86 results about "Thrombotic disease" patented technology

The invention relates to a monoclonal antibody with anticoagulant activity and application thereof, the antibody or fragment comprises a light chain variable region and a heavy chain variable region, and the amino acid sequence of the light chain variable region of the antibody or fragment is as shown in SEQ ID NO: 1; the amino acid sequence of the variable region of the heavy chain is as shown in SEQ ID NO: 3. The monoclonal antibody disclosed by the invention has the effect of inhibiting the activity of a co-coagulation pathway in a coagulation cascade reaction, and can be applied to prevention and treatment of thrombotic diseases.

Provided are an siRNA which inhibits plasma coagulation factor XI gene expression, a pharmaceutical composition containing the siRNA, a conjugate, a reagent kit, and a use of the siRNA, the pharmaceutical composition thereof and the conjugate in preparing a drug used for treating and / or preventing thrombotic diseases and ischemic strokes.

The present disclosure relates to a method for treating or preventing a thrombotic disorder, comprising administering to a subject in need thereof an effective amount of the Compound (1) or a pharmaceutically acceptable salt thereof, at a dose in the range of 0.01-0.3 mg / kg, inclusive. The present disclosure further relates to compositions for use in such a method.

In one aspect, the invention provides compositions and methods for preventing, reducing, and / or treating a disease, disorder or condition associated with fibrin-induced activation of the complement system and the associated activation of the coagulation and / or contact systems comprising administering a therapeutic amount of a MASP-2 inhibitory antibody to a subject in need thereof. In some embodiments, the methods of the invention provide anticoagulation and / or antithrombosis and / or antithrombogenesis without affecting hemostasis. In one embodiment of this aspect of the invention, the compositions and methods are useful for treating a subject is suffering from, or at risk of developing, a disease, disorder or condition associated with complement-related inflammation, excessive coagulation or contact system activation initiated by fibrin or activated platelets.

The invention belongs to the technical field of biological medicines, and relates to a Rubicon permeable membrane peptide and application thereof. Specifically, the permeable membrane peptide fragment sequence is designed on the basis of an amino acid sequence of interaction of Rubi protein and Btk, and seven permeable membrane sections of arginine are connected to the tail end of the permeable membrane peptide fragment sequence through disulfide bonds. Immunofluorescence experiments prove that the peptide fragment can efficiently penetrate a platelet membrane to enter cells, and co-immunoprecipitation experiments prove that the peptide fragment has strong affinity with Btk. Platelet aggregation experiments show that the peptide fragment can significantly inhibit platelet activation under collagen stimulation. In an animal model, the peptide fragment is injected before instantaneous middle cerebral artery occlusion or reperfusion of a mouse, and ischemia-reperfusion injury can be effectively relieved. The invention provides a novel potential drug candidate for treating thrombotic diseases and ischemia-reperfusion injury.

The invention provides a pharmaceutical composition. The pharmaceutical composition is prepared from aspirin, atorvastatin, valsartan, hydrochlorothiazide, folic acid substances and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition provided by the invention has the advantages that the pharmaceutical composition provided by the invention has a multi-target synergistic prevention effect on vascular diseases, especially cerebral embolism, that is, the composition not only can reduce blood pressure, blood fat and blood homocysteine level, but also has an effect of preventing thrombosis, and reduces the risk of cerebral apoplexy. In addition, the form of the pharmaceutical composition is beneficial to improving the medication compliance of patients.

A series of sofalcone derivatives are provided.SOLUTION: A series of sofalcone derivatives provided by the present invention are, for example, compounds having a structure of formula (I), and have platelet aggregation inhibitory and antithrombotic effects. The sofalcone derivatives of the present invention are TxA2 receptor antagonists, have an inhibitory effect on platelet agglutination, and do not easily affect the hemostatic function. The present invention also provides a method for preparing the sofalcone derivative, and a method for using the sofalcone derivative for preventing or treating thrombotic diseases, or for inhibiting platelet aggregation.SELECTED DRAWING: None

The present invention discloses a trimer of Asn-Gly-Pro, namely [Asn-Gly-Pro]3, discloses its preparation method and its application in the treatment of venous thrombotic diseases. Experiments have proved that [Asn-Gly-Pro]3 of the present invention not only has a good anti-venous thrombosis effect, but also the anti-venous thrombosis effect is significantly stronger than that of Asn-Gly-Pro. Therefore, it is proposed that the present invention provides an effective technical means for anti-venous thrombosis.

This invention relates to the fields of molecular biology and biomedicine, disclosing plasma-active peptides with antithrombotic effects and their uses. The invention obtains various active peptides from plasma through screening and solid-phase synthesis, and confirms their biological activity through in vitro platelet aggregation experiments and in vivo arterial thrombosis model experiments. Results show that peptides 1957, 1960, and 1961 significantly inhibit collagen-induced platelet aggregation, exhibiting good antiplatelet activity; animal experiments show that peptides 1955, 1957, 1960, and 1961 significantly inhibit arterial thrombosis. These active peptides are derived from endogenous plasma components, belonging to natural antithrombotic substances, possessing good physiological compatibility and safety advantages, and reducing the risk of immunogenicity and adverse reactions. These peptides can exert antithrombotic effects without relying on traditional antiplatelet drugs, providing a new source of active molecules and treatment options for the prevention and treatment of thrombotic diseases.

The invention belongs to the technical field of medicines, and discloses application of pantethine in preparation of medicines for preventing and / or treating thrombotic diseases or medicines for inhibiting platelet activation or regulating vascular endothelial cell functions. In-vivo and in-vitro experiments prove that pantethine can remarkably relieve thrombus load in a mouse thrombus model, down-regulate expression of vWF (von Willebrand Factor), up-regulate expression of TFPI (Tissue Factor Path Inhibitor) and TH BD (Thromboregulatory Protein), and antagonize platelet adhesion, aggregation and activation induced by a platelet activator. The action mechanism is closely related to inhibition of reactive oxygen species (ROS) generation and NF-kappa B signal channel activation, and improvement of endothelial cell functions. It can be known from the invention that pantethine plays an antithrombotic role from multiple aspects, and is suitable for preparation of antithrombotic drugs for prevention or treatment. The invention provides a new drug choice for prevention and treatment of thrombotic diseases.

The application provides a highland thrombosis disease risk early warning system, comprising: a sensing acquisition module, which is used for acquiring patient characteristic data, the patient characteristic data including physical sign data and individual baseline data; an index analysis module, which is used for preprocessing the patient characteristic data and generating risk indexes; a risk assessment module, which is used for assessing a risk coefficient according to the risk indexes; and a risk early warning module, which is used for obtaining a risk degree corresponding to the risk coefficient according to a pre-constructed risk classification standard, and implementing corresponding risk early warning according to the risk degree. The application solves the problem in the prior art that a portable health monitoring device cannot accurately measure core hemodynamic parameters closely related to thrombosis, and also cannot accurately perform risk early warning on highland thrombosis diseases according to the acquired parameters.

The invention discloses a recombinant human serum albumin-arteplase nano-drug (rHSA-HSAbp-rt-PA) as well as a preparation method and an application of the recombinant human serum albumin-arteplase nano-drug (rHSA-HSAbp-rt-PA). The nano-drug comprises arteplase (rt-PA), human serum albumin adhesion peptide (HSAbp) and recombinant human serum albumin (rHSA), and the sequence of the human serum albumin adhesion peptide is VGPLGPHYYYCAADLWRL. According to the present invention, the recombinant human serum albumin-arteplase nano-drug is connected through the human serum albumin adhesion peptide, such that the chemical cross-linking step is avoided, the preparation method is simple, and the recombinant human serum albumin-arteplase nano-drug has the half-life period of as long as 29 min, has good treatment effect, and has wide application prospects in the treatment of thrombotic diseases.

The present invention relates to a fluorescent probe based on a lanthanide metal organic framework, a preparation method and an application, and belongs to the field of nanomaterial technology. The fluorescent probe provided by the present invention is obtained by covalently cross-linking a lanthanide metal organic framework with a neutrophil elastin binding peptide and a P-selectin binding peptide, and the surface of the lanthanide metal organic framework is modified with a tetracyclic antibiotic and arginine. The fluorescent probe prepared by the present invention specifically targets activated platelets and neutrophils, does not affect cell survival rate, does not cause hemolysis of red blood cells, and can be applied to the preparation of diagnostic products for thrombotic diseases. The use of a fluorescent probe loaded with urokinase achieves stable and efficient delivery of urokinase, inhibits platelet aggregation, slows down blood clot contraction, has a good thrombolytic effect, and has the potential to be used in the preparation of drugs for the treatment of thrombotic diseases. The materials required for the present invention are easy to obtain, the preparation method is simple, and a new method is provided for the diagnosis and treatment of thrombotic diseases.

The invention discloses an application of a TBOA analogue in preparation of a kit for testing platelet stress self-regulating force, and the platelet stress self-regulating force is reflected by the aggregation degree of platelets after being intervened by the TBOA analogue. The application focuses on a new mechanism of platelet activation, that is, when platelets are stimulated by activators such as thrombin, normal reactions of activation and aggregation are driven and maintained by adjusting uptake of glutamic acid by EAATs. Due to the clear action mechanism, the application can provide indexes and methods with higher specificity in diagnosis, treatment and prognosis evaluation of thrombotic diseases, and the pertinence is extremely high. According to the application, the influence of the TBOA analogue on the platelet aggregation degree is utilized to test the stress self-regulating force of the platelet, and new clinical application of the TBOA analogue is developed.

The application discloses a polypeptide FXIa inhibitor FXIapepin with high inhibition and high specificity. Since FXIa can be used as a low hemorrhage risk anti-thrombus treatment target, the polypeptide inhibitor can be used for preparing a drug for developing a low hemorrhage risk treatment or prevention of a thrombotic disease, and has a wide application prospect.

The invention provides an isoquinoline derivative with a novel structure, a pharmaceutically acceptable salt thereof, a preparation method of the isoquinoline derivative, a pharmaceutical composition containing the isoquinoline derivative and pharmaceutical application of the isoquinoline derivative, and belongs to the technical field of medicines. In-vitro experiments show that the isoquinoline derivative has significant inhibitory activity on arachidonic acid-induced platelet aggregation, and the antiplatelet activity of part of compounds is superior to that of aspirin. In a rat carotid artery thrombosis model induced by FeCl3, the isoquinoline derivative remarkably prolongs thrombosis time and reduces thrombus weight, and the in-vivo antithrombotic curative effect of the isoquinoline derivative is equivalent to that of aspirin and ticagrelor. A mouse tail bleeding model shows that the side effects of bleeding amount and bleeding time of the isoquinoline derivative are obviously lower than those of aspirin and ticagrelor. Therefore, the series of isoquinoline derivatives have the advantages of efficient antithrombotic effect and low bleeding risk, and have good application prospects in preparation of drugs for preventing and treating thrombotic diseases. In addition, the preparation method provided by the invention has the advantages of easily available raw materials, simple steps and strong operability, and the obtained target product has high quality and good efficiency.

The invention discloses an antithrombotic peptide Sibakazin of Simulium bannaense and application of the antithrombotic peptide Sibakazin, and belongs to the field of biomedicine. The anti-thrombus peptide Sibakazin is cyclic protein of three pairs of intramolecular disulfide bonds formed by the twenty-sixth cysteine and the fifty-first cysteine, the twenty-eighth cysteine and the forty-seventh cysteine, and the thirty-sixth cysteine and the seventy-first cysteine coded by a blood sucking insect Simulium bannaense anti-thrombus peptide gene. The amino acid sequence of the gene is shown as SEQ ID NO: 1. The antithrombotic peptide provided by the invention can inhibit platelet aggregation induced by ADP or collagen, and has a significant thrombus formation inhibition function in vivo; in addition, the antithrombotic peptide is obtained through prokaryotic expression, large-scale industrial production is easy, and the antithrombotic peptide can be applied to preparation of drugs for inhibiting platelet aggregation and treating thrombotic diseases.

The present invention relates to using c-Src SH3 RT-loop as a target for anti-thrombosis. Specifically, the present invention provides the use of a c-Src SH3 RT-loop antagonist for preparing a composition or preparation, and the composition or preparation is used for: (a) interfering with the interaction between integrin β3 and c-Src; (b) inhibiting platelet spreading on solid-phase fibrinogen; (c) inhibiting platelet aggregation and / or adhesion; and / or (d) preventing and / or treating thrombosis. The present invention discovers for the first time that a drug combination or preparation targeting the RT-loop region of the c-Src SH3 domain can effectively treat thrombotic diseases without increasing the risk of bleeding.

The application specifically discloses a kind of nanovaccine for thrombosis prevention and its preparation method and application, it is related to thrombotic disease, especially related to the nanovaccine for treating thrombotic disease.The nanovaccine provided by the application has good immunogenicity without macromolecular heterologous protein carrier such as KLH;The process simplicity and repeatability are improved by reducing complex chemical coupling and purification steps;The dependence on traditional high-stimulating immune adjuvant is reduced, and the biological safety is improved;The stability of antigen in gastrointestinal environment is significantly improved;Active targeting delivery of M cells and dendritic cells is realized;Dendritic cell maturation and antigen presentation are promoted, and mucosal immunity and systemic immunity level are improved;The advantages such as effectively inhibiting thrombosis are realized, and a new type of oral antithrombotic vaccine system with high compliance suitable for long-term thrombosis prevention is constructed.

The present invention discloses a recombinant human serum albumin-alteplase nanodrug (rHSA-HSAbp-rt-PA), its preparation method, and application. The nanodrug comprises alteplase (rt-PA), a human serum albumin adhesion peptide (HSAbp), and recombinant human serum albumin (rHSA), wherein the sequence of the HSA adhesion peptide is VGPLGPHYYYCAADLWRL. The rHSA-alteplase nanodrug is linked via the HSA adhesion peptide, avoiding the chemical cross-linking step and simplifying the preparation method. The rHSA-alteplase nanodrug has a half-life of up to 29 minutes, exhibits improved therapeutic efficacy, and has broad application prospects in treating thrombotic diseases.

Disclosed are aptamers, aptamer antidotes, and their use in the treatment of thrombosis and other thrombotic conditions.

The invention discloses an antithrombotic peptide Bannaensin of Simulium bannaense and application thereof, and belongs to the field of biomedicine. The anti-thrombus peptide Bannaensin is one of the twenty-second cysteine, the seventy-second cysteine, the thirty-first cysteine, the fifty-fifth cysteine, the forty-eighth cysteine and the sixty-eighth cysteine coded by a blood sucking insect Simulium bannaense anti-thrombus peptide gene, and the other is one of the twenty-second cysteine, the thirty-first cysteine, the fifty-fifth cysteine, the forty-eighth cysteine and the sixty-eighth cysteine coded by a blood sucking insect Simulium bannaense anti-thrombus peptide gene. The 110th cysteine and the 160th cysteine, the 119th cysteine and the 1343rd cysteine, and the 1336th cysteine and the 1366th cysteine form six pairs of cyclic proteins with intramolecular disulfide bonds, and the amino acid sequence of the cyclic proteins is shown as SEQ ID NO: 1. The antithrombotic peptide of the present invention can inhibit platelet aggregation induced by ADP or collagen, and shows significant antithrombotic activity in vivo; the antithrombotic peptide is obtained through prokaryotic expression, large-scale production can be achieved, and the antithrombotic peptide can be applied to preparation of drugs for inhibiting platelet aggregation and treating thrombotic diseases.

The present invention relates to a monoclonal antibody having an anticoagulant activity and the use thereof. The antibody or a fragment comprises a light chain variable region and a heavy chain variable region, wherein the light chain variable region of the antibody or fragment has an amino acid sequence as shown in SEQ ID NO: 1, and the heavy chain variable region has an amino acid sequence as shown in SEQ ID NO: 3. The monoclonal antibody of the present invention has the effect of inhibiting the activity of a common coagulation pathway in the coagulation cascade reaction, and can be used in the prevention and treatment of thrombotic diseases.

This disclosure relates to 5-amino-2,3-dihydro-1,4-phthalazinedione and its pharmaceutically acceptable salts for the prevention or treatment of thrombotic diseases. The invention particularly relates to the use of 5-amino-2,3-dihydro-1,4-phthalazinedione sodium salt for this purpose. Pharmaceutical compositions, advantageous formulation techniques, and therapeutic methods are disclosed.

The invention relates to the use of antibodies and antibody that target semaphorin 3A (Sema3A), and fragments thereof, and their use for treating thrombotic diseases of the retina comprising.

This invention provides a gene encoding a coral-derived anticoagulant polypeptide and its applications, belonging to the field of bioactive peptide technology. The invention provides an anticoagulant polypeptide GcKuz1, which includes the mature peptide segment shown in SEQ ID No. 1. The polypeptide GcKuz1 of this invention exerts antithrombotic and anticoagulant effects by binding to KLKB1 in the thrombin system. This polypeptide does not cause hemolysis or cytotoxicity, and has no bleeding risk, exhibiting good biocompatibility. The anticoagulant polypeptide of this invention has therapeutic effects on thrombotic diseases, such as arterial thrombotic diseases, venous thrombotic diseases, and capillary thrombotic diseases.

The invention relates to an application of a patent medicine Tenapanor approved by FDA in preparing a medicament for resisting platelet and arterial thrombosis. The medicament can be used for effectively inhibiting platelet activation and aggregation and arterial thrombosis block formation. The invention relates to an FDA approved patent medicine Tanipanol capable of effectively inhibiting platelet activation and aggregation induced by a natural agonist ADP and carotid artery and mesenteric artery thrombosis. Tanipamox is used as a novel candidate drug for resisting formation of platelets and arterial thrombosis blocks in fundamental research of thrombotic diseases, and has potential application value in prevention and treatment of arterial thrombosis related diseases.

The invention relates to the field of natural product chemistry, sugar chemistry and biological medicine, and particularly provides glycosaminoglycan and / or a series of derivatives thereof as well as a preparation method and application of the glycosaminoglycan and / or the series of derivatives thereof, the glycosaminoglycan is extracted from starfish glabrata, and the preparation method comprises the following steps: extracting by adopting a papain combined alkaline hydrolysis method; the invention discloses an ALHX-2M series derivative and application of the ALHX-2M series derivative in prevention or treatment of thrombotic diseases, and the ALHX-2M series derivative is obtained by performing separation and purification through ion exchange column chromatography and molecular exclusion column chromatography to obtain ALHX-2M, and further performing deacetylation, deamination and depolymerization treatment and gel column chromatography separation and purification on the ALHX-2M series derivative and the application of the ALHX-2M series derivative in prevention or treatment of thrombotic diseases. The glycosaminoglycan and the derivative thereof take an endogenous blood coagulation factor X enzyme complex (FXase) as an action target, the anticoagulation activity and the antithrombotic activity of the glycosaminoglycan and the derivative thereof are superior to those of low-molecular-weight heparin, the bleeding risk under the equivalent antithrombotic dosage is remarkably reduced, and the glycosaminoglycan and the derivative thereof can be used for medicines or functional foods for preventing and treating thrombotic cardiovascular and cerebrovascular diseases.

The invention provides syringic acid as well as preparation, a pharmaceutical composition and medical application thereof. The purity of the syringic acid is 95% or above, and the syringic acid can be extracted from motherwort. The syringic acid disclosed by the invention has a good dissolving effect on fibrin in thrombus formation, is relatively high in blood-brain barrier transmittance, has thrombus dissolving and antithrombotic effects, and can be used for preparing medicines for treating thrombotic diseases. The syringic acid can be processed into oral preparations such as tablets, capsules, granules, dripping pills and other common preparations or sustained release preparations, injection preparations such as injection freeze-dried powder injections, and external preparations such as ointments or emulsifiable paste according to a conventional production process of pharmaceutics, and is used for treating thrombotic diseases, especially cerebral thrombosis diseases.

The application discloses four kinds of tetra-cyclic compounds with selective adenosine diphosphate inhibition, which have the following formula structure, wherein the amino acids represented by AA are L-Ser residues, L-Glu residues, L-Lys residues and L-Tyr residues respectively, the application discloses a preparation method of the tetra-cyclic compounds and application of the tetra-cyclic compounds in treating arterial thrombosis diseases. Experiments prove that the adenosine diphosphate selective inhibitor has good anti-arterial thrombosis effect. Thus, the application provides an effective technical means for resisting arterial thrombosis.