322 results about "Antithrombotic Agent" patented technology

A kit and for flushing a medical device a method of preparing the kit is disclosed. The kit includes a container containing a mixed solution a unit dose of a pharmacologically effective amount of an antimicrobial agent and a second agent. The mixed solution has been mixed in a carrier solution and lyophilized. The second agent is an anticoagulant, an antithrombotic agent or a chelating agent. The kit and method are useful for maintaining the patency of indwelling medical devices such as catheters and for preventing infections caused by bacterial growth in catheters.

Bioabsorbable polymer scaffolds with coatings are disclosed that include immobilized antithrombotic agents on the scaffolds or in or on the coatings. The agents act synergistically with antiproliferative agents released from coatings by providing hemocompatibility during and without interfering with antiproliferative agent release. Methods of modifying scaffolds and coatings with the antithrombotic agents are disclosed.

A medical device comprising a supporting structure capable of containing or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient may contain one or more therapeutic agents or substances, with the carrier preferably including a coating on the surface thereof, and the coating containing the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature. Drugs that are suitable for use in this invention include, but are not limited to,

This drug can be used in combination with another drug including those selected from anti-proliferative agents, anti-platelet agents, anti-inflammatory agents, anti-thrombotic agents, cytotoxic drugs, agents that inhibit cytokine or chemokine binding, cell de-differentiation inhibitors, anti-lipaedemic agents, matrix metalloproteinase inhibitors, cytostatic drugs, or combinations of these drugs.

The invention discloses a compound (6S)-4,5,6,7- tetrahydro-3H-imidazole[4,5-c]-pyridine-6-formyl-L-amino acid, and relates to seventeen compounds 5a-q shown as the general formula I, a preparation method and application in preparation of anti-thrombosis medicines. The blood clot dissolving effect of the compounds is evaluated on a rat cervical arteriovenous shunt thrombosis cannula model. The preparation method is simple, raw materials are easy to obtain, safe and low in cost, and the compounds shown as the general formula I have anti-platelet aggregation activity and anti-thrombosis activity and can be applied to preparation of anti-thrombosis medicines.

The invention discloses (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives, and a synthesis method and application thereof. The structural formula of the compounds is shown as a general formula I. Hexa hydro-pyrazino-pyridino-indoldione compounds are structurally modified by natural amino acid, the water solubility and in-vivo absorption are improved and the anti-thrombotic activity is improved. In-vitro and in-vivo anti-thrombotic activity experiments indicate that the compounds in the general formula I have excellent anti-thrombotic activity, and can be prepared into anti-thrombotic medicines.

The invention discloses RGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD tetrapeptide and are shown in the general formula I. In the general formula I, R represents Arg-Gly-Asp-Val, Arg-Gly-Asp-Phe or Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD tetrapeptide (wherein R represents Arg-Gly-Asp-Val, Arg-Gly-Asp-Phe or Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention provides a novel preparation method which is easily industrially achieved and is simple and convenient to carry out and is established under a new intermediate. The invention relates to a novel preparation method of micromolecule anticoagulant Ticagrelor, and synchronously relates to an intermediate body for synthesizing the Ticagrelor and a preparation method of the intermediate. With the adoption of the synthesis method provided by the invention, the side reaction in the reaction process can be effectively reduced, the purity of the intermediate is improved, and the purifying way of the intermediate is simplified.

A drug delivery device is provided with openings for directional delivery of a plurality of therapeutic agents to blood vessels or other lumens or organs. In particular, the invention relates to the delivery of different therapeutic agents, different quantities of therapeutic agents, or different release profiles of the same or different therapeutic agents in different directions from the drug delivery device. The invention is useful, for example, for delivering antirestenotic, antithrombotic, antiplatelet, antiproliferative, antineoplastic, immunosuppressive, angiogenic, anti-inflammatory, or antiangiogenic agents and/or vasodilators to a blood vessel. In one embodiment, antiproliferative, antineoplastic, angiogenic, antiangiogenic, anti-inflammatory, and/or antirestenotic agents are delivered to the wall of a blood vessel and antithrombotic agents, antiplatelet agents, and/or vasodilators are delivered to the lumen of a blood vessel.

The present invention embodies: methods; compounds, their pharmaceutically acceptable analogs, isomer, salts, hydrates, solvates and prodrug derivatives, and pharmaceutically acceptable compositions thereof that have particular biological properties; devices; diagnostic and other assays; and the uses of such methods, compounds, devices and assays. Common throughout these embodiments is specific selective reduction of intravascular thromboplastin antecedent activity, which results in a safe antithrombotic effect. A particularly prominent application or the invention relates to diagnosis and treatment of patients which have, or are at risk of, developing thrombosis, thrombotic injury, or vaso-occlusive diseases, such as myocardial infarction, stroke, restenosis after angioplasty, thrombotic diseases, etc. Another particularly prominent feature of the present invention is its high level of hemostatic safety at optimal efficacy. Also, the present invention is compatible for use in combination with other traditional therapeutic agent such as another antithrombotic, antiplatelet, thrombolytic, or anticoagulant agents.

The present invention provides new methods of treating thrombosis and cardiovascular diseases using of antithrombotic agents, as well as methods of determining therapeutically effective amounts of antithrombotic agents and unit dose formulations thereof.

Novel recombinant anticoagulation proteins, methods of their use and methods of their production are described. In particular, recombinant fusions of annexin V (ANV) and Kunitz protease inhibitors (KPI) that possess potent anticoagulant activity are provided. The fusions, abbreviated ANV:KPI, utilize ANV having high affinity for phosphatidyl-L-serine with various KPI's to target serine proteases in membrane-associated coagulation complexes in the blood coagulation cascade. ANV:KPIs are potentially useful antithrombotic drugs permitting localized passivation of thrombogenic vessel walls and associated thrombi.

The invention discloses 14 novel compounds, which are represented by the formula I, of bi[indole-3-yl)-acetylamino acid] connected by ethyl, wherein the AA is selected from L-Ala, Gly, L-Phe, L-Trp, L-Tyr, L-Ile, L-Leu, L-Glu, L-Asp, L-Met, L-Ser, L-Thr, L-Pro, and L-Val residuals, discloses a preparation method of the compounds, and also discloses antithrombotic activity of the compounds, and applications of the compounds as a antithrombotic agent.

The invention provides 15 6,7-dibydroxyl-1,1-dibydroxyl-tetrahydroisoquinoline-3-formyl amino acids of a general formula I. In the general formula I, AA is selected from L-Ala, Gly, L-Phe, L-Val, L-Leu, L-Ile, L-Trp, L-Ser, L-Thr, L-Tyr, L-Lys, L-Pro, L-Asp, L-Arg and L-Glu residues. The invention provides preparation methods of amino acids, and further provides the antithrombotic effect thereof on a rat carotid artery/jugular vein bypass intubation antithrombotic model. Therefore, the 15 6,7-dibydroxyl-1,1-dibydroxyl-tetrahydroisoquinoline-3-formyl amino acids of the general formula I has application prospect in clinical antithrombotic agents.

The invention relates to the technical field of medicine, in particular to a new benzoxanthone type compound and an application thereof in pharmacy. Benzoxanthone type derivatives are one type of topoisomerase I inhibitors in new structure, which are found in recent years, and have obvious cell proliferation activity. The invention provides the new benzoxanthone type compound and pharmaceutical salts thereof, and the structure of the compound is as shown in the general formula (I). The invention further provides the application of the benzoxanthone type compound and the pharmaceutical salts thereof in the preparation of the topoisomerase inhibitors, anti-tumor medicaments, antifungal medicaments, antiviral medicaments, anti-hypertensive medicaments or anti-thrombotic medicaments.

The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption.

Compounds of the following formula (I):

where a, b, R¹, R², R³, R⁴ and R⁶ are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Glycosaminoglycans derived from K5 polysaccharide having high anticoagulant and antithrombotic activity and useful for the control of coagulation and as antithrombotic agents are obtained starting from an optionally purified K5 polysaccharide by a process comprising the steps of N-deacetylation/N-sulfation, C5 epimerization, O-oversulfation, selective O-desulfation, 6-O-sulfation, N-sulfation, and optional depolymerization, in which said epimerization is performed with the use of the enzyme glucoronosyl C5 epimerase in solution or in immobilized form in the presence of divalent cations. New, particularly interesting antithrombin compounds are obtained by controlling the reaction time in the selective O-desulfation step and submitting the product obtained at the end of the final N-sulfation step to depolymerization.

The invention relates to a method of treating and preventing thromboembolic disorders, comprising administering dipyridamole in combination with an antithrombotic selected from direct thrombin inhibitors, factor Xa inhibitors and combined thrombin/factor Xa inhibitors to a patient, pharmaceutical compositions suitable for this method of treatment as well as the use of dipyridamole for the manufacture of these pharmaceutical compositions.

The invention discloses a method for screening an antithrombotic drug based on magnetic bead separation. According to the method, magnetic separation and chemical information collection (liquid chromatography-mass spectrometry) techniques are adopted; a target protein bonder is analyzed; the method is used for screening and evaluating the antithrombotic action of a drug. According to the method for screening the antithrombotic drug based on the magnetic bead separation, an optimal incubation temperature, an incubation time, a pH (potential of Hydrogen) value of a solution during incubation, ionic strength and a denaturizing cleaning solution are screened out through lots of experiments. A screening and evaluating method provided by the invention can be used for screening a large-scale natural product library or a combinatorial chemical library; in comparison with a conventional ultraviolet screening method, the screening efficiency can be obviously improved; a screening time is shortened; moreover, a synergistic effect between compounds can be discovered; the method for screening the antithrombotic drug based on the magnetic bead separation has the advantages of strong operability, quickness, high efficiency, accuracy, good repeatability and the like.