656 results about "Platelet inhibition" patented technology

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 P2_τ receptor antagonist, in an amount effective to elevate its extracellular concentration to bind to P2_τ receptors and inhibit P2_τ 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 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.

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.

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.

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.

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.