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85 results about "Factor Xa Inhibitor" patented technology
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Direct factor Xa inhibitors ('xabans') are a class of anticoagulant drugs which act directly upon factor X in the coagulation cascade, without using antithrombin as a mediator.
Antidotes for factor xa inhibitors and methods of using the same
ActiveUS20090098119A1Reduce and remove intrinsic procoagulantReduce and remove and anticoagulant activityOrganic active ingredientsHydrolasesMedicineAntidote
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
Owner:ALEXION PHARMA INC
Antidotes for factor Xa inhibitors and methods of using the same
ActiveUS8153590B2Reduces and removes anticoagulant effectReduced activityPeptide/protein ingredientsMammal material medical ingredientsAntidoteFactor Xa Inhibitor
Owner:ALEXION PHARMA INC
Triazole-derivatives as factor Xa inhibitors
The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.
Owner:SANOFI AVENTIS DEUT GMBH
Antidotes for factor Xa inhibitors and methods of using the same
ActiveUS8268783B2Reduces and removes anticoagulant effectReduced activityBiocidePeptide/protein ingredientsFactor XAntidote
Owner:ALEXION PHARMA INC
Combination anticoagulant therapy with a compound that acts as a factor xa inhibitor
InactiveUS20080254036A1Predictable levelImprove efficacyBiocideAntipyreticFactor iiFactor Xa Inhibitor
The present invention is directed to methods of using combination therapies containing [2-({4-[(dimethylamino)iminomethyl]phenyl}carbonylamino)-5-methoxyphenyl]-N-(5-chloro(2-pyridyl))carboxamide for the treatment of thrombotic disease(s) and pharmaceutical compositions thereof.
Owner:MILLENNIUM PHARMA INC
Antidotes for factor xa inhibitors and methods of using the same
ActiveUS20100255000A1Preventing and reducing bleedingReduces and removes anticoagulant effectPeptide/protein ingredientsHydrolasesMedicineAntidote
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor X and factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of reversing anticoagulation, stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
Owner:ALEXION PHARMA INC
Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
ActiveUS8455439B2Low effective doseReduce potential side effectsPeptide/protein ingredientsMammal material medical ingredientsAntidoteFactor Xa Inhibitor
The present invention relates to antidotes of anticoagulants targeting factor Xa which antidotes are used in combination with blood coagulating agents or other heparin antidotes to prevent or reduce bleeding in a subject. The antidotes described herein have reduced or no intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is or will be undergoing anticoagulant therapy with a factor Xa inhibitor.
Owner:ALEXION PHARMA INC
Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
ActiveUS20100125052A1Reduce potential side effectsLow effective dosePeptide/protein ingredientsMammal material medical ingredientsMedicineAntidote
The present invention relates to antidotes of anticoagulants targeting factor Xa which antidotes are used in combination with blood coagulating agents or other heparin antidotes to prevent or reduce bleeding in a subject. The antidotes described herein have reduced or no intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is or will be undergoing anticoagulant therapy with a factor Xa inhibitor.
Owner:ALEXION PHARMA INC
Prophylaxis of thromboembolic events in cancer patients
The present invention generally relates a method of prophylaxis of thrombotic and thromboembolic events in a cancer patient in need thereof comprising administering to said patient a therapeutically effective amount of a factor Xa inhibitor, especially apixaban or a polymorph or pharmaceutically acceptable solvate form thereof. The factor Xa inhibitor may be used in combination with therapeutic agents.
Owner:BRISTOL MYERS SQUIBB CO
Indole derivatives as factor Xa inhibitors
The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.
Owner:SANOFI AVENTIS DEUT GMBH
Azaindole-derivatives as factor Xa inhibitors
The present invention relates to compounds of the formula Iwherein R0, R1, R2, R3, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and / or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and / or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and / or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Owner:SANOFI AVENTIS DEUT GMBH
Use Of Dipyridamole For Treatment Of Resistance To Platelet Inhibitors
InactiveUS20090048173A1Reduce decreaseBiocidePeptide/protein ingredientsDipyridamolePlatelet inhibitor
Owner:EISERT WOLFGANG +1
Indazole-derivatives as factor Xa inhibitors
The present invention relates to a compound of the formula Iwherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and / or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and / or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and / or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Owner:SANOFI AVENTIS DEUT GMBH
Beta-Aminoacid-Derivatives As Factor Xa Inhibitors
The present invention relates to compounds of the formula I, in which R0; R1; R2; R3; R4; R5, R, Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboemboic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and / or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and / or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and / or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Owner:SANOFI AVENTIS DEUTSCHLAND GMBH
Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.
Owner:SANOFI AVENTIS DEUT GMBH
Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof
InactiveUS20030065176A1Good choicePrevent coagulationOrganic compound preparationOrganic chemistry methodsPharmaceutical medicinePyrrole
The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.
Owner:LG CHEM INVESTMENT LTD
Pharmaceutical Composition Comprising A Plurality of Mini-Tablets Comprising A Factor XA Inhibitor
A modified release pharmaceutical composition for oral administration comprising plural mini-tablets, comprising a therapeutically effective amount of a Factor Xa inhibitor within a matrix of polymer(s). The mini-tablets are suitably encapsulated within a gelatin capsule. A manufacturing process and method of use are also described.
Owner:GLAXO GROUP LTD
Pyrrole-derivatives as factor Xa inhibitors
The present invention relates to compounds of the formulae I and Ia,wherein R0; R1; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae I and Ia are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and / or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and / or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and / or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae I and Ia, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Owner:SANOFI AVENTIS DEUT GMBH
Electrochemical Determination of Factor XA Inhibitors
ActiveUS20090236238A1Current maximum and retardedMaximum and retarded reactionImmobilised enzymesBioreactor/fermenter combinationsFactor XFactor ii
Methods and devices for determining factor Xa inhibitors, in particular heparins and fractionated or low-molecular-weight heparins, as well as direct factor Xa inhibitors in blood samples. The methods include contacting a blood sample with a detection reagent that contains at least one thrombin substrate having a peptide residue that can be cleaved by thrombin and is amidically bound via the carboxyl end to an electrogenic substance, and with a known amount of factor X reagent and an activator reagent which induces the conversion of factor X into factor Xa. Subsequently, in a second step, the amount or activity of the electrogenic substance that is cleaved from the thrombin substrate by the factor Xa-mediated thrombin activation and / or the time course thereof is determined as the measurement signal using electrochemical methods. In a third step, the amount of the factor Xa inhibitor in the sample of the blood to be analyzed or a measured quantity that correlates therewith, in particular a clotting time that correlates therewith, is determined on the basis of this measurement signal.
Owner:ROCHE DIAGNOSTICS OPERATIONS INC
Methods and formulations of treating thrombosis with betrixaban and a p-glycoprotein inhibitor
InactiveUS20120095019A1Increase exposureReduce the amount requiredBiocideAnimal repellantsBetrixabanFactor Xa Inhibitor
This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods.
Owner:ALEXION PHARMA INC
Use of dipyridamole in combination with antithrombotics for treatment and prevention of thromboembolic diseases
InactiveUS20090075949A1Good coagulationEnhancing thrombin formationBiocideSalicyclic acid active ingredientsAntithrombotic AgentDipyridamole
The invention relates to a method of treating and preventing thromboembolic disorders, comprising administering dipyridamole in combination with an antithrombotic selected from direct thrombin inhibitors, factor Xa inhibitors and combined thrombin / factor Xa inhibitors to a patient, pharmaceutical compositions suitable for this method of treatment as well as the use of dipyridamole for the manufacture of these pharmaceutical compositions.
Owner:EISERT WOLFGANG
Compositions and methods for cell transplantation
ActiveUS20150037291A1Effective and safe combinationAvoid harmful effectsOrganic active ingredientsBiocideEnzyme Inhibitor AgentFactor Xa Inhibitor
The present invention relates to compositions and methods for cell transplantation. In particular, the present invention provides a composition comprising procoagulant cells and at least one factor Xa inhibitor, preferably rivaroxaban, as well as at least one thrombin inhibitor, preferably bivalirudin.
Owner:UNIVERSITE CATHOLIQUE DE LOUVAIN
Solid dosage formulation containing a Factor Xa inhibitor and method
InactiveUS20050059719A1Improve oral bioavailabilityLow dissolutionBiocidePill deliverySolubilityCo administration
An oral solid dosage formulation is provided which contains a Factor Xa inhibitor for which oral bioavailability is not reduced by co-administration of antacids, H2 antagonists and proton pump inhibitors. Such solid dosage formulation includes the Factor Xa inhibitor of the structure, a pharmaceutically acceptable carrier, and an acid component, such as tartaric acid, whereby upon ingestion of the oral solid dosage formulation, the acid component increases solubility of the Factor Xa inhibitor in the local environment of the dissolving solid dosage formulation resulting in an otherwise lower degree of supersaturation of the Factor Xa inhibitor in such environment, than if the acid were not present. The result is that precipitation of the Factor Xa inhibitor in the form of its insoluble free base is minimized during dissolution of the Factor Xa inhibitor thereby increasing its oral bioavailability. A method for enhancing bioavailability of the Factor Xa inhibitor is also provided wherein an acid such as tartaric acid is incorporated with the solid dosage pharmaceutical carrier for the Factor Xa inhibitor.
Owner:BRISTOL MYERS SQUIBB CO
Method for determining coagulation inhibitors
ActiveCN102590490AMicrobiological testing/measurementBiological testingFactor Xa InhibitorBiochemistry
A homogeneous method of determining inhibitors of proteolytically active coagulation factors (anticoagulants) in a sample, in particular direct thrombin and factor Xa inhibitors, and also a test kit to be used in such a method. Use is made of ligands which bind to the proteolytically active coagulation factor but are not cleaved by the latter and compete with the anticoagulant to be determined.
Owner:SIEMENS HEALTHCARE DIAGNOSTICS PRODS
Method of determining inhibitors of coagulation
ActiveUS8889370B2Enhanced light scatteringMicrobiological testing/measurementBiological testingThrombin activityAnticoagulant
Owner:SIEMENS HEALTHCARE DIAGNOSTICS PRODS
FACTOR Xa INHIBITOR FORMULATION AND METHOD
An injectable Factor Xa inhibitor formulation is provided which includes the Factor Xa inhibitor razaxaban or apixaban, a solubilizing agent which is a substituted β-cyclodextrin, preferably, sulfobutyl ether β-cyclodextrin (SBE-CD) or hydroxypropyl-β-cyclodextrin (HPB-CD), and water. A method for preventing or treating venous thrombosis, deep venous thrombosis and acute coronary syndrome employing the above formulation is also provided.
Owner:BRISTOL MYERS SQUIBB CO
FACTOR Xa INHIBITOR FORMULATION AND METHOD
Owner:BRISTOL MYERS SQUIBB CO
METHOD OF TREATING PATIENTS COADMINISTERED A FACTOR Xa INHIBITOR AND VERAPAMIL
InactiveUS20190142839A1Moderate impairmentGuaranteed functionBlood disorderNitrile/isonitrile active ingredientsVerapamilFactor ii
The present disclosure in various embodiments teaches methods of treating patients in need of treatment with a Factor Xa inhibitor, and who are also concomitantly administered verapamil.
Owner:MORGANDANE SCI LLC
Factor Xa inhibitors
InactiveUS6759384B1Peptide/protein ingredientsMammal material medical ingredientsFactor VIII ActivityProteinase activity
The invention provides compounds which specifically inhibit factor Xa activity having the structure A1-A2-(A3)m-B, where m is 0 or 1. A compound of the invention is characterized, in part, in that it exhibits a specific inhibition of factor Xa activity with a Ki<=100 muM, preferably <=2 nM, and does not substantially inhibit the activity of other proteases involved in the coagulation cascade. The invention further provides methods of specifically inhibiting the activity of factor Xa and of inhibiting blood clotting in vitro and in an individual and methods of detecting factor Xa levels or activity.
Owner:SELECTIDE CORPORATIO
Pyrrolidin-2-one derivatives as inhibitors of factor Xa
Owner:GLAXO GRP LTD
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