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.EBI Merck Frosst Canada& Co.
20121197 148 Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.EBI Trigen Ltd.
20100660 28 Phenyltriazolinones as potent factor Xa inhibitors.EBI Bristol-Myers Squibb
20006499 24 Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.EBI GlaxoSmithKline
20004577 6 Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa.EBI Korea Research Institute of Bioscience and Biotechnology
20038105 50 Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.EBI Philipps University Marburg
19908842 84 Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.EBI National Human Genome Research Institute
19904934 31 4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.EBI University of Lisbon
19577470 49 Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.EBI ActivX Biosciences, Inc
19541481 57 Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI Bristol-Myers Squibb Company
19200624 32 Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.EBI F Hoffmann - La Roche Ltd
19181521 69 Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor.EBI Universit£ Montpellier 1
19193009 25 Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation.EBI University of Bari
3550086 31 Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.EBI TBA
 15 Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moietyEBI TBA
 37 Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI TBA
 32 Bisbenzamidine isoxazoline derivatives as factor Xa inhibitorsEBI TBA
 27 Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogatesEBI TBA
 24 Inhibition of human cytomegalovirus protease by benzoxazinones and evidence of antiviral activity in cell cultureEBI TBA
 25 Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogatesEBI TBA
 5 Synthesis of 7α-methoxy-2-(1,3-dithiolan-2-ylidene)cephem sulphones. A new series of human leukocyte elastase inhibitorsEBI TBA
 45 A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastaseEBI TBA
 8 Tricyclic cephems as inhibitors of human leukocyte elastase. thieno[3,4-c]cepham sulfones and pyrrolo[3,4-c]cepham sulfonesEBI TBA
 7 Tricyclic cephems as inhibitors of human leukocyte elastase. Furo[3,4-c]cepham sulfonesEBI TBA
 55 The design of potent and stable benzisothiazolone inhibitors of human leukocyte elastaseEBI TBA
 18 Inhibitors of human leukocyte elastase. 3.1 inhibition by tetrahydrobenzisothiazolinylmethyl aryl carboxylatesEBI TBA
 14 Inhibitors of human leukocyte elastase. 2.1 synthesis and sar of benzisothiazolinylmethyl aryl ethersEBI TBA
 1 Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastaseEBI TBA
 12 Alkoxy substituted benzisothiazolone (BIT) derivatives: potent inhibitors of human leukocyte elastaseEBI TBA
 27 Synthesis and porcine pancreatic elastase inhibitory evaluation of 6α-(sulfonyl)oxy-and 6α-chloropenicillanate sulfone esters and 3α-(acyloxy)methyl-6α-chloropenam sulfonesEBI TBA
 46 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...EBI TBA
 2 Synthesis of new thiazinoindole derivatives and their evaluation as inhibitors of human leukocyte elastase and other related serine proteasesEBI TBA
 18 Examination of peptidic α′,β-diamino-α,α-difluoroketones as inhibitors of human leukocyte elastaseEBI TBA
 19 A benzisothiazolone class of potent, selective mechanism-based inhibitors of human leukocyte elastaseEBI TBA
 4 elastase inhibitors containing conformationally restricted lactams as P3-P2 dipeptide replacementsEBI TBA
 7 Janus compounds: dual inhibitors of proteinasesEBI TBA
 30 Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted β-lactam antibioticsEBI TBA
 6 Inhibition of human leukocyte elastase. 7. Inhibition by 6-substituted penicillin amides.EBI TBA
 32 Inhibition of human leukocyte elastase. 6. Inhibition by 6-substituted penicillin esters.EBI TBA
 18 Inhibition of human leukocyte elastase. 5. Inhibition by 6-alkyl substituted penem benzyl esters.EBI TBA
 17 Inhibition of human leukocyte elastase (HLE) by novel bicyclic β-lactamsEBI TBA
 13 Cephem sulfones as inactivators of human leukocyte elastase. II. Keto-enol tautomerish in cephem-4-ketones.EBI TBA
 13 Characterization of LY806303 as a potent and selective inhibitor of thrombinEBI TBA
 2 The effect of N-acyl substituents on the stability of monocyclic β-lactam inhibitors of human leukocyte elastaseEBI TBA
 1 Potential mechanism-based inhibitors of proteolytic enzymesEBI TBA
 6 Synthesis of a peptidyl 2,2-difluoro-3-aminopropionateEBI TBA
 1 A general synthesis of 4-alkyl/aryl substituted saccharinsEBI TBA
19297158 30 Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.EBI Millennium Pharmaceuticals, Inc
19297154 88 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.EBI Millennium Pharmaceuticals, Inc
19250826 100 Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.EBI The Medicines Company (Leipzig) GmbH
19231206 20 Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.EBI Pfizer Global Research and Development
19128974 28 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.EBI Daiichi Sankyo Co., Ltd.
19046881 61 Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.EBI Bristol-Myers Squibb Company
19036586 128 Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.EBI Curacyte Discovery GmbH
18729445 70 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.EBI University of Ljubljana
18701300 55 Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.EBI University of Leipzig
18675545 9 Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors.EBI Daiichi Sankyo Co., Ltd.
18674905 58 Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.EBI Chugai Pharmaceutical Co., Ltd
18667303 27 Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.EBI Kissei Pharmaceutical Co., Ltd
18644722 36 Synthesis and evaluation of acylguanidine FXa inhibitors.EBI Bristol-Myers Squibb Research and Development
18550370 33 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.EBI Bristol-Myers Squibb Company
18507371 24 Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.EBI Takeda Pharmaceutical Co., Ltd.
18412326 16 Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.EBI University of Ljubljana
9834152 29 Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.EBI National University of Singapore
18159923 24 7-fluoroindazoles as potent and selective inhibitors of factor Xa.EBI Johnson & Johnson Pharmaceutical Research and Development
18054228 23 Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.EBI GlaxoSmithKline
17933529 35 Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17855089 25 Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17643988 92 Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.EBI Bristol-Myers Squibb Company
17583500 31 Aminopyrrolidineamide inhibitors of site-1 protease.EBI Pfizer Global Research and Development-Groton Laboratories
17566736 60 Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.EBI Pfizer Global Research and Development
17555959 27 Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.EBI Daiichi Pharmaceutical Co., Ltd
17462889 110 From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.EBI Curacyte Discovery GmbH
17420122 18 Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI GlaxoSmithKline
17419055 30 Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.EBI Daiichi Asubio Pharma Co., Ltd
17416533 39 Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.EBI Astellas Pharma Inc.
17145787 8 Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.EBI Gilead Sciences, Inc.
17064913 29 Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.EBI Astellas Pharma Inc.
16970403 74 Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.EBI University of Antwerp
16793264 13 Potent 4-amino-5-azaindole factor VIIa inhibitors.EBI Celera Genomics
16714109 40 Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.EBI Celera
16540315 23 Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.EBI Mochida Pharmaceutical Co., Ltd
16460935 39 A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.EBI Johnson & Johnson Pharmaceutical Research and Development
16257204 37 Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.EBI Celera
16213711 37 Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16137886 88 Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.EBI Merck Research Laboratories
16125385 55 The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.EBI Pfizer Global Research and Development
15588093 3 A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.EBI Boehringer Ingelheim (Canada) Ltd.
15501047 75 Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI Merck KGaA
15456260 21 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.EBI Daiichi Pharmaceutical Co. Ltd
15203158 84 Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI Merck KGaA
15203149 72 Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.EBI Aventis Pharma Deutschland GmbH
15149685 55 Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.EBI University of Ljubljana
15149641 44 A novel series of potent and selective small molecule inhibitors of the complement component C1s.EBI 3-Dimensional Pharmaceuticals Inc
15125963 20 Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.EBI Daiichi Pharmaceutical Co. Ltd
15115382 16 Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.EBI University of Antwerp
15081014 35 Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
15080981 72 N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
15013007 319 Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.EBI Millennium Pharmaceuticals, Inc.
15013006 69 Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.EBI Millennium Pharmaceuticals, Inc.
15006404 56 Thrombin inhibitors built on an azaphenylalanine scaffold.EBI University of Ljubljana
14980671 78 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.EBI Millennium Pharmaceuticals Inc.
14980670 107 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.EBI Millennium Pharmaceuticals Inc.
14698147 60 Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
14667222 74 Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations.EBI Yale University
14552766 12 Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.EBI Pharmacia Corporation
14552764 5 A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.EBI Merck KGaA
12951087 23 Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.EBI University of Ljubljana
12824026 14 Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.EBI Pharmacia Corporation
12824021 39 Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.EBI Boehringer Ingelheim Pharma KG
12824020 31 Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI Boehringer Ingelheim Pharma KG
12729667 47 Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.EBI Bristol-Myers Squibb Co.
12723948 30 Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.EBI Ajinomoto Company Inc.
12668020 29 Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals, Inc.
12668013 42 Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.EBI Aventis Pharma Deutschland GmbH
12643903 81 Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.EBI Bristol-Myers Squibb Co.
12639568 52 Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.EBI Millennium Pharmaceuticals Inc.
12639567 135 Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI Millennium Pharmaceuticals Inc.
12617892 43 Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.EBI University of Ljubljana
12593666 30 Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI Senju Pharmaceutical Co.
12593648 53 Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.EBI Aventis Pharmaceuticals
12565972 69 Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
12565935 5 Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.EBI The Oxford Centre for Molecular Sciences and The Dyson Perrins Laboratory
12565931 37 Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.EBI Bristol-Myers Squibb Co.
12540231 39 Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.EBI MRL Rome
12482444 38 Design and synthesis of factor Xa inhibitors and their prodrugs.EBI Millennium Pharmaceuticals, Inc.
12467634 67 3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.EBI currently NAEJA Pharmaceutical Inc.
12372533 69 P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12372529 21 Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12161131 1 Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry.EBI Minase Research Institute
12113838 36 Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.EBI Millennium Pharmaceuticals, Inc.
12113833 183 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI Celera
12113832 120 2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI Celera
12039587 39 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.EBI Aventis Pharmaceuticals
12039586 42 Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.EBI Aventis Pharmaceuticals
12039584 59 Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
12039583 140 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.EBI Millennium Pharmaceuticals, Inc.
12036353 38 Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.EBI Pfizer Global Research and Development
12031331 48 Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
11965378 78 Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.EBI Berlex Biosciences
11965377 66 Design and synthesis of aminophenol-based factor Xa inhibitors.EBI Berlex Biosciences
11960487 30 Structure-based design of novel potent nonpeptide thrombin inhibitors.EBI Boehringer Ingelheim Pharma KG
11958994 31 Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.EBI Aventis Pharmaceuticals
11934589 57 Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.EBI Corvas International, Inc.
11934583 20 Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors.EBI Shire BioChem.
11881991 21 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.EBI Protherics Molecular Design
11844691 107 4-amidinobenzylamine-based inhibitors of urokinase.EBI Universitat Jena
11844670 27 Design and synthesis of peptide-based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase.EBI Dainippon Pharmaceutical Co., Ltd.
11689072 49 Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.EBI Axys Pharmaceuticals Inc.
11677132 65 Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.EBI COR Therapeutics, Inc.
11527714 66 Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.EBI COR Therapeutics, Inc.
11527709 19 Optimization of a screening lead for factor VIIa/TF.EBI Axys Pharmaceuticals, Inc.
11495587 198 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.EBI Axys Pharmaceuticals Inc.
11459634 94 Development of potent and selective factor Xa inhibitors.EBI Axys Pharmaceuticals, Inc.
11425539 23 Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI Shionogi & Co., Ltd.
11327591 1 Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.EBI INETI
11266180 74 The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.EBI Prosthetics Molecular Design
11266160 57 Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.EBI DuPont Pharmaceuticals Company
11212109 14 The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.EBI Roche Discover Welwyn
11206465 13 Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.EBI Aventis Pharma
11150162 15 Design and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.EBI Colorado State University
11087565 86 Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.EBI DuPont Pharmaceuticals Company
11078188 20 1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.EBI Shionogi & Co., Ltd
11078187 36 Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI Shionogi & Co., Ltd
11063603 53 Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.EBI Pfizer Global Research and Development
11055344 37 Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.EBI Corvas International, Inc.
10937736 35 Nonbenzamidine compounds as selective factor Xa inhibitors.EBI Aventis Pharmaceuticals
10866393 24 Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.EBI DuPont Pharmaceuticals Company
10866385 13 Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.EBI The Oxford Centre for Molecular Sciences
10853669 102 Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI Berlex Biosciences
10853668 52 Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.EBI Berlex Biosciences
10782677 73 Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI Corvas International, Inc.
10782664 42 Isoxazolines and isoxazoles as factor Xa inhibitors.EBI The DuPont Pharmaceuticals Company
10698439 68 Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI Rhone-Poulenc Rorer
10639285 13 2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.EBI University of Leipzig
10639283 135 Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.EBI Berlex Biosciences
10636250 20 Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.EBI 3-Dimensional Pharmaceuticals
10636232 58 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.EBI COR Therapeutics, Inc.
10617091 73 Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.EBI Corvas International, Inc.
10560742 85 3-Amidinophenylalanine-based inhibitors of urokinase.EBI Universität Jena
10522707 16 2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.EBI GlaxoWellcome Medicines Research Centre
10509929 116 Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI Rhône-Poulenc Rorer
10508439 4 Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.EBI Washington University
10498211 42 Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI Corvas International, Inc.
10476876 1 Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.EBI Fujisawa Pharmaceutical Co., Ltd.
10425087 110 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.EBI DuPont Pharmaceuticals Company
10397495 49 Thrombin inhibitors based on [5,5] trans-fused indane lactams.EBI Glaxo Wellcome Research and Development
10346927 114 Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI Berlex Biosciences
10340616 6 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.EBI Università degli Studi di L'Aquila
10328312 27 Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.EBI DuPont Pharmaceuticals Company
10230630 36 Thrombin inhibitors based on a propargylglycine template.EBI Biotech Research Institute
10212122 35 Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI Molecumetics Ltd.
10206557 36 Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.EBI Corvas International, Inc.
9934495 26 Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.EBI Corvas International, Inc.
9876114 111 Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.EBI Institut für Biochemie
9873692 54 Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI DuPont Pharmaceuticals Company
9873654 37 5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.EBI GlaxoWellcome Research and Development
9873610 48 Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.EBI Boehringer Ingelheim (Canada) Ltd
9873607 21 The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.EBI DuPont Pharmaceuticals Company
9873569 16 Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI Corvas International, Inc.
9873520 27 Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.EBI Berlex Biosciences
9873451 19 Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.EBI Berlex Biosciences
9873397 37 In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals
9871780 85 Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.EBI Boehringer Ingelheim (Canada) Ltd
9871680 5 Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.EBI ProScript, Inc.
9871674 34 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.EBI DuPont Merck Pharmaceutical Company
9871629 6 Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.EBI Cinc
9871573 15 Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI Biotech Research Institute
9871540 100 Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.EBI DuPont Merck Pharmaceutical Company
9822554 14 1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
9822552 2 Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.EBI Institut Jacques Monod (UMR CNRS 7592/Universités Paris VI and VII)
9784099 84 Design of benzamidine-type inhibitors of factor Xa.EBI Institut für Biochemie
9767628 31 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.EBI GlaxoWellcome Medicines Research Centre
9733491 21 Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.EBI Novartis Pharma AG
9733480 93 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.EBI Berlex Biosciences
9733479 18 (Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.EBI Berlex Biosciences
9667976 58 beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.EBI Boehringer Ingelheim (Canada) Ltd.
9651152 20 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.EBI Hoechst Marion Roussel Inc.
9572899 19 Novel thieno[2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase.EBI University of Leipzig
9484495 74 Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.EBI Collegeville
9438022 55 Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.EBI DuPont Merck Pharmaceutical Company
9406601 109 Peptidomimetic inhibitors of the human cytomegalovirus protease.EBI Boehringer Ingelheim Ltd.
9379436 46 Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.EBI ZENECA Pharmaceuticals
9371237 69 Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.EBI Merck Research Laboratories
9341917 69 7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase.EBI Southern Methodist University
9341916 30 Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.EBI Rhône-Poulenc Rorer
9191969 31 Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.EBI Institut de Recherche Servier
9171866 12 Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.EBI Merck Research Laboratories
8917639 50 Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.EBI Corvas International, Inc.
8917638 26 Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.EBI Corvas International Inc.
8676347 39 Nonpeptidic inhibitors of human neutrophil elastase. 7. Design, synthesis, and in vitro activity of a series of pyridopyrimidine trifluoromethyl ketones.EBI ZENECA Pharmaceuticals
8426361 111 Highly selective tripeptide thrombin inhibitors.EBI Lilly Research Laboratories
8176703 14 Design of orally active, non-peptidic inhibitors of human leukocyte elastase.EBI ZENECA Pharmaceuticals Group
8164262 38 Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.EBI Daiichi Pharmaceutical Company, Ltd.
8035417 23 Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
7966161 45 Cephem sulfones as inactivators of human leukocyte elastase. 5. 7 alpha-Methoxy- and 7 alpha-chloro-1,1-dioxocephem 4-ketones.EBI Pharmacia Farmitalia Carlo Erba
7932559 42 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.EBI Zeneca Pharmaceuticals Group
7932558 30 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.EBI ZENECA Pharmaceuticals Group
7932532 23 Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors.EBI A Business Unit of ZENECA Inc.
7877139 8 Orally bioavailable benzisothiazolone inhibitors of human leukocyte elastase.EBI Sterling Winthrop Inc.
7837246 39 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.EBI ZENECA Pharmaceuticals
7837244 33 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.EBI ZENECA Pharmaceuticals
7837243 25 Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency.EBI ZENECA Pharmaceuticals
7837235 9 Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone.EBI ZENECA Pharmaceuticals
7830264 16 Inhibition of human neutrophil elastase. 3. An orally active enol acetate prodrug.EBI Marion Merrell Dow Research Institute
7739015 12 Phosphonates and phosphinates: novel leaving groups for benzisothiazolone inhibitors of human leukocyte elastase.EBI Sterling Winthrop Pharmaceuticals Research Division
7739010 118 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI Thrombosis Research Institute
7629790 32 New orally active serine protease inhibitors.EBI Minase Research Institute
7608910 1 Orally active beta-lactam inhibitors of human leukocyte elastase. 3. Stereospecific synthesis and structure-activity relationships for 3,3-dialkylazetidin-2-ones.EBI Merck Research Laboratories
7562931 41 Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.EBI ZENECA Pharmaceuticals
7473596 35 A novel class of cyclic beta-dicarbonyl leaving groups and their use in the design of benzisothiazolone human leukocyte elastase inhibitors.EBI Sterling Winthrop Pharmaceuticals Research Division
7473571 90 Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI Lilly Research Laboratories
3848491 5 Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases.EBI TBA
3844034 13 Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase.EBI TBA
3647139 9 Inhibition of human sputum elastase by substituted 2-pyrones.EBI TBA
3361575 65 (Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase.EBI Searle Research and Development
2391693 17 Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.EBI Merck Sharp and Dohme Research Laboratories
2391692 27 Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.EBI Merck Sharp and Dohme Research Laboratories
2391691 55 Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.EBI Merck Sharp and Dohme Research Laboratories
2296031 48 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.EBI Merrell Dow Research Institute
1479581 11 Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.EBI Boehringer Ingelheim Pharmaceuticals
28408226 51 Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.EBI Mochida Pharmaceutical Co. Ltd.
22803662 7 Synthesis, antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines.BDB Giresun University
21171894 6 Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.BDB Bristol-Myers Squibb Company
20545486 1 Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-▀-lactam inhibitor of human leukocyte elastase.BDB University of Lisbon
11496832 7 Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.BDB Università di Ferrara
17581239 25 Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.BDB Pfizer Global Research and Development,
19900814 15 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.BDB Daiichi Sankyo Co, Ltd
19884015 17 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.BDB Daiichi Sankyo Co, Ltd
19896847 36 Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.BDB Bristol-Myers Squibb Company
19811924 23 Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.BDB Dainippon Sumitomo Pharma Co
19409795 186 Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores.BDB BioCryst Pharmaceuticals
18998662 15 Design, Structure-Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors.BDB Bristol-Myers Squibb Company
16821772 270 Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.BDB Curacyte Chemistry GmbH
17850059 195 N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.BDB Montana State University
18459730 144 Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.BDB University of Namur
17174550 26 Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.BDB Bristol-Myers Squibb Company
17914785 67 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.BDB Bristol-Myers Squibb Company
14521405 29 Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.BDB Bristol-Myers Squibb Company
17338508 25 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.BDB GSK
11342132 24 Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors.BDB Boehringer Ingelheim Pharma KG
11027132 6 Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa.BDB Berlex
10417407 14 Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.BDB Berlex
17227710 141 Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa.BDB Berlex
17536795 118 Thiophene-anthranilamides as highly potent and orally available factor xa inhibitorsBDB Berlex Biosciences
9468142 60 Design of potent selective zinc-mediated serine protease inhibitors.BDB Arris
15261268 26 Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.BDB Aventis Pharma Deutschland GmbH
15261269 35 Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.BDB Aventis Pharma Deutschland GmbH
16621549 40 Novel 5-azaindole factor VIIa inhibitors.BDB Celera
15632123 9 A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.BDB Genentech
13678408 30 Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors.BDB Pharmacia Corporation
12954058 193 Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.BDB Pharmacia Corporation
14561089 6 Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.BDB Pharmacia Corporation
15522303 73 Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).BDB Celera
12742021 191 Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.BDB Celera
10779411 24 Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.BDB Axys Pharmaceutical
11731301 192 Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.BDB Axys Pharmaceutical
10966741 12 Crystal structures of human factor Xa complexed with potent inhibitors.BDB Aventis Pharma
11292354 48 A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.BDB Axys Pharmaceuticals Corporation
12061878 100 Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.BDB Aventis Pharma Deutschland GmbH
16460932 27 Discovery of novel heterocyclic factor VIIa inhibitors.BDB Celera
15857135 128 Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.BDB Aventis Pharma Deutschland GmbH
16621574 28 Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.BDB F. Hoffmann-La Roche Ltd.
15664864 44 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.BDB F. Hoffmann-La Roche Ltd.
16213138 80 Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.BDB F. Hoffmann-La Roche Ltd.
10479289 55 Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.BDB Rhone-Poulenc Rorer
16161994 25 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.BDB Bayer HealthCare AG
17181160 82 Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.BDB Daiichi Asubio Medical Research Laboratories LLC (DAIAMED)
16870435 29 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.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
16434195 23 Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
15582405 64 5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
15454209 50 5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.BDB Bristol-Myers Squibb Company
15454208 48 SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.BDB Bristol-Myers Squibb Company
16963264 22 Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
16682200 41 Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.BDB Bristol-Myers Squibb Company
16730984 25 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.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
15771420 58 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.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
12593649 15 Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.BDB Aventis Pharma
16697194 22 Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.BDB GlaxoSmithKline
16982192 8 Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors.BDB GlaxoSmithKline
16982190 46 Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.BDB GlaxoSmithKline
15999990 30 Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.BDB Aventis Pharma