51 results about "Antithrombotic Agent" patented technology

The invention discloses a scorpion-derived polypeptide and application thereof, and belongs to the technical field of functional proteins. The amino acid sequence of the polypeptide derived from the Buthus martensii Karsch is as shown in SEQ ID NO. 1, SEQ ID NO. 2, SEQ ID NO. 3, SEQ ID NO. 4 or SEQ ID NO. 5. The polypeptide derived from the Buthus martensii Karsch is a polypeptide derived from the Buthus martensii Karsch. The invention also provides an application of the buthus martensii-sourced polypeptide with the amino acid sequence shown as SEQ ID NO. 1 in preparation of a blood coagulation promoting drug and an application of the buthus martensii-sourced polypeptide with the amino acid sequence shown as SEQ ID NO. 2, SEQ ID NO. 3, SEQ ID NO. 4 or SEQ ID NO. 5 in preparation of a blood coagulation promoting drug. The buthus martensii-sourced polypeptide provided by the invention has a relatively good application value in the aspect of research and development of antithrombotic drugs or coagulant drugs.

An antithrombotic surface-modified biomaterial is provided comprising a biomaterial substrate coated with a polymerizable dopamine-containing bioadhesive to which is attached one or more antithrombotic agents. A method of preparing the surface-modified biomaterial is also provided. The surface-modified biomaterial is beneficial for use in blood-contacting medical devices such as catheters, dialyzers and blood oxygenators to prevent or minimize the occurrence of thrombosis on the surface thereof.

The invention provides application of an SNP (Single Nucleotide Polymorphism) marker of MIA2 in predicting the curative effect of an antithrombotic drug on thrombus, and belongs to the fields of molecular biology and cardiovascular medicine. According to the application disclosed by the invention, one or more of rs11845046 and rs10134365 of the MIA2 gene is found to be related to the prediction of the curative effect of dabigatran on thrombus for the first time. Gene polymorphism analysis and an ROC curve verify that the curative effect of an NVAF patient after the NVAF patient is treated by using the antithrombotic drug is related to the genotypes of rs11845046 and rs10134365 of the MIA2 gene in a patient sample, and when the genotype of the rs11845046 is GG or the genotype of the rs10134365 is CC, the drug effect of the subject taking the antithrombotic drug is good but the probability of bleeding events is increased.

The invention relates to a recombinant hirudin fusion protein, a coding gene and a prokaryotic expression method and application of the recombinant hirudin fusion protein. The recombinant hirudin fusion protein comprises an HMg variant amino acid sequence and a fusion tag. The recombinant hirudin fusion protein has the advantages that the hirudin variant in poecilobdella manillensis is adopted to construct an efficient prokaryotic expression system, the hirudin yield and activity are improved under the condition that post-translational modification is not needed, the anticoagulant efficiency and the production process of the recombinant hirudin fusion protein provide an important basis for development of a new generation of antithrombotic drugs, and the recombinant hirudin fusion protein has wide application prospects. The progress of cardiovascular disease treatment and hirudin production is expected to be promoted.

The invention discloses a chondroitin sulfate oligosaccharide derivative and a preparation method and application thereof.The chondroitin sulfate oligosaccharide derivative is shown in the formula (I), the definition of substituent groups in the formula is shown in the specification, and the derivative comprises di-, tetra-and hexasaccharide derivatives of chondroitin sulfate B and T, has endogenous anticoagulation and anti-inflammatory activity, and can be used for preparing the chondroitin sulfate oligosaccharide derivative. The compound can be developed into anticoagulant and antithrombotic drugs.

The invention provides a method for analyzing trace elements in dinodon rufozonatum and an antithrombotic activity application of the dinodon rufozonatum. The method comprises the following steps: pretreatment of a dried snake or decocted liquid sample, microwave digestion, acid removal and constant volume, and ICP-MS detection of 25 trace elements. The antithrombotic activity application of the method for analyzing the trace elements in the dinodon rufozonatum is characterized in that the trace elements such as selenium, chromium and vanadium related to the antithrombotic activity are detected, the content range of the trace elements is strictly controlled, element-activity correlation verification is carried out in combination with an antithrombotic activity verification experiment, and the dinodon rufozonatum antithrombotic preparation is provided. The composition comprises dinodon rufozonatum alcohol extract and pharmaceutical auxiliary materials in a mass ratio of (4-9): 1, and the content of antithrombotic elements in the dinodon rufozonatum alcohol extract meets specific standards. The development and application of the preparation provide a new choice for the field of antithrombotic drugs, fully explore the medicinal value of dinodon rufozonatum, and have broad market prospects and important scientific significance.

The invention provides application of mycophenolic acid methyl ester in preparation of antithrombotic drugs, and belongs to the technical field of antithrombotic drugs. The antithrombotic activity of the compound mycophenolic acid methyl ester is found for the first time, and experimental support and theoretical basis are provided for developing novel drugs for treating or preventing thrombus.

The invention discloses an application of PEAR1 gene polymorphism in predicting the bleeding risk of a non-valvular atrial fibrillation patient under the treatment of an antithrombotic drug. The specific related SNP site is rs12407843, further research is carried out in healthy people and NVAF patients, and it is found that when the rs12407843 genotype is GG, the antithrombotic efficacy of a subject taking the antithrombotic drug is better than that of GA and AA carriers, but the probability of bleeding events is increased. The invention further discloses a method, a system and equipment for predicting the curative effect of the antithrombotic drug after thrombus treatment, so that a doctor is assisted in evaluating the treatment effect of a thrombus patient, and a clinician is guided to formulate a personalized treatment scheme for the patient.

This invention relates to the field of biomedicine, specifically to the application of banana fruit extract in the preparation of anticoagulant or antithrombotic drugs. The banana fruit extract provided by this invention contains flavonoids, polyphenols, polysaccharides, hydroxyanthraquinones, triterpenoids, and other components. Flavonoids and polyphenols have been widely proven to have anti-inflammatory and antioxidant effects, which can synergistically enhance the anticoagulant effect. The high potassium content of banana fruit can indirectly improve vascular function by regulating sodium-potassium balance. The banana fruit extract provided by this invention can inhibit platelet production or promote platelet metabolism, prolong clotting time, and inhibit platelet aggregation. Its natural plant components interfere with platelet aggregation by inhibiting the production of thromboxane A2, achieving anticoagulant and antithrombotic effects. The mechanism of action of banana fruit extract differs from traditional anticoagulants such as heparin, reducing the risk of bleeding. Its natural component characteristics provide a direction for the development of novel plant-derived anticoagulant drugs.

The invention discloses an antithrombotic drug derived carbon dot as well as a preparation method and application thereof. Comprising the steps that an antithrombotic drug is selected as a precursor, the antithrombotic drug comprises at least one of an antiplatelet drug with a pharmacodynamic group, an anticoagulant drug with a pharmacodynamic group and a fibrinolytic drug with a pharmacodynamic group, the molecular weight of the antithrombotic drug is 100-2000 Da, and the thermal stability decomposition temperature is larger than or equal to 200 DEG C; the pharmacodynamic groups comprise at least one of sulfonic acid groups, acetoxy groups, indole rings and coumarin structures; performing gradient carbonization treatment on the precursor in a plurality of temperature zones, wherein the plurality of temperature zones comprise a low-temperature zone capable of retaining pharmacodynamic groups, a medium-temperature zone for regulating and controlling a carbon hybridization ratio and a high-temperature zone for performing heteroatom doping; and performing purification and drying treatment to obtain the antithrombotic drug derived carbon dots. Through the preparation method, the antithrombotic drug derived carbon dots with a thrombolysis function and high safety can be obtained, and the problem that the curative effect and safety of an existing antithrombotic drug are unbalanced is solved.

Embodiments of the invention are directed to a thrombus profiling assay that combines high shear flow and stenotic geometries with multi-color fluorescence imaging to comprehensively characterize thrombi forming under the physiological settings of arterial thrombosis.

The invention provides application of Dipheylazaine A in preparation of antithrombotic drugs, and belongs to the technical field of biological medicines.The Dipheylazaine A can reverse PTK787 induced zebra fish vascular injury and arachidonic acid induced zebra fish thrombosis, has the activity of promoting angiogenesis and resisting thrombus, and can be used for preparing antithrombotic drugs. Candidates can be provided for research and development of related drugs or antithrombotic drugs for promoting angiogenesis to treat cardiovascular diseases, and wide market application prospects are achieved.

The present disclosure provides use of icaritin in preparing a drug for preventing and treating a bleeding disorder and belongs to the field of medicine. The icaritin can relieve platelet dysfunction, shorten thromboplastin time, and promote blood coagulation, and can be used for preventing and treating the bleeding disorder, especially for treating hemorrhagic transformation after cerebral infarction, gastrointestinal bleeding caused by a thrombolytic or antithrombotic drug for cerebral infarction, or a bleeding complication of a thrombolytic or antithrombotic drug for myocardial infarction.

The invention discloses an endothelium targeted controlled-release antithrombotic drug intelligent monitoring biodegradable heart occluder, and relates to the field of medical instruments, the heart occluder comprises an occluder main body and a sheathing canal for regulating and controlling the occluder main body, the occluder main body is composed of a double-disc-shaped biological skeleton, a fixed deformation body and a biological flow blocking film, the double-disc-shaped biological skeleton is composed of two attaching discs which are mutually symmetrical to form a left center disc face and a right center disc face, a support outer disc is arranged on the side surfaces of the attaching discs in a surrounding mode, and a double-layer antithrombotic drug controlled release layer is arranged on the surface of the support outer disc; the two attaching plates are tightly connected with the fixed deformation body, an ultrasonic blood flow sensor is arranged in the fixed deformation body, an impedance sensor is arranged at the position, located on one side of the ultrasonic blood flow sensor, in the fixed deformation body, and the biological flow blocking films are arranged on the surfaces of the opposite sides of the two attaching plates respectively. The plugging device is periodically degraded in the body of a patient to reduce complications caused by foreign matter retention, and aiming at thrombus formation on the surface of the plugging device, middle and low doses of antithrombotic drugs are locally controlled, so that whole-body adverse reactions caused by long-term oral administration of the antithrombotic drugs after the plugging operation are reduced. Thrombus risk and occluder endothelialization process are dynamically monitored to assist in repair and regeneration of heart tissue.

The present application relates to a kind of cis 4-(5,6-diphenylpyrazin-2-aminyl) cyclohexyloxy acetic acid compound and its synthesis method and application, belong to the technical field of drug synthesis.The cis 4-(5,6-diphenylpyrazin-2-aminyl) cyclohexyloxy acetic acid compound has simple molecular structure, simple synthesis path and low production cost.Through in vitro platelet aggregation inhibition activity test, it is found that the synthesized compound shows excellent anti-platelet aggregation effect.In addition, in rat pharmacokinetic study, it is found that the compound shows excellent pharmacokinetic characteristics, has high bioavailability and longer half-life, can effectively improve its activity as antithrombotic drug, and shows excellent prevention and treatment effect in antithrombotic, vasodilator and anti-pulmonary arterial hypertension etc..

The invention discloses tanshinone derivatives with antithrombotic activity as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The tanshinone derivative is obtained by structurally modifying tanshinone IIA and cryptotanshinone, the polarity and pharmacological activity are remarkably improved, the bioavailability is greatly improved, the problem that the tanshinone IIA and the cryptotanshinone are limited in clinical application is solved, and the problems that the tanshinone IIA and the cryptotanshinone are high in lipid solubility, difficult to prepare into proper dosage forms, affected in absorption and distribution of drugs, short in half-life period, required to be frequently administered and poor in bioavailability are solved. And inconvenience is brought to the patient. Part of tanshinone derivatives have remarkable anticoagulant activity; the synthetic method is simple to operate and controllable in condition, a series of derivatives can be efficiently synthesized, and the derivatives have the biological activities of anticoagulation, platelet aggregation resistance, thrombosis resistance and the like, are the key for the antithrombotic drugs to play a therapeutic role, provide efficient and safe candidate drugs for cardiovascular and cerebrovascular diseases, and have remarkable technical advantages and huge market potential.

The present invention provides a leech-derived polypeptide having both analgesic and antithrombotic functions, a precursor protein thereof, and applications thereof, belonging to the technical field of functional peptides. The leech-derived polypeptide provided by the present invention has an amino acid sequence as shown in SEQ ID NO: 1. The leech-derived polypeptide provided by the present invention can inhibit the activity of proteases such as elastase, FXIIa, and kallikrein, and has good anticoagulant effects, while also having good analgesic and antithrombotic effects. The polypeptide has the characteristics of a simple structure, strong analgesic and antithrombotic activities, and can be used as an analgesic and antithrombotic drug.

The present application belongs to the technical field of biological medicine, and particularly relates to an earthworm anti-platelet oligopeptide and application thereof. The present application is an anti-platelet oligopeptide discovered by combining a Pheretima aspergillum (E. Perrier) transcriptome database with active-oriented separation. The oligopeptide can not only inhibit the activation and aggregation of platelets, but also effectively inhibit the adhesion and expansion of platelets, and can effectively inhibit various functions of platelets at an in-vitro level. In summary, the oligopeptide of the present application can significantly inhibit platelets, and is suitable for anti-thrombus drug research and development.

Provided herein are compositions containing guest / host inclusion complexes. In particular, each complex includes S-nitrosoglutathione (GSNO) as the guest and substituted or unsubstituted cyclodextrin as the host, such as alpha cyclodextrin. The compositions may be used as an antibacterial and antithrombotic agent in catheter lock solutions and to deliver nitric oxide to a subject in need thereof.

The invention discloses a preparation method of a chiral 2-((1-(5, 6-diphenyl pyrazine-2-yl)-3, 3-dimethyl piperidine-4-yl) oxy) acetic acid compound, and belongs to the technical field of medicinal chemistry. The novel preparation method developed by the invention has the characteristics of short synthetic route, low cost and easiness in industrial amplification, and in addition, the chiral 2-((1-(5, 6-diphenylpyrazine-2-yl)-3, 3-dimethylpiperidine-4-yl) oxy) acetic acid compound has the characteristic of high activity and can be used as an active ingredient for antithrombotic drugs.

The invention relates to the field of pharmaceutical preparations, in particular to an antithrombotic aspirin composite sustained release tablet and a preparation process thereof. The preparation process of the antithrombotic aspirin composite sustained-release tablet comprises the following steps: preparing the composite carrier, preparing the drug-loaded compound and preparing the aspirin composite sustained-release tablet. The preparation method comprises the following steps: reacting L-methionine with 1, 4-butanediol to prepare an intermediate A, reacting the intermediate A with di-p-nitrophenyl adipate to prepare an intermediate B, reacting the intermediate B with carboxyl-terminated mPEG to obtain an amphipathic composite carrier, and loading aspirin and tanshinone IIA by using the composite carrier to obtain the aspirin-tanshinone IIA loaded aspirin-tanshinone IIA loaded aspirin-tanshinone IIA loaded aspirin-tanshinone IIA loaded aspirin-tanshinone IIA loaded aspirin-tanshinone. The preparation method comprises the following steps: preparing a medicine-carrying compound, mixing the medicine-carrying compound with other raw materials to prepare a sustained-release tablet, oxidizing and releasing the antithrombotic medicines aspirin and tanshinone IIA by the methylthio group of the medicine-carrying compound, and meanwhile, protecting the aspirin from being oxidized and hydrolyzed by reducing the level of active oxygen, so that the controlled-release effect of the medicines is achieved, and local precise release of the medicines is realized.

Disclosed is applicability in novel uses of a DO3A-based material containing a gadolinium complex as an antithrombotic agent or a coagulant, on the basis of a discovery finding that the DO3A-based material containing the gadolinium complex which has been used as an anti-inflammatory agent has a novel effect of suppressing a thrombus induced by thrombin or dissolving blood, without being involved in the function of platelet action which stops bleeding at a damaged or injured area.

The application discloses a 5,6-diphenylpyrazine-2-azacycle compound and a preparation method and application thereof. The 5,6-diphenylpyrazine-2-azacycle compound is synthesized by a more simple and economical method, and it is found through anti-platelet aggregation activity detection that the prepared 5,6-diphenylpyrazine-2-azacycle compound has excellent anti-platelet aggregation activity and small toxic side effect, and can be used as an active ingredient of an antithrombotic drug. In addition, the activity of the synthesized 5,6-diphenylpyrazine-2-azacycle compound is greatly influenced by chiral compounds, and the activity of an R-type compound is obviously greater than that of an S-type compound, so that the R-type compound can play a more excellent antithrombotic effect as an active ingredient of an IP receptor agonist or other antithrombotic drug.

This invention discloses a novel Prussian blue nanomedicine for rapid photothermal thrombolysis and long-term inhibition of thrombus recurrence. Specifically, the nanomedicine uses Prussian blue nanoparticles as a drug carrier, rutin as an antithrombotic drug that inhibits platelet aggregation, and is encapsulated with a phase change material nanomedicine prepared from a mixture of hexadecyl alcohol and oleic acid, with the surface modified by RGD peptide. Prussian blue, as an inorganic nanomaterial, inherently possesses catalase-like (CAT) activity and exhibits good light absorption in the near-infrared region. Relying on the ability of RGD peptide to specifically bind and activate platelets, the nanomedicine is first targeted and delivered to the thrombus site. Under near-infrared light irradiation, the Prussian blue nanoparticles undergo photothermal conversion, generating heat to dissolve the thrombus. Simultaneously, the thermally induced phase change triggers drug release, and the drug, in conjunction with the antioxidant effect of Prussian blue, provides a long-term inhibitory effect against thrombus recurrence. Therefore, the Prussian blue nanomedicine provided by this invention not only enables rapid photothermal thrombolysis but also provides long-term inhibition of thrombus recurrence, offering a new approach to antithrombotic treatment strategies.

The invention relates to the technical field of biological medicine, and discloses a recombinant antiplatelet thrombolysin protein as well as a nucleotide sequence, a preparation method and application thereof. The recombinant antiplatelet thrombolysin protein provided by the invention is a high-purity, high-quality and high-activity protein obtained by optimizing an amino acid sequence of a natural antiplatelet thrombolysin protein, expressing and purifying the protein, takes GPIb as a therapeutic target, has remarkable activity compared with the natural antiplatelet thrombolysin protein, and can be used for preparing a medicine for treating the thrombolysin. A brand-new direction and a brand-new view angle are provided for research and development of antithrombotic drugs.

This disclosure provides oral, sublingual or buccal use of P1,P4-diadenosine tetraphosphates as antithrombotic agents in vivo, and in particular as antiplatelet agents for prevention and / or treatment of diseases related to platelet activation and aggregation. The disclosure also provides formulations which enhance the oral, sublingual or buccal bioavailability of the P1,P4-diadenosine tetraphosphates.

The invention discloses application of Serpin protein based on mosquito salivary glands in preparation of antithrombotic drugs, and relates to the technical field of protein engineering, and the technical key points are as follows: the antithrombotic drugs comprise the Serpin protein extracted from the aedes albopictus salivary glands, and the Serpin protein can effectively prolong APTT, PT and TT of blood, reduce the content of Fib in the blood, and interact with a blood coagulation factor X. The invention also discloses a preparation method of the Serpin protein based on mosquito salivary glands, and the application of the Serpin protein based on mosquito salivary glands in preparation of antithrombotic drugs based on mosquito salivary glands in preparation of antithrombotic drugs based on mosquito salivary glands in preparation of antithrombotic drugs based on mosquito salivary glands. The Serpin protein of the aedes albopictus salivary gland can prolong PT, APTT and TT of blood in vitro and reduce the content of Fib in the blood; the Serpin protein has a therapeutic effect on formed thrombus in an in-vivo experiment, can relieve the blood coagulation degree and reduce the expression of blood coagulation factors, and can interact with a mouse blood coagulation factor X, so that the Serpin protein has important significance in understanding the anticoagulation mechanism of the Serpin protein and evaluating the potential of the Serpin protein as an antithrombotic therapeutic drug.

Disclosed is applicability in novel uses of a DO3A-based material containing a gadolinium complex as an antithrombotic agent or a coagulant, on the basis of a discovery finding that the DO3A-based material containing the gadolinium complex which has been used as an anti-inflammatory agent has a novel effect of suppressing a thrombus induced by thrombin or dissolving blood, without being involved in the function of platelet action which stops bleeding at a damaged or injured area.

The invention relates to ADAMTS13 protein variants comprising residues 1 to 685 of ADAMTS13 and wherein one or more N-linked glycosylation sites are added as compared to wild-type ADAMTS13 and / or one or more existing N-linked glycosylation sites are shifted as compared to wild-type ADAMTS13. The invention further relates to compositions comprising such ADAMTS13 variants, methods for their preparation and uses thereof, in particular as an antithrombotic agent, and in the treatment of thrombotic disease, thrombotic microangiopathy, thrombotic thrombocytopeniaurpura (TTP), hemolytic-uremic syndrome (HUS), ischemic stroke, systemic thrombosis, COVID19, antiphospholipid syndrome, pre-eclampsia / HELLP syndrome, sepsis and sickle cell disease.