31 results about "P2Y12" patented technology

A method is provided for measuring inhibition of platelet reactivity in an individual treated with a drug-eluting stent (DES). First, a blood sample is obtained from an individual treated with a DES and a P2Y12 antagonist. The blood sample is then mixed with particles comprising an attached GPIIb / IIIa receptor ligand, adenosine diphosphate (ADP) and prostaglandin E1 (PGE1). The mixture is incubated under conditions suitable for agglutinating particles, and platelet-mediated agglutination is assessed in the mixture. The absence or reduction of agglutination indicates that the individual treated with a DES has reduced platelet reactivity. Also provided is a kit for measuring inhibition of platelet aggregation by a P2Y12 receptor antagonist that includes a GPIIb / IIIa receptor ligand immobilized on a particle, adenosine diphosphate (ADP), prostaglandin E1 (PGE1), an anticoagulant, and a buffer to maintain the anticoagulated blood in a condition suitable for platelet aggregation.

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.

The present invention relates to certain novel pyridin compounds of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, and processes for their preparation, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

The invention relates to 2-phenyl-6-aminocarbonyl-pyrimidine 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 (I).

The present invention relates to certain novel pyridin compounds of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-thrombotic agents etc, and processes for their preparation, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

The present invention relates to certain new pyridin analogues of 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.

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.

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.

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.

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.

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.

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.

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.

The invention discloses a blood purification modified membrane and a preparation method thereof. The preparation method comprises the following steps: (1) preparation of citric acid-coupled chitosan; (2) preparation of CA‑CTS-loaded ticagrelor microspheres; and (3) preparation of a blood purification modified membrane. The invention utilizes the hydrophilicity and anticoagulant properties of citric acid to prepare a blood purification modified membrane by putting ticagrelor into the microsphere particles, so that the modified membrane can directly act on the P2Y12 receptor, thereby directly inhibiting Platelet activity, in order to achieve the effect of slow-release anti-inflammatory and anti-thrombotic, and the release is stable. The blood purification modified membrane of the present application has low cost, good anti-inflammatory and antithrombotic properties, can release ticagrelor into the blood stably and slowly, and has good blood compatibility.

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.