139 results about "Hypolipidemic Agents" patented technology

This invention reveals the beneficial use of vitamin E tocotrienols for inhibition of chlamydial infections. Chlamydial infection levels in mouse macrophages treated with tocotrienol were decreased >50%, with concomitant aberrant pathogen development. The number of large and small inclusions in tocotrienol-versus-control cells was decreased 3-fold and 2-fold, respectively. When treated with delta tocotrienol, Chlamydia in human lymphocytes was inhibited by at least 2.6-fold in 1.5 days. Dietary delta tocotrienol inhibited Chlamydia infection and persistence in hypercholesterolemic patients with a corresponding drop in LDL. These studies demonstrate that tocotrienol lowers cholesterol, thus preventing or diminishing the cholesterol hijacking by Chlamydia obligatory for its infectivity and replication. Therefore, hypolipidemic agents used to treat cardiovascular diseases, metabolic syndrome, and diabetes are used as monotherapies, or in combination with tocotrienol to treat Chlamydia.

The present invention discusses a novel process for the synthesis of [R-(R*,R*)]-2-(4-fluorophenyl)-B,D-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium, atorvastatin. The compound so prepared is useful as inhibitor of the HMG-CoA reductase and may thus be used as hypolipidemic and hypocholesterolemic agent.

The present invention relates to a preparation method of medicine for reducing blood-lipid-Reshufatadine compound. Said method uses side chain aldehyde compound and triphenyl phosphorus ylide reagent compound and makes them undergo the condensation reaction so as to obtain Reshufatadine compound with high yield. Said invention also provides its key intermediate compound.

The invention discloses an extract of agrimony total flavonoids and an extraction and preparation method thereof; the total amount of ketosteroid compounds accounts for 25 percent to 100 percent of the total extraction matter. The invention takes agrimony as raw material and organic solvent whether containing or not containing water as extraction solvent. The extraction procedure is as following: extracting, leaching with solvent and adsorbing resin column to make purification process or using inorganic acid to regulate the PH value of concentrated solution to be no higher than 3, and then obtaining the extraction matter of agrimony after processing. Experiments prove that the extraction matter of agrimony total flavonoids has functions of antioxidation, anti-myocardial ischemia and reducing blood lipid. The extraction matter of agrimony total flavonoids can be used as food preservative and health product additive; the extraction matter of agrimony total flavonoids, carriers acceptable in pharmacy or excipient are made into various pharmaceutical dosage forms for anti-myocardial ischemia and reducing blood lipid. The invention has the advantages of simple technics and good treatment effect and can be widely used for curing or preventing coronary heart disease, hyperlipoidemia, high blood pressure or preventing cardio-cerebrovascular diseases such as atherosclerosis, etc.

The invention relates to a statins antilipemic drugs furazan nitroxides derivates and a preparation method thereof, and solves the problems of nonlipid-lowering and low activity in statins antilipemic drugs and adverse effect. The invention is shown as formula (1).

Compounds are provided which have the structure wherein Q is C or N; R2a, R2b, R2c, X1 to X7, R1, R2, R3, R3a, R4, A, Y, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents. The present invention further provides a method for treating obesity and dyslipidemia in mammals including humans through simultaneous inhibition of peroxisome proliferator activated receptor-γ (PPARγ) and stimulation of peroxisome proliferator activated receptor-α (PPARα).

The invention relates to the technical field of medicines, and provides application of metrn1 protein in preparation of a lipid-lowering drug or a health-care food. An in vivo experiment shows that the blood lipid level of metrn1 fat cell specificity overexpression mice is obviously lower than that of normal mice when the normal mice and the metrn1 fat cell specificity overexpression mice are supplied with triglyceride lavage; the result shows that the metrn1 protein has an effect of reducing blood lipid. The metrn1 protein is intrinsic protein of a human body. Therefore, the safety of the metrn1 protein as a potential drug is high.

A 2,3,5,4'-tetrahydroxy distyrene-2-O-beta-D-glucoside used for hypoglycemic medicine is prepared from the decoction of fleece flower root through extracting, separating and purifying. It can suppress the increasement of serum cholesterol, decrease low-density serum lipoprotein cholesterol and improve activity of liver esterase.

The present invention particularly relates to a nature crocin extraction separation method and preparation for a crocin blood fat reduction drug. The extraction separation method comprises: carrying out cleaning and impurity removing on dried cape jasmi fruits, extracting with deionized water, filtering to removing residue, carrying out online membrane separation and concentration fusion and macroporous absorption resin chromatography purification, and finally carrying out low-temperature spray drying to prepare the crocin. According to the present invention, the key of the invention is to create the extraction agent, and the water containing a certain auxiliary solvent is adopted to extract the crocin, wherein the extraction rate can be more than 95%; the online membrane separation and concentration fusion and the macroporous absorption resin chromatography purification are integrated; the high purity crocin production method has a characteristic of low cost and is suitable for industrial expansion production; and the compounded pharmaceutical preparation has effects of significant blood fat reduction, no side effect, effective cardiovascular and cerebrovascular related disease prevention, and blood circulation promotion, and is the preferred health care drug for crowds with high blood pressure, high blood fat and high blood sugar.

The invention belongs to the field of biotechnology and in particular relates to a polysaccharide extract of Chinese caterpillar fungi as well as a preparation method and application of the polysaccharide extract. The preparation method of the polysaccharide extract of the Chinese caterpillar fungi comprises the following steps: after submerged fermentation culture of mycelium of the Chinese caterpillar fungi, removing the mycelium of a fermented product by virtue of centrifugal separation to obtain a fermentation broth; after removing small molecule substances of the fermentation broth by virtue of ultrafiltration, concentrating the fermentation broth; and carrying out treatments of protein removal, ethanol precipitation, decoloring by hydrogen peroxide, dialysis and vacuum freeze-drying on the concentrated fermentation broth to prepare the polysaccharide extract of the Chinese caterpillar fungi. The preparation method is simple in process and is capable of carrying out efficient mass production with high quality. The prepared polysaccharide extract of the Chinese caterpillar fungi is nonhazardous to a human body, has good physiological function of reducing blood fat and can be used for developing a medicament or health food with the capability of reducing blood fat.

The preparation process of 5-methyl pyrazine-2-carboxylic acid with pyruvic aldehyde and o-diaminobenzene as basic material includes the cyclization in the presence of catalyst, oxidation with inorganic oxidant, acidification with sulfuric acid, decarbolxylation, extraction and separation with butanone, crystallization, drying and crushing. The 5-methyl pyrazine-2-carboxylic acid product has smelting point of 164-172 deg.c. The product is used as the intermediate for the medicine for treating diabetes and hyperlipemia.

The invention provides a nigre resource obtained by the alkali refining of rice bran crude oil. The preparation technology comprises the following steps of: by taking diethyl ether as an extract solvent, washing nigre by diethyl ether of which the weight is 3-10 times as heavy as the weight of the nigre, separating fatty acid from phytosterol-containing rice bran oil, freezing the rice bran oil, crystallizing, separating out phytosterol crude product and rice bran oil, dissolving the phytosterol curde product by 94%-97% of ethanol, and decoloring by adding activated carbon to obtain phytosterol finished product finally. The phytosterol extracted from the rice bran crude oil is all natural, free from toxicity and side effects, less in damage to phytosterol products, good in beta-sitosterol retaining property, high in content which can be more than 40%, low in solvent loss, higher in yield, better in safety, and is more suitable for the addition agent and the like for pharmacy (antilipemic agent), food and cosmetics.

The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and / or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.

The present invention relates to novel compounds of formula (I) and their pharmaceutically acceptable salts, wherein ring “Ar1” represents a monocyclic or polycyclic aromatic or partially saturated aromatic polycyclic, which may optionally contain up to 3 heteroatoms selected from N, S or O. The said monocyclic or polycyclic ring may be unsubstituted or have up to 4 substituents which may be identical or different; m and n independently represents an integer from 0 to 6; A represents O, S or bond; Y is selected from (CH2)p′(CH2)pB(CH2)q′(CH2)rB(CH2)pD(CH2)p′ where p, q and r each independently represents an integer from 0 to 6; B and D independently represents S, O, NR4 or a bond, with a proviso that when B and D represents hereto atom p is not zero; R4 represents hydrogen, alkyl, alkenyl, —S(O)2—R8 or —C(O)R8 where R8 is alkyl, alkoxy; R5 and R6 independently represents hydrogen, alkyl, cycloalkyl or alkoxy; R5 and R6 together may form 3-8 membered cyclic ring which may optionally contains one or two hereto atoms selected from O, S or N; R7 represents hydrogen, optionally substituted groups selected form alkyl, cycloalkyl, alkenyl or alkynyl. The present invention also relates to a process for preparation of compounds of formula (I), to pharmaceutical compositions containing compounds of formula (I) and their use in particular as antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic agents.

The invention discloses an officinal composition for lowering blood fat. Active ingredients are atorvastatin and probucol. The invention provides a better fat regulating drug for patients clinically suffering from severe lipid metabolism disorders and especially has favorable synergistic effect on patients at high liver function damaging risk level by drug combination; two kinds of drugs complement advantages so as to obviously lower the possibility of side effect occurrence because of increased amount of atorvastatin. The officinal composition for lowering blood fat is prepared from active ingredients and pharmaceutically acceptable supplementary materials, but is not limited in preparations, such as tablets, dispersible tablets, sustained release tablets and the like.

The invention provides an environment-friendly preparation method for a lipid-lowering drug ciprofibrate. The preparation method comprises the following steps of by taking hydroxyphenyl ethene as a raw material, carrying out Bargellini and annulation reaction to prepare the ciprofibrate. Compared with the traditional method, the method has the advantages of less reaction steps, short production cycle and high total yield, is easy to operate, mild and easy-control in conditions, convenient for postprocessing and environment-friendly, and is a brand new method for industrialized synthesis of the ciprofibrate.

Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

The present invention relates to a pharmaceutical composition and method for treating and preventing musculoskeletal and connective tissue diseases of unknown etiology, such as different forms of arthritis and other rheumatic conditions, comprising a combination of therapeutic agents that improve the processes of blood circulation and angiogenesis in the affected tissues, as well as other supporting therapies. Among the components of herein proposed pharmaceutical composition, are: vitamin K, polyunsaturated fatty acids (blood thinner), and niacin (vasodilator and hypolipidemic agent).

Pharmaceutical products comprising a hypolipidemic agent and a testosterone ester such as testosterone undecanoate are provided. Methods of safely treating a testosterone deficiency or its symptoms with the inventive pharmaceutical products are also provided.

The invention discloses new dihydrogen homoisoflavonoid, and a preparation method and application thereof. The new dihydrogen homoisoflavonoid is separated to extract polygonatum sibiricum. Experiments prove that the dihydrogen homoisoflavonoid can remarkably inhibit lipid accumulation in Hep-G2 cells, also can remarkably reduce the triglyceride (TG) content and the total cholesterol (TC) content of the cells, is more excellent that a positive control medicine simvastatin in the aspect of reducing the TG, and has excellent blood fat-reducing activity. The discovery of the new dihydrogen homoisoflavonoid provides a new lead compound for developing a new blood fat-reducing medicine, and good development and application prospect is achieved. The preparation process is simple, stable and reliable, the purity of the compound is high (above 98 percent), industrialized popularization is facilitated, a new approach is opened up for research and development of the blood fat reducing medicines, and good social and economic benefits are achieved.

The invention relates to an ezetimibe intermediate and a synthesis method of ezetimibe, and mainly solves the technical problems of low yield, low purity, severe conditions and the like in existing methods. According to a technical scheme of the invention, the preparation method includes: subjecting a compound 1 to Aldol condensation reaction under the condition of a self-made isopropoxy titanium trichloride catalyst to generate a compound 2, controlling the Aldol condensation temperature below -5DEG C, in terms of dropwise adding of the catalyst, adding a system A into a catalyst system, conducting ring closing on a compound 2 under the catalysis of TBAF, and removing silicon protecting group under the fluoride salt condition to generate ezetimibe. The synthesis route has mild conditions, the obtained intermediate and end product have high yield, and the purity is high.

The invention belongs to the field of biological medicine, and specifically relates to an application of a lignan compound in the preparation of drugs for reducing blood fat. The disclosed triterpene lignan compound is (-)-syringaresinol-4-O-glucoside, and the structural formula of the lignan compound is represented by the formula (I). The provided compound can prominently inhibit lipid accumulation in-vitro, is capable of obviously reducing the cholesterol and triglyceride in the animal blood of a hyperglycemia model, and has a prominent effect on reducing blood fat. The lignan compound can be used as a novel drug for reducing blood fat, and can be used to treat hyperglycemia, and the drug is user-friendly.

Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and / or preventing complications in patients with diabetes and / or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and / or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome.

The invention belongs to the technical field of medicine and specifically provides methylpyrazine derivative biological arginine hydrate, a preparation method thereof and application thereof in preparing blood fat reducing medicine. The prepared methylpyrazine derivative biological arginine hydrate disclosed by the invention is radiated by Cu-K alpha, and an X ray diffraction spectrogram represented by 2 theta has the characteristic peaks at the 5.7+ / -0.2 degree, 9.1+ / -0.2 degree, 16.2+ / -0.2 degree, 24.5+ / -0.2 degree, 24.8+ / -0.2 degree and 27.8+ / -0.2 degree positions. The prepared methylpyrazine derivative biological arginine hydrate disclosed by the invention has high stability; the purity basically cannot change when the methylpyrazine derivative biological arginine hydrate is placed ina dissolved state and a solid state; the solubility of the methylpyrazine derivative biological arginine hydrate in different media is 2.5 times of an existing crystal form; furthermore, the methylpyrazine derivative biological arginine hydrate has the advantages of higher bioavailability and better industrial application prospect.

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient.Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and / or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and / or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and / or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and / or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

The invention provides an abietane type diterpenoid compound with blood lipid lowering activity as well as a preparation method and application of the abietane type diterpenoids compound. Particularly, the compound provided by the invention has a structure shown as the formula I in the description, wherein the definition of all radicals is described in the description. The compound provided by the invention has the activity of increasing low-density lipoprotein intake in vivo or in vitro, and has the potential of being used as novel blood lipid lowering medicine.

The invention discloses a rapid detection method for six blood fat reducing medicine illegally added into Chinese patent medicine and health food with a blood fat reducing function. The rapid detection method comprises the following steps: after carrying out extraction treatment on a sample with methyl alcohol, adopting an ultra-high performance liquid chromatography-tandem mass spectrometry, carrying out chromatographic column separation, using a formic acid solution and acetonitrile as a moving phase for gradient elution, carrying out mass spectrum ESI positive ion and multi-reaction monitoring mode measurement, and carrying out external standard method quantification. The method is good in linear relation, quick, simple, convenient and accurate, can serve as a qualitative and quantitative detection method for illegally added chemical medicine in the blood fat reducing health food, and can be used for screening illegally added chemical medicine in the Chinese patent medicine and health food. Effective basis is provided for controlling the quality of health food and striking the behaviors of illegal addition in health food industry.