18 results about "Induced platelet aggregation" patented technology

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.

Disclosed in the present invention are a crystalline form B of a tetrahydrothienopyridine compound having a structure as represented by Compound I, a preparation method, a composition and an application thereof, for use in solving the problems in the prior art of lots of impurities, low content, bad crystalline form stability, and inability to form a drug. The crystalline form B uses Cu-Kα radiation, and X-ray powder diffraction expressed at a 2θ angle has characteristic peaks at 11.21±0.2°, 12.61±0.2°, 14.69±0.2°, 16.14±0.2°, 17.81±0.2°, 20.22±0.2°, and 22.10±0.2°. The crystalline form B of the present invention has few of impurities, good stability, good crystallinity, and reproducibility, and is suitable for industrial production. Moreover, the crystalline form B has an unexpectedly stronger anti-ADP-induced platelet aggregation effect and better fluidity.

Pharmaceutical compositions comprising anti-CEACAM1mAb and their use in the inhibition of NET-mediated activity and in the prevention and treatment of pathologies associated with these activities are provided, and are exemplified by mAb CM24 that also exhibit effective inhibition of cancer cell migration and NET-induced platelet aggregation. Prognostic methods based on NET-biomarkers for use in patient selection and monitoring of therapeutic efficacy are also presented.

The invention discloses a 5 / 8 / 5 chitosan clostridium diterpenoid compound, a biosynthetic gene cluster and application of the biosynthetic gene cluster, and relates to the technical field of biological medicines. A 5 / 8 / 5 chitin type diterpenoid biosynthetic gene cluster Thm in trichoderma harzianum is identified through a genome mining system, chitin diterpenoid compounds with diversified structures are obtained by means of heterologous expression, the obtained compounds are subjected to anti-thrombotic activity comprehensive evaluation, and the result shows that the compounds 6 and 31 can obviously inhibit vascular thrombosis, the compound 6 has a remarkable inhibition effect on collagen-induced platelet aggregation, and the compound 31 has a better inhibition capability on thrombin-induced platelet activation. The compounds 6 and 31 show powerful antithrombotic effects in artery, vein and pulmonary artery thrombosis models, so that powerful technical support is provided for development of antithrombotic drugs.

The present application relates to a new use of Veronica longifolia quinone A, and in particular to the use of Veronica longifolia quinone A in the preparation of a drug for preventing or treating thromboembolic diseases. The present application finds that Veronica longifolia quinone A can significantly inhibit the platelet aggregation activity induced by different inducers in vitro: in the thrombus model experiment in vivo, the Veronica longifolia quinone A of the present application can well inhibit the FeCl3-induced carotid artery thrombosis in mice. At the same time, it is found that the Veronica longifolia quinone A of the present application does not have obvious bleeding tendency. It is shown that Veronica longifolia quinone A is expected to play a certain positive role in the prevention or treatment of thromboembolic diseases.

The present invention belongs to the technical field of medical uses of small molecule compounds, and relates to diphenylpyrazine compounds and compositions thereof, applications and preparation methods. It mainly relates to the use of diphenylpyrazine compounds and compositions thereof in the preparation of drugs for inhibiting platelet aggregation, and specifically relates to the use of diphenylpyrazine compounds and compositions thereof in the preparation of drugs for treating cardiovascular and cerebrovascular diseases and other vascular thrombosis and embolic diseases related to platelet aggregation. The present invention confirms through in vitro platelet aggregation experiments that the diphenylpyrazine compounds exhibit extremely strong inhibitory effects on both AA-induced platelet aggregation and ADP-induced platelet aggregation, have lower toxicity, and have outstanding clinical advantages.

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 application discloses a cinnoline PAR4 antagonist and medical application thereof. The application relates to a compound of formula (I), stereoisomers, tautomers, pharmaceutically acceptable salts, esters, solvates or prodrugs thereof. The compound of the application can inhibit and prevent platelet aggregation induced by PAR4, can be used for treating and preventing thromboembolic diseases, and thus can be used as an anti-platelet drug.

Pharmaceutical compositions containing anti-CEACAM 1 mAbs and their use in inhibiting NET-mediated activities and in the prevention and treatment of conditions associated with these activities are provided, exemplified by mAb CM24, which has also been shown to effectively inhibit cancer cell migration and NET-induced platelet aggregation. Additionally, prognostic methods based on NET biomarkers for use in patient selection and monitoring treatment efficacy are presented.

The invention discloses an anticoagulant active site of massa medicata fermentata fujianensis as well as a preparation method and application thereof, and belongs to the field of biological medicines. The massa medicata fermentata fujianensis is used for preparing anticoagulant drugs for the first time. The method comprises the following steps: soaking a fermented mass raw material with methanol, performing reflux extraction, and recovering a solvent under reduced pressure to obtain a total extract; and separating the total extract by adopting macroporous adsorption resin column chromatography to obtain a water part, a 30% methanol part, a 50% methanol part and a pure methanol part. Platelet aggregation detection results show that all the parts can inhibit ADP-induced platelet aggregation, and the anticoagulant effect of the 30% methanol part is most prominent and is similar to that of a positive drug. According to the preparation method of the anticoagulant active part of the massa medicata fermentata fujianensis, the anticoagulant active part in the massa medicata fermentata fujianensis can be effectively separated and enriched, and the obtained anticoagulant active part can be applied to preparation of anticoagulant drugs and has good industrial application prospects and clinical value.

The invention discloses a lophatherum gracile extract in preparation of a medicine for treating and preventing thrombosis and application of the lophatherum gracile extract in preparation of the medicine for treating and preventing thrombosis, and the medicine comprises the lophatherum gracile extract. The common lophatherum herb extract can inhibit platelet agonist-induced platelet blood clot formation so as to prevent and treat thrombosis, and can inhibit a platelet agonist-induced platelet aggregation function so as to prevent and treat thrombosis. A platelet activation function induced by a platelet agonist can be inhibited so as to prevent and treat thrombosis, and platelet microtubule morphological change induced by the platelet agonist can be inhibited so as to prevent and treat thrombosis; the invention proves that the lophatherum gracile extract has the effects of inhibiting platelet aggregation, activation, particle release and microtubule morphological change for the first time, has small toxic and side effects, provides a new research and development direction for clinical treatment of thrombotic diseases, and shows that the lophatherum gracile extract can be used as a new type of health care product medicine for preventing thrombotic diseases.

This invention relates to an IRAK4 degrading agent and its uses. This degrading agent can be used to treat or prevent diseases such as cancer, neurodegenerative diseases, viral diseases, autoimmune diseases, inflammatory diseases, hereditary diseases, hormone-related diseases, metabolic diseases, organ transplant-related diseases, immunodeficiency diseases, destructive bone diseases, proliferative diseases, infectious diseases, cell death-related conditions, thrombin-induced platelet aggregation, liver diseases, pathological immune conditions involving T cell activation, cardiovascular diseases, or CNS diseases.

The application discloses a tetrazole derivative, which has a structure shown in a general formula I. The application also discloses a composition containing the tetrazole derivative and application of the tetrazole derivative in preparation of a drug for preventing and resisting stroke. The inventors of the application have confirmed through multiple experiments that the compound has obvious inhibiting effect on ADP-induced platelet aggregation activity, outstanding damage protection effect on OGD / R fetal rat primary cortical neuron cells and neuron-like cells induced and differentiated from neuroblastoma cells (N2A), good anti-stroke efficacy on an animal model of focal cerebral ischemia constructed by a line plug method for temporarily blocking a middle cerebral artery and good rat oral pharmacokinetic properties. Therefore, the compound can be applied to a drug for treating and preventing stroke as a neuroprotective agent.

Preparation method of the C-type protein of Protobothrops mucrosquamatus venom and its application as a diagnostic reagent. A novel target protein Protocetin is isolated and purified from domestic Protobothrops mucrosquamatus venom through three-step chromatography, which has the function of inducing platelet aggregation. Based on the fact that Protocetin can activate platelets through GPIb by acting on vWF, leading to platelet aggregation, it can be used to detect the function of vWF and the aggregation function of platelets, and thus can be used clinically to detect hemophilia and platelet-related diseases associated with abnormal structure and function of GPIb.

The present application belongs to the technical field of medical uses of small-molecular compounds, and relates to a diphenylpyrazine compound, a composition thereof, the uses thereof, and a preparation method therefor. The present application mainly relates to the use of the diphenylpyrazine compound and the composition thereof in preparing drugs for inhibiting platelet aggregation, and further particularly relates to the use of the diphenylpyrazine compound and the composition thereof in preparing drugs for treating platelet aggregation related cardiovascular and cerebrovascular diseases and other vascular thrombotic and embolic diseases. By means of an in-vitro human platelet aggregation experiment, the present application proves that the diphenylpyrazine compound exhibits an extremely strong inhibition effect on both AA-induced platelet aggregation and ADP-induced platelet aggregation and also has lower toxicity and outstanding clinical advantages.

The invention relates to an IRAK4 degradation agent and application thereof. The degrading agent can be used for treating or preventing cancer, neurodegenerative diseases, viral diseases, autoimmune diseases, inflammatory diseases, hereditary diseases, hormone-related diseases, metabolic diseases, diseases related to organ transplantation, immunodeficiency diseases, destructive bone diseases, proliferative diseases, infectious diseases, conditions related to cell death, and the like. Thrombin-induced platelet aggregation, liver diseases, pathological immune conditions involving T cell activation, cardiovascular diseases or CNS diseases, etc.

The application discloses a kind of dihydroindole aromatic acid ether derivatives and preparation method and purposes thereof.The application specifically discloses a kind of dihydroindole aromatic acid ether derivatives shown in formula (I), or its tautomer, cis-trans isomer, isotopically labeled compound and pharmaceutically acceptable salt thereof.The derivatives show anti-platelet aggregation activity in AA and ADP induced platelet aggregation experiment.The compound of the application can be used for preventing and / or treating ischemic stroke, alzheimer's disease, vascular dementia and / or Parkinson's disease and the like diseases.

The invention provides RGD (arginine-glycine-aspartic acid) modified hydrogel and application thereof, relates to the technical field of biological materials, and has the technical key points that the RGD modified hydrogel is provided and is characterized in that the RGD modified hydrogel is prepared from a PEGDA (polyethylene glycol diacrylate) prepolymer, Irgacure 2959 and acryloylated RGD peptide. The application illustrates that aPL induces platelet aggregation, thrombosis and inflammatory response by activating alphaIIb beta3 integrin, and further damages the function of the trophoblast. The RGD functionalized hydrogel based on PEG and the alphaIIb beta3 antibody can significantly inhibit platelet aggregation (decreasing amplitude to 83%), delay fibrin clot formation (OD405 is reduced by 67%), and reduce release of inflammatory factors such as IL-6 / TNF-alpha (decreasing amplitude to 70-80%). More importantly, the intervention measures can protect the migration ability of the trophoblast, which is a key process of placenta vascular remodeling. The integrin targeting biological material strategy provides a new way for preventing and treating APS-related pregnancy complications through local antithrombotic and anti-inflammatory dual effects.