Abstract:
Methods of modulating platelet procoagulant response are taught herein. Inhibition of platelet procoagulant response with agents that inhibit the Ca 2 +-sensitive K + channels, or Gardos channels, preferably while maintaining platelet bleeding arrest function, may be used to treat a variety of disorders.
Abstract:
The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4 (6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.
Abstract:
A platelet substitute consisting of large unilamellar lipid vesicles that contain phosphatidylserine or another procoagulant (clot-promoting) phospholipid, a protein that has binding affinity for collagen or other component of the vessel wall that becomes exposed upon vessel injury, and/or a phospholipid scramblase, has been developed. This platelet substitute provides a means for selectively delivering procoagulant phospholipids and/or fatty acids to the site of vessel injury through targeted adherence to collagen or other component exposed upon vessel injury. These are particularly effective due to the combination of targeting procoagulant vesicles to a site of injury, and triggered exposure of phosphatidylserine (PS) on the surface.
Abstract:
A platelet substitute consisting of large unilamellar lipid vesicles that contain phosphatidylserine or another procoagulant (clot-promoting) phospholipid, a protein that has binding affinity for collagen or other component of the vessel wall that becomes exposed upon vessel injury, and/or a phospholipid scramblase, has been developed. This platelet substitute provides a means for selectively delivering procoagulant phospholipids and/or fatty acids to the site of vessel injury through targeted adherence to collagen or other component exposed upon vessel injury. These are particularly effective due to the combination of targeting procoagulant vesicles to a site of injury, and triggered exposure of phosphatidylserine (PS) on the surface.
Abstract:
The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: (I) alone or in combination with a second agent which can be aspirin or a thrombolytic agent.
Abstract:
La presente descripción proporciona métodos para fabricar una proteína derivada de fXa a gran escala, lo que produce un alto rendimiento de producto proteico altamente puro. El método puede incluir agregar un detergente a una muestra que contiene una construcción de polinucleótidos que codifica la proteína y purifica la proteína a través de un cromatógrafo por afinidad basado en el inhibidor la tripsina de soja (STI), un cromatógrafo de modo mixto y de intercambio de iones y una interacción hidrofóbica.
Abstract:
The present disclosure provides methods for manufacturing a fXa derivative protein at large scale leading to high yield of highly pure protein product. The method may include adding a detergent to a sample that contains a polynucleotide construct encoding the protein and purifying the protein through a soybean trypsin inhibitor (STI)-based affinity chromatograph, an ion exchange and mixed mode chromatograph and a hydrophobic interaction.
Abstract:
Abstract - 599556 Disclosed herein is the use of a first therapeutic agent of [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2Hquinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for the treatment of a condition in a mammal selected from the group consisting of acute myocardial infarction, unstable angina, chronic stable angina, transient ischemic attacks, strokes, peripheral vascular disease, preeclampsia/eclampsia, deep venous thrombosis, embolism, disseminated intravascular coagulation and thrombotic cytopenic purpura, thrombotic and restenotic complications following invasive procedures resulting from angioplasty, carotid endarterectomy, post CABG (coronary arteryl bypass graft) surgery, vascular graft surgery, stent placements and insertion of endovascular devices and prosthesis, wherein the medicament is for administration in combination with a second therapeutic agent which is selected from the group consisting of a specific inhibitor of thrombin, a P-selectin inhibitor, a specific inhibitor of factor XIIa, low molecular weight heparin, acenocoumarol, clorindione, dicumarol, diphenadione, ethyl biscoumacetate, phenprocoumon, phenindione, tioclomarol, an anti-tissue factor antibody, fragmin, NAP-5, rNAPc2, a P2Y12 receptor antagonist, a tissue factor pathway inhibitor, ramatroban, terbogrel, (3-{ 6-[(4-chlorophenylsulfonyl)amino]-2-methyl-5,6,7,8-tetrahydronaphth-1-yl} propionic acid, ethyl (1R,3aR,4aR,6R, 8aR, 9S, 9aS)-9-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-1-methyl-3-oxododecahydronaphtho[2,3-C] furan-6-ylcarbamate, 2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid, naproxen, sulindac, indomethacin, mefenamate, droxicam, diclofenac, sulfinpyrazone, piroxicam, ibuprofen, a beta blocker, a calcium channel blocker and PSGL-1.
Abstract:
Disclosed herein is the use of a first therapeutic agent of [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2Hquinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for the treatment of a condition in a mammal selected from the group consisting of acute myocardial infarction, stable angina, chronic stable angina, transient ischemic attacks, strokes, peripheral vascular disease, preeclampsia/eclampsia, deep venous thrombosis, embolism, disseminated intravascular coagulation and thrombotic cytopenic purpura, thrombotic and restenotic complications following invasive procedures resulting from angioplasty, carotid endarterectomy, post CABG (coronary arteryl bypass graft) surgery, vascular graft surgery, stent placements and insertion of endovascular devices and prosthesis, wherein the medicament is for administration in combination with a second therapeutic agent which is selected from the group consisting of betrixaban, a specific inhibitor of factor IXa, a specific inhibitor of factor XI, a specific inhibitor of factor XIa, a specific inhibitor of factor VIIa, YM-150, Daiichi DU-176b, N-{ (1R)-2-[4-(1-methyl-4-piperidinyl)-1-piperazinyl]-2-oxo-1-phenylethyl} -1H-indole-6-carboxamede, apixaban, rivaroxaban, otamixaban, razaxaban, AZD0837, RB2006, ximelagatran, dabigatran, bivalirudin, argatroban, phenocoumarol, synthetic pentasaccharides, such as fondaparinux, idraparinux, biotinylated idraparinux; abciximab, eptifibatide, tirofiban, dipyridamole, Aggrenox, cilostazol, ifetroban, isogrel, furegrelate, resveratrol, ozagrel, an anticoagulant agent and an antiplatelet agent.
Abstract:
La presente invenci?n proporciona m?todos y composiciones para la inhibici?n r?pida e irreversible de la agregaci?n de plaquetas en los sujetos humanos que los necesitan administrando los compuestos de la f?rmula: (I) solos o en combinaci?n con un segundo agente el cual puede ser aspirina o un agente anti trombol?tico.