635 results about "Antithrombotic" patented technology

A catheter including a main body having a first end, a second end, a lumen extending between the first end and the second end, a first section located proximal the first end of the main body and second section located proximal the second end of the main body. An inhibitory polymer is disposed at the first section. The inhibitory polymer includes one or more members selected from the group consisting of antiproliferatives, antithrombotics, thrombolytics, and fibrinolytics. An antimicrobial agent is disposed at the second section. The main body has a length such that when the catheter is at least partially implanted the first end accesses a body vessel and at least a portion of the second section is disposed within a subcutaneous space of a patient.

The present invention provides compounds of Formula (I):or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W 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.

A vascular or endoluminal stent is adapted to be implanted in a vessel, duct or tract of a human body to maintain an open lumen at the site of the implant. The sidewall of the open-ended tubular structure of the stent is a base layer of a metal biologically compatible with blood and tissue of the human body. An intermediate metal particle layer of substantial greater radiopacity overlies the base layer, with particles bonded to the base layer and to each other to leave interstices therebetween as a repository for retaining and dispensing drugs or other agents for time release therefrom after the stent is implanted, to assist the stent in maintaining the lumen open. The particles are composed primarily of a noble metal—an alloy of platinum-iridium. The sidewall has holes extending therethrough, and the particle layer resides along the outward facing and inward facing surfaces, and the edges of the through holes and open ends of the sidewall. The larger particles are bonded to surfaces of the sidewall and progressively smaller particles are bonded to those and to each other up to the outer portion of the particle layer. Exposed surfaces of the particle layer are coated with ceramic-like iridium oxide or titanium nitrate, as a biocompatible material to inhibit irritation of tissue at the inner lining of the vessel when the stent is implanted. One or more anti-thrombotic, anti-platelet, anti-inflammatory and / or anti-proliferative drugs are retained in the interstices, together with a biodegradable carrier for time release therefrom. In an alternative embodiment, the intermediate layer is solid and the biodegradable carrier and drugs or agents therein are applied to the surface of the ceramic-like coating. Gene transfer is alternatively used to control tissue proliferation.

The present invention relates to a process for the preparation of thieno[3,2-c]pyridine derivatives having pharmacologically significant anti-aggregating and anti-thrombotic properties.

The present invention relates to the synthesis of beta-tetrahydro carboline carboxylic acid and its nanoparticle preparation; liquid phase process of gradually grafting peptide to obtain protected tetrapeptide intermediate, which, after eliminating its Boc, is condensated with N-Boc-beta-tetrahydro carboline carboxylic acid and further HF treated to eliminate its protection to obtain the said compound; the nanoparticle of tetrahydro carboline carboxylic acid and the in-vitro and in-vivo activity of said compound in-vitro and in-vivo experiments show that the compound of the present invention has excellent activity of resisting blood platelet aggregation, effect of resisting cell adhesion and effect of resisting thrombus.

This invention relates to processes for the production of tocotrienol compounds from biological sources such as palm oil, cereals, grains, and grain oils. The tocotrienol products are recovered in high yields. These tocotrienols are useful as pharmaceuticals, in foodstuffs and as dietary supplements. These compositions are hypocholesterolemic, antioxidizing, antithrombotic, antiatherogenic, antiinflammatory and immunoregulatory in nature. Tocotrienols are known to lower the levels of low density lipoproteins in the bloodstream.

A biocompatible biological component is provided comprising a membrane-mimetic surface film covering a substrate. Suitable substrates include hydrated substrates, e.g. hydrogels which may contain drugs for delivery to a patient through the membrane-mimetic film, or may be made up of cells, such as islet cells, for transplantation. The surface may present exposed bioactive molecules or moieties for binding to target molecules in vivo, for modulating host response when implanted into a patient (e.g. the surface may be antithrombogenic or antiinflammatory) and the surface may have pores of selected sizes to facilitate transport of substances therethrough. An optional hydrophilic cushion or spacer between the substrate and the membrane-mimetic surface allows transmembrane proteins to extend from the surface through the hydrophilic cushion, mimicking the structure of naturally-occurring cells. An alkylated layer directly beneath the membrane-mimetic surface facilates bonding of the surface to the remainder of the biological component. Alkyl chains may extend entirely through the hydrophilic cushion when present. To facilitate binding, the substrate may optionally be treated with a polyelectrolyte or alternating layers of oppositely-charged polyelectrolytes to facilitate charged binding of the membrane-mimetic film or alkylated layer beneath the membrane-mimetic film to the substrate. The membrane-mimetic film is preferably made by in situ polymerization of phospholipid vesicles.

The invention discloses a halogen substituted 2-(a-hydroxyl amyl) benzoate compound, a preparation method and medicinal application thereof, which belong to the technical field of organic chemical synthesis. The structural formula of the compound which is showed as above has an antimer structure, wherein <R1> represents a halogen atom; n is equal to 1 to 3; and M represents a univalent metallic ion or a bivalent metallic ion or a trivalent metallic ion or an organic base. The compound has the advantages of better activity on preventing and treating cardio-cerebral ischemia diseases, improving cardio-cerebral circulation disturbance and resisting thrombus, and the like.

Aiming at the conditions that heparin has severe bleeding side effects in clinical practice and clinical application thereof is restricted, the invention discloses a technique for producing ultra-low molecular heparin sodium (calcium). The technique comprises the following steps of: taking heparin sodium solution, adding sodium nitrite solution for cracking; adjusting the lysis buffer by using alkaline; absorbing impurities by using an anion-exchange column; washing for obtaining ultra-low molecular heparin calcium; carrying out filtration by using an ultrafiltration membrane and obtaining a precipitate by using alcohol; and after desalting, dehydration, re-precipitation, cooling and drying, obtaining a finished product of ultra-low molecular heparin calcium. The product has better and safer antithrombotic effect under low level of anticoagulation, and can be widely used for preventing and treating diseases such as deep vein thrombosis, pulmonary embolism, disseminated intravascular coagulation, and the like.

Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer, and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

The invention relates to implantable vascular access ports that can release agents such as antibiotics, anti-thrombogenics and anti-proliferatives. The invention also relates to ports having locking mechanisms that prevent accidental disengagement, and structures that facilitate surgical implantation and provide for long-term stability and use of the port.

A medical device adapted for contact with a vessel or cavity in the body including a tubular portion is provided. The device has an external surface including an external substance that is at least one of a coating or an impregnation, comprising alexidine in an amount that is both anti thrombogenically effective and anti microbially effective. The device also has an internal surface including an internal substance that is at least one of a coating or an impregnation, comprising alexidine in an amount that is both anti thrombogenically effective and anti microbially effective.

The present invention relates to a process for the preparation of thieno[3,2-c]pyridine derivatives having pharmacologically significant anti-aggregating and anti-thrombotic properties.

The invention relates to a method for preparing the suaveolic round leaf extractive which contains celery element or the chromocor compound with celery element as corn, or relative salt. The invention also provides relative quality control method, while said extractive can be used to prepare the drug for treating virus B hepatitis, thrombus, cancer, or the like.

The invention discloses 1-(4-hydroxy-3-methoxycarbonylphenyl)-beta-carboline-3-formyl-RGD tetrapeptide with a structure as shown in the formula. The invention also discloses a preparation method of the compound, a nano-structure of the compound, an anti-tumor effect of the compound, an effect of the compound in inhibiting adhesion, invasion and migration of tumor cells, further discloses anti-inflammatory and antithrombotic effects of the compound and expounds an application of the compound in medical science.

The present invention relates to compounds of the formula I, in which R0; R1; R2; R3; R4; R5, R, Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboemboic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and / or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and / or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and / or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Disclosed herein are methods for modifying a substrate having a hydrophobic surface. Also disclosed are modified hydrophobic substrates. The modified hydrophobic substrates and methods disclosed herein advantageously improve cell affinity and antithrombogenicity of hydrophobic surfaces.

Diagnostic methods for determining whether an individual will benefit from a particular anti-thrombotic therapeutic agent are disclosed. The methods involve obtaining a biological sample that comprises platelets, from a patient who has been pre-administered a particular therapeutic agent, which is an antagonist of a receptor associated with the biochemical pathways involved in platelet aggregation, and exposing the platelets to an agonist of the receptor. If the antagonist is ineffective, the platelets will eject microparticles, will have a different size distribution than platelets not exposed to the agonist, and will experience a change in their surface charge. In one embodiment, the diagnostic methods involve using single particle optical sizing techniques to determine the presence of such ejected microparticles, or a change in platelet size due to its activation by the agonist. In another embodiment, electrophoretic quasi-elastic light scattering techniques are used to determine the presence of a change in surface charge on the platelets. Once an effective therapeutic agent, or an effective dosage of such therapeutic agent, has been identified, the patient can begin therapy knowing that the agent will be effective.

Methods of thrombolysis that allow the use of a fibrinolytic composition comprising reversibly inactivated acidified plasmin and the localized delivery of the plasmin to a vascular thrombotic occlusion are disclosed. Further disclosed is a method for administering a therapeutic dose of a fibrinolytic composition substantially free of plasminogen activator to a human or animal having a vascular thrombotic occlusion. The fibrinolytic composition includes a reversibly inactivated acidified plasmin substantially free of plasminogen activator. Intravascular catheter delivery of the fibrinolytic composition directly into or in the immediate vicinity of the thrombus is disclosed to minimize the systemic degradation of fibrin while retaining the maximum plasmin activity against the thrombus.

The present invention relates to methods and compositions for identifying and treating subjects in need of antithrombotic therapies but who are not responsive to aspirin.

The present invention describes various devices and methods wherein a cytostatic antiproliferative drug, either alone or in combination with other drugs, is placed between internal body tissues to prevent the formation of scar tissue and / or adhesions during healing of a wound or surgical site. Specific devices to achieve this administration include, but are not limited to, a permanent implant or a biodegradable material having an attached antiproliferative drug such as sirolimus. These antiproliferative drugs may be combined with other drugs including, but not limited to, antiplatelets, antithrombotics or anticoagulants. The present invention also contemplates methods to a reduce scar tissue and / or adhesions or adhesion formation at an anastomosis site. In particular, a cytostatic antiproliferative drug is administered to an arteriovenous shunt anastomoses in patients having end-stage renal disease.

The present invention relates to methods and compositions for identifying and treating subjects in need of antithrombotic therapies but who are not responsive to aspirin.

The present invention provides a more safe and highly effective stent having functions such as anti-inflammatory action, antithrombotic action, maintenance of tissue restoration response and maintenance of endothelial regeneration. More specifically, the drug / gene eluting stent has a layer containing a gene encoding a hybrid polypeptide on the surface. The hybrid polypeptide is preferably a bound of fibronectin-derived collagen binding domain (FNCBD) polypeptide and an anti-inflammatory factor or an angiogenic factor. The uniform fine particle size capsules can directly deliver the gene encoding the hybrid polypeptide to the lesion and have benefits of reducing the given doses, and thus improving safety and efficacy and further maintaining the efficacy for a long period.

Disclosed are novel inhibitors of the AxI receptor tyrosine kinase (RTK) and methods of using such inhibitors in a variety of therapeutic approaches in the areas of cancer therapy and anti-thrombosis (anti-clotting) therapy.

The invention discloses a fusion protein for resisting formation of thrombus targetedly, which comprises the following parts: (a) protein domains of nematode anticoagulant peptide 5, of which the amino acid sequence has at least 80 percent of similarity with a sequence shown as SEQ ID No.1; (b)protein domains of Hirulog, of which the amino acid sequence has at least 80 percent of similarity with a sequence shown as SEQ ID No.2; (c) protein domains of RGD peptide, consisting of 3 to 10 amino acids and containing an Arg-Gly-Asp sequence; and (d) human coagulation factor X a recognition sites, of which the amino acid sequence is shown as SEQ ID No.3. The invention also discloses a gene encoding the fusion protein, a recombined expression vector containing the gene, a transformant containing the recombined expression vector, and a method for preparing the fusion protein. The prepared fusion protein can inhibit formation and development of thrombus from a plurality of approaches and take effect on thrombus positions targetedly, and is suitable for preventing and treating thrombotic disorders.

The invention discloses a method for evaluating chemical composition of Rosa xanthina on the basis of antithrombotic spectrum-effect relationship. The method comprises the following steps: preparing extract of different polar components of the Rosa xanthina with a modern separation technology; establishing fingerprint of extract of each component with high-performance liquid chromatography, and calibrating characteristic peaks; evaluating antithrombotic activity of different extract on the basis of platelet aggregation inhibition rate, prothrombin time, thrombin time and activated partial thromboplastin time as indexes; substituting fingerprint characteristic peak data and pharmacodynamical activity data into a mathematical model for spectrum-effect correlation analysis, and evaluating pharmacodynamical activity of the characteristic peaks. With adoption of the method for evaluating the chemical composition of the Rosa xanthina on the basis of the antithrombotic spectrum-effect relationship, the antithrombotic chemical composition in the Rosa xanthina can be evaluated rapidly and accurately, a scientific and effective method is provided for research of pharmacodynamic material basis and quality control of the Rosa xanthina, and reference is provided for further development of Rosa xanthina drugs or health care products for treating thrombotic diseases.