Title: Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.
Journal: Bioorganic & medicinal chemistry letters 20140201
Title: Pharmacophore fingerprint-based approach to binding site subpocket similarity and its application to bioisostere replacement.
Journal: Journal of chemical information and modeling 20120827
Title: Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2).
Journal: Journal of medicinal chemistry 20120426
Title: Serine proteases mediate inflammatory pain in acute pancreatitis.
Journal: American journal of physiology. Gastrointestinal and liver physiology 20110601
Title: The influence of direct thrombin inhibitors on the formation of platelet-leukocyte aggregates and tissue factor expression.
Journal: Thrombosis research 20101001
Title: Antithrombotic and anticoagulant profiles of TAK-442, a novel factor Xa inhibitor, in a rabbit model of venous thrombosis.
Journal: Journal of cardiovascular pharmacology 20100801
Title: 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.
Journal: Drug metabolism and disposition: the biological fate of chemicals 20100301
Title: Anti-thrombin therapy during warm ischemia and cold preservation prevents chronic kidney graft fibrosis in a DCD model.
Journal: American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons 20100101
Title: Direct thrombin inhibitor prevents delayed graft function in a porcine model of renal transplantation.
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Title: Compounds binding to the S2-S3 pockets of thrombin.
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Title: The effect of ex vivo anticoagulants on whole blood platelet aggregation.
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Title: Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
Journal: Journal of medicinal chemistry 20081009
Title: Pro-inflammatory response and adverse drug reactions: mechanisms of action of ximelagatran on chemokine and cytokine activation in a monocyte in vitro model.
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Title: Effect of low and high dose melagatran and other antithrombotic drugs on platelet aggregation.
Journal: Journal of thrombosis and thrombolysis 20080401
Title: Melagatran for thromboprophylaxis after mechanical valve implantation: results in a heterotopic porcine model.
Journal: The Journal of thoracic and cardiovascular surgery 20070801
Title: The direct thrombin inhibitor ximelagatran/melagatran: a systematic review on clinical applications and an evidence based assessment of risk benefit profile.
Journal: Expert opinion on drug safety 20070701
Title: Antithrombotic and anticoagulant effects of the direct thrombin inhibitor dabigatran, and its oral prodrug, dabigatran etexilate, in a rabbit model of venous thrombosis.
Journal: Journal of thrombosis and haemostasis : JTH 20070601
Title: Effects of thrombin inhibition with melagatran on renal hemodynamics and function and liver integrity during early endotoxemia.
Journal: American journal of physiology. Regulatory, integrative and comparative physiology 20070301
Title: Thermodynamic inhibition profile of a cyclopentyl and a cyclohexyl derivative towards thrombin: the same but for different reasons.
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Title: Effects of melagatran on activated partial thromboplastin time and on ecarin clotting time in cord versus adult plasma.
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Title: Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
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Title: Antithrombotic effects of ximelagatran plus acetylsalicylic acid (ASA) and clopidogrel plus ASA in a human ex vivo arterial thrombosis model.
Journal: Thrombosis and haemostasis 20060301
Title: Ximelagatran: direct thrombin inhibitor.
Journal: Vascular health and risk management 20060301
Title: A combination of a thrombin inhibitor and dexamethasone prevents the development of experimental disseminated intravascular coagulation in rats.
Journal: Thrombosis research 20060101
Title: Comparable pharmacokinetics and pharmacodynamics of melagatran in Japanese and caucasian volunteers after oral administration of the direct thrombin inhibitor ximelagatran.
Journal: Clinical pharmacokinetics 20060101
Title: Population pharmacokinetics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in atrial fibrillation patients receiving long-term anticoagulation therapy.
Journal: Clinical pharmacokinetics 20060101
Title: Assessment of bleeding after concomitant administration of antiplatelet and anticoagulant agents in lower limb arthroplasty.
Journal: Pathophysiology of haemostasis and thrombosis 20060101
Title: Differences in the clinically effective molar concentrations of four direct thrombin inhibitors explain their variable prothrombin time prolongation.
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Title: [The new antithrombotic agents].
Journal: Presse medicale (Paris, France : 1983) 20051022
Title: The antithrombotic effect of melagatran in combination with clopidogrel and/or aspirin (carotid artery primary thrombosis study).
Journal: Journal of cardiovascular pharmacology 20051001
Title: Long-term treatment with ximelagatran, an oral direct thrombin inhibitor, persistently reduces the coagulation activity after a myocardial infarction.
Journal: Journal of thrombosis and haemostasis : JTH 20051001
Title: Prevention of clot formation during haemodialysis using the direct thrombin inhibitor melagatran in patients with chronic uraemia.
Journal: Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20050901
Title: Melagatran anticoagulation during haemodialysis--'Primum non nocere'.
Journal: Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20050901
Title: New antithrombotics in the prevention of thromboembolic disease.
Journal: European journal of internal medicine 20050801
Title: Drug insight: an overview of current anticoagulation therapy after heart valve replacement.
Journal: Nature clinical practice. Cardiovascular medicine 20050801
Title: Pharmacokinetics and pharmacodynamics of ximelagatran.
Journal: Seminars in vascular medicine 20050801
Title: Low potential for interactions between melagatran/ximelagatran and other drugs, food, or alcohol.
Journal: Seminars in vascular medicine 20050801
Title: Comparison of two different ecarin clotting time methods.
Journal: Journal of thrombosis and thrombolysis 20050801
Title: Additive effects of anticoagulants: recombinant human activated protein C and heparin or melagatran, in tissue factor-activated umbilical-cord plasma.
Journal: Thrombosis and haemostasis 20050701
Title: Recombinant human activated protein C, heparin and melagatran in umbilical cord versus adult plasma.
Journal: Acta paediatrica (Oslo, Norway : 1992) 20050701
Title: The effects of ximelagatran and warfarin on the prophylaxis of a caval vein thrombosis and bleeding in the anaesthetized rat.
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Title: [Thromboprophylaxis in hip and knee arthroplasty. Are the new anticoagulants better than those previously used?].
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Title: Different antithrombotic properties of factor Xa inhibitor and thrombin inhibitor in rat thrombosis models.
Journal: European journal of pharmacology 20050502
Title: The oral direct thrombin inhibitor, ximelagatran, an alternative for anticoagulant treatment during the puerperium and lactation.
Journal: BJOG : an international journal of obstetrics and gynaecology 20050501
Title: Ximelagatran and melagatran vs. low-molecular-weight heparin in major orthopedic surgery: relationship between efficacy and safety and timing of initial administration.
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Title: The direct thrombin inhibitor melagatran/ximelagatran.
Journal: The Medical journal of Australia 20050307
Title: Anticoagulant action of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in umbilical cord and adult plasma: an in vitro examination.
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Title: Prevention of venous thromboembolism after orthopedic surgery: the EXPRESS study.
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Title: The direct thrombin inhibitor melagatran/ximelagatran.
Journal: The Medical journal of Australia 20041018
Title: Drotrecogin alfa activated (recombinant human activated protein C) in combination with heparin or melagatran: effects on prothrombin time and activated partial thromboplastin time.
Journal: Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20041001
Title: Thrombin inhibitor reduces myocardial infarction in apoE-/- x LDLR-/- mice.
Journal: American journal of physiology. Heart and circulatory physiology 20040801
Title: Significantly lower need for blood transfusions associated with post-operatively initiated subcutaneous melagatran/oral ximelagatran compared with enoxaparin.
Journal: Thrombosis and haemostasis 20040801
Title: No pharmacokinetic or pharmacodynamic interaction between atorvastatin and the oral direct thrombin inhibitor ximelagatran.
Journal: Journal of clinical pharmacology 20040801
Title: No pharmacokinetic or pharmacodynamic interaction between digoxin and the oral direct thrombin inhibitor ximelagatran in healthy volunteers.
Journal: Journal of clinical pharmacology 20040801
Title: Drotrecogin alfa (activated, Xigris) in combination with heparin or melagatran: an in vitro investigation.
Journal: Journal of thrombosis and thrombolysis 20040801
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Title: The beginning of the end of warfarin?
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Title: The therapeutic potential of ximelagatran to become the anticoagulant of choice in medicine: a review of recently completed clinical trials.
Journal: Expert opinion on pharmacotherapy 20040601
Title: Effect of recombinant factor VIIa on melagatran-induced inhibition of thrombin generation and platelet activation in healthy volunteers.
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Journal: Journal des maladies vasculaires 20040501
Title: Combined effects of melagatran and eptifibatide on platelet aggregation inhibition but not thrombin generation inhibition.
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Title: Recombinant factor VIIa as an antidote for anticoagulant treatment.
Journal: Seminars in hematology 20040101
Title: Ximelagatran/Melagatran: a review of its use in the prevention of venous thromboembolism in orthopaedic surgery.
Journal: Drugs 20040101
Title: Inhibition of thrombin-induced feedback activation of factor V: a potential pathway for inhibition of thrombin generation by melagatran.
Journal: Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20040101
Title: [Low molecular weight heparin, fondaparinux and melagatran: new data and clinical studies].
Journal: Pharmazie in unserer Zeit 20040101
Title: Oral anticoagulation: preparing for change.
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Title: 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.
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Title: [Melagatran and ximelagatran. Pharmacologic characteristics and anesthesiological aspects].
Journal: Der Anaesthesist 20031201
Title: Consistent pharmacokinetics of the oral direct thrombin inhibitor ximelagatran in patients with nonvalvular atrial fibrillation and in healthy subjects.
Journal: European journal of clinical pharmacology 20031001
Title: Oral direct thrombin inhibitors in clinical development.
Journal: Journal of internal medicine 20031001
Title: Pharmacokinetics and anticoagulant effect of the direct thrombin inhibitor melagatran following subcutaneous administration to healthy young men.
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Title: Improving antithrombotic treatment in patients after myocardial infarction.
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Title: Three vehicle formulations for melagatran, a direct thrombin inhibitor, evaluated in a vena cava thrombosis model in the rat.
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Title: Determination of melagatran in rabbit plasma by high-performance liquid chromatography with automated column switching.
Journal: Biomedical chromatography : BMC 20030901
Title: Pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, are not influenced by acetylsalicylic acid.
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Title: The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review.
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Title: Clinical experience of melagatran/ximelagatran in major orthopaedic surgery.
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Title: Medical indications and considerations for future clinical decision making.
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Title: 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.
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Title: D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.
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Title: The influence of direct and antithrombin-dependent thrombin inhibitors on the procoagulant and anticoagulant effects of thrombin.
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Title: In vitro effect of melagatran and lepirudin on clot-bound thrombin.
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Title: Characterization of in vitro biotransformation of new, orally active, direct thrombin inhibitor ximelagatran, an amidoxime and ester prodrug.
Journal: Drug metabolism and disposition: the biological fate of chemicals 20030501
Title: The METHRO trials.
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Title: Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young healthy male subjects.
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Title: Predicting the pharmacology of thrombin inhibitors.
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Title: Orally active direct thrombin inhibitors.
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Title: Melagatran attenuates fibrin and platelet deposition in a porcine coronary artery over-stretch injury model.
Journal: Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20030401
Title: Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives.
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Journal: MMW Fortschritte der Medizin 20030306
Title: The benefit-to-risk profile of melagatran is superior to that of hirudin in a rabbit arterial thrombosis prevention and bleeding model.
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Title: Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement.
Journal: Thrombosis and haemostasis 20030201
Title: Inhibition of endothelial cell-mediated generation of activated protein C by direct and antithrombin-dependent thrombin inhibitors.
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Title: Thrombin-induced platelet activation and its inhibition by anticoagulants with different modes of action.
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Title: Determination of ximelagatran, an oral direct thrombin inhibitor, its active metabolite melagatran, and the intermediate metabolites, in biological samples by liquid chromatography-mass spectrometry.
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Journal: Therapeutische Umschau. Revue therapeutique 20030101
Title: Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor.
Journal: Clinical pharmacokinetics 20030101
Title: 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.
Journal: Clinical pharmacokinetics 20030101
Title: No influence of obesity on the pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran.
Journal: Clinical pharmacokinetics 20030101
Title: 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.
Journal: Clinical pharmacokinetics 20030101
Title: Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran.
Journal: Clinical pharmacokinetics 20030101
Title: No influence of mild-to-moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor.
Journal: Clinical pharmacokinetics 20030101
Title: Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Journal: Clinical pharmacokinetics 20030101
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Journal: Bulletin de l'Academie nationale de medecine 20030101
Title: Effects of the oral direct thrombin inhibitor ximelagatran on p-selectin expression and thrombin generation in atrial fibrillation.
Journal: Pathophysiology of haemostasis and thrombosis 20030101
Title: Effects of lepirudin, argatroban and melagatran and additional influence of phenprocoumon on ecarin clotting time.
Journal: Thrombosis research 20030101
Title: Novel anticoagulants for the prevention and treatment of venous thromboembolism.
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Title: Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial.
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Title: Influence of lepirudin, argatroban, and melagatran on prothrombin time and additional effect of oral anticoagulation.
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Title: Pharmacokinetics, pharmacodynamics and clinical effects of the oral direct thrombin inhibitor ximelagatran in acute treatment of patients with pulmonary embolism and deep vein thrombosis.
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Title: Effects of ximelagatran, the oral form of melagatran, in the treatment of caval vein thrombosis in conscious rats.
Journal: Thrombosis research 20020815
Title: Monitoring of anticoagulant effects of direct thrombin inhibitors.
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Title: Comparative antithrombotic potencies of direct thrombin inhibitors and low-molecular-weight heparins in an ex vivo human experimental thrombosis model.
Journal: Seminars in thrombosis and hemostasis 20020801
Title: 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.
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Title: Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.
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Title: Maximized hemostasis.
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Title: 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).
Journal: Thrombosis and haemostasis 20020401
Title: Factor V Leiden (G1691A) and prothrombin gene G20210A mutations as potential risk factors for venous thromboembolism after total hip or total knee replacement surgery.
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Title: Prophylaxis of venous thromboembolism with subcutaneous melagatran in total hip or total knee replacement: results from Phase II studies.
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Title: 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.
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Title: Determination of melagatran, a novel, direct thrombin inhibitor, in human plasma and urine by liquid chromatography-mass spectrometry.
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Title: Factorising ligand affinity: a combined thermodynamic and crystallographic study of trypsin and thrombin inhibition.
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Title: Anticoagulation: the present and future.
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Title: 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.
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