 Patent Application Title |
Patent App Num. |
Date |
| Seroma control for surgical patients | 20120016347 | 20120119 |
| Apparatus and methods for significant reduction of seroma formation, seroma related complications and time until drain removal following surgery are disclosed. Talc, with and without thrombin, bleomycin, erythromycin, tetracycline, doxycycline, polidocanol alone or in combination or combined with talc and/or thrombin for use in operatives wound and lymph node dissections to reduce seromas are disclosed.
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| Method of using salmon thrombin to alleviate pain | 20120009175 | 20120112 |
| A method of alleviating pain associated with tissue damage includes applying salmon thrombin at a tissue damage site, as a single substance in liquid form, or as a powder, a foam, and/or a gel that includes salmon thrombin. A pain relief substance includes a salmon thrombin preparation.
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| Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders | 20120003227 | 20120105 |
| Disclosed herein are methods for treating a vascular inflammatory disorder or endothelial cell disorder using inhibitor compounds that inhibit the expression or biological activity of Tie-1, Tie-1 endodomain, thrombin, VEGFR2, VEGFR2 endodomain, EphA2, and any of the cytokines or kinases that are upregulated by activation of Tie-1 or thrombin, as provided herein. Also disclosed are the use of combinations of inhibitor compounds or the use of an eNOS activator compound in combination with any one or more of the inhibitor compounds. Also disclosed are methods for inhibiting the pro-coagulant activity of thrombin using a Tie-1 or Tie-1 endodomain inhibitor compound or an EphA2 inhibitor compound. Methods for diagnosing and monitoring vascular inflammatory disorders or endothelial cell disorders that include the measurement of any of the polypeptides... |
| Medicinal products for the treatment of blood coagulation disorders | 20110318330 | 20111229 |
| A virally safe, thrombin-free factor-Xla concentrate or a coagulation factor concentrate which contains factor XIa as an active pharmaceutical ingredient and which is obtained by fractionation of plasma or serum or by genetic engineering and is suitable for the treatment of coagulation disorders attributable to diminished and/or delayed thrombin formation.
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| Methods for treating cancer | 20110319340 | 20111229 |
| The present invention includes methods of treating cancer in a subject, comprising administering to the subject a therapeutically effective amount of a non-proteolytically activated thrombin receptor agonist.
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| Methods for reducing platelet activation and for the treatment of thrombotic events | 20110319349 | 20111229 |
| or its pharmaceutically acceptable salt, ester or prodrug, wherein the substituents are defined herein, optionally in the appropriate pharmaceutically acceptable carrier for the route of administration selected.
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| Fused ring thrombin receptor antagonists | 20110301112 | 20111208 |
| represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
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| Inhibitors of plasma kallikrein | 20110301215 | 20111208 |
| The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.
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| Transgenic prothrombin and related thrombin precursors and transgenics, methods, compositions, uses and the like relating thereto | 20110283375 | 20111117 |
| The invention provides, among other things, activatable prothrombin, compositions comprising prothrombin, transgenic organisms for making prothrombin, methods for making the transgenic organisms, methods for making prothrombin-comprising compositions and for further purifying prothrombin from the compositions. Illustrative embodiments of the invention particularly provide transgenic mammals that express an exogenous gene for prothrombin and excrete the prothrombin encoded by the gene into their milk. In a highly particular illustrative embodiment in this regard the invention provides transgenic female pigs that express prothrombin in their milk. In this regard, the invention relates particularly to female pigs having stably incorporated in their genomes a DNA comprising a region that encodes prothrombin operably linked to a mammary gland-specific promoter. Further in this regard the invention relates to the milk containing the... |
| Unsaturated fatty acids as thrombin inhibitors | 20110268800 | 20111103 |
| A preparation having at least one unsaturated fatty acid and the use of at least one unsaturated fatty acid having a chain length of 18 or 20 carbon atoms and of plant drugs containing the unsaturated fatty acid as a free fatty acid or a fatty acid radical of a triglyceride. The fatty acid has a chain length of 18 carbon atoms which are provided with 1 to 3 double bonds and the fatty acid has a chain length of 20 carbon atoms which are provided with 1 to 4 double bonds. The double bond or one of the double bonds are located in position 9 or 11 of the carbon chain. The unsaturated fatty acid is supplied in the all-cis configuration. The at least one... |
| Exo- and diastereo- selective synthesis of himbacine analogs | 20110251392 | 20111013 |
| This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
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| Haemostatic kit, a method of preparing a haemostatic agent and a method of promoting haemostatis | 20110245867 | 20111006 |
| A haemostatic kit to be used as a medical device provides for a containment unit and a haemostatic agent in said containment unit, said haemostatic agent occupying less than 90% of the volume of the containment unit. This allows for facile and consequently sterile preparation of, for instance, a gelatin paste for use in haemostatis when combined with saline, thrombin or another agent to assist in haemostatis.
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| Compositions and methods of use for soluble thrombomodulin variants | 20110207670 | 20110825 |
| The present invention provides a method for preventing and/or treating a patient with acute kidney injury caused by a variety of conditions. The method comprises administering to the patient soluble thrombomodulin variants that do not bind thrombin. In conjunction with standard of care, soluble thrombomodulin variants that do not bind thrombin will prevent or reduce acute kidney injury and subsequent morbidity and mortality.
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| method and assembly for measuring thrombin generation in plasma | 20110195441 | 20110811 |
| Disclosed is a method for measuring thrombin generation in a whole blood sample. The whole blood sample may be applied forthwith, without prior processing. The blood cells and blood plasma in the whole blood sample are separated by (lateral) flow migration. Also disclosed is an assembly of a sample support and a device dedicated to measure thrombin generation in a whole blood sample. Advantageously, the sample support comprises a separator medium allowing separation of whole blood into blood cells and blood plasma by means of (lateral) flow migration.
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| Thrombin generation determination method | 20110183365 | 20110728 |
| A method for measuring a generation of thrombin in a sample of whole blood as a function of time includes adding to a sample of whole blood a fluorogenic substrate and a thrombin activator to form an activated sample. A conversion product is permitted to form in the activated sample. Fluorescence is measured as a function of time from a fluorescent group that is released during the formation of the conversion product with the use of a fluorescence detector. The fluorescence detector operates in an extended range mode and has an increased sensitivity. Thrombin generation as a function of time can then be calculated from the measured fluorescence as a function of time.
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| Medical devices for delivering fluids during surgery and methods for their use | 20110166550 | 20110707 |
| Provided is a surgical applicator and applicator tip configured to attach in fluid communication, for the delivery of beneficial fluids. The applicator tip may also be configured to reversibly attach, in fluid communication, with a pledget. For example, the applicator tip may include male or female threads, and the pledget has threads that are complementary to the thread configuration of the tip. The applicator tip may further comprise at least one fluid transfer lumen for transfer of a fluid from the tip to the pledget. In one embodiment of the invention, the tip includes male threads and the pledget includes a pledget attachment portion. There are also provided methods for connecting the tip to the pledget. In one embodiment, a tip comprising male threads is attached... |
| Thrombin activator compositions and methods of making and using the same | 20110151536 | 20110623 |
| Disclosed are compositions for activating thrombin precursors to thrombin. The compositions provided include polypeptide compositions wherein the pre-pro-sequence comprises a thrombin cleavage site. The compositions provided also include polynucleotides encoding said polypeptides and recombinant systems for expressing said polypeptides. This disclosure also relates to methods for producing said compositions, recovering said compositions, activating said compositions purifying said compositions and producing active thrombin molecules using the active form of said compositions.
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| Electrospun dextran fibers and devices formed therefrom | 20110150973 | 20110623 |
| The invention generally relates to dextran fibers which are preferably electrospun and devices formed from such fibers. In particular, such devices may include substances of interest (such as therapeutic substances) associated with the electrospun fibers. Upon exposure to a liquid the electrospun fibers dissolve immediately and the substances of interest are released into the liquid. Exemplary devices include bandages formed from electrospun dextran fibers and associated agents that promote hemostasis, such as thrombin and fibrinogen.
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| Heterocyclic carboxamides for use as thrombin inhibitors | 20110130432 | 20110602 |
| This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production. Formula (I)
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| Thrombin derived peptides for smooth muscle relaxation | 20110117075 | 20110519 |
| Agonists of a non-proteolytically activated thrombin receptor, and more particularly, thrombin peptide derivatives, can be used in methods to cause smooth muscle relaxation. Compositions comprising thrombin peptide derivatives can be administered to a subject with a disease or disorder that can be ameliorated by relaxation of smooth muscle. Such compositions can also be administered to a subject to facilitate medical, diagnostic or surgical procedures.
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| Chlorothiophene-amides as inhibitors of coagulation factors xa and thrombin | 20110112075 | 20110512 |
| wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in... |
| Chlorothiophene-isoxazoles as inhibitors of coagulation factors xa and thrombin | 20110112074 | 20110512 |
| wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are 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... |
| Method of treating peripheral arterial disease | 20110110920 | 20110512 |
| An agonist of a non-proteolytically activated thrombin receptor can be used in a method for treating peripheral arterial disease. The agonist can be a thrombin peptide derivative. In some embodiments, the peripheral arterial disease is characterized by intermittent claudication. The thrombin peptide derivatives to be used in the methods can have amino acid sequences similar to a region of thrombin. Usually, the thrombin peptide derivatives are 12-23 amino acid residues in length. In some cases, the thrombin peptide derivatives are dimers, and in particular, dimers that result from formation of a disulfide bond between two cysteine residues of peptide monomers.
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| Methods for treating bleeding disorders | 20110110921 | 20110512 |
| A method of factor XI-dependent blood coagulation enhancement in a subject in need of enhanced blood coagulation comprising administering a therapeutically effective amount of a composition comprising a non-anticoagulant sulfated polysaccharide (NASP) to the subject. A method of factor XI-dependent blood coagulation enhancement in a subject in need of enhanced blood coagulation comprising: (i) selecting a subject that is not deficient for factor XI; and (ii) administering a therapeutically effective amount of a composition comprising a non-anticoagulant sulfated polysaccharide (NASP) to the subject, wherein the NASP enhances blood coagulation in a factor XI-dependent manner. A method of identifying a non-anticoagulant sulfated polysaccharide (NASP) which is capable of enhancing blood coagulation in dependence on FXI, the method comprising: a) combining a blood or plasma sample comprising activation... |
| Process for the preparation of pyrazinone thrombin inhibitor and its intermediates | 20110105753 | 20110505 |
| Improved process for the preparation of 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide of formula (I) and its intermediates is provided.
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| 2,3-dihydro-1h-isoindol-1-imine derivatives useful as thrombin par-1 receptor antagonist | 20110105490 | 20110505 |
| The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.
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| Methods for treating acute myocardial infarction | 20110105400 | 20110505 |
| The present invention includes methods of treating acute myocardial infarction in a subject, comprising administering to the subject a therapeutically effective amount of a non-proteolytically activated thrombin receptor agonist.
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| Method for measuring activated factor vii level in a sample | 20110097754 | 20110428 |
| The present disclosure relates to a method for measuring the activated factor VII level in a sample to be tested, including the steps of: a) mixing the test sample with a plasma free of factor VII (FVII) and free of at least another factor selected from among factor VIII (FVIII), factor IX (FIX), and factor XI (FXI), the test sample+plasma having a final FVII+FVIIa concentration of 10 pM to 80 pM; b) adding initiating components from the thrombin generation reaction; c) obtaining a thrombogram when carrying out a thrombin generation test (TGT) on the mixture from step b); d) comparing at least one of the thrombogram parameters from step c) with a homologous parameter obtained from standard thrombograms established on the basis of standard samples, the... |
| Hcv e2 construct compositions and methods | 20110091495 | 20110421 |
| A construct comprising the ectodomain of the Hepatitis C Virus (HCV) E2 sequence and a mammalian expression system therefor is disclosed. The construct comprises a CMV promoter, prolactin signal sequence, the ectodomain of HCV E2 sequence truncated at aa 664, a thrombin cleavage site and a human Fc domain. The method also relates to an expression system for the construct, which is stably expressed in human embryonic kidney cells 293T. Continuous protein expression in a bioreactor allows for 4 mg of purified protein per liter of cell supernatant.
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| Heparin-conjugated fibrin gel and method and kit for preparing same | 20110091443 | 20110421 |
| A method of preparing a heparin-conjugated fibrin gel is provided, which includes activating heparin, conjugating the activated heparin with fibrinogen to prepare heparin-conjugated fibrinogen, mixing free fibrinogen with the heparin-conjugated fibrinogen to prepare a fibrinogen mixture, and mixing thrombin with the fibrinogen mixture. In addition, a heparin-conjugated fibrin gel prepared by the above method and a kit for preparing the same are provided. According to the method of preparing the heparin-conjugated fibrin gel, the heparin-conjugated fibrin gel having an affinity for drugs such as growth factors may be easily prepared at low costs, and can also be used as a therapeutic drug excellently effective on generation of tissues such as bones, skin, blood vessels, cartilages, etc. by sustainably releasing drugs such as growth factors to a... |
| New paediatric indications for direct thrombin inhibitors | 20110015129 | 20110120 |
| The invention relates to new paediatric indications for direct thrombin inhibitors such as dabigatran etexilate.
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| Biological bioadhesive compositions and methods of preparation and use | 20110008316 | 20110113 |
| The present invention relates generally to the preparation and use of biological tissue adhesives which rely on combining fibrinogen and thrombin. More particularly, the present invention relates to a method of preparing a fibrin sealant whereby said sealant is formed by reconstituting the fibrinogen or the thrombin component in the presence of biological and/or non-biological agents such as drugs, chemicals, and proteins. Preferably, these agents are introduced in solution, such as for example, a corticosteroid-containing solution like a betamethasone solution containing betamethasone acetate or betamethasone sodium phosphate; a triamicinolone solution; or a methylprednisolone solution. These solutions may be substituted for, or provided as a complement to, other solutions that are typically used in the preparation of fibrin sealants such as, for example, calcium chloride. The invention... |
| Combination therapy for chronic dermal ulcers | 20100330028 | 20101230 |
| Disclosed is a method of promoting healing of a chronic dermal ulcer, such as a diabetic ulcer, in a subject. The method comprises administering to the subject a combination one or more agonists of the non-proteolytically activated thrombin receptor and one or more angiogenic growth factors.
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| thrombin function compounds and pharmaceutical compositions based on them | 20100324058 | 20101223 |
| This invention relates to new chemical compounds, application of these compound as thrombin inhibitors, and pharmaceutical compositions based on them, and can be used to treat and prevent thrombin-dependent thromboembolic events, and in research.
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| Combined vascular and closure sheath | 20100312273 | 20101209 |
| The technology described herein provides an apparatus and associated methods for the rapid percutaneous occlusion of a vascular access site. In one exemplary embodiment, a combined vascular and closure sheath is provided. This device includes a vascular sheath having a vascular sheath lumen, a proximal end and a distal end, and an exterior surface. The combined vascular and closure sheath includes a closure sheath, being lesser in length and greater in diameter than the vascular sheath and having a proximal end and a distal end, disposed circumferentially around the exterior surface of the vascular sheath at the proximal end of the vascular sheath, thereby forming a closure sheath lumen between the exterior surface of the vascular sheath and an interior surface of the closure sheath, the... |
| Aminoisoquinoline thrombin inhibitor with improved bioavailability | 20100305153 | 20101202 |
| The invention relates to the compound N-(2-oxo-2-propoxyethyl)-β-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.
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| Combination therapy for cardiac revascularization and cardiac repair | 20100303793 | 20101202 |
| An agonist of the non-proteolytically activated thrombin receptor and an angiogenic growth factor can be used in combination in methods of therapy to stimulate cardiac revascularization, to stimulate vascular endothelial cell proliferation, to stimulate vascular endothelial cell migration and to promote repair of cardiac tissue.
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| Use of mutated antithrombins for treating or preventing coagulation disorders | 20100298224 | 20101125 |
| Use of a mutated antithrombin having substantially no activity, in particular no anticoagulant activity, possibly in association with an anticoagulant, for the preparation of a drug intended for the prevention or treatment of pathologies linked to or associated with coagulation disorders.
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| Fusion tag comprising an affinity tag and an ef-hand motif containing polypeptide and methods of use thereof | 20100297734 | 20101125 |
| The application discloses a fusion tag comprising an affinity tag and a polypeptide comprising one or more EF hand motif(s). Preferably, said fusion tag comprises a polyhistidine tag, one or more EF hand motif(s) of calmodulin and a thrombin cleavage site. Methods of using said fusion tag to purify a polypeptide of interest are also disclosed.
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| Composition for treating retinopathy or glaucoma comprising thrombin derived peptides | 20100297100 | 20101125 |
| Disclosed is a composition for treating retinopathy comprising thrombin derived peptide as an effective component.
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| Antibiotic formulation and method of treatment | 20100291220 | 20101118 |
| A formulation comprised of particles which may be in groups and are comprised of a biocompatible polymer and an antimicrobial drug for controlled release of the drug is disclosed. The particles may be in an aqueous solution comprising thrombin and be dispersed in a gel. The formulation is administered to an area such as an open wound having an orthopedic implant therein and provides a therapeutically effective level of drug to the patient over therapeutically effective period of time.
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| Compositions and methods for fusion protein separation | 20100285526 | 20101111 |
| The present invention relates to compositions and methods for fusion protein separation utilizing a peptide linker comprising a novel thrombin cleavage site.
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| Antibiotic/bone morphogenic protein formulation and method of treatment | 20100285137 | 20101111 |
| A formulation comprised of particles which may be in groups and are comprised of a biocompatible polymer and an antimicrobial drug for controlled release of the drug is disclosed. The particles may be in an aqueous solution comprising thrombin and be dispersed in a gel. The formulation is administered to an area such as an open wound having an orthopedic implant therein and provides a therapeutically effective level of drug to the patient over therapeutically effective period of time.
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| Fibrin sealant | 20100284998 | 20101111 |
| A fibrin sealant, comprises (a) thrombin, (b) fibrinogen, (c) polyP, and (d) calcium. The thrombin and the fibrinogen are separated prior to application.
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| Injectable radio-opaque compositions for tissue augmentation | 20100284919 | 20101111 |
| Injectable radio-opaque compositions for tissue augmentation and in particular hard tissue augmentation, and kits and methods of using thereof are described herein. The injectable compositions form porous, biologically degradable, fibrin matrices. The compositions are formed from fibrinogen, thrombin or another agent that causes the fibrinogen to crosslink, and strontium salts. Optionally an iodinated contrast agent is further incorporated in the composition. In certain aspects, the compositions have substantially no exothermicity when forming the matrix and the resulting matrices exhibit mechanical properties typically seen in elastomers. Adequate radio-opacity is achieved through the incorporation of strontium salts in combination or not with iodinated contrast agents.
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| Transgenic production in saliva | 20100281549 | 20101104 |
| The invention relates to the production of proteins and other substances of interest in saliva of transgenic animals, particularly in mammals that produce large quantities of saliva, particularly monogastric ruminants, and ovine, caprine and bovine mammals. Preferred embodiments of the invention relate in particular to the production of foreign and modified proteins in the transgenic saliva of these animals, including particularly human fibrinogen, human prothrombin and human thrombin, among others. The invention relates as well to methods, devices, genetic constructs and to transgenic constructs for making the proteins and other substances of interest, to novel saliva and saliva-derived compositions, novel products produced from the saliva, and to uses of the saliva, saliva-derived compositions and novel products.
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| Anticoagulation of human blood ex vivo | 20100280412 | 20101104 |
| The present invention relates to a method for the anticoagulation of human blood ex vivo in which blood calcium concentration remains the same, no thrombin is formed and thrombocyte function is not affected. The invention further relates to a blood coagulation factor Xa inhibitor that can be advantageously used in this method, an agent that contains an inhibitor of the blood coagulation factor Xa, and a kit for diagnosing cellular blood components. The anticoagulated blood obtained according to the invention can be used for examining cellular blood components, for example for the diagnosis of thrombocyte function.
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| Exo-selective synthesis of himbacine analogs | 20100267947 | 20101021 |
| This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
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| Exosite-directed thrombin inhibitors | 20100267638 | 20101021 |
| Disclosed are an amino acid sequence of the human blood clotting factor Va, peptides containing such sequence, and additional peptides of interest that significantly inhibit thrombin generation. Also disclosed are pharmaceutical compositions containing these peptides and related therapeutic methods for inhibiting thrombin generation and treating blood coagulation disorders.
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| Purification and use of a factor for supporting wound healing | 20100261651 | 20101014 |
| A process for manufacturing of a composition containing a purified factor for supporting wound healing selected from the group consisting of Hepatocyte Growth Factor (HGF) platelet derived growth factor (PDGF), Epidermal growth factor (EGF), transforming growth factor alfa (TGF-α), Transforming growth factor beta (TGF-β), insulin like growth factor (IGF-1) and Fibroblast growth factor (FGF) from sources, such as blood, containing the factor for supporting wound healing, wherein the manufacturing process comprises purification steps which are performed in the presence of antithrombin III (AT-III).
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| Antidotes for factor xa inhibitors and methods of using the same | 20100255000 | 20101007 |
| 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.
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| Apparatus and method for electrochemical detection | 20100252452 | 20101007 |
| The present invention is directed to a sensor with opposing electrodes and test strips using this sensor. The invention can be used to measure blood or plasma coagulation in assays like prothrombin time (PT) and thrombin potential, for example, in point-of-care monitoring of anticoagulants.
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| agent for reducing a side effect of an anticancer drug | 20100247510 | 20100930 |
| The present invention provides an agent for reducing a side effect of an anticancer drug, which comprises a thrombin-like enzyme.
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| Apparatus and method for assaying coagulation in fluid samples | 20100240136 | 20100923 |
| This invention is a disposable cartridge for use at the patient side to perform traditional coagulation assays on fresh whole blood or blood derivative samples. The cartridge, in use with an electronic analyzer allows a fluid sample to be metered and quantitatively mixed with reagents which activate the coagulation cascade. An artificial substrate for thrombin, the enzyme whose action results in clot formation is also provided. Clot formation is subsequently detected using a microfabricated sensor also housed within the cartridge which detects electrochemically the product of the thrombin reaction upon the synthetic substrate.
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| Apparatus and method for assaying coagulation in fluid samples | 20100240067 | 20100923 |
| This invention is a disposable cartridge for use at the patient side to perform traditional coagulation assays on fresh whole blood or blood derivative samples. The cartridge, in use with an electronic analyzer allows a fluid sample to be metered and quantitatively mixed with reagents which activate the coagulation cascade. An artificial substrate for thrombin, the enzyme whose action results in clot formation is also provided. Clot formation is subsequently detected using a microfabricated sensor also housed within the cartridge which detects electrochemically the product of the thrombin reaction upon the synthetic substrate.
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| Multi component non-woven | 20100239560 | 20100923 |
| The formation of a non-woven, free from organic solvent, formed through parallel formation of fibers on a collection device is disclosed. As the individual fibers are dry prior to contact with other fibers, the different contents of the various fiber types do not interact. However, when wetted, the fibers will start to be dissolved, or swell, and the different contents will be released and then interact. For the example of thrombin and fibrinogen, the interaction will initiate the formation of a fibrin coagulum by the cleavage of fibrinogen through the action of thrombin to form fibrin monomers that spontaneously polymerize to form a three dimensional network of fibrin.
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| Preparation and use of low-bleeding anticoagulant fusion protein | 20100234291 | 20100916 |
| Provided is an anticoagulant fusion protein comprising oligopeptide recognizable and cleavable by either factor XIa and factor Xa or thrombin and factor Xa. Also provided are the preparation method of the anticoagulant fusion protein and medicinal use thereof.
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| Method and apparatus for producing autologous thrombin | 20100226909 | 20100909 |
| A device for isolating a component of a multi-component composition. The device includes a housing, a chamber, and a withdrawal port. The chamber is rotatably mounted within the housing. The chamber includes a chamber base and a sidewall. The side wall extends from the chamber base. At least a portion of the sidewall is defined by a filter that permits passage of a first component of the multi-component composition out of the chamber through the filter and to the housing base. The filter restricts passage of a second component of the multi-component composition through the filter. The withdrawal port extends from a position proximate to the housing base to an exterior of the device. The withdrawal port permits the withdrawal of the first component from the... |
| Protease-stable, cell wall-lysing enzymes | 20100216711 | 20100826 |
| The present invention relates to a modified polypeptide with a biological activity to lyse cell walls of bacteria, wherein the polypeptide has no caspase, clostripain, enterokinase, factor Xa, granzyme B, staphylococcus peptidase I (V8 Protease), plasmin, streptopain, bacillolysin and/or thrombin cleavage site. The invention further relates to nucleic acids with a sequence encoding a polypeptide according to the present invention.
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| Method of evaluating thrombogenic microparticles | 20100216174 | 20100826 |
| A method and a kit are disclosed for evaluating thrombogenic microparticles (MP). The principle is based on the evaluation of thrombin generation in platelet poor plasma (PPP) and in plasma made microparticle free (MPFP) by centrifugation or filtration. The difference in thrombin generation between PPP and MPFP correlates with number and activity of thrombogenic microparticles. Evaluating thrombin generation of different standardized amounts of MPs in standard MPFP allows to calculate the number of thrombogenic MP from the difference in thrombin generation between PPP and MPFP.
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| Controlled release endoprosthetic device | 20090326633 | 20091231 |
| wherein the micro-deepenings of said structural member and/or said polymer member comprise a pharmaceutical composition containing one or more active ingredients selected from the group consisting of agents to inhibit or at least reduce excessive proliferation of vessel wall cells, agents to enhance the downstream perfusion of tissue, agents to promote and/or to enhance the neo-formation of capillaries, agents designed to modulate the amount or activity of coagulation factors, agents to reduce the amount of Thrombin- and/or Fibrin-formation, embedded therein for release from the member, with such in its expanded state.
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| Novel compounds 148 | 20090318517 | 20091224 |
| This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.
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| Measuring thrombin activity in whole blood | 20090311730 | 20091217 |
| The invention relates to a method for in vitro determining thrombin activity in a sample wherein the sample is a blood sample and thrombin generation is measured by the steps of: —contacting a layer of said sample with a fluorogenic substrate of thrombin, wherein said layer has a thickness within a range of 0.05 to 5 mm and a surface within a range of 10 to 500 mm2; —allowing thrombin to generate in said sample; —measuring the fluorescence emitted from the surface of the layer, by the fluorescent group released from the fluorogenic substrate as a result of enzymatic action of generated thrombin on said fluorogenic substrate.
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| Method of treating endothelial dysfunction | 20090304671 | 20091210 |
| Endothelial dysfunction (ED) is associated with a number of diseases and disorders. Agonists of the non-proteolytically activated thrombin receptor can be used in methods to treat ED or ED-related diseases and disorders.
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| Method of preparing cell for bone tissue formation and application of cell for bone tissue formation | 20090298173 | 20091203 |
| It is intended to provide a method of efficiently and stably preparing a cell having a bone tissue formation ability by a simple operation. Further, it is intended to provide a method of preparing a composition for bone tissue formation with high safety and an excellent therapeutic effect by a simple operation. The cell for bone tissue formation is obtained by (1) culturing bone marrow after isolating it from a living body, diluting it at a predetermined dilution ratio and inoculating it to a culture vessel, (2) culturing the remaining adhesive cells after removing floating components, (3) inducing differentiation of proliferated cells to bone cells and (4) recovering the cells. The thus obtained cells, a thrombin solution, platelet-rich plasma and air are mixed at a predetermined... |
| Novel thrombolytic enzyme and a process for its preparation | 20090285793 | 20091119 |
| The invention relates to a thrombolytic enzyme referred to as Thrombinase having a molecular weight of 31,000 to 32,000. Such a thrombolytic enzyme can be used for dissolving blood clots. The process comprises culturing a filtrate of Bacillus sphaericus sero type H5a 5b, removing the cell, subjecting the cell supernatant to filtration, salting out the retentate, subjecting the precipitate to dialysis, reprecipitating the precipitate and then reconstituting in buffer and finally decolourizing, purifying and dialyzing.
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| Exo- and diastereo- selective syntheses of himbacine analogs | 20090281321 | 20091112 |
| This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
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| Exo- and diastereo- selective syntheses of himbacine analogs | 20090281321 | 20091112 |
| This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
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| Method and apparatus for determining hemocompatibility | 20090269790 | 20091029 |
| Provided herein are techniques for screening materials for hemocompatibility. Hemocompatible materials may be advantageous when incorporated into devices that may come into direct contact with blood or other bodily fluids. Such techniques take advantage of conformational changes in fibrinogen when adsorbed onto certain materials. As a result of conformational changes, the fibrinogen has altered responsiveness to cleavage by thrombin. Accordingly, the products of thrombin cleavage of fibrinogen may be assessed to determine the hemocompatibility of a material.
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| Methods for controlling angiogenesis and cell proliferation | 20090269422 | 20091029 |
| The present invention relates generally to methods of inhibiting angiogenesis in a patient by administering an effective angiogenesis-inhibiting amount of a thrombin inhibitor, and to the treatment of disease states that result from uncontrolled cell proliferation by administering a thrombin inhibitor alone or co-administering a thrombin inhibitor with an anticancer or cytotoxic agent. Specifically, the thrombin inhibitors used in the methods of the present invention are hirudins.
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| Methods for controlling angiogenesis and cell proliferation | 20090269422 | 20091029 |
| The present invention relates generally to methods of inhibiting angiogenesis in a patient by administering an effective angiogenesis-inhibiting amount of a thrombin inhibitor, and to the treatment of disease states that result from uncontrolled cell proliferation by administering a thrombin inhibitor alone or co-administering a thrombin inhibitor with an anticancer or cytotoxic agent. Specifically, the thrombin inhibitors used in the methods of the present invention are hirudins.
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| Method and apparatus for determining hemocompatibility | 20090269790 | 20091029 |
| Provided herein are techniques for screening materials for hemocompatibility. Hemocompatible materials may be advantageous when incorporated into devices that may come into direct contact with blood or other bodily fluids. Such techniques take advantage of conformational changes in fibrinogen when adsorbed onto certain materials. As a result of conformational changes, the fibrinogen has altered responsiveness to cleavage by thrombin. Accordingly, the products of thrombin cleavage of fibrinogen may be assessed to determine the hemocompatibility of a material.
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| Method for determining prothrombin time | 20090263903 | 20091022 |
| The present invention relates to tests for monitoring oral anticoagulation therapy and hepatocellular carcinoma (HCC). Particularly, the invention provides a method for determining prothrombin time of a plasma or whole blood sample taking account the effect which protein induced by vitamin K absence or antagonists (Pivka) has on clotting time and INR result. The primary object of the invention is to harmonise prothrombin time methods for international normalized ratio (INR) results and measure INRpivka.
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| Thiophene derivatives as factor xia inhibitors | 20090253766 | 20091008 |
| or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, L1, R3, and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
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| Simple method of transplanting injectable chordrocyte for autologous chondrocyte transplantation | 20090254065 | 20091008 |
| A method of transplanting an injectable chondrocyte is developed for autologous chondrocyte transplantation, comprising mixing matrices including fibrin, hyaluronic acid and collagen, which are the main ingredients of animal cartilage, and injecting the resulting mixture into a damaged cartilage region. One 1 ml syringe is prepared by mixing 1 ml of a chondrocyte culture with white or light-yellow lyophilized powder (fibrinogen). A second 1 ml syringe is prepared by mixing 1 ml of chondrocyte culture with white lyophilized powder (thrombin), adding 0.1 cc of that mixture to the entire contents of two vials containing chondrocyte suspension, and mixing well. The two syringes are then mounted on a syringe stand, and a mixing tip is mounted to their tips. The contents are mixed in the mixing tip... |
| Thiophene derivatives as factor xia inhibitors | 20090253766 | 20091008 |
| or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, L1, R3, and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
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| Simple method of transplanting injectable chordrocyte for autologous chondrocyte transplantation | 20090254065 | 20091008 |
| A method of transplanting an injectable chondrocyte is developed for autologous chondrocyte transplantation, comprising mixing matrices including fibrin, hyaluronic acid and collagen, which are the main ingredients of animal cartilage, and injecting the resulting mixture into a damaged cartilage region. One 1 ml syringe is prepared by mixing 1 ml of a chondrocyte culture with white or light-yellow lyophilized powder (fibrinogen). A second 1 ml syringe is prepared by mixing 1 ml of chondrocyte culture with white lyophilized powder (thrombin), adding 0.1 cc of that mixture to the entire contents of two vials containing chondrocyte suspension, and mixing well. The two syringes are then mounted on a syringe stand, and a mixing tip is mounted to their tips. The contents are mixed in the mixing tip... |
| Reinforced absorbable multilayered hemostatic wound dressing | 20090246238 | 20091001 |
| The present invention is directed to a reinforced absorbable multilayered hemostatic wound dressing comprising a first absorbable nonwoven fabric, a second absorbable woven or knitted fabric, thrombin and/or fibrinogen.
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| Fibrin foam and process | 20090246260 | 20091001 |
| A fibrin wound dressing is made by mixing quantities of fibrinogen solution and thrombin solution with air. The resulting foam is very light weight, and with the proper attention to the amount of thrombin, is also sufficiently viscous to rest on a vertical surface without dripping. The wound dressing may also be formulated for its ability to continue migration of healing substances, such as PDGF, from the dressing to the wound site. Thrombin substitutes, such as other clotting proteins, may be used instead of thrombin. The resulting foam may also be lyophilized or ground and lyophilized for later reconstitution. A therapeutic drug or other additive may also be added to the wound dressing.
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| Fibrin foam and process for making | 20090246261 | 20091001 |
| A fibrin wound dressing is made by mixing quantities of fibrinogen solution and thrombin solution with air. The resulting foam is very light weight, and with the proper attention to the amount of thrombin, will rest on a vertical surface without dripping. The wound dressing may also be formulated for its ability to continue migration of healing substances, such as PDGF, from the dressing to the wound site. Thrombin substitutes, such as other clotting proteins, may be used instead of thrombin. The resulting foam may also be lyophilized or ground and lyophilized for later reconstitution. A therapeutic drug or other additive may also be added to the wound dressing. A fibrin foam may be made by injecting fibrinogen foam into a clotting protein, such as thrombin.
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| Novel use of bivalirudin in the treatment of acute coronary syndrome | 20090247465 | 20091001 |
| A method of treating acute coronary syndrome (ACS) in a patient, comprising administering a therapeutically effective amount of an indirect thrombin inhibitor to the patient, and subsequently administering a therapeutically effective amount of a direct thrombin inhibitor to the patient wherein the direct thrombin inhibitor is administered prior to and during an invasive bodily procedure.
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| Electrochemical determination of factor xa inhibitors | 20090236238 | 20090924 |
| 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... |
| Kit of lyophilized thrombin and lyophilized fibrinogen used to compound fibrin membrane, and its application | 20090232790 | 20090917 |
| A kit of lyophilized thrombin and lyophilized fibrinogen comprises fibrinogen of 50-100 mg/ml, thrombin of 100-1000 IU/ml and 20-60 mmol/L CaCl2 used to compound fibrin membrane. The lyophilized thrombin and lyophilized fibrinogen are applied in a clinical tumor operation for reducing the risk of tumor metastasis after the operation. The solutions of thrombin and fibrinogen are daubed on the surface of a tumor, where they mix and form a solid-meshy fibrin membrane that prevents pervasion of tumor cells caused by incision and trauma in the tumor operation, thereby reducing the risk of palindromia and metabasis after the operation and improving the patient's life span.
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| Methods and compositions for tissue regeneration | 20090232791 | 20090917 |
| Disclosed is a kit comprising a first component comprising fibrinogen, aprotinin, and a buffered solution, and a second component comprising, fibroblasts, keratinocytes, thrombin, glycerol, human serum albumin, and a buffered solution, wherein the first and second components are comprised in separate sterile containers.
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| Nanometer mesoporous silica-based xerogel styptic material and its preparing process and application | 20090232902 | 20090917 |
| The invention disclosed a novel mesoporous silica-based xerogel and its use in hemorrhage control. The mesoporous silica-based xerogel material has tunable mesopores (1-50 nm), high specific surface area (100-1400 m2/g), macroscopical morphology (powder, film, disc, column, etc.) and adjustable compositions (SiO2, CaO and P2O5, etc.) as well as good biodegradation. The mesoporous silica-based xerogels herein effectively promote the blood clotting under various conditions including slow and severe hemorrhage, even at the blood oozing site of bone defect. Meanwhile, the networks of silica-based xerogel with good elastic and mechanic properties, formed by adsorbing a large amount of water, can modulate the cell behavior and tissue growth, and thus promote the wound healing. Additionally, due to the mesoporous structure, the materials have the potential to load drug, thrombin... |
| Unsaturated fatty acids as thrombin inhibitors | 20090234007 | 20090917 |
| A preparation having at least one unsaturated fatty acid and the use of at least one unsaturated fatty acid having a chain length of 18 or 20 carbon atoms and of plant drugs containing the unsaturated fatty acid as a free fatty acid or a fatty acid radical of a triglyceride. The fatty acid has a chain length of 18 carbon atoms which are provided with 1 to 3 double bonds and the fatty acid has a chain length of 20 carbon atoms which are provided with 1 to 4 double bonds. The double bond or one of the double bonds are located in position 9 or 11 of the carbon chain. The unsaturated fatty acid is supplied in the all-cis configuration. The at least one... |
| Kit of lyophilized thrombin and lyophilized fibrinogen used to compound fibrin membrane, and its application | 20090232790 | 20090917 |
| A kit of lyophilized thrombin and lyophilized fibrinogen comprises fibrinogen of 50-100 mg/ml, thrombin of 100-1000 IU/ml and 20-60 mmol/L CaCl2 used to compound fibrin membrane. The lyophilized thrombin and lyophilized fibrinogen are applied in a clinical tumor operation for reducing the risk of tumor metastasis after the operation. The solutions of thrombin and fibrinogen are daubed on the surface of a tumor, where they mix and form a solid-meshy fibrin membrane that prevents pervasion of tumor cells caused by incision and trauma in the tumor operation, thereby reducing the risk of palindromia and metabasis after the operation and improving the patient's life span.
... |
| Methods and compositions for tissue regeneration | 20090232791 | 20090917 |
| Disclosed is a kit comprising a first component comprising fibrinogen, aprotinin, and a buffered solution, and a second component comprising, fibroblasts, keratinocytes, thrombin, glycerol, human serum albumin, and a buffered solution, wherein the first and second components are comprised in separate sterile containers.
... |
| Nanometer mesoporous silica-based xerogel styptic material and its preparing process and application | 20090232902 | 20090917 |
| The invention disclosed a novel mesoporous silica-based xerogel and its use in hemorrhage control. The mesoporous silica-based xerogel material has tunable mesopores (1-50 nm), high specific surface area (100-1400 m2/g), macroscopical morphology (powder, film, disc, column, etc.) and adjustable compositions (SiO2, CaO and P2O5, etc.) as well as good biodegradation. The mesoporous silica-based xerogels herein effectively promote the blood clotting under various conditions including slow and severe hemorrhage, even at the blood oozing site of bone defect. Meanwhile, the networks of silica-based xerogel with good elastic and mechanic properties, formed by adsorbing a large amount of water, can modulate the cell behavior and tissue growth, and thus promote the wound healing. Additionally, due to the mesoporous structure, the materials have the potential to load drug, thrombin... |
| Unsaturated fatty acids as thrombin inhibitors | 20090234007 | 20090917 |
| A preparation having at least one unsaturated fatty acid and the use of at least one unsaturated fatty acid having a chain length of 18 or 20 carbon atoms and of plant drugs containing the unsaturated fatty acid as a free fatty acid or a fatty acid radical of a triglyceride. The fatty acid has a chain length of 18 carbon atoms which are provided with 1 to 3 double bonds and the fatty acid has a chain length of 20 carbon atoms which are provided with 1 to 4 double bonds. The double bond or one of the double bonds are located in position 9 or 11 of the carbon chain. The unsaturated fatty acid is supplied in the all-cis configuration. The at least one... |
| Stabilized thrombin compositions | 20080311104 | 20081218 |
| Stabilized thrombin compositions, processes for preparing them, and kits comprising them are disclosed. The compositions comprise thrombin, a bacteriostatically effective amount of benzyl alcohol or chlorobutanol, and 0.10%-5.0% (w/v) sucrose in aqueous solution. The compositions are stable when stored at 2° C.-8° C. for four weeks or more.
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| Thrombin-free biological adhesive and use thereof as a medicament | 20080311190 | 20081218 |
| The invention relates to a thrombin-free, fibrinogen-based biological adhesive for therapeutic use, which comprises factor VIIa and a source of calcium ions. The invention also relates to the use of the biological adhesive as a medicament, in particular as a dressing for biological tissues, wounds or biomaterials.
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| Methods of measuring inhibition of platelet aggregation by thrombin receptor antagonists | 20080299587 | 20081204 |
| A method is provided for measuring inhibition of platelet aggregation by a thrombin receptor antagonist. First, a blood sample is obtained from a patient treated with a thrombin receptor antagonist. The blood sample is mixed in combination with particles including an immobilized GPIIb/IIIa receptor ligand and a thrombin receptor activator. The combination is then incubated under conditions suitable for agglutinating the particles, and platelet-mediated agglutination is assessed in the mixture. The absence of agglutination indicates that the patient has reduced ability to form platelet thrombi in response to the thrombin receptor antagonist treatment. Also provided is a kit for measuring inhibition of platelet aggregation by a thrombin receptor antagonist that includes a GPIIb/IIIa receptor ligand immobilized on a particle, a thrombin receptor activator, an anticoagulant, and... |
| Method for activating prethrombin-1 | 20080293122 | 20081127 |
| Methods for converting prethrombin-1 to thrombin are disclosed. An aqueous solution of prethrombin-1 is applied to oscutarin-C immobilized on a solid support so as to provide from 500 mg to 4000 mg of prethrombin-1 per mL of the solid support and a contact time between the prethrombin-1 and the oscutarin-C of from 1.8 to 3.5 minutes. The resulting active thrombin may be captured on an ion exchange chromatography medium or an affinity chromatography medium.
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| Dna and rna conformational switches as sensitive electronic sensors of analytes | 20080293160 | 20081127 |
| The electrical conductivity of DNA and other oligonucleotide constructs is dependent on its conformational state. Such a dependence may be harnessed for the electronic sensing of external analytes, for instance, adenosine or thrombin. Such a DNA sensor incorporates an analyte receptor, whose altered conformation in the presence of bound analyte switches the conformation, and hence, the conductive path between two oligonucleotide stems, such as double-helical DNA. Two distinct designs for such sensors are described that permit significant electrical conduction through a first or “detector” double-helical stem only in the presence of the bound analyte. In the first design, current flows through the analyte receptor itself whereas, in the second, current flows in a path adjacent to the receptor. The former design may be especially suitable for... |
| Bioabsorbable synthetic nonwoven fabric holding thrombin | 20080286347 | 20081120 |
| A safe and effective hemostatic is provided. The invention relates to a bioabsorbable synthetic nonwoven fabric holding thrombin as an effective ingredient and a hemostatic comprising said bioabsorbable synthetic nonwoven fabric. The bioabsorbable synthetic nonwoven fabric holding thrombin in accordance with the present invention may be prepared by a process which comprises the steps of immersing a bioabsorbable synthetic nonwoven fabric into a solution containing thrombin and of lyophilizing the obtained nonwoven fabric. The bioabsorbable synthetic nonwoven fabric holding thrombin in accordance with the present invention allows for quicker and more effective hemostasis.
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| Dry hemostatic compositions and methods for their preparation | 20080286376 | 20081120 |
| Dry cross-linked gelatin compositions are prepared that rapidly re-hydrate to produce gelatin hydrogels suitable as hemostatic sealants. Gelatin is cross-linked in the presence of certain re-hydration aids, such as polyethylene glycol, polyvinylprovidone, and dextran, in order to produce a dry cross-linked gelatin powder. The use of the re-hydration aids has been found to substantially increase the re-hydration rate in the presence of an aqueous re-hydration medium, typically thrombin-containing saline.
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| Thrombin purification | 20080280343 | 20081113 |
| The invention relates to thrombin compositions with reduced levels of high molecular weight impurities. In particular, the levels of factor Va, prions and/or viral agents are greatly reduced. This invention also relates generally to methods for the preparation of thrombin having a high degree of purity and high specific activity. More specifically, the invention encompasses steps to exclude high molecular weight impurities from thrombin preparations by size exclusion filtration. In additional embodiments, the preparation of thrombin additionally includes an ion exchange filtration step. The methods of the invention are particularly suited for large scale purification of thrombin. This invention also relates generally to stabilized formulations containing thrombin compositions. More specifically, the present invention relates to stabilized, liquid formulations containing thrombin having a high degree of purity... |
| Cartilage implant plug with fibrin glue and method for implantation | 20080274157 | 20081106 |
| The invention is directed toward a cartilage repair assembly comprising a shaped structure of subchondral bone with an integral overlying cartilage cap which is treated to remove cellular debris and proteoglycans and milled cartilage in a bioabsorbable carrier. The shaped structure is dimensioned to fit in a drilled bore in a cartilage defect area so that said shaped bone and cartilage cap when centered in the bore does not engage the side wall of the bore and is positioned from the side wall of the bone a distance ranging from 10 microns to 1000 microns and is surrounded by milled cartilage and a fibrin thrombin glue. A method for inserting the assembly into a cartilage defect area is disclosed.
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| Charged phospholipid compositions and methods for their use | 20080275007 | 20081106 |
| The invention provides a pharmaceutical composition comprising a synthetic or naturally occurring charged phospholipid, which is formulated into a dosage form for administration to a subject or which is administered as a food additive. Negatively charged phospholipid composition increase the net negative charge on intravascular lipoproteins, enhance the clearance of cholesterol and regulate the function of lipolytic enzymes, retard prothrombin formation and aid in the clearance of virus and bacterial particles. Negatively charged lipid compositions can therefore be administered to humans and animals for the treatment of hyperlipidemia and blood coagulation disorders and to reduce the levels of virus, bacteria, and endotoxins in the blood stream. Positively charged lipid compositions can be administered to delay lipoprotein clearance from the plasma compartment and give longer duration of... |
| Process for obtaining recombinant prothrombin activating protease (rlopap) in monomeric form; the recombinant prothrombin activating protease (rlopap) as well as its amino acid sequence; the use of this protease as a defibrinogenase | 20080267944 | 20081030 |
| This invention refers to the process for obtaining the recombinant prothrombin activating protease (rLopap) in monomeric form, the recombinant prothrombin activating protease (rLopap), as well as its amino acid sequence. In addition to that, this invention also refers to the use of this protease for depleting the blood fibrinogen, and serve as diagnosis kit for dysprothrombinemias. This invention describes the obtainence in recombinant form and the characterization of a prothrombin activator protease of 21 kDa, named rLopap (Lonomia obliqua prothrombin activator protease), with serineproteases characteristics however it shows sequence of conserved amino acids as in a lipocalin family. The protein presents pro-coagulating activity, depleting blood fibrinogen and prolonging the coagulation time of human blood/plasma. The obtainence of rLopap in its recombinant form and showing adequate activity... |
| New salts | 20080269176 | 20081030 |
| wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents C1-2 alkyl; and n represents 0, 1 or 2, which salts are useful as prodrugs of competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required.
... |
| Fibrin compositions containing strontium compounds | 20080260714 | 20081023 |
| A composition for use in bone healing and bone regeneration in the form of a viscoelastic hydrogel gel or liquid formulation comprising fibrinogen, thrombin and an inorganic component comprising a strontium (Sr) containing compound and/or possibly another metal such as a calcium containing compound. The strontium containing compound can be dissolved in the thrombin solutions or added to the clot in crystalline particulate form. Upon mixing the components, gelation takes place to form a matrix. The composition may also comprise an iodine-containing compound which acts as a plasticizer.
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| Hemostat | 20080260810 | 20081023 |
| The present invention is directed towards a hemostat comprising an absorbable foam, an absorbable woven or knitted fabric, thrombin and/or fibrinogen.
... |
| System/unit and method employing a plurality of magnetoelastic sensor elements for automatically quantifying parameters of whole blood and platelet-rich plasma | 20080261261 | 20081023 |
| A system/analyzer-unit and method/platform—using information obtained from at least one, adapted for a plurality of, magnetoelastic sensor elements in contact with one or more samples comprising blood from a patient—for automatically quantifying one or more parameters of the patient's blood. Information obtained from emissions measured from each of the sensor elements is uniquely processed to determine a quantification about the patient's blood, such as, quantifying platelet aggregation to determine platelet contribution toward clot formation; quantifying fibrin network contribution toward clot formation; quantifying platelet-fibrin clot interactions; quantifying kinetics of thrombin clot generation; quantifying platelet-fibrin clot strength; and so on. Structural aspects of the analyzer-unit include: a cartridge having at least one bay within which a sensor element is positioned; each bay in fluid communication with both (a)... |
| Imidazole derivatives as inhibitors of tafia | 20080262028 | 20081023 |
| or any stereoisomeric form of the compound of the formula I or a mixture of these forms in any ratio or a physiologically acceptable salt of the compound of the formula I which inhibit the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor), and to a process for their preparation and to their use to treat described diseases where the substituents are as described in the specification.
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| Methods and devices for lung treatment | 20080249503 | 20081009 |
| A method of treating a lung comprises deploying a delivery catheter through a bronchial tree into a targeted lung region and delivering a fibrinogen suspension through the delivery catheter so that the fibrinogen suspension exits the distal end of the delivery catheter into the targeted lung region. Thrombin is also delivered through the delivery catheter so that the thrombin exits the distal end of the delivery catheter into the targeted lung region. The lung is promoted to collapse.
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| Antibodies to complementary peptides of thrombin or portions thereof | 20080241149 | 20081002 |
| Disclosed are antibodies and antigen-binding fragments that bind to a complementary peptide having an amino acid sequence that is encoded by the complement of a nucleotide sequence encoding thrombin or a portion thereof. Such antibodies and antigen-binding fragments can be agonists or antagonists of thrombin receptor-mediated events. Also disclosed are methods of using the agonist antibodies and antigen-binding fragments of the invention to activate the non-proteolytically activated thrombin receptor (NPAR) in a subject in need of such treatment. In addition, methods of using the antagonist antibodies and antigen-binding fragments of the invention to inhibit activation of the NPAR in a subject in need of such treatment are disclosed.
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| Bioactive parstatin peptides and methods of use | 20080242613 | 20081002 |
| Bioactive peptides that have a molecular weight of approximately 4.5 kDa and correspond to amino-terminal fragments of protease-activated receptor-1 (PAR-1), which are cleaved and released upon the proteolytic activation of PAR-1 by proteases including, but not limited to, thrombin in humans and animals are disclosed. Such synthetic or recombinantly expressed or endogenously produced or chimeric synthetic peptides that are active in vitro and in vivo and modulate endothelial cell functions and physiological and pathological processes are named herein as parstatin. Parstatin peptides, fragments, analogs, derivatives have the ability to inhibit endothelial cell growth, migration and differentiation, to induce endothelial cell apoptosis, to block angiogenesis and have cardioprotective effects in ischemia/reperfusion injury. Methods for treating angiogenesis-related diseases and endothelium dysfunction-related cardiovascular diseases are disclosed.
... |
| Biodegradable metal barrier layer for a drug-eluting stent | 20080243240 | 20081002 |
| An implantable medical device includes a substrate, a drug-impregnated layer deposited over the substrate, and a barrier layer at least partially covering the drug-impregnated layer. The barrier layer may be a biodegradable metal, biodegradable metal oxide, or biodegradable metal alloy, such as, magnesium, a magnesium oxide or a magnesium alloy. The drug-impregnated layer includes a therapeutic substance, such as, antineoplastic, anti-inflammatory, antiplatelet, anticoagulant, fibrinolytic, thrombin inhibitor, antimitotic, antiallergic, and antiproliferative substances.
... |
| Reduction of adverse events after percutaneous intervention by use of a thrombin receptor antagonist | 20080234236 | 20080925 |
| Disclosed are methods of preventing adverse clinical events in a patient undergoing a percutaneous coronary intervention procedure or a peripheral percutaneous interventional procedure comprising administering a therapeutically effective amount of a thrombin receptor antagonist, such as SCH 530348, to the patient. Administration of a loading dose of about 40 mg of SCH 530348 in as little as one hour prior to the procedure can result in therapeutically effective levels of platelet aggregation.
... |
| Thrombin inhibiting 2,4-dioxo-3,4-dihydropyrimidine derivatives | 20080214589 | 20080904 |
| There is provided a compound of formula I wherein R1 to R5, A, G, L and X have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).
... |
| Agent for promoting osteogenesis and/or inhibiting bone resorption | 20080206226 | 20080828 |
| Provided is a novel agent for promoting osteogenesis and/or inhibiting bone resorption, which: can be directly taken from daily meals by mouth for long periods without any trouble in taste; directly impart a promoting effect on osteogenesis and an inhibiting effect on bone resorption to the bone; and can be expected to have therapeutic effects for preventing or ameliorating/treating various bone diseases. The above agent includes, as an active ingredient, any one or more of β2-microglobulin, histone, complement component 3, monocyte chemotactic protein 1, lysozyme, ribonuclease, prothrombin, cytochrome P-450, plasminogen, transferrin, thrombin, plasmin, complement component 4, and β defensin, and enzymatic digestion products thereof. Those substances have a remarkable inhibiting effect on bone resorption by osteoclasts and/or a promoting effect on osteogenesis via promotion of the... |
| Thrombin inhibiting 2-oxo-1,2,5,6-tetrahydropyridine derivatives | 20080207695 | 20080828 |
| There is provided a compound of formula (I) wherein R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 to R8, A and G have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).
... |
| Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders | 20080199426 | 20080821 |
| Disclosed herein are methods for treating a vascular inflammatory disorder or endothelial cell disorder using inhibitor compounds that inhibit the expression or biological activity of Tie-1, Tie-1 endodomain, thrombin, VEGFR2, VEGFR2 endodomain, EphA2, and any of the cytokines or kinases that are upregulated by activation of Tie-1 or thrombin, as provided herein. Also disclosed are the use of combinations of inhibitor compounds or the use of an eNOS activator compound in combination with any one or more of the inhibitor compounds. Also disclosed are methods for inhibiting the pro-coagulant activity of thrombin using a Tie-1 or Tie-1 endodomain inhibitor compound or an EphA2 inhibitor compound. Methods for diagnosing and monitoring vascular inflammatory disorders or endothelial cell disorders that include the measurement of any of the polypeptides... |
| Indications for direct thrombin inhibitors | 20080200514 | 20080821 |
| The invention relates to new indications for direct thrombin inhibitors such as dabigatran etexilate in the CNS and other fields.
... |
| Use of an immunoglobulin domain-containing cell surface recognition molecule for treating diseases | 20080193414 | 20080814 |
| The invention relates to the use of INSP052 for treatment and/or prevention of infectious disease, properdin-related disease, MBL2-related disease, MASP1-related disease, MASP2-related disease, Antithrombin III-related disease, Complement factor H-related disease and/or Albumin-related disease. Combinations of INSP052 with an interferon, a TNF antagonist or a further anti-infectious or anti-blood clotting agent are also within the present invention.
... |
| Method for determining coagulation activation and device for carrying out said method | 20080194036 | 20080814 |
| The invention relates to a method for determining the generation of thrombin or factor Xa, said generation of activated coagulation factors in various sample materials, such as whole blood or plasma with different thrombocyte quantities, being triggered by phospholipid micelles with different tissue factor contents (0 to 1000 pM). According to the invention, the generation of thrombin is determined in a coagulation machine, which can simultaneously determine classic conventional coagulation parameters. The device for carrying out the method for the parallel determination of thrombin generation and classic conventional coagulation parameters has a rotating cuvette plate, into which a cuvette ring and cuvette elements are inserted. According to the invention, at least one section of the cuvette ring contains a test station for at least two fluorescent... |
| Remedy for angiospasm accompanying subarachnoid hemorrhage containing thrombin receptor antagonist as the active ingredient | 20080194559 | 20080814 |
| A therapeutic agent for subarachnoid hemorrhage or a drug for improving prognosis of subarachnoid hemorrhage, comprising a compound having a PAR1 inhibitory effect, its pharmaceutically acceptable salt or a hydrate thereof.
... |
| Disintegration promoters in solid dose wet granulation formulations | 20080194560 | 20080814 |
| Also disclosed are methods of treating patients at risk for acute coronary syndrome by administering such a rapidly disintegrating solid dosage form.
... |
| Exosite-directed thrombin inhibitors | 20070299013 | 20071227 |
| Disclosed are an amino acid sequence of the human blood clotting factor Va, peptides containing such sequence, and additional peptides of interest that significantly inhibit thrombin generation. Also disclosed are pharmaceutical compositions containing these peptides and related therapeutic methods for inhibiting thrombin generation and treating blood coagulation disorders.
... |
| Combination of organic compounds | 20070299047 | 20071227 |
| The present invention relates to a pharmaceutical composition, comprising a PPAR agonist, or pharmaceutically acceptable salts thereof, alone or in combination with at least one active ingredient selected from the group consisting of (i) HDL increasing compounds; (ii) anti-diabetics; (iii) an anti-hypertensive agent; (iv) cholesterol absorption modulator; (v) apo-A1 analogs and mimetics; (vi) renin inhibitors; (vii) thrombin inhibitors; (viii) aldosterone inhibitors; (ix) GLP-1 agonists; (x) glucagon receptor antagonists; (xi) cannabinoid receptor 1 antagonists; (xii) anti-obesity agents; and (xiii) inhibitors of platelet aggregation or, in each case, a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable carrier.
... |
| Thrombin derivatives and medicinal composition containing the same | 20070282095 | 20071206 |
| The present invention provides a thrombin derivative, comprising an A chain and a B chain, the B chain having an amino acid sequence in which one or more kinds of active center amino acids selected from the group consisting of serine at position 205, glycine at position 203, aspartic acid at position 99, and histidine at position 43 in an amino acid sequence of a thrombin B chain are substituted, having the properties: (1) cleaving a thrombin substrate at the ratio of 10% or less when it is reacted with the thrombin substrate in 50 mM Tris-HCl (pH 7.4) containing 0.1 M NaCl at 37° C. for 3 hours, and (2) maintaining a structure of exosite I.
... |
| Stabilized proteins with engineered disulfide bonds | 20070276128 | 20071129 |
| The present invention relates to methods of introducing one or more cysteine residues into a polypeptide which permit the stabilization of the polypeptide by formation of at least one bond, preferably a disulfide bond, between different domains of the polypeptide. The invention also relates to polypeptides containing such introduced cysteine residue(s), nucleic acids encoding such polypeptides and pharmaceutical compositions comprising such polypeptides or nucleic acids. The invention also relates to vectors, viral particles and host cells containing such nucleic acids, and methods of using them to produce the polypeptides of the invention. Exemplified polypeptides include plasma proteins, including hepatocyte growth factor activator and plasma hyaluronin binding protein, as well as blood coagulation factors, such as Factor VIII, Factor V, Factor XII and prothrombin.
... |
| Thrombin receptor antagonists | 20070270439 | 20071122 |
| R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
... |
| Antibiotic formulation and method of treatment | 20070254008 | 20071101 |
| A formulation comprised of particles which may be in groups and are comprised of a biocompatible polymer and an antimicrobial drug for controlled release of the drug is disclosed. The particles may be in an aqueous solution comprising thrombin and be dispersed in a gel. The formulation is administered to an area such as an open wound having an orthopedic implant therein and provides a therapeutically effective level of drug to the patient over therapeutically effective period of time.
... |
| Antibiotic/bone morphogenic protein formulation and method of treatment | 20070254009 | 20071101 |
| A formulation comprised of particles which may be in groups and are comprised of a biocompatible polymer and an antimicrobial drug for controlled release of the drug is disclosed. The particles may be in an aqueous solution comprising thrombin and be dispersed in a gel. The formulation is administered to an area such as an open wound having an orthopedic implant therein and provides a therapeutically effective level of drug to the patient over therapeutically effective period of time.
... |
| Dry hemostatic compositions and methods for their preparation | 20070248685 | 20071025 |
| Dry cross-linked gelatin compositions are prepared that rapidly re-hydrate to produce gelatin hydrogels suitable as hemostatic sealants. Gelatin is cross-linked in the presence of certain re-hydration aids, such as polyethylene glycol, polyvinylprovidone, and dextran, in order to produce a dry cross-linked gelatin powder. The use of the re-hydration aids has been found to substantially increase the re-hydration rate in the presence of an aqueous re-hydration medium, typically thrombin-containing saline.
... |
| New amidino derivatives and their use as thrombin inhibitors | 20070249578 | 20071025 |
| wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
... |
| Fused ring thrombin receptor antagonists | 20070244163 | 20071018 |
| represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
... |
| Multi-functional bioactive wound dressing | 20070237809 | 20071011 |
| A novel, lightweight bioactive wound dressing is provided which offers infection-resistance as well as localized wound healing properties. The wound dressing is comprised of preformed fibrous matter, which is comprised of either a composition which intrinsically provides multiple chemical groups which are functional for subsequent chemical reaction; or is a composition which has been chemically modified at its exterior surface to present a range of chemical groups which are functional for subsequent chemical reaction. These multiple functional chemical groups serve as a plurality of anchorage sites and backbone for the subsequent immobilization of an independently bound biologically active protein. Preferably, a broad-spectrum antibiotic such as the fluoroquinolone, ciprofloxacin, is incorporated into the preformed fibrous matter, using a newly created Pad/Autoclaving technique. Following antibiotic incorporation, the exterior... |
| Tra combination therapies | 20070238674 | 20071011 |
| Examples of cardiovascular agents suitable for co-formulation or co-administration with the thrombin receptor antagonist include an endothelin antagonist selected from the group consisting of tezosentan, bosentan, and sitaxsentan.
... |
| Tissue sealant | 20070231372 | 20071004 |
| The present invention relates to a tissue sealant which is safe and effective. In accordance with the present invention, a tissue sealant comprising as an effective ingredient thrombin and fibrinogen characterized in that a bioabsorbable synthetic nonwoven fabric is used as a supporting material; use of a combination of a bioabsorbable synthetic nonwoven fabric as a supporting material and thrombin and fibrinogen as an effective ingredient for a tissue sealant; use of a combination of a bioabsorbable synthetic nonwoven fabric holding thrombin as an effective ingredient, and fibrinogen as an effective ingredient for a tissue sealant; a tissue sealing kit comprising a bioabsorbable synthetic nonwoven fabric holding thrombin as an effective ingredient, and a container comprising fibrinogen as an effective ingredient; and a tissue sealing kit... |
| Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists | 20070232635 | 20071004 |
| represents an optional double bond and wherein Gn, Jn, R3, R8, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.
... |
| Hemostatic material | 20070224251 | 20070927 |
| The present invention provides a hemostatic material which is excellent in hemostatic property, biodegradability and bioabsorbability, uniformity and stability of the quality, as well as reduces a risk of contamination with a pathogenic organism derived from an animal. The hemostatic material comprises a thrombin and a synthetic polypeptide capable of forming a triple helical structure. The polypeptide may show a peak of the molecular weight in the range from 5×104 to 100×104 in the molecular weight distribution. The polypeptide may contain at least a peptide unit represented by the formula: -Pro-X-Gly- (in the formula, X represents Pro or Hyp). The thrombin may be a recombinant. In the hemostatic material, the proportion of the thrombin may be about 0.1 to 500 units (U) relative to 1 mg... |
| Pyridines and pyridine n-oxides as modulators of thrombin | 20070225282 | 20070927 |
| wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.
... |
| New mandelic acid derivatives and their use as thrombin inhibitors | 20070218136 | 20070920 |
| There is provided a compound of formula (I) wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g., thrombosis) or as anticoagulants.
... |
| Monitoring heparin by microelectronic devices | 20070212786 | 20070913 |
| In one aspect, the present invention provides a device and method for real-time, direct detection of heparin in buffer and in serum comprising a microfluidic field-effect device as an affinity biosensor. The sensor is based on an electrolyte-insulator-silicon structure, and is manufactured by a standard high-yield silicon microfabrication process. The binding of heparin to the sensor surface induces a change in the insulator-electrolyte surface potential, which is measured as a change in sensor capacitance. To ensure the binding selectivity, protamine and antithrombin III are used as affinity probes.
... |
| Methods for reducing platelet activation and for the treatment of thrombotic events | 20070213303 | 20070913 |
| or its pharmaceutically acceptable salt, ester or prodrug, wherein the substituents are defined herein, optionally in the appropriate pharmaceutically acceptable carrier for the route of administration selected.
... |
| Intravenous blood-replacement solutions | 20070207962 | 20070906 |
| A theory has been presented that provides a simplified explanation of a cohesive mechanism of embryological development, hemostasis, coagulation, wound repair and tissue maintenance that operates continuously in the animal body to oppose the effects of stress. The theory endeavors to fit all known facts, and is based on the hypothesis that coagulation Factors VII and VIII are respectively local and systemic stress agents that regulate thrombin activity and synergize each other's effects. Stress Theory may explain the etiologies of several hitherto mysterious disease syndromes, and the stress mechanism and may play a more pervasive role in disease than is generally appreciated. The theory offers fresh avenues for research and clinical strategy.
... |
| Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery | 20070202140 | 20070830 |
| Disclosed herein are methods of preventing, inhibiting, or ameliorating complications associated with cardiopulmonary bypass surgery by the use of a thrombin receptor antagonist compound. Among the thrombin receptor antagonist compounds useful in these methods are those of Formulas I and II, described herein. Examples of such thrombin receptor antagonists include:
... |
| New mandelic acid derivatives and their use as thrombin inhibitors | 20070202174 | 20070830 |
| There is provided a compound of formula (I) wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g., thrombosis) or as anticoagulants.
... |
| Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist | 20070203193 | 20070830 |
| and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.
... |
| Method to treat atherosclerosis | 20070196355 | 20070823 |
| A theory has been presented that provides a simplified explanation of a cohesive mechanism of embryological development, hemostasis, coagulation, wound repair and tissue maintenance that operates continuously in the animal body to oppose the effects of stress. The theory endeavors to fit all known facts, and is based on the hypothesis that coagulation Factors VII and VIII are respectively local and systemic stress agents that regulate thrombin activity and synergize each other's effects. Stress Theory may explain the etiologies of several hitherto mysterious disease syndromes, and the stress mechanism and may play a more pervasive role in disease than is generally appreciated. The theory offers fresh avenues for research and clinical strategy.
... |
| Method of providing anesthesia | 20070191430 | 20070816 |
| A theory has been presented that provides a simplified explanation of a cohesive mechanism of embryological development, hemostasis, coagulation, wound repair and tissue maintenance that operates continuously in the animal body to oppose the effects of stress. The theory endeavors to fit all known facts, and is based on the hypothesis that coagulation Factors VII and VIII are respectively local and systemic stress agents that regulate thrombin activity and synergize each other's effects. Stress Theory may explain the etiologies of several hitherto mysterious disease syndromes, and the stress mechanism and may play a more pervasive role in disease than is generally appreciated. The theory offers fresh avenues for research and clinical strategy.
... |
| Boronic acid thrombin inhibitors | 20070185060 | 20070809 |
| A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH2) or an amino-protecting group; aa1 is an amino acid residue having a side chain selected from formula (A) and (B)—(CO)a—(CH2)b-Dc-(CH2)d-E (A), —(CO)a—(CH2)b-Dc-Ce(E1)(E2)(E3) wherein E1, E2 and E3 are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E1, E2 and E3 is hydrogen and the other two are a said hydrocarbyl ring, E, E1, E2 and E3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R9 is a straight chain alkyl group interrupted by one or more... |
| Method for diagnosing liver fibrosis | 20070178442 | 20070802 |
| A method for the detection of the presence and/or the severity of a liver disease in a patient comprising measuring in an isolated sample TIMP-1 (tissue inhibitor of metalloproteinase I), ferritin, at least one additional parameter selected from the group consisting of A2M (alpha-2-macroglobulin) and PI (prothrombin index) and optionally measuring at least one additional biochemical or clinical parameter and diagnosing the presence and/or severity of a liver disease based on the presence or measured levels of these parameters. The method can be used for monitoring therapeutic treatment of liver fibrosis and staging of liver fibrosis.
... |
| Method for diagnosing liver fibrosis | 20070178443 | 20070802 |
| The invention concerns a method for the detection of the presence and/or the severity of a liver disease in a patient comprising measuring in an isolated sample TIMP-1 (Tissue Inhibitor of Metalloproteinase I), A2M (a-2-macroglobulin), PLT (number of blood plateletes, PI (prothrombin index), optionally at least one additional parameter selected from the group consisting of urea and GGT (γ-glutamyltranspeptidase) and optionally measuring at least one additional biochemical or clinical parameter and diagnosing the presence and/or severity of a liver disease based on the presence or measured levels of these parameters. The method can be used for monitoring therapeutic treatment of liver fibrosis and staging of liver fibrosis.
... |
| Thrombin receptor antagonists | 20070179187 | 20070802 |
| R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
... |
| Diagnostic method for stroke | 20070166758 | 20070719 |
| Stroke is diagnosed in a subject by determining the concentration of at least one polypeptide selected from Apo C-III, Serum Amyloid A, Apo C-I, Antithrombin III fragment and Apo A-I in a sample of body fluid taken from the subject.
... |
| Method for enhancing bone formation | 20060293231 | 20061228 |
| This invention provides a method for facilitating bone formation in a subject comprising delivering to a bone formation-requiring site a composition of matter comprising platelet-rich plasma, calcium, a PAR-activating agent and a bone forming material. This invention further provides a method for facilitating bone formation in a subject comprising (a) delivering to a bone formation-requiring site in the subject a composition of matter comprising platelet-rich plasma, calcium and a bone-forming material, and (b) contacting the composition so delivered with a PAR-activating agent other than thrombin. This invention further provides a method for facilitating clot formation in platelet-rich plasma with a PAR-activating agent other than thrombin. This invention further provides a method of producing a formable gel comprising the step of admixing platelet-rich plasma, calcium, a bone-forming... |
| Inactivation resistant factor viii | 20060293238 | 20061228 |
| The present invention provides novel purified and isolated nucleic acid sequences encoding procoagulant-active FVIII proteins. The nucleic acid sequences of the present invention encode amino acid sequences corresponding to known human FVIII sequences, wherein residue Phe309 is mutated. The nucleic acid sequences of the present invention also encode amino acid sequences corresponding to known human FVIII sequences, wherein the APC cleavage sites, Arg336 and Ile562, are mutated. The nucleic acid sequences of the present invention further encode amino acid sequences corresponding to known human FVIII sequences, wherein the B-domain is deleted, the von Willebrand factor binding site is deleted, a thrombin cleavage site is mutated, an amino acid sequence spacer is inserted between the A2- and A3-domains. Methods of producing the FVIII proteins of the invention,... |
| Agent for promoting osteogenesis and/or inhibiting bone resorption | 20060286084 | 20061221 |
| Provided is a novel agent for promoting osteogenesis and/or inhibiting bone resorption, which: can be directly taken from daily meals by mouth for long periods without any trouble in taste; directly impart a promoting effect on osteogenesis and an inhibiting effect on bone resorption to the bone; and can be expected to have therapeutic effects for preventing or ameliorating/treating various bone diseases. The above agent includes, as an active ingredient, any one or more of β2-microglobulin, histone, complement component 3, monocyte chemotactic protein 1, lysozyme, ribonuclease, prothrombin, cytochrome P-450, plasminogen, transferrin, thrombin, plasmin, complement component 4, and β defensin, and enzymatic digestion products thereof. Those substances have a remarkable inhibiting effect on bone resorption by osteoclasts and/or a promoting effect on osteogenesis via promotion of the... |
| Method for monitoring coagulability and hypercoagulable states | 20060286614 | 20061221 |
| The assay of soluble endothelial protein C receptor (sEPCR) is useful to monitor effective thrombin levels and a hypercoagulable state. An assay for sEPCR is therefore useful to monitor ongoing effectiveness of anticoagulant therapy. A sEPCR ELISA assay is particularly useful for this purpose. A state of hypercoagulability in patients or normal individuals can also be identified by such an assay.
... |
| Coagulation tests at ambient temperature | 20060281140 | 20061214 |
| A method of determining prothrombin time (PT) in a whole blood, anti-coagulated blood, blood plasma or anti-coagulated blood plasma sample at an ambient temperature in the range of 15° C. to 45° C. is described. The method is performed with liquid reagents and the PT, preferably expressed as International Normalized Ratio (INR), is calculated based on said temperature and the clotting time (CT). A test kit is also described for analysis of PT which comprises temperature recoding means, and one or several separate sealed vessels containing reagents, optionally in lyophilized form for reconstitution prior to use, for clotting one or more defined volumes of whole blood, anti-coagulated blood, blood plasma or anti-coagulated blood plasma sample, and optionally time registration means and volume determining means.
... |
| Thrombin-like recombinant baxtroxobin expressed by pichia sp.and production method thereof | 20060281147 | 20061214 |
| A recombinant thrombin-like enzyme batroxobin expressed by yeast, a production method thereof, and use of the batroxobin as a hemostatic agent or antithrombotic agent is disclosed. In order to express recombinant thrombin-like enzyme, an expression vector is prepared by inserting cDNA encoding the enzyme, the transformed cell is prepared by introducing the expression vector into the cell, the transformed cell then is incubated and the recombinant thrombin-like enzyme is obtained from the cell. The recombinant thrombin-like enzyme may be usefully used as a hemostatic agent because the enzyme effectively decrease bleeding time and blood coagulation time and does not affect various blood coagulation factors. The recombinant thrombin-like enzyme is also useful for a hemostatic agent or antithrombotic agent comprising the recombinant thrombin-like enzyme as an active... |
| Composition for coating support for preparation of cell sheet support for preparation of cell sheet and process for producing cell sheet | 20060281173 | 20061214 |
| Disclosed are a method for manufacturing a cell sheet, comprising culturing cells on a fibrin-coated surface of a substrate until the cells reach confluency, continuing the cultivation of the cells for a sufficient time period to cause the degradation of fibrin at the bottom of the cells, and detaching the cultured cells from the substrate surface in a sheet-like form to give a cell sheet; a substrate for cell sheet preparation, a surface of which is coated with fibrin; and a composition for use in coating with fibrin a surface of a substrate for cell sheet preparation, the composition comprising fibrinogen and thrombin. The invention enables to cell sheets to be manufactured by a simple manipulation using a substrate coated with a commercial, commonly available material... |
| Method and device for improving protein stability and solubility | 20060275884 | 20061207 |
| A method for expressing proteins as a fusion chimera with a domain of p26 or alpha crystallin type proteins to improve the protein stability and solubility when over expressed in bacteria such as E. coli is provided. Genes of interest are cloned into the multiple cloning site of the Vector System just downstream of the p26 or alpha crystallin type protein and a thrombin cleavage site. Protein expression is driven by a strong bacterial promoter (TAC). The expression is induced by the addition of 1 mM IPTG that overcomes the lac repression (lac Iq). The soluble recombinant protein is purified using a fusion tag.
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| Synthetic peptide inhibitors of thrombin and thrombin activation of protease activated receptors 1 and 4 | 20060276402 | 20061207 |
| The invention relates to synthetic peptide analogs of D-Arg-Oic-Pro-Gly-Phe and methods of their use to inhibit human platelet aggregation, thrombosis and cell activation mediated by PAR1 and PAR4.
... |
| Beta-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins | 20060276408 | 20061207 |
| There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the β-sheet mimetic is a thrombin inhibitor.
... |
| Compositions and methods for fusion protein separation | 20060276625 | 20061207 |
| The present invention relates to compositions and methods for fusion protein separation utilizing a peptide linker comprising a novel thrombin cleavage site.
... |
| Thrombin purification | 20060270014 | 20061130 |
| This invention relates generally to methods for the preparation of thrombin having a high degree of purity and high specific activity. More specifically, the invention encompasses steps to exclude high molecular weight impurities from thrombin preparations by size exclusion filtration. In additional embodiments, the preparation of thrombin additionally includes an ion exchange filtration step. The methods of the invention are particularly suited for large scale purification of thrombin. The invention also relates to thrombin compositions with reduced levels of high molecular weight impurities. In particular, the levels of factor Va, prions and/or viral agents are greatly reduced.
... |
| Thrombin purification | 20060270015 | 20061130 |
| The invention relates to thrombin compositions with reduced levels of high molecular weight impurities. In particular, the levels of factor Va, prions and/or viral agents are greatly reduced. Ts invention also relates generally to methods for the preparation of thrombin having a high degree of purity and high specific activity. More specifically, the invention encompasses steps to exclude high molecular weight impurities from thrombin preparations by size exclusion filtration. In additional embodiments, the preparation of thrombin additionally includes an ion exchange filtration step. The methods of the invention are particularly suited for large scale purification of thrombin. This invention also relates generally to stabilized formulations containing thrombin cormpositions. More specifically, the present invention relates to stabilized, liquid formulations containing thrombin having a high degree of purity... |
| Formulation and method for preventing infection | 20060263401 | 20061123 |
| The packet of formulation comprised of two groups of spherical particles is disclosed. Each group is comprised of 100 or more particles and may be comprised of many thousands of particles. The groups of particles may be in an aqueous solution comprising thrombin and be dispersed in a gel. The particles in a single group may have substantially the same size and shape and are comprised of a biocompatible polymer and a pharmaceutically active drug such as an antibiotic. The packet is opened and administered to an area such as an open wound where the groups of particles provide for controlled release drug such as antibiotic in order to prevent infection.
... |
| Capillary membrane stabilization and reduction of tissue injury through use of biodegradable macromolecules with antioxidants and/or other chemicals | 20060264357 | 20061123 |
| The present invention provides a method of treating a human subject to prevent leakage of serum proteins from capillary endothelial junctions during a period of increased capillary permeability and at the same time preventing the harmful effects of free radicals on capillaries and surrounding tissues. The method comprises administering to a subject an effective amount of a composition comprising at least one polysaccharide selected from the group of HES, glycogen and dextran of varying molecular sizes and at least one active agent selected from the group consisting of dehydroascorbic acid, von Willebrand Factor, hemoglobin, polysaccharide-conjugated hemoglobin, Cerovive, edaravone, dimethylthiourea, citicoline, poly(ADP-ribose) polymerase inhibitor, oxidant detoxification catalyst, adenosine 2a (A2a) receptor agonist, adenosine 1 (A1) receptor agonist, adenosine, inosine, xanthin oxidase inhibitor, polyethylene-glycol-modified albumin, adenosine triphosphate, histamine,... |
| Methods and devices for contributing to the treatment of aneurysms | 20060264368 | 20061123 |
| The present invention relates to methods and devices to contribute to the treatment of aneurysms. More specifically, the present invention relates to methods and devices to contribute to contribute to the treatment of aneurysms by delivering bioactive agents via various delivery devices of collagen III and/or collagen III and thrombin.
... |
| Method for making a reinforced absorbable multilayered hemostatic wound dressing | 20060257457 | 20061116 |
| The present invention is directed to a method of making a reinforced absorbable multilayered hemostatic wound dressing comprising a first absorbable nonwoven fabric, a second absorbable woven or knitted fabric, thrombin and/or fibrinogen.
... |
| Reinforced absorbable multilayered hemostatis wound dressing | 20060257458 | 20061116 |
| The present invention is directed to a reinforced absorbable multilayered hemostatic wound dressing comprising a first absorbable nonwoven fabric, a second absorbable woven or knitted fabric, thrombin and/or fibrinogen.
... |
| Novel nucleic acid molecules and polypeptides encoding baboon tafi | 20060257921 | 20061116 |
| The present invention relates to the isolation and identification of novel baboon nucleic acid molecules and proteins and polypeptides encoded by such nucleic acid molecules, or degenerate variants thereof, which proteins and polypeptides comprise novel baboon thrombin-activatable fibrinolysis inhibitors or “TAFI” enzyme molecules. Because the novel baboon TAFI proteins and polypeptides of the invention inhibit the breakdown of blood clots, they may be therapeutically useful for the treatment of blood disorders wherein clotting needs to be regulated or promoted, such as hemophilia or von Willebrand's disease or in other situations, such as trauma, wherein blood clotting or coagulation needs to be regulated or promoted. The sequences of the invention are also useful in screening methods for the identification of compounds that modulate the expression of the... |
| Variants of antithrombin iii | 20060259987 | 20061116 |
| Disclosed are compositions and methods related to variant antithrombin III molecules.
... |
| Method and apparatus for producing autologous clotting components | 20060243676 | 20061102 |
| A method and apparatus for obtaining various components of a multi-component material. Generally, a component of a whole blood sample may be concentrated from a patient and re-introduced to the same patient. For example, a clotting component, such as thrombin, from a whole blood sample may be extracted and concentrated in an apparatus and collection to be reapplied or reintroduced into a patient.
... |
| Means for stabilization of thrombin and compositions | 20060246052 | 20061102 |
| The present invention is to provide a means for the stabilization of thrombin and a stabilized thrombin-containing composition having a good reproducibility of the measurement. There are provided a means for the stabilization of thrombin, characterized in that, effective amount(s) of one or more which is/are selected from calcium ion, surfactant and protein is/are contained and a stabilized thrombin-containing composition as well. There are also provided a means for the stabilization of thrombin where an effective amount of a water-soluble organic acid is jointly used in addition to the above and a stabilized thrombin-containing composition as well. There is further provided a thrombin-containing composition having an extremely high measurement reproducibility using thrombin and stabilizer for thrombin where one or more high-molecular polysaccharides or synthetic polymers is/are... |
| Exo- and diastereo- selective syntheses of himbacine analogs | 20060247450 | 20061102 |
| This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
... |
| Fibrin cell supports and method of use thereof | 20060240555 | 20061026 |
| The present invention relates to fibrin cell supports for cell cultures formed by the mixture of plasma proteins including fibrinogen and thrombin. The fibrin cell supports are preferably used for preparing a culture of cells such as keratinocytes, recovering the culture in the form of a reconstituted tissue, and transporting same. The reconstituted tissue is particularly suitable for use as a skin graft.
... |
| Amino acid-substituted coagulation factor v | 20060241039 | 20061026 |
| There is provided FV derivatives that reduce blood clotting activity, by reducing thrombin generation, when compared to wild-type FV. In particular, the FV of the present invention comprises single-point and multi-point mutations, encompassed by aspartic acid 79 to glutamic acid 119. The derivatives can be used to treat patient with conditions necessitating reduced clotting activity.
... |
| Use of thrombin-derived peptides for the therapy of chronic dermal ulcers | 20060241049 | 20061026 |
| Disclosed is a method of promoting healing of a chronic dermal skin ulcer, such as a diabetic ulcer, on a subject. The method comprises the step of contacting the chronic dermal skin ulcer with an effective amount of an agonist of the non-proteolytically activated thrombin receptor.
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| Fluorinated pyridine n-oxide thrombin modulators and process for n-oxidation of nitrogen containing heteroaryls | 20060241148 | 20061026 |
| or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.
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| Stability for injection solutions | 20060233778 | 20061019 |
| A primary package containing a low molecular weight peptide-based thrombin inhibitors which package is sealed with a rubber stopper or plunger containing bromobutyl rubber.
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| Hematological assay and kit | 20060234325 | 20061019 |
| The present invention is directed to a kit and a method for a fast and direct determination of the coagulation potential of a sample of blood or plasma utilising a thrombin substrate. The kit comprises at least one activator of the plasmatic substrate with a KM preferably coagulation system and a thrombin less than or equal to 200 μM in a relatively low concentration with respect to the sample whereby the substrate is wholly consumed within 5 to 600 seconds. Observations are made leading to a determination of the maximum rate of substrate consumption.
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| New pharmaceutical compositions for treatment of thrombosis | 20060222640 | 20061005 |
| The present invention relates to novel pharmaceutical compositions comprising at least one direct thrombin inhibitor and at least one additional active compound selected from the groups consisting of platelet inhibitors, low molecular weight heparins (LMWH) and heparinoids as well as unfractionated heparin, factor Xa inhibitors, combined thrombin/factor Xa inhibitors, fibrinogen receptor antagonists (glycolprotein IIb/IIa antagonists) and Vitamin K antagonists, optionally together with one or more pharmaceutically acceptable excipients or carriers for the treatment of thrombosis.
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