83 results about "Factor Xa Inhibitor" patented technology

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

The invention relates to compounds of formula (Ic)processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.