325 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.

A system and compositions including zotarolimus and paclitaxel are disclosed, as well as methods of delivery, wherein the drugs have effects that complement each other. Medical devices are disclosed which include supporting structures that include at least one pharmaceutically acceptable carrier or excipient, which carrier or excipient can include one or more therapeutic agents or substances, with the carrier including at least one coating on the surface thereof, and the coating associated with 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. These compositions and systems can be used in combination with other drugs, including 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 and other drugs.

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 present invention relates to compositions and methods for inhibiting thrombosis without compromising hemostasis. Compositions include anti-factor XI monoclonal antibodies (aXIMabs) capable of binding to an epitope on the heavy chain of human FXI, particularly the A3 domain of the heavy chain of human FXI. Compositions also include epitope-binding fragments, variants, and derivatives of the monoclonal antibodies, cell lines producing these antibody compositions, and isolated nucleic acid molecules encoding the amino acid sequences of the antibodies. The invention further includes pharmaceutical compositions comprising the anti-factor XI monoclonal antibodies of the invention, or epitope-binding fragments, variants, or derivatives thereof, in a pharmaceutically acceptable carrier. Methods of the invention comprise administering the compositions described above to a subject in need thereof for the purpose of inhibiting thrombosis, reducing a required dose of an antithrombotic agent in the treatment of thrombosis, treating metastatic cancer, or treating an acute inflammatory reaction. Methods for making an anti-factor XI monoclonal antibody, or epitope-binding fragments, variants, or derivatives thereof, are also provided.

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 present invention provides a method for testing quickly and easily the manner in which an antithrombotic agent inhibits the acceleration of blood coagulation when a platelet agonist causes acceleration of blood coagulation. The invention is a test method wherein a system in which an anticoagulant is added to a portion of blood sampled from a patient being administered an antithrombotic agent (X system blood), and a system in which an anticoagulant and adenosine diphosphate or collagen are added to a portion of the abovementioned blood (Y system blood) are simultaneously measured by thromboelastograph; and the efficacy of the antithrombotic agent is assessed by comparing the R values of the X system blood and the Y system blood. If the R value of the Y system blood is not found to differ significantly from the R value of the X system blood, the drug is judged to be working. Adenosine diphosphate and collagen can be used as the anticoagulant. The present invention provides a heretofore unknown method for easily assessing the efficacy of an antithrombotic agent.

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.

Methods of prophylaxis or treatment of a disease state initiated by or characterized by platelet aggregation, that employ a fruit extract or active fraction thereof, are disclosed. In one embodiment, the fruit extract or active fraction thereof, is obtained from the fruit of plants of the families Solanaceae, Rutaceae, Cucurbitaceae, Rosaceae, Musaceae, Anacardiaceae, Bromeliaceae, Vitaceae, Arecaceae, Ericaceae and Lauraceae. Pharmaceutical compositions comprising a fruit extract or active fraction thereof having platelet aggregation inhibitory activity are also disclosed.

The invention discloses a preparation method of a compound Apixaban as an anti-thrombotic drug. The method disclosed by the invention comprises the following steps of: with a compound 11 shown as the formula 1 as a starting raw material, subjecting the compound 11 and amino protected paraiodoaniline 19 to coupling reaction in the existence of a cuprous reagent and an inorganic base to obtain a compound 20; subjecting the compound 20 and a compound 21 to [3+2] cyclization-elimination reaction to obtain a compound 22; removing a protecting group of the compound 22 to obtain a compound 23, or subjecting the compound 20 and the compound 21 to [3+2] cyclization reaction, directly carrying out elimination reaction under an acidic condition, and meanwhile, removing the protecting group to obtain the compound 23; subjecting the compound 23 to ammonolysis reaction to obtain a compound 24; subjecting the compound 24 and 5-chlorovaleryl halogen to amidation reaction to obtain a compound 25; and cyclizing the compound 25 under an alkaline condition to obtain the Apixaban, or subjecting the compound 24 and 5-chlorovaleryl bromine to amidation and cyclization two-step one-pot method reaction under the alkaline condition to obtain a target product, namely the Apixaban.

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.

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.

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 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 discloses a Fuc3S4S substituted oligo-glycosaminoglycan with the weight-average molecular weight of about 4.5-9kD, a medicine composition containing the Fuc3S4S substituted oligo-glycosaminoglycan, preparation methods thereof and an application thereof in preparing medicines for preventing or treating thrombotic diseases. The oligo-glycosaminoglycan has a structure shown as the formula (I); in the formula (I), a substituent group is defined as the specification. The Fuc3S4S substituted oligo-glycosaminoglycan and the medicine composition thereof have strong-effect factor X enzyme inhibition activity and HC-II depended antithrombase activity, and can be used for preparing antithrombus medicines.

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 invention discloses a (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid kyrine conjugate, a preparation method and application thereof. The preparation method of the conjugate comprises the following steps of: preparing N-[(3S)-N-Boc-1,2,3,4- tetrahydroisoquinoline-3-formoxyl]-AA1-AA2-Arg (NO2)-OBzl by coupling N-[(3S)-N-Boc-1,2,3,4-tetrahydroisoquinoline-3-formoxyl]-AA1 and AA2-Arg (NO2)-OBzl; and detracting a protecting group, wherein AAl is selected from Gly, Asp or Gln, and AA2 is selected from Gly, Asp or Gln. The conjugate has excellent antithrombotic activity, can be clinically used as an antithrombotic agent, can be automatically assembled into nano particles in a water solution and is stable in the water solution; and the particle diameter is mostly from 200nm to 600nm.

Organoboronic acids, for example Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2, are made by hydrolysing their diethanolamine adducts under conditions which avoid substantial C—B bond breakage. The product acids are substantially free of degradation product derived from cleavage of the C—B bond thereof. The acids are used to make base addition salts thereof. The salts are formulated into anti-thrombotic pharmaceutical formulations.

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.

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.

The present invention relates to compositions and methods for inhibiting thrombosis without compromising hemostasis. Compositions include anti-factor XI monoclonal antibodies (aXIMabs) capable of binding to an epitope on the heavy chain of human FXI, particularly the A3 domain of the heavy chain of human FXI. Compositions also include epitope-binding fragments, variants, and derivatives of the monoclonal antibodies, cell lines producing these antibody compositions, and isolated nucleic acid molecules encoding the amino acid sequences of the antibodies. The invention further includes pharmaceutical compositions comprising the anti-factor XI monoclonal antibodies of the invention, or epitope-binding fragments, variants, or derivatives thereof, in a pharmaceutically acceptable carrier. Methods of the invention comprise administering the compositions described above to a subject in need thereof for the purpose of inhibiting thrombosis, reducing a required dose of an antithrombotic agent in the treatment of thrombosis, treating metastatic cancer, or treating an acute inflammatory reaction. Methods for making an anti-factor XI monoclonal antibody, or epitope-binding fragments, variants, or derivatives thereof, are also provided.

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.