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31 results about "P2Y12" patented technology

P2Y₁₂ is a chemoreceptor for adenosine diphosphate (ADP) that belongs to the Gᵢ class of a group of G protein-coupled (GPCR) purinergic receptors. This P2Y receptor family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. The P2Y12 receptor is involved in platelet aggregation and is thus a biological target for the treatment of thromboembolisms and other clotting disorders. Two transcript variants encoding the same isoform have been identified for this gene.

Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor

InactiveUS20090048216A1Inhibits thrombosis formationInhibits propagationBiocideSalicyclic acid active ingredientsAspirinOral medication
The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula:alone or in combination with a second agent which can be aspirin or a thrombolytic agent.
Owner:ALEXION PHARMA INC

Bicyclic heterocyclic compound

InactiveUS20100113391A1Excellent P2Y1 inhibitory actionBiocideAntipyreticQuinoloneQuinazoline
[Problem]Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor.[Means for Solution]The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.
Owner:ASTELLAS PHARMA INC

2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as p2y12 receptor

The invention relates to 2-phenyl-6-aminbcarbonyl-pyrimidinc derivatives and their use as P2Y12 receptor antagonists in the treatment and / or prevention and / or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formula (1).
Owner:IDORSIA PHARM LTD

Biomarker for predicting II-type diabetic vascular complication risk and application thereof

The invention belongs to the technical field of biology and diagnosis, and relates to a receptor of a definite, effective and visualized platelet reactivity biomarker P2Y12 and an application thereof for diagnosing and predicting the II-type diabetic vascular complication risk. The platelet activation biomarker P2Y12 can detect expression levels of platelet through fluorescent quantitative polymerase chain reaction (PCR), Western blot, enzyme linked immunosorbent assay (ELISA), flow cytometry, UV spectrophotometry-near infrared spectrometry, high performance liquid chromatography, colorimetry, a mass spectrum identification method and the like and detect content of P2Y12 in whole blood. The invention also provides a method of biomarker P2Y12 for diagnosing and predicting vascular complication of subjects as well as a medicine for treating II-type diabetic vascular complication and a screening method of the medicine. The invention further provides an intervene plane for individualizing P2Y12 inverse agonist and accurately treating the vascular complication of II-type diabetic patients.
Owner:FUDAN UNIV

New pyridine analogues

The present invention relates to certain new pyridin analogues of Formula (I) Chemical formula should be inserted here. Please see paper copy Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
Owner:ASTRAZENECA AB

Method For Treatment Of Macular Degeneration By Modulating P2Y12 or P2X7 Receptors

Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and / or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and / or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
Owner:MITCHELL CLAIRE +1

Reagent card for detecting therapeutic effect of thienopyridine antiplatelet drugs and application method and application of reagent card

The invention provides a reagent card for detecting the therapeutic effect of thienopyridine antiplatelet drugs and an application method and application of the reagent card. The reagent card comprises four detection channels which are sequentially arranged in parallel and are independent of one another, the detection channel I contains channel I detection reagent, and the channel I detection reagent contains a lyophilized agent, wherein the lyophilized agent is obtained by firmly bonding activated dye microspheres with receptor ligand of blood platelets GpIIb / IIIa through amido bonds, then adding blood coagulation factors, and conducting freeze-drying; the detection channel II contains channel II detection reagent, and the channel II detection reagent contains a lyophilized agent serving as a blood platelet maximum activating agent; the detection channel III contains no detection reagent, the detection channel IV contains channel IV detection reagent, and the channel IV detection reagent contains a lyophilized agent serving as a blood platelet P2Y12 receptor activating agent and P2Y1 receptor antagonist. By means of the reagent card, the therapeutic effect of thienopyridine antiplatelet drugs can be detected easily, fast, conveniently and accurately.
Owner:北京乐普诊断科技股份有限公司

Computer drug design method using P2Y12 as target and application thereof

InactiveCN106407737AInhibition of P2Y12 activitySpecial data processing applicationsProtein targetStructure function
The invention relates to a computer drug design method using a P2Y12 as a target and application thereof, and belongs to the technical fields of target computer-aided drug design, small molecule drug virtual screening, molecular docking and full atom molecular dynamics. The computer drug design method is a drug virtual screening design method including using the P2Y12 as the target and using a Chembridge small molecule database as a search database. The invention includes target protein spatial structure analysis, a binding pocket definition method and a structure-function relationship analysis method. The computer drug design method has been verified for many times in a drug design method of associated protein targets, and is high in success rate. The computer drug design method has been used for virtual screening of inhibitors of GPCRs.
Owner:张崇骞

Application of CFTR gene to preparation of thrombotic disease early warning or diagnosing medicine

The invention discloses application of a CFTR gene to preparation of thrombotic disease early warning or diagnosing medicine. The CFTR gene codes a chloride ion channel with cAMP dependency, and it isfound that the expression of the CFTR gene on the peripheral blood platelets and mononuclear cells of a patient with a coronary heart disease is reduced remarkably; statistics difference is shown among patient groups with stable angina pectoris and acute coronary syndromes. On an animal cell model, the specificity restraining CFTR gene is found to remarkably promote thrombosis, and has the effects of promoting platelet aggregation and up regulating a P2Y12 receptor-mediated platelet aggregation signal channel. The new medical application of the CFTR gene to thrombotic disease early warning and diagnosing is mined, the new application field of gene treatment is expanded, and the new clinical diagnosis marker is provided for early warning and diagnosing of a critical thrombotic disease.
Owner:SUN YAT SEN UNIV

Application of P2Y12 receptor and antagonist thereof in diagnosis and treatment of acute pancreatitis

The invention discloses an application of a P2Y12 receptor and an antagonist thereof in diagnosis and treatment of acute pancreatitis, and discloses an application of the P2Y12 receptor as a target in screening of a diagnostic reagent for acute pancreatitis and an application of the P2Y12 receptor as a biomarker in screening of the diagnostic reagent for acute pancreatitis, provides a new target spot and a biomarker screened by a diagnostic reagent for the diagnosis of acute pancreatitis; meanwhile, the invention discloses application of the P2Y12 antagonist in preparation of drugs for treating acute pancreatitis, and provides a new treatment basis and a drug screening basis for treatment of acute pancreatitis. Therefore, the P2Y12 receptor and the antagonist thereof have a good application prospect and an important research value.
Owner:THE FIRST AFFILIATED HOSPITAL OF SOOCHOW UNIV

P2Y12 receptor platelet aggregation detection reagent card and production method thereof

The invention provides a P2Y12 receptor platelet aggregation detection reagent card and a production method thereof. The P2Y12 receptor platelet aggregation detection reagent card comprises four detection channels, the first channel contains a lyophilized reagent coated with BSA and fibrinogen and contains no activators, the second channel contains a lyophilized reagent coated with the BSA and fibrinogen and also contains a platelet maximum activator iso-TRAP (thrombin receptor activating peptide), the third channel contains no lyophilized reagents, and the fourth channel contains the lyophilized reagent coated with the BSA and fibrinogen, and also contains a platelet P2Y12 receptor activator ADP (adenosine diphosphate) and a P2Y1 receptor antagonist PGE1 (prostaglandin E1). The patient'sP2Y12 receptor pathway-correlated platelet aggregation function is rapidly and effectively detected through optical nephelometry by using the detection reagent card. The card has the advantages of high sensitivity, strong specificity, easiness in operation, and suitableness for bedside fast detection, and can well predict the future thrombus or bleeding risk in patients treated with the P2Y12 receptor antagonists.
Owner:北京乐普诊断科技股份有限公司

Modified membrane for blood purification and preparation method thereof

ActiveCN113368700ALow costGood anti-inflammatory and anti-thrombotic propertiesSemi-permeable membranesHaemofiltrationTicagrelorReceptor
The invention discloses a modified membrane for blood purification and a preparation method thereof. The preparation method comprises the following steps: (1) preparing citric acid-coupled chitosan; (2) preparing CA-CTS loaded ticagrelor microspheres; and (3) preparing the modified membrane for blood purification. The modified membrane for blood purification is prepared by putting ticagrelor into microsphere particles in virtue of the hydrophilicity and anticoagulation performance of citric acid, and the modified membrane can directly act on a P2Y12 receptor, so the activity of platelets can be directly inhibited, slow-release anti-inflammatory and antithrombotic effects are achieved, and release is stable. The modified membrane for blood purification is low in cost and good in anti-inflammatory and anti-thrombotic performance, ticagrelor can be stably and slowly released into blood, and good blood compatibility is achieved.
Owner:XIANGYA HOSPITAL CENT SOUTH UNIV +1

Treatment effect of 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi

The invention provides a treatment effect of a 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi. The 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative has the following generalformula structure: (with reference to the specification), wherein R<1> represents C1-C6 alkyl acyloxy; R<2> and R<3> can be the same or different, and are respectively independently selected from C1-C6 alkyl, C1-C6 alkoxy, a halo substituent of C1-C6 alkyl, C1-C6 naphthenic base, C1-C6 alkyl sulphanyl, aryl, a substituent group of aryl, heteroaryl, a substituent group of heteroaryl or heterocyclic alkyl. According to the invention, the new 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative is synthesized, which is a blood platelet adenosine diphosphate receptor inhibitor and is used fortreating thrombi; active molecules are formed in a body and are combined with a blood platelet P2Y12 receptor to exert effects; the 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative has an excellent anticoagulant effect and meanwhile, has excellent bioavailability.
Owner:RIZHAO PUDA PHARMA TECH CO LTD

SNP detection kit for determining gene related to drug use curative effect of clopidogrel

The invention discloses an SNP detection kit for determining a gene related to the drug use curative effect of clopidogrel. The detection kit comprises an MassARRAY chip and three primers, namely theforward primer, the reverse primer and the extension primer, at three SNP sites, namely rs16863356, rs7634096 and rs12497330, of a detection gene P2Y12, the sequences of the primers are sequentially shown as SEQ ID No.1-9, and the primers are used for identifying the polymorphic sites of the gene related to the drug effect and the adverse reaction of the clopidogrel. The kit can conduct high-fluxdetection on the three sites and has the advantages of high sensitivity, high specificity, stable detection result, high reliability and the like; and meanwhile the kit is suitable for the gene analysis fields of clinical disease mutation detection, pharmacogenomics analysis, medicolegal expertise and the like.
Owner:SHANGHAI JIAO TONG UNIV

Gene SNP detection kit for determining the therapeutic effect of clopidogrel

The invention discloses an SNP detection kit for determining a gene related to the drug use curative effect of clopidogrel. The detection kit comprises an MassARRAY chip and three primers, namely theforward primer, the reverse primer and the extension primer, at three SNP sites, namely rs16863356, rs7634096 and rs12497330, of a detection gene P2Y12, the sequences of the primers are sequentially shown as SEQ ID No.1-9, and the primers are used for identifying the polymorphic sites of the gene related to the drug effect and the adverse reaction of the clopidogrel. The kit can conduct high-fluxdetection on the three sites and has the advantages of high sensitivity, high specificity, stable detection result, high reliability and the like; and meanwhile the kit is suitable for the gene analysis fields of clinical disease mutation detection, pharmacogenomics analysis, medicolegal expertise and the like.
Owner:SHANGHAI JIAO TONG UNIV

Antiplatelet activity of the acanthus mollis seeds' total extract and its constituents

Acanthus mollis seeds' methanol extract exhibits an advantageous antiplatelet activity towards AA- and TRAP-6-induced platelet aggregation, i.e., inhibits two important pathways leading to platelet aggregation (pathway mediated by TxA2 formed from AA by the action of COX-1 as well as thrombin receptor PAR-1-mediated platelet aggregation, respectively). The antiplatelet activity towards AA is due to the DIBOA-Glc content. The DIBOA-Glc activity is enhanced in the presence of Verbascoside and / or Isoverbascoside. The antiplatelet activity towards TRAP-6 is exclusively attributed to Isoverbascoside. The constituents of Acanthus mollis seeds is a new therapeutic agent for CVD patients which can replace aspirin in aspirin resistant patients (DIBOA-Glc alone or in combination with Verbascoside or / and Isoverbascoside) and also may be used as a specific antagonist of the platelet thrombin receptor PAR-1 (Isoverbascoside). Moreover, the total extract may be used as a supplement with aspirin and a P2Y12 antagonist in some patients.
Owner:TSELEPIS ALEXANDROS +2

Model for predicting anti-platelet curative effect of clopidogrel and application thereof

PendingCN113593718AImprove consistencyPrediction results are accurate and reliableChemical property predictionDrug referencesPlateletGenotype
The invention relates to a model for predicting an anti-platelet curative effect of clopidogrel and application thereof. The model comprises a data input unit, an assignment unit, a curative effect prediction unit and a report output unit, wherein the data input module is used for acquiring and inputting three independent risk factor data of CYP2C19 genotype, age and fibrinogen of a detected object and storing the data; the assignment module comprises a CYP2C19 genotype subunit, an age subunit and a fibrinogen subunit which are arranged in parallel, and the curative effect prediction unit receives assignment of the assignment module and performs clopidogrel anti-platelet curative effect prediction according to the total score of the assignment; and the report output unit outputs the prediction information of the curative effect prediction unit. Compared with the prior art, the model disclosed by the invention can be used for guiding accurate selection of a platelet P2Y12 receptor inhibitor, the predicted clopidogrel curative effect result is accurate and reliable, and balance can be achieved between antithrombotic benefit and bleeding risk.
Owner:ZHONGSHAN HOSPITAL FUDAN UNIV

Application of GFA (Guanfu base A) in preparation of drug for neuropathic pain

ActiveCN109091479APain-Reducing BehaviorPain behavior reductionOrganic active ingredientsNervous disorderInflammatory factorsDisease
The invention provides an application of GFA (Guanfu base A) in preparation of a drug for neuropathic pain. Experiments prove that GFA can reduce expression of a P2Y12 receptor of DRG (dorsal root ganglion) SGCs (satellite glial cells), inhibit transmission of nociceptive information mediated by a P2Y12 receptor and inflammatory factors in DRG and reduce pain behavior of rats suffering from neuropathic pain, and can be applied to preparation of the drug for neuropathic pain and diseases related to nerve injury.
Owner:NANCHANG UNIV

A reagent card for detecting the curative effect of thienopyridine antiplatelet drugs and its use method and application

The invention provides a reagent card for detecting the therapeutic effect of thienopyridine antiplatelet drugs and an application method and application of the reagent card. The reagent card comprises four detection channels which are sequentially arranged in parallel and are independent of one another, the detection channel I contains channel I detection reagent, and the channel I detection reagent contains a lyophilized agent, wherein the lyophilized agent is obtained by firmly bonding activated dye microspheres with receptor ligand of blood platelets GpIIb / IIIa through amido bonds, then adding blood coagulation factors, and conducting freeze-drying; the detection channel II contains channel II detection reagent, and the channel II detection reagent contains a lyophilized agent serving as a blood platelet maximum activating agent; the detection channel III contains no detection reagent, the detection channel IV contains channel IV detection reagent, and the channel IV detection reagent contains a lyophilized agent serving as a blood platelet P2Y12 receptor activating agent and P2Y1 receptor antagonist. By means of the reagent card, the therapeutic effect of thienopyridine antiplatelet drugs can be detected easily, fast, conveniently and accurately.
Owner:北京乐普诊断科技股份有限公司

Application of receptor p2y12 of ADP (adenosine diphosphate) in angiogenesis

ActiveCN103816541AStrong interspecies conservationPeptide/protein ingredientsGenetic material ingredientsP2Y12Disease
The invention relates to an application of a receptor p2y12 of ADP (adenosine diphosphate) in angiogenesis. Concretely, the receptor p2y12 of ADP is specifically expressed in vascular endothelial cells, and a specific inhibitor of p2y12 is used for inhibiting p2y12 expression and preventing blood vessels among somites from generating growth defects; the ligand ADP of p2y12 is also involved in angiogenesis, and a high-selectivity antagonist is utilized to block ADP to activate p2y12 to have an exception which is the same as the above exception; an ADP-p2y12 signal is involved in the angiogenesis process in modes of migrating and proliferating tip cells, namely regulating tip cell behaviors; otherwise, p2y12 overexpression can promote the obtaining of tip cell, namely the number of endothelial cells with excessive migration and endothelial cells involved in angiogenesis among somites is obviously increased; in addition, the ADP-p2y12 signal inhibits a notch pathway so as to regulate angiogenesis in vivo. The application of the receptor p2y12 of ADPin angiogenesis provides a new target for related diseases of intervention in angiogenesis.
Owner:SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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