664 results about "Platelet inhibition" patented technology

The invention discloses a micro plasminogen mutant with a function of inhibiting platelet aggregation, which has an amino acid sequence of KLYDYCKGDWPCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN. A preparation method of the micro plasminogen mutant comprises the following steps of: replacing a D-V-P-Q sequence at 7 to 10 positions of a micro plasminogen sequence with a K-G-D-W-P sequence; forming a convex Loop structure on the replaced sequence; and placing a K-G-D sequence at the top end of the Loop structure. Meanwhile, the invention provides application of the micro plasminogen mutant to preparation of a medicament for preventing and treating thrombotic diseases and ophthalmic diseases.

This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:

The present invention concerns methods and reagents useful in modulating platelet-derived endothelial cell growth factor (ECGF1) and / or platelet-derived endothelial cell growth factor receptor (e.g., ECGF1r) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against ECGF1 and / or ECGF1r gene expression and / or activity. The small nucleic acid molecules are useful in the diagnosis and treatment of cancer, proliferative diseases, macular degeneration, diabetic retinopathy, and any other disease or condition that responds to modulation of ECGF1 and / or ECGF1r expression or activity.

A complex is provided for the treatment of neurogenic conditions having the formula: where R1 is M is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium (II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium (II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium (II):transporter ligand.

The present invention provides novel compounds of dinucleotide polyphosphates and the method of preventing or treating diseases or conditions associated with platelet aggregation. The method comprises administering systemically to a patient a pharmaceutical comprising a purinergic P2τ receptor antagonist, in an amount effective to elevate its extracellular concentration to bind to P2τ receptors and inhibit P2τ receptor-mediated platelet aggregation. Methods of systemic administration include injection by intravenous, intramuscular, intrasternal and intravitreal routes, infusion, transdermal administration, oral administration, rectal administration and intra-operative instillation.

A hemostasis analyzer, such as the Thrombelastograph® (TEG®) hemostasis analyzer is utilized to measure continuously in real time, the hemostasis process from the initial fibrin formation, through platelet-fibrin interaction and lysis to generate blood hemostasis parameters. The measured blood hemostasis parameters permit evaluation of platelet inhibition therapy.

A polymeric composition that generates nitric oxide and a process for rendering the surface of a substrate nonthrombogenic by applying a coating of the polymeric composition to the substrate are disclosed. The composition comprises: (1) a crosslinked chemical combination of (i) a polymer having amino group-containing side chains along a backbone forming the polymer, and (ii) a crosslinking agent containing functional groups capable of reacting with the amino groups; and (2) a plurality of nitric oxide generating functional groups associated with the crosslinked chemical combination. Once exposed to a physiological environment, the coating generates nitric oxide thereby inhibiting platelet aggregation. In one embodiment, the nitric oxide generating functional groups are provided by a nitrated compound (e.g., nitrocellulose) imbedded in the polymeric composition. In another embodiment, the nitric oxide generating functional groups comprise N2O2− groups covalently bonded to amino groups on the polymer.

The tubiflorous desert cistanche preparation containing phenethyl alcohol glycoside contains echinacoside in 10-70 wt% and acteoside in 1-40 wt%. The preparation of the present invention may be applied as active component for preparing medicine treating and preventing senile dementia and for preparing medicine inhibiting platelet aggregation.

This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae III, IIIa, and IIIb, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae IIIa and IIIb, which are potent and have a good oral bioavailability.

The present invention is directed to an antibody or derivative thereof of human origin for inhibiting platelet aggregation, characterized in that it is effective by substantially exclusive binding to the activated state of platelet integrin receptor GPIIb / IIIa.

The invention relates to a Rosmarinus officinalis extract, its preparing process and use, wherein the active constituents of the extract include carnosic acid 15-40%, carnosol 5-12% and ursolic acid 14-35%. The preparing process comprises drying the Rosmarinus officinalisl medicinal material in shade, cutting into chunks, charging solvent for extracting, cooling down the merged filtrate and filtrating, decolorizing with activated charcoal, drying and disintegrating. The extract can be used for preparing medicament for treating ischemic cardiovascular and cerebrovascular diseases.

The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and / or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and / or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and / or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

A method for treating acute coronary syndromes (i.e., unstable angina or non-Q-wave MI) or transient ischemic attacks in a human or animal patient by placing a heat exchange apparatus in the patient's vasculature and using that heat exchange apparatus to cool the patient to a temperature (e.g. 30-36° C.) at which platelet inhibition (i.e., inhibition of platelet activation and / or aggregation and / or adhesion) occurs. Anti-shivering drugs or anesthesia may be administered to patients whose body temperature is cooled below that patient's shivering threshold (typically approximately 35.5 C). If it is determined that platelet inhibition is no longer desirable, such as when the patient is about to undergo a surgical or interventional procedure wherein bleeding could be problematic, the hypothermia-induced platelet inhibition may be rapidly reversed by using the intravascular heat exchange apparatus to re-warm the patient's body to normothermia or near normothermia.

This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation, preferably in a reversible manner. The compounds useful for this invention include compounds of general Formulae I and III-XII, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and III-XII.

The body of a herbaceous plant, Cistanche tubulosa (Schenk.) Wight, is used to make a medicinal preparation containing phenylethanoid glycosides and comprising 10–70% of echinacoside by weight of the preparation and 1–40% of acteoside by weight of the preparation. The medicinal preparation is used as an active ingredient of medicinal composition for use in prevention of senile dementia, and inhibition of aggregation of blood platelets.

The invention relates to a Chinese medicinal pill preparation for treating coronary disease which is prepared from 30 kinds of Chinese herbs including astragalus root, prepared rhizome of rehmannia, Chinese angelica root, root of red rooted saliva, Ligusticum wallichii, Loranthus mulberry mistletoe, pericarpium trichosanthis, corydalis tuber, root of herbaceous peony, grassleaved sweetflag rhizome, spatholobus stem, grassleaved sweetflag rhizome, black sesame seeds, dodder seed, white atractylodes rhizome, curcuma aromatica, prepared fleece flower root, epimeddium, spine date seed, schisandra fruit, donkey-hide gelatin, ganoderma lucidum, poria cocos, burred tuber, zedoary, ophiopogon root, oyster shell, pilose asiabell root, sandalwood and licorice root through steps of disintegrating, charging bee honey and modulating.

The invention relates to tetrahydrothieno-[2,3-c]pyridine deuterated derivatives and a preparation method and medicament applications thereof, belonging to the field of medicinal chemistry. The derivatives contain salt of a compound in the formula I, and enantiomer and racemate of the compound in the formula I. The in-vitro whole-blood hydrolysis experiment results show that the stability of the compound in the formula I on esterase is good, and the hydrolysis rate of methyl carboxylate is obviously slower than that of non-deuterated methyl ester. The compound in the formula I can be effectively converted into pharmacological active metabolite in a human body to achieve the effect of inhibiting the platelet aggregation, and the concentration of the active metabolite is obviously higher than that of a non-deuterated compound of clopidogrel or a corresponding structure. The pharmacodynamic experiment results show that the compound in the formula I has the effect of obviously inhibiting the platelet aggregation, and the effect of inhibiting the platelet aggregation is obviously better than that of the non-deuterated compound of clopidogrel and the corresponding structure. Therefore, the compound in the formula I can be used for preparing medicaments for preventing or treating related thrombus and embolism diseases.

This invention is directed to quinoline / quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and / or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders / conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and / or T cell activation and proliferation.

This invention relates to novel fused bicyclic compounds of the general formula (I):whereinthe symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb / IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.

A Chinese medicine in the form of injection for treating the acute stage of ischemic apoplexy and cerebral embolism is prepared from 3 Chinese-medicinal materials; red sage root, red peony root and grass-leaved sweetflag rhizome. Its advantage is high curative effect.

The invention discloses a preparation method of an anticoagulant material with function of inducing and catalyzing release of endogenous NO. The method comprises the steps of: configuring an alkaline Tris-buffer buffer solution, and adding a compound with certain concentration and pyrogallol structure and a compound with disulfide bond or diselenium bond and containing amino or thiol at two ends; and placing the substrate materials in a reaction solution, controlling the reaction temperature, reacting for 1-24 h, removing the substrate, and cleaning and drying to obtain the objective material. The invention has the advantages of simple operation, mild reaction conditions and easy operation. The component unit of the compound with disulfide bond or diselenium bond and containing amino or thiol at two ends has controllable content; the modified coating prepared by the method has excellent adhesion, and catalyzes the blood NO donors to continuously release NO molecules through in situ catalysis, inhibits activation and aggregation of platelets, inhibits proliferation of smooth muscle cells, and protects vascular endothelium.

A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.

Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-heme proteins, S-nitroso-t-PA, S-nitroso-cathepsin; S-nitroso-lipoproteins; and S-nitroso-immunoglobulins. The invention also relates to therapeutic use if S-nitroso-protein compounds for regulating protein function, cellular metabolism and effecting vasodilation, platelet inhibition, relaxation of non-vascular smooth muscle, and increasing blood oxygen transport by hemoglobin and myoglobin. The compounds are also used to deliver nitric oxide in its most bioactive form in order to achieve the effects described above, or for in vitro nitrosylation of molecules present in the body. The invention also relates to the nitrosylation of oxygen, carbon and nitrogen moieties present on proteins and amino acids, and the use thereof to achieve the above physiological effects.

A complex is provided for the treatment of neurogenic conditions having the formula:where R1 isM is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium(II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium(II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium(II):transporter ligand.

This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5′-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5′-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5′-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.

The present invention provides soluble forms of CD39L3 polypeptides and compositions, and methods useful inhibiting platelet activation and recruitment for the treatment and prevention of thrombotic disorders in mammals administered with soluble forms of CD39L3 polypeptides.

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and / or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and / or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and / or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma. The formula I-II is shown in the description.

The invention relates to the research field of medicinal chemistry, in particular to a novel scutellarein-6-site derivative (I), as well as a preparation method and an application thereof to medicines for preventing and treating thrombus. Pharmacological test results show that compared with scutellarin and scutellarein, the compound has better function of inhibiting platelet aggregation. The scutellarein-6-site derivative (I) provided by the invention can be used for treating a series of diseases caused by the thrombus, such as myocardial infarction, ischemia injury and so on.