Glycine, N-[(1R)-2-[(2S)-2-[[[[4-(aminoiminomethyl)phenyl]methyl]amino]carbonyl]-1-azetidinyl]-1-cyclohexyl-2-oxoethyl]-
| Title | Journal |
|---|---|
| Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia. | Bioorganic & medicinal chemistry letters 20140201 |
| Pharmacophore fingerprint-based approach to binding site subpocket similarity and its application to bioisostere replacement. | Journal of chemical information and modeling 20120827 |
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). | Journal of medicinal chemistry 20120426 |
| Serine proteases mediate inflammatory pain in acute pancreatitis. | American journal of physiology. Gastrointestinal and liver physiology 20110601 |
| The influence of direct thrombin inhibitors on the formation of platelet-leukocyte aggregates and tissue factor expression. | Thrombosis research 20101001 |
| Antithrombotic and anticoagulant profiles of TAK-442, a novel factor Xa inhibitor, in a rabbit model of venous thrombosis. | Journal of cardiovascular pharmacology 20100801 |
| Investigation of the involvement of P-glycoprotein and multidrug resistance-associated protein 2 in the efflux of ximelagatran and its metabolites by using short hairpin RNA knockdown in Caco-2 cells. | Drug metabolism and disposition: the biological fate of chemicals 20100301 |
| Anti-thrombin therapy during warm ischemia and cold preservation prevents chronic kidney graft fibrosis in a DCD model. | American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons 20100101 |
| Direct thrombin inhibitor prevents delayed graft function in a porcine model of renal transplantation. | Transplantation 20090615 |
| Compounds binding to the S2-S3 pockets of thrombin. | Journal of medicinal chemistry 20090514 |
| The effect of ex vivo anticoagulants on whole blood platelet aggregation. | Platelets 20090201 |
| Online capillary solid phase extraction and liquid chromatographic separation with quantitative tandem mass spectrometric detection (SPE-LC-MS/MS) of ximelagatran and its metabolites in a complex matrix. | Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20090115 |
| Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. | Journal of medicinal chemistry 20081009 |
| Pro-inflammatory response and adverse drug reactions: mechanisms of action of ximelagatran on chemokine and cytokine activation in a monocyte in vitro model. | Toxicology in vitro : an international journal published in association with BIBRA 20080901 |
| Effect of low and high dose melagatran and other antithrombotic drugs on platelet aggregation. | Journal of thrombosis and thrombolysis 20080401 |
| Melagatran for thromboprophylaxis after mechanical valve implantation: results in a heterotopic porcine model. | The Journal of thoracic and cardiovascular surgery 20070801 |
| The direct thrombin inhibitor ximelagatran/melagatran: a systematic review on clinical applications and an evidence based assessment of risk benefit profile. | Expert opinion on drug safety 20070701 |
| Antithrombotic and anticoagulant effects of the direct thrombin inhibitor dabigatran, and its oral prodrug, dabigatran etexilate, in a rabbit model of venous thrombosis. | Journal of thrombosis and haemostasis : JTH 20070601 |
| Effects of thrombin inhibition with melagatran on renal hemodynamics and function and liver integrity during early endotoxemia. | American journal of physiology. Regulatory, integrative and comparative physiology 20070301 |
| Thermodynamic inhibition profile of a cyclopentyl and a cyclohexyl derivative towards thrombin: the same but for different reasons. | Angewandte Chemie (International ed. in English) 20070101 |
| Effects of melagatran on activated partial thromboplastin time and on ecarin clotting time in cord versus adult plasma. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20061101 |
| [Clinical use of a new class of anticoagulant drugs: the direct thrombin inhibitors]. | Giornale italiano di cardiologia (2006) 20061101 |
| Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. | Bioorganic & medicinal chemistry letters 20060515 |
| Antithrombotic effects of ximelagatran plus acetylsalicylic acid (ASA) and clopidogrel plus ASA in a human ex vivo arterial thrombosis model. | Thrombosis and haemostasis 20060301 |
| Ximelagatran: direct thrombin inhibitor. | Vascular health and risk management 20060301 |
| A combination of a thrombin inhibitor and dexamethasone prevents the development of experimental disseminated intravascular coagulation in rats. | Thrombosis research 20060101 |
| Comparable pharmacokinetics and pharmacodynamics of melagatran in Japanese and caucasian volunteers after oral administration of the direct thrombin inhibitor ximelagatran. | Clinical pharmacokinetics 20060101 |
| Population pharmacokinetics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in atrial fibrillation patients receiving long-term anticoagulation therapy. | Clinical pharmacokinetics 20060101 |
| Assessment of bleeding after concomitant administration of antiplatelet and anticoagulant agents in lower limb arthroplasty. | Pathophysiology of haemostasis and thrombosis 20060101 |
| Differences in the clinically effective molar concentrations of four direct thrombin inhibitors explain their variable prothrombin time prolongation. | Thrombosis and haemostasis 20051101 |
| [The new antithrombotic agents]. | Presse medicale (Paris, France : 1983) 20051022 |
| The antithrombotic effect of melagatran in combination with clopidogrel and/or aspirin (carotid artery primary thrombosis study). | Journal of cardiovascular pharmacology 20051001 |
| Long-term treatment with ximelagatran, an oral direct thrombin inhibitor, persistently reduces the coagulation activity after a myocardial infarction. | Journal of thrombosis and haemostasis : JTH 20051001 |
| Prevention of clot formation during haemodialysis using the direct thrombin inhibitor melagatran in patients with chronic uraemia. | Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20050901 |
| Melagatran anticoagulation during haemodialysis--'Primum non nocere'. | Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20050901 |
| New antithrombotics in the prevention of thromboembolic disease. | European journal of internal medicine 20050801 |
| Drug insight: an overview of current anticoagulation therapy after heart valve replacement. | Nature clinical practice. Cardiovascular medicine 20050801 |
| Pharmacokinetics and pharmacodynamics of ximelagatran. | Seminars in vascular medicine 20050801 |
| Low potential for interactions between melagatran/ximelagatran and other drugs, food, or alcohol. | Seminars in vascular medicine 20050801 |
| Comparison of two different ecarin clotting time methods. | Journal of thrombosis and thrombolysis 20050801 |
| Additive effects of anticoagulants: recombinant human activated protein C and heparin or melagatran, in tissue factor-activated umbilical-cord plasma. | Thrombosis and haemostasis 20050701 |
| Recombinant human activated protein C, heparin and melagatran in umbilical cord versus adult plasma. | Acta paediatrica (Oslo, Norway : 1992) 20050701 |
| The effects of ximelagatran and warfarin on the prophylaxis of a caval vein thrombosis and bleeding in the anaesthetized rat. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20050601 |
| [Thromboprophylaxis in hip and knee arthroplasty. Are the new anticoagulants better than those previously used?]. | Ugeskrift for laeger 20050523 |
| Different antithrombotic properties of factor Xa inhibitor and thrombin inhibitor in rat thrombosis models. | European journal of pharmacology 20050502 |
| The oral direct thrombin inhibitor, ximelagatran, an alternative for anticoagulant treatment during the puerperium and lactation. | BJOG : an international journal of obstetrics and gynaecology 20050501 |
| Ximelagatran and melagatran vs. low-molecular-weight heparin in major orthopedic surgery: relationship between efficacy and safety and timing of initial administration. | Journal of thrombosis and haemostasis : JTH 20050501 |
| The direct thrombin inhibitor melagatran/ximelagatran. | The Medical journal of Australia 20050307 |
| Anticoagulant action of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in umbilical cord and adult plasma: an in vitro examination. | Thrombosis research 20050101 |
| Ximelagatran--a promising new drug in thromboembolic disorders. | Current pharmaceutical design 20050101 |
| [Effective thrombosis prophylaxis with melagatran]. | Zeitschrift fur Orthopadie und ihre Grenzgebiete 20050101 |
| [New anticoagulants in clinical practice]. | Orvosi hetilap 20041205 |
| Advances in anticoagulation therapy: the role of selective inhibitors of factor Xa and thrombin in thromboprophylaxis after major orthopedic surgery. | Seminars in thrombosis and hemostasis 20041201 |
| Prevention of venous thromboembolism after orthopedic surgery: the EXPRESS study. | Journal of thrombosis and haemostasis : JTH 20041101 |
| The direct thrombin inhibitor melagatran/ximelagatran. | The Medical journal of Australia 20041018 |
| Drotrecogin alfa activated (recombinant human activated protein C) in combination with heparin or melagatran: effects on prothrombin time and activated partial thromboplastin time. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20041001 |
| Thrombin inhibitor reduces myocardial infarction in apoE-/- x LDLR-/- mice. | American journal of physiology. Heart and circulatory physiology 20040801 |
| Significantly lower need for blood transfusions associated with post-operatively initiated subcutaneous melagatran/oral ximelagatran compared with enoxaparin. | Thrombosis and haemostasis 20040801 |
| No pharmacokinetic or pharmacodynamic interaction between atorvastatin and the oral direct thrombin inhibitor ximelagatran. | Journal of clinical pharmacology 20040801 |
| No pharmacokinetic or pharmacodynamic interaction between digoxin and the oral direct thrombin inhibitor ximelagatran in healthy volunteers. | Journal of clinical pharmacology 20040801 |
| Drotrecogin alfa (activated, Xigris) in combination with heparin or melagatran: an in vitro investigation. | Journal of thrombosis and thrombolysis 20040801 |
| [Prevention and treatment of deep vein thrombosis with ximelagatran]. | Deutsche medizinische Wochenschrift (1946) 20040723 |
| The beginning of the end of warfarin? | The Medical journal of Australia 20040607 |
| The therapeutic potential of ximelagatran to become the anticoagulant of choice in medicine: a review of recently completed clinical trials. | Expert opinion on pharmacotherapy 20040601 |
| Effect of recombinant factor VIIa on melagatran-induced inhibition of thrombin generation and platelet activation in healthy volunteers. | Thrombosis and haemostasis 20040601 |
| [Ximelagatran/Melagatran. Perspectives for new oral antithrombin drugs]. | Journal des maladies vasculaires 20040501 |
| Combined effects of melagatran and eptifibatide on platelet aggregation inhibition but not thrombin generation inhibition. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20040301 |
| Recombinant factor VIIa as an antidote for anticoagulant treatment. | Seminars in hematology 20040101 |
| Ximelagatran/Melagatran: a review of its use in the prevention of venous thromboembolism in orthopaedic surgery. | Drugs 20040101 |
| Inhibition of thrombin-induced feedback activation of factor V: a potential pathway for inhibition of thrombin generation by melagatran. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20040101 |
| [Low molecular weight heparin, fondaparinux and melagatran: new data and clinical studies]. | Pharmazie in unserer Zeit 20040101 |
| Oral anticoagulation: preparing for change. | Journal of the American Medical Directors Association 20040101 |
| The direct thrombin inhibitor melagatran followed by oral ximelagatran compared with enoxaparin for the prevention of venous thromboembolism after total hip or knee replacement: the EXPRESS study. | Journal of thrombosis and haemostasis : JTH 20031201 |
| [Melagatran and ximelagatran. Pharmacologic characteristics and anesthesiological aspects]. | Der Anaesthesist 20031201 |
| Consistent pharmacokinetics of the oral direct thrombin inhibitor ximelagatran in patients with nonvalvular atrial fibrillation and in healthy subjects. | European journal of clinical pharmacology 20031001 |
| Oral direct thrombin inhibitors in clinical development. | Journal of internal medicine 20031001 |
| Pharmacokinetics and anticoagulant effect of the direct thrombin inhibitor melagatran following subcutaneous administration to healthy young men. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20031001 |
| Improving antithrombotic treatment in patients after myocardial infarction. | Lancet (London, England) 20030906 |
| Three vehicle formulations for melagatran, a direct thrombin inhibitor, evaluated in a vena cava thrombosis model in the rat. | Biopharmaceutics & drug disposition 20030901 |
| Determination of melagatran in rabbit plasma by high-performance liquid chromatography with automated column switching. | Biomedical chromatography : BMC 20030901 |
| Pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, are not influenced by acetylsalicylic acid. | European journal of clinical pharmacology 20030801 |
| The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review. | Thrombosis research 20030715 |
| Clinical experience of melagatran/ximelagatran in major orthopaedic surgery. | Thrombosis research 20030715 |
| Medical indications and considerations for future clinical decision making. | Thrombosis research 20030715 |
| Effects of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, and dalteparin on the endogenous thrombin potential in venous blood from healthy male subjects. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20030701 |
| D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety. | Bioorganic & medicinal chemistry letters 20030616 |
| The influence of direct and antithrombin-dependent thrombin inhibitors on the procoagulant and anticoagulant effects of thrombin. | Thrombosis research 20030601 |
| In vitro effect of melagatran and lepirudin on clot-bound thrombin. | Thrombosis research 20030601 |
| Characterization of in vitro biotransformation of new, orally active, direct thrombin inhibitor ximelagatran, an amidoxime and ester prodrug. | Drug metabolism and disposition: the biological fate of chemicals 20030501 |
| The METHRO trials. | Expert opinion on investigational drugs 20030501 |
| [Chromogenic substrate as antidote against the thrombin inhibitor Melagatran?]. | Hamostaseologie 20030501 |
| Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young healthy male subjects. | European journal of clinical pharmacology 20030501 |
| Predicting the pharmacology of thrombin inhibitors. | Journal of thrombosis and haemostasis : JTH 20030501 |
| Orally active direct thrombin inhibitors. | Seminars in vascular medicine 20030501 |
| Melagatran attenuates fibrin and platelet deposition in a porcine coronary artery over-stretch injury model. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20030401 |
| Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives. | Journal of medicinal chemistry 20030327 |
| [The first oral thrombin inhibitor. Competition to heparins and marcumar?]. | MMW Fortschritte der Medizin 20030306 |
| The benefit-to-risk profile of melagatran is superior to that of hirudin in a rabbit arterial thrombosis prevention and bleeding model. | Journal of thrombosis and haemostasis : JTH 20030301 |
| Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement. | Thrombosis and haemostasis 20030201 |
| Inhibition of endothelial cell-mediated generation of activated protein C by direct and antithrombin-dependent thrombin inhibitors. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20030201 |
| Thrombin-induced platelet activation and its inhibition by anticoagulants with different modes of action. | Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20030201 |
| Determination of ximelagatran, an oral direct thrombin inhibitor, its active metabolite melagatran, and the intermediate metabolites, in biological samples by liquid chromatography-mass spectrometry. | Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20030115 |
| [New anticoagulants -- their clinical significance]. | Therapeutische Umschau. Revue therapeutique 20030101 |
| Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. | Clinical pharmacokinetics 20030101 |
| No influence of ethnic origin on the pharmacokinetics and pharmacodynamics of melagatran following oral administration of ximelagatran, a novel oral direct thrombin inhibitor, to healthy male volunteers. | Clinical pharmacokinetics 20030101 |
| No influence of obesity on the pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran. | Clinical pharmacokinetics 20030101 |
| Pharmacokinetics of melagatran and the effect on ex vivo coagulation time in orthopaedic surgery patients receiving subcutaneous melagatran and oral ximelagatran: a population model analysis. | Clinical pharmacokinetics 20030101 |
| Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran. | Clinical pharmacokinetics 20030101 |
| No influence of mild-to-moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. | Clinical pharmacokinetics 20030101 |
| Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions. | Clinical pharmacokinetics 20030101 |
| [Treatment and prevention of venous thromboembolic events: present and future antithrombotic agents]. | Bulletin de l'Academie nationale de medecine 20030101 |
| Effects of the oral direct thrombin inhibitor ximelagatran on p-selectin expression and thrombin generation in atrial fibrillation. | Pathophysiology of haemostasis and thrombosis 20030101 |
| Effects of lepirudin, argatroban and melagatran and additional influence of phenprocoumon on ecarin clotting time. | Thrombosis research 20030101 |
| Novel anticoagulants for the prevention and treatment of venous thromboembolism. | Wiener medizinische Wochenschrift (1946) 20030101 |
| Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial. | Lancet (London, England) 20021109 |
| Influence of lepirudin, argatroban, and melagatran on prothrombin time and additional effect of oral anticoagulation. | Clinical chemistry 20021001 |
| Pharmacokinetics, pharmacodynamics and clinical effects of the oral direct thrombin inhibitor ximelagatran in acute treatment of patients with pulmonary embolism and deep vein thrombosis. | Thrombosis research 20020815 |
| Effects of ximelagatran, the oral form of melagatran, in the treatment of caval vein thrombosis in conscious rats. | Thrombosis research 20020815 |
| Monitoring of anticoagulant effects of direct thrombin inhibitors. | Seminars in thrombosis and hemostasis 20020801 |
| Comparative antithrombotic potencies of direct thrombin inhibitors and low-molecular-weight heparins in an ex vivo human experimental thrombosis model. | Seminars in thrombosis and hemostasis 20020801 |
| Inhibition of thrombin abrogates the instant blood-mediated inflammatory reaction triggered by isolated human islets: possible application of the thrombin inhibitor melagatran in clinical islet transplantation. | Diabetes 20020601 |
| Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1. | Bioorganic & medicinal chemistry letters 20020408 |
| Maximized hemostasis. | Thrombosis and haemostasis 20020401 |
| Local proCPU (TAFI) activation during thrombolytic treatment in a dog model of coronary artery thrombosis can be inhibited with a direct, small molecule thrombin inhibitor (melagatran). | Thrombosis and haemostasis 20020401 |
| Factor V Leiden (G1691A) and prothrombin gene G20210A mutations as potential risk factors for venous thromboembolism after total hip or total knee replacement surgery. | Thrombosis and haemostasis 20020401 |
| Prophylaxis of venous thromboembolism with subcutaneous melagatran in total hip or total knee replacement: results from Phase II studies. | Thrombosis research 20020301 |
| A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. MElagatran for THRombin inhibition in Orthopaedic surgery. | Thrombosis and haemostasis 20020201 |
| Determination of melagatran, a novel, direct thrombin inhibitor, in human plasma and urine by liquid chromatography-mass spectrometry. | Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20020105 |
| Melagatran. Exanta, H 319/68. | Drugs in R&D 20020101 |
| Effect of phenprocoumon on monitoring of lepirudin, argatroban, melagatran and unfractionated heparin with the PiCT method. | Pathophysiology of haemostasis and thrombosis 20020101 |
| Factorising ligand affinity: a combined thermodynamic and crystallographic study of trypsin and thrombin inhibition. | Journal of molecular biology 20011026 |
| Effect of melagatran on prothrombin time assays depends on the sensitivity of the thromboplastin and the final dilution of the plasma sample. | Thrombosis and haemostasis 20010801 |
| Anticoagulation: the present and future. | Clinical and applied thrombosis/hemostasis : official journal of the International Academy of Clinical and Applied Thrombosis/Hemostasis 20010701 |
| Advances in the development of thrombin inhibitors. | Expert opinion on investigational drugs 20010501 |
| [Direct thrombin antagonists]. | Herz 20010401 |
| The effects of oral and intravenous direct thrombin inhibitors on the size of photochemically induced cortical infarction in rats. | Thrombosis research 20010315 |
| Effect of activated prothrombin complex concentrate or recombinant factor VIIa on the bleeding time and thrombus formation during anticoagulation with a direct thrombin inhibitor. | Thrombosis research 20010201 |
| Effects of agents, used to treat bleeding disorders, on bleeding time prolonged by a very high dose of a direct thrombin inhibitor in anesthesized rats and rabbits. | Thrombosis research 20010201 |
| The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. | Thrombosis research 20010201 |
| [New thrombolytic agents]. | Medizinische Monatsschrift fur Pharmazeuten 20010201 |
| [Treatment of deep vein thrombosis. Current and future questions]. | Bulletin de l'Academie nationale de medecine 20010101 |
| [Thrombosis in spite of warfarin--what should be done?]. | Duodecim; laaketieteellinen aikakauskirja 20010101 |
| Protease inhibitors: current status and future prospects. | Journal of medicinal chemistry 20000210 |
| Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. | Thrombosis and haemostasis 19980101 |