63 results about "Platelet Aggregation Inhibition" patented technology

The invention discloses a method for evaluating chemical composition of Rosa xanthina on the basis of antithrombotic spectrum-effect relationship. The method comprises the following steps: preparing extract of different polar components of the Rosa xanthina with a modern separation technology; establishing fingerprint of extract of each component with high-performance liquid chromatography, and calibrating characteristic peaks; evaluating antithrombotic activity of different extract on the basis of platelet aggregation inhibition rate, prothrombin time, thrombin time and activated partial thromboplastin time as indexes; substituting fingerprint characteristic peak data and pharmacodynamical activity data into a mathematical model for spectrum-effect correlation analysis, and evaluating pharmacodynamical activity of the characteristic peaks. With adoption of the method for evaluating the chemical composition of the Rosa xanthina on the basis of the antithrombotic spectrum-effect relationship, the antithrombotic chemical composition in the Rosa xanthina can be evaluated rapidly and accurately, a scientific and effective method is provided for research of pharmacodynamic material basis and quality control of the Rosa xanthina, and reference is provided for further development of Rosa xanthina drugs or health care products for treating thrombotic diseases.

[Problem] To provide a compound having excellent platelet aggregation inhibitory activity.

[Means for Resolution] It was found that quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R⁰)C(O)-lower alkylene-CO₂R⁰, lower alkylene-CO₂R⁰, lower alkenylene-CO₂R⁰, —O-lower alkylene-CO₂R⁰, —O-(lower alkylene which may be substituted with —CO₂R⁰)-aryl or —O-lower alkenylene-CO₂R⁰ (wherein R⁰ is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. In addition, it was confirmed that these quinolone derivatives also have excellent platelet aggregation inhibitory activity. Based on the above, these quinolone derivatives or pharmaceutically acceptable salts thereof are useful as platelet aggregation inhibitors.

[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.

The invention relates to a method for preparing a related substance B in a platelet aggregation inhibition medicament-clopidogrel bisulfate. The method comprises the steps of: adopting dienone and L-2-chlorophenylglycine methyl ester to obtain tetrahydropyridone through a closed-loop reaction; then obtaining a 2-aminothienopyridine derivative through a Gewald reaction; and finally obtaining a target product through diazotization and acid hydrolysis. The process takes the synthesis of a pyridine ring first and then the synthesis of a thiophene ring as a route, obtains the target product with higher yield through a classical reaction, and provides novel thought for the synthesis of the related substance B of the clopidogrel bisulfate.

The invention discloses a synthetic method of sulfo bagasse xylan phthalate. The synthetic method comprises the following steps: by taking bagasse xylan as a starting material, taking phthalic anhydride as a carboxylic acid esterification agent and taking triethylamine as a catalyst, synthesizing bagasse xylan phthalate in a dimethylformamide solvent; and then further synthesizing a sulfo bagasse xylan phthalate double esterification derivative in an alkaline water solvent by taking sodium trisulfamate as a second esterification agent. The bagasse xylan double esterification derivative namely sulfo bagasse xylan phthalate prepared by using the synthetic method disclosed by the invention integrates the properties of bagasse xylan carboxylic ester and bagasse xylan sulfate, and is easy to control synthesis process conditions; products have relatively high biological activity and good water solubility and surface activity; and modified double-active bagasse xylan has certain effects on the aspects of anti-HIV activity, anti-coagulation activity and platelet aggregation inhibition, and has relatively high application values in the fields of fine chemicals, foods and medicines.

The invention discloses a spirulina gamma-linolenic acid extractive and a preparation method of the spirulina gamma-linolenic acid extractive. The spirulina gamma-linolenic acid extractive has high antioxidation activity and antiplatelet activity. According to the spirulina gamma-linolenic acid extractive, spirulina powder is taken as a raw material; and by ultrasonic processing, organic solvent extraction, vacuum filtration, vacuum concentration, vacuum freezing drying and gas chromatograph-mass spectrometer measurement, the powdered spirulina gamma-linolenic acid extractive can be finally obtained. A DPPH (1.1-diphenyl-2-1picryhydrazyl radial) scavenging test, a lipid oxidation inhibition test and a platelet aggregation inhibition test show that the spirulina gamma-linolenic acid extractive has high antioxidation activity and antiplatelet activity, and finally prove that the mode of extracting gamma-linolenic acid from spirulina is an economic and effective mode. The method disclosed by the invention can be applied to the field of development of health-care food.

A method for producing paeonoside metabolic hormone-I by fermenting short Lactobacillus is carried out by inducing L.brevis AS 1.12 into culture medium with tomato juice 200g/L, protein peptone 7.5g/L, yeast paste 7.5g/L, glucose 10g/L, Tween-80 0.3 ml/L and pH=7.0-8.5, anaerobic culturing at 25-37 degree for 12-24 hrs, centrifugal collecting bacterial cells, washing by normal saline, centrifuging, dispersing obtained cells into buffer liquid of 0.05M phosphate, adding into substrate paeonoside or its analogs hydroxy-paeonoside or methyl-paeonoside or benzoyl-paeonoside or mixture of paeonoside and its analogs, converting at 30-40 degree for 2-24 hrs, extracting by ethyl acetate, drying concentrated extract to obtain concrete, chromatographying by silica-gel column to obtain final product. It's simple, cheap, efficient, fast and controllable and has friendly environment. It can be used for anti-inflammatory, stress ulcer, analgesic and antispasmodic, ecstatic coronary blood vessel, myocardial ischemia and platelet aggregation-inhibition.

The invention relates to the field of medicines, and particularly relates to an application of a ginseng total sub-glycoside combination, ginseng prosapogenin or ginseng protosaponin in the preparation of medicines for treating tinnitus, dizziness and Meniere's syndrome. Plants for preparing the ginseng total sub-glycoside medicine combination are panax plants, and are preferably selected from at least one of ginseng, pseudo-ginseng, panax japonicus, American gingseng and Korean ginseng. The ginseng total sub-glycoside combination is a mixture of ginsenoside partially hydrolyzed and a degradation product, namely secondary saponin, part of glycosyl of which is removed. The physiological activity of the ginseng total sub-glycoside combination is greatly enhanced, and the ginseng total sub-glycoside combination has the physiological activities such as blood vessel expansion, heart dynamic enhancement and platelet aggregation inhibition. The ginseng total sub-glycoside combination, the ginseng prosapogenin or the ginseng protosaponin is used for treating the Meniere's syndrome, is definite in curative effect and has high effective rate, small individual difference and high safety without side effects.

The present invention relates to a chronotherapeutically combined pharmaceutical formulation for preventing and treating cardiovascular diseases, which is based on the principle of administering a plurality of drugs at certain time intervals (chronotherapy). Specifically, the combined pharmaceutical formulation comprises a HMG-CoA reductase inhibitor, such as simvastatin, and aspirin. Because the combined pharmaceutical formulation was developed based on the principle of administering drugs at certain time intervals, so-called chronotherapy, it shows an excellent effect of preventing or treating cardiovascular disease compared to those of the individual administration and simultaneous administration of the single preparations. Also, it is a once-daily dosage form which increases the medication compliance of patients. Particularly, even though the content of aspirin in the combined pharmaceutical formulation is reduced, the platelet aggregation inhibitory effect of aspirin in the combined pharmaceutical formulation is equal to that of the amount of aspirin used in the prior art, while the aspirin in the combined pharmaceutical formulation shows a antihypertensive effect. In addition, the chronotherapeutically combined pharmaceutical formulation allows the two drugs, which interact with each other, to be stored for a long period of time, and the combined pharmaceutical formulation ensures the human body-safety and efficacy of the two drugs.

The invention belongs to the technical field of pharmaceutical chemistry, and particularly provides a novel preparation method of a compound for preparing platelet aggregation inhibitors with a general formula (I). The preparation route adopts a one-pot method, and the intermediate directly enters the next reaction without being purified or separated. The method can prepare the target compound I in one step. Compared with the synthesis techniques provided in the prior literature, the invention increases the yield, simplifies the operation steps and shortens the production cycle, thereby finally reducing the production cost and meeting the requirements for green synthesis techniques. In the compound I, R is a methyl or ethyl group.

The invention relates to a method for detecting biological activity of resina draconis, which realizes control on whole efficacy of complex components of the resina draconis. The method comprises the following steps of: crushing the resina draconis into ethanol, carrying out ultrasonic extraction, drying the extracts, using dimethyl sulfoxide for dissolving to obtain solution, continuously diluting, and obtaining solution with geometric proportion concentration; respectively measuring blood plasma recalcification time contraction rate and platelet aggregation inhibition ratio of the resina draconis; and carrying out titer calculation according to a parallel line assay method based on quantitative responses (2.2) of appendix X IV of Chinese Pharmacopoeia II. The method is simple and easy to operate, is accurate to measure, and can be used for controlling the whole efficacy of the resina draconis with undefined active constituents.

The invention relates to an anti-HIV aedes albopictus protein with a platelet aggregation inhibiting function. An amino acid sequence of the anti-HIV aedes albopictus protein is shown as SEQ ID NO:1. A preparation method of the anti-HIV aedes albopictus protein comprises the following steps: purifying total RNA of aedes albopictus salivary glands and amplifying so as to obtain total cDNA, then amplifying genes of the total cDNA taken as a template and cloning the genes into a prokaryotic expression vector, carrying out inducible expression via IPTG, carrying out denaturation and renaturation folding on an expressed inclusion body, then filtering the inclusion body via a gel, and carrying out separation and purification on the inclusion body by ion exchange chromatography so as to obtain the anti-HIV aedes albopictus protein. The anti-HIV aedes albopictus protein has the activities of inhibiting the proliferation of the HIV in cells and the platelet aggregation induced by multiple agonists, and has the advantages of no cytotoxicity and strong anti-HIV specificity. Thus, the anti-HIV aedes albopictus protein can be used for preparing medicines for resisting AIDS (Acquired Immune Deficiency Syndrome) and related diseases.

The present invention provides: (1) pharmaceutical compositions for angiogenic therapy which contain, as the active ingredients, at least one substance selected from substances having vasodilating effect and/or platelet aggregation inhibitory effect, and substances producing them; and a gene encoding an angiogenesis factor; (2) agents for potentiating the angiogenic effect of a gene encoding an angiogenesis factor that contain, as the active ingredient, at least one substance selected from substances having vasodilating effect and/or platelet aggregation inhibitory effect and substances producing them; (3) an angiogenic agent which contains a prostacyclin synthase gene as the active ingredient; (4) pharmaceutical compositions for angiogenic therapy which contain ets-1 gene and another gene encoding an angiogenesis factor as the active ingredients; (4) an agent which contain ets 1 gene as the active ingredient for potentiating the angiogenic effect of another gene encoding an angiogenesis factor; and (5) an angiogenic agent which contains ets-1 gene as the active ingredient.

The invention relates to a compound traditional Chinese medicine composition for preventing and treating the disturbance of coronary microcirculation and an animal experiment method. The compound traditional Chinese medicine composition is prepared from the following traditional Chinese medicines in parts by weight: radix astragali, angelica, scorpio and scolopendra. The preparation method of thecompound traditional Chinese medicine composition comprises the following steps: preparing the traditional Chinese medicines in parts by weight: radix astragali, angelica, scorpio and scolopendra, soaking the traditional Chinese medicines into water which is 15 times of the total weight of the traditional Chinese medicines for 40 minutes, carrying out decoction with strong fire for 70 minutes forthe first time, adding water which is 10 times of the total weight of the traditional Chinese medicines, carrying out decoction with soft fire for 50 minutes for the second time, adding water which is6 times of the total weight of the traditional Chinese medicines, carrying out decoction with soft fire for 50 minutes for the third time, combining three decoction solutions, filtering by virtue ofgauze, concentrating to 150ml through water bath at 100 DEG C, and storing the combined decoction solution in a refrigerator at 4 DEG C, so as to obtain the finished product. The compound traditionalChinese medicine composition has the efficacies of expanding blood vessels, inhibiting platelet aggregation and inflammation and the like, is capable of improving the disturbance of coronary microcirculation and can be applied to the technical field of the traditional Chinese medicine.

The present invention discloses warfarin-4-O-acetyl-Tyr-Ile-Gly-Ser-Lys, a preparation method, anti-arterial thrombus activity, anti-venous thrombosis activity, in vivo vitamin K content lowering activity, in vivo blood coagulation factor II content lowering activity, and platelet aggregation inhibition activity thereof, such that the invention discloses applications of warfarin-4-O-acetyl-Tyr-Ile-Gly-Ser-Lys in preparation of anti-arterial thrombus drugs, anti-venous thrombosis drugs, platelet aggregation inhibition drugs, vitamin K antagonists, and blood coagulation factor II antagonists.

The present invention relates to an antithrombotic composition including Polygonum cuspidatum Sieb. et Zucc. and Cinnamomum cassia Blume as active ingredients, and preferably includes an extract obtained by mixing Polygonum cuspidatum Sieb. et Zucc. and Cinnamomum cassia Blume in a weight ratio of 1:2-2:1 and extracting the mixture. The composition of the present invention is highly effective in antithrombotic effects, identified as a platelet aggregation inhibitory effect, a thrombosis inhibitory effect, a thrombosis-delaying effect, and the like, and thus can be used as an effective herbal-medicine-based agent for preventing or treating thrombosis, an antithrombotic health food, and the like.

The invention belongs to the technical field of medicine and relates to a ticagrelor sesquihydrate capsule and a preparation method thereof. The ticagrelor sesquihydrate capsule has the advantages of simple process, low cost, high bioavailability, and platelet aggregation inhibition ability improved by almost 10%. The invention also relates to a use of the ticagrelor sesquihydrate capsule in treatment on cardio-cerebrovascular system diseases.

The invention discloses a health-care beer composed of resveratrol and a corresponding health beer manufacturing method. The beer has the functions of anti-tumor, antioxidation, cardiovascular disease resistance, cardiovascular disease resistance, bacteria resistance, antiinflammatory action, platelet aggregation inhibition, immune regulation, chemoprevention and the like and is especially suitable for the middle and the old.

The invention relates to application of Fluevirosines A in preparation of an anti-platelet aggregation drug. The application of the Fluevirosines A in the preparation of the anti-platelet aggregation drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type, the Fluevirosines A has outstanding substantive characteristics and meanwhile has a remarkable improvement in platelet aggregation inhibition obviously.

The invention discloses a wood pineapple extract for treating cardiovascular and cerebrovascular diseases and preparation method thereof. In which, the wood pineapple extract is beta-sitosterol and flavones extracted from wood pineapple leaves by the process of: extracting the wood pineapple leaves by ethanol to obtain wood pineapple ethanol total extract; separating the wood pineapple ethanol total extract roughly to obtain petroleum ether extracting extraction position and ethyl acetate extraction position; and purifying and separating the petroleum ether extracting extraction position and ethyl acetate extraction position to obtain the wood pineapple extract for treating cardiovascular and cerebrovascular diseases: beta-sitosterol and flavones. The obtained extract has the functions of antithrombotic, platelet aggregation inhibition, blood viscosity reduction and cardiac muscle cell protection.

The invention discloses a platelet aggregation inhibition preparation, which belongs to the technical field of biomedicine. The platelet aggregation inhibition preparation comprises active ingredients and an auxiliary material, wherein the concentration of the active ingredients is 0.1-50 mg/ml, and the active ingredients are eptifibatide and pharmaceutically-acceptable eptifibatide derivatives; the auxiliary material is a buffer system of citric acid and sodium citrate; and in the buffer system, the concentrations of the citric acid and the sodium citrate are respectively 0.5-50 mg/ml and 0.5-50 mg/ml. The six-month accelerated test and the 24-month long-term stability test prove that the active ingredients are stable in the injection prepared from the eptifibatide preparation. In particular, the small volume injection prepared from the eptifibatide preparation has the advantages of good stability and accurate curative effect, and can maintain good stability during storage and transportation.