37 results about "Ca2 antagonist" patented technology

The invention relates to a process for producing azelnidipine. A yield improving and refining and purifying method is provided for synthesizing a dihydropyridine calcium antagonist. The process comprises the following steps of: performing N-alkylation cyclization, esterification and Pinner synthesis on epoxy chloropropane and aminodiphenylmethane serving as initial raw materials to obtain 3,3-diaminoacrylic acid-1-diphenylmethyl-3-azetidinyl ester acetate; and performing Hantzsch synthesis with 2-(3-nitrobenzylidene)isopropyl acetoacetate to prepare the azelnidipine, wherein the 2-(3-nitrobenzylidene)isopropyl acetoacetate is obtained by performing Knoevenagel reaction on nitrobenzaldehyde and isopropyl acetoacetate, and alpha-crystal form azelnidipine is prepared by crystal transition. By the process, the defects of a large number of side reactions, high production cost and the like of the foreign process are overcome, the process has the advantages of mild reaction condition, high yield, high product quality, no use of a class 1 solvent benzene, and the like, and the product is further purified.

The present invention relates to a planar-shaped drug preparation that quickly dissolves or decomposes in an aqueous environment, for the application of active ingredient combinations for the treatment of hypertension, wherein the drug preparations contain at least two active ingredients that are suitable for the treatment of hypertension, and wherein the antihypertensive drug is selected from the group that encompasses beta receptor blockers, alpha receptor blockers, calcium antagonists, ACE inhibitors, AT1 antagonists, centrally acting antihypertensive drugs, direct vasodilators, and diuretics. The present invention also relates to the use of active ingredient combinations according to the invention for the production of an oral drug preparation for the treatment of high blood pressure, to a method for the therapeutic treatment of hypertension, and to a method for the production of a planar-shaped drug preparation.

A composite medicine for treating hypertension contains proportionally one or two antihypertensive medicines chosen from calcium antagon, alpha receptor blocker, beta receptor blocker, renin-angiotonin system regulator and diuretic, one Ca containing component and the farmacologically acceptable auxiliary.

The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.

The invention relates to a drug composition. The drug composition consists of an effective treating amount of calcium antagonist (CCB), an angiotensin II receptor blocker (ARB), a thiazide diuretic, a folic acid compound and a pharmaceutically acceptable carrier, wherein the content of the CCB is 2-240 mg, the content of the ARB is 4-600 mg, the content of the thiazide diuretic is 0.625-25 mg, and the content of the folic acid compound is 0.4-0.4 mg. The drug composition has the advantages that the drug composition can effectively improve the treatment effect of reducing blood pressure of class-2 and class-3 hypertensive patients, strengthen the effect of protecting target organs of the patients and reduce the occurrence risk of cerebral apoplexy complications caused by high blood pressure. In addition, the drug composition can be conveniently taken by patients, the treatment compliance is greatly improved, and the medical costs can be also reduced.

The invention relates to a physiological regulator and treatment technology for preventing sugar hearts of apples from digestion. In order to solve the problems of nutrient loss, drug resistance of fruit trees and the like caused by application of different types of non-organic fertilizers in production, amino acid produced by strains is used to replace nitrogen fertilizers for enhancing phagocytosis of cells to drug-resistant bacteria pathogens, activating signal paths and improving fruit quality. According to the invention, a composite antagonist is adopted, and after a calcium antagonist inthe composite antagonist is combined with receptors on channels, the internal flow of Ca<2+> is reduced by reducing opening probability of the channels. According to correlation between the content of calcium elements and the degree of sugar hearts of apples, the lower the content of calcium ions in fruits is, the more easily the apples form water stain-like sugar hearts. The calcium antagonist is added into fruit trees to reduce circulation of calcium ions, so that the concentration of calcium ions is reduced, and then the sugar-heart ratio of apples is increased.

A dihydropyridine (DHP) calcium antagonist compound and its preparation method and medical use are related to preparation methods of compounds of general formulas (I) and (II) as shown below and their pharmaceutical salts and applications for treating cardiovascular diseases, and R1 represents a substituted or unsubstituted heterocyclic, aromatic ring or aralkyl group, and the substituent may be C1-C4 alkyl, C1-C4 alkoxyl, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro, amino or hydroxyl group; R2 represents a C1-C8 alkyl group; R3 and R4 are the same or different, and each represents a hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro or amino group or a C1-C4 alkyl, C1-C4 alkoxyl, C1-C4 alkenyl, or C1-C4 alkinyl group; R5 and R6 are the same or different, and each represents a C1-C4 alkyl group; X represents O, S or a single bond; m=0-6, n=1-6, and m and n are the same or different.

Dibenzo quinolizine compound entity has relatively low hygroscopicity and relatively high storage stability, and is applicable to preparation of analgesic, sedative, hypnotic and tranquillizing medicines, medicines for treating hypertension, arrhythmia and functional dyspepsia, stopping cough, resisting schizophrenia and heroin and other drug dependence, reversing tumor cell drug resistance and delaying or reducing myocardial ischemia reperfusion injury, calcium antagonists, and medicines for protecting the liver and preventing visceral implicated reaction and other effects, which are applied to humans or animals.

The invention provides a self-assembling light-emitting conductive nano medicinal crystal and ultra-thin film, and the preparing process, wherein non-resilient electronic tunneling interaction is employed for self-assembling oxidation resistant enzyme oxygen free radical antagonist, beta-receptor agonist, P2 receptor agonist, benzene alkylamines calcium antagonist monomer, and bibasic, ternary and quaternary compound.

A method of treating or preventing adhesion formation during or following a surgical procedure comprising administering to a patient in need thereof at least one medicament selected from the group consisting of potassium channels; modulators of macrophage activation and leucocyte attraction through cytokines, or their inhibitors, antibodies or inhibitors blocking the effect of VEGF expression; prostaglandin E1; free radical scavengers, lipid peroxysomes; pregnatrienes; calcium antagonists; hypoxia; acidosis; MP; dopamine; and ATP-MgCl2, wherein the method prevents adhesion formation by preventing anoxemia.

The invention relates the method for forecasting the drug-effect. The method measures the polymorphism gene type to forecast the drug-effect of calcium antagonist drug. The method forecasts the drug-effect of calcium antagonist drug by measuring the polymorphism gene type of key enzyme gene on the aminothiopropionic acid metabolism path.; at the mean time, according to the effect, prepare the compound drug which can improve the drug-effect of calcium antagonist by adjusting the preparation of aminothiopropionic acid metabolism path. The invention improves the effective rate of clinical drug therapeutics and the safety of clinical drug, and reduces the drug toxin side effect and cost.

The invention provides application of a traditional Chinese medicine composition in preparation of a drug for treating drug-induced abdominal pain and / or constipation caused by a selective calcium antagonist. The traditional Chinese medicine composition is mainly prepared from cloves and cortex cinnamomi. It is proved through clinical tests that the traditional Chinese medicine composition can significantly relieve abdominal pain and constipation caused by the selective calcium antagonist, particularly, abdominal pain and constipation caused by a dihydropyridine calcium antagonist, and the traditional Chinese medicine composition particularly has a very significant treatment effect on abdominal pain and constipation caused by nifedipine and amlodipine.

The invention relates to a novel sulfur-containing diphenyl thiazine compound, which has less hygroscopicity and good storage stability, and is suitable for preparing medicines for treating or preventing analgesia, calmness, hypnosis, hypertension, arrhythmia, functional dyspepsia, cough relieving, mental dissociation, drug dependence for heroin, and reverse tumor cells drug resistance, and is capable of delaying or mitigating myocardial Ischemia reperfusion injury, protecting liver, and preventing internal organ infection reaction.

The invention discloses a valsartan / felodipine compound preparation and a preparation method thereof. The valsartan / felodipine compound preparation comprises a main drug and an auxiliary material, the main drug comprises valsartan and felodipine; and the auxiliary material comprises a filler, a disintegrating agent, an adhesive, a lubricant and a flow aid. The method comprises the following steps: selecting raw materials, preparing the raw materials, mixing the raw materials, preparing a soft material, pelletizing the material, drying the material, granulating the material, totally blending, and obtaining the finished product. The valsartan / felodipine preparation composition can be used for treating hypertension by oral administration, the valsartan is a specific angiotensin II (AT1) receptor antagonist which has therapeutic effect through oral administration, the felodipine belongs to a third generation calcium antagonist, the product of the invention is the compound preparation of two brand-name drugs for treating hypertension, the compound preparation is suitable for patients who cannot control blood pressure by using a single medicine for treatment, curative effect of the compound preparation is good, usage of medication is convenient, and medication compliance for patients is greatly increased.

This invention relates to the advanced material field of the quantum information, it relates to the self assembling bi-stable quantum line array and its production method of nanometer medicine concretely. The invention self assembles antioxidase oxygen free-radical antagonist by the interaction of the inelasticity electron tunnel penetration, the beta-acceptor excitant, the P2 acceptor excitant, the benzene alkane amine calcium antagonist / or purine nucleic acid monomer and their binary , three-element, four -element and five -element compound. The invention quantum line array have regular geometry configuration, the dimension is controllable and adjustable, the inelasticity electron tunnel penetration, the quantum bit electricity characteristic and the Kondo effect. The invention not only benefits the study of the innovation medicine of target disease form, but also benefits the study of quantum bio-information sensor new material and nanometer structure magnetism memory (MRAM).

A dihydropyridine (DHP) calcium antagonist compound and its preparation method and medical use are related to preparation methods of compounds of general formulas (I) and (II) as shown below and their pharmaceutical salts and applications for treating cardiovascular diseases, and R1 represents a substituted or unsubstituted heterocyclic, aromatic ring or aralkyl group, and the substituent may be C1-C4 alkyl, C1-C4 alkoxyl, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro, amino or hydroxyl group; R2 represents a C1-C8 alkyl group; R3 and R4 are the same or different, and each represents a hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro or amino group or a C1-C4 alkyl, C1-C4 alkoxyl, C1-C4 alkenyl, or C1-C4 alkinyl group; R5 and R6 are the same or different, and each represents a C1-C4 alkyl group; X represents O, S or a single bond; m=0-6, n=1-6, and m and n are the same or different.

The present invention discloses an application of medicine composition containing medicinal dose calcium antagonist, medicinal dose phenoxy acid medicine and pharmaceutically-acceptable carrier in the preparation of medicine with synergistic action of reducing blood pressure or / and synergistic action of reducing blood lipid or / and synergistic action of changing vascular compliance or / and synergistic action of delaying targent organ damage. Said invention also relates to the application of said medicine composition in preparation of medicine for preventing, curing and delaying angiocardiopathy and cerebrovascular diseases.

A composite medicine for treating hypertension and the diseases associated with prostatoplasia contains Tansuoluoxin or its active metabolite or its precursor or its addition salt, antagon or its metabolite or its salt, and medicinal carrier or excipient.

This invention relates to a method for the production of (2R,3S)-3-(4-methoxyphenyl)glycidic acids and esters thereof, which are synthetic intermediates for the production of the calcium antagonist diltiazem. The method involves the stereoselective enzymatic ester hydrolysis of racemic trans-3-(4-methoxyphenyl)glycidic acid ester to yield the resolved (2R,3S) compound as the ester. Membrane reactor methods and apparatus for the conduct of this enzymatic resolution process are also disclosed herein, as is the use of bisulfite anion in the aqueous reaction phase as a means of minimizing the inhibitory effect of an aldehyde reaction by-product on the reaction's progress. The benefits of selected solvent systems from which may be obtained highly resolved ester product are also disclosed. These enriched organic solutions may be used in subsequent transformations. Alternatively, optically pure product may be obtained directly therefrom.

The invention provides amorphous lercanidipine hydrochloride and a preparation method thereof. Lercanidipine hydrochloride is a third-generation dihydropyridine calcium antagonist and is mainly used for hypertension and angina in clinic. The invention provides amorphous lercanidipine hydrochloride with the purity being at least 98.5%, particularly at least 99.5% and more particularly at least 99.7%. The invention also provides a preparation method of high-purity amorphous lercanidipine hydrochloride.

The invention relates to a novel crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2, a pharmaceutical composition containing the crystal form, and a preparation method and applications of the crystal form. Compared with the prototype compound, the crystal form of the invention has the advantages that the improvement effect on memory acquisition impairment caused by transient cerebral ischemia reperfusion is obviously enhanced, and the crystal form can be used for preparing calcium antagonists, anti-senile dementia drugs, anti-depression drugs, learning and memory enhancing drugs andthe like. The phenchlobenpyrrone crystal form provided by the invention has characteristics of simple operation of preparation method, easy crystallization process control, high crystallinity, good crystal form reproducibility and good stability, and is suitable for preparation process application and long-term storage.

The invention discloses a dihydropyridine calcium antagonist salt composition as well as a preparation method and an application thereof. The pharmaceutical composition comprises a salt formed by levamlodipine and an acidic polymer. The dihydropyridine calcium antagonist salt composition is in a stable amorphous state, and the amorphous state is kept for at least three months under accelerated stability conditions (40 DEG C, 75% relative humidity). The dihydropyridine calcium antagonist salt composition has higher instantaneous solubility and dissolution rate than a control substance in the pH environment of saliva, stomach funguses and intestinal tracts. The dihydropyridine calcium antagonist salt composition has better thermal stability, and can bear higher process temperature in a preparation process according to the glass transition temperature of the dihydropyridine calcium antagonist salt composition.

The invention provides a slow-release preparation of calcium antagonist and salt thereof and a preparation method thereof. The slow-release preparation comprises a slow-release phase which contains active pharmaceutical ingredients, the active pharmaceutical ingredients include 5-40mg of amlodipine or salt thereof calculated by amlodipine, 4-32mg of lacidipine or salt thereof calculated by lacidipine, 5-40mg of nisoldipine or salt thereof calculated by nisoldipine, 5-40mg of cilnidipine or salt thereof calculated by cilnidipine, 2-32mg of benidipine or salt thereof calculated by benidipine, 10-80mg of lercanidipine or salt thereof calculated by lercanidipine and 5-80mg of manidipine or salt thereof calculated by manidipine; in release media meeting sink conditions, higher than 90% of weight of the active pharmaceutical ingredients are released within a release period of 6-14h. The slow-release preparation is convenient to use, good in treatment effect, high in taking compliance, little in adverse reaction, quick in action, capable of maintaining stable and effective blood concentration for a long time, ingenious in design, simple in structure, high in stability and suitable for large-scale popularization and application.

The invention relates to a new crystal form A of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, as well as a medicine composition comprising the crystal form and application thereof. The crystal form Acan be used for preparing medicines such as high-selective calcium antagonists and medicines for improving disordered brain function, resisting Alzheimer's disease and depression, and enhancing learning and memory capability. The preparation method of the trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 crystal form A is simple in operation and is controllable in crystallization process. The producthas high crystallization degree and good repeatability, and can be absorbed and utilized by body better.

The invention relates to a new crystal form A of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, as well as a medicine composition comprising the crystal form and application thereof. The crystal form Acan be used for preparing medicines such as high-selective calcium antagonists and medicines for improving disordered brain function, resisting Alzheimer's disease and depression, and enhancing learning and memory capability. The preparation method of the trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 crystal form A is simple in operation and is controllable in crystallization process. The producthas high crystallization degree and good repeatability, and can be absorbed and utilized by body better.

The invention relates to the field of advanced quantum information materials, in particular relating to a self-assembly nano-medicament bi-stable quantum wire array and a preparation method thereof. The self-assembly nano-medicament bi-stable quantum wire array is prepared by self-assembling an antioxidase oxygen radical antagonist, a beta-receptor agonist, a P2 receptor agonist, a benzene alkyl amine calcium antagonist and / or a purine nucleic acid monomer as well as binary, ternary, quaternary and quinary complexes of the components under interaction of inelastic electron tunneling. The quantum wire array has the advantages of regular geometric structure, controllable and adjustable dimension, inelastic electron tunneling and quantum bit electrical properties and kondo effect. The self-assembly nano-medicament bi-stable quantum wire array and the preparation method thereof are beneficial to research of innovative medicaments with a targeted disease mechanism and research of a new quantum biological information sensing material and a nano-structured magnetic random access memory (MRAM).