67 results about "Anti alzheimer" patented technology

The present invention provides an osmotic device containing controlled release venlafaxine in the core in combination with an anti-Alzheimer's or an anti-Parkinson's drug in a rapid release external coat. Memantine is used as an anti-Alzheimer's drug or an anti-Parkinson's drug. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray-coated rather than compression-coated onto the device. The device is useful for the treatment of depression in Alzheimer's disease and / or Parkinson's disease patients. The device and method can also be used to treat or ameliorate other symptoms associated with Alzheimer's disease, Parkinson's disease or any other neurological disorder. Other dosage forms that provide a controlled, sustained or extended release of venlafaxine in combination with a rapid or immediate release of memantine are useful in the invention.

The invention is related to compound which comprises at least one radical C═Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C═Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

A turmeric, turmeric components, curcumin or curcuminoid modified nut or seed butter spread known as A which is resistant to oxidation with improved cu / co / tc / tu / mx solubility and possessing some human health benefits comprising: 0.2-70% of components selected from the group consisting of curcumin, curcuminoids, turmeric components and turmeric; and 30-99.8% of nut or seed particles and / or nut / seed butters as a dispersing medium. This spread has increased resistance to oxidation and bacterial attack as compared to the nut or seed butter alone. Based on health studies of curcumin, the modified nut or seed butter spread is also expected to have significant preventative health benefits including effectiveness as a chemopreventive, anti-Alzheimer's, anti-inflammatory, and antibacterial agent. The nut / seed butter medium improves the solubility and bioavailability of cu / co / tc / tu / mx. The invention is taste perfected for the western palate, it will serve as a novel vehicle for making curcumin / turmeric consumption an integral part of the western diet.

The present invention provides an osmotic device containing controlled release venlafaxine in the core, wherein the osmotic device exhibits a reduced food effect as compared to a reference controlled release capsule formulation. Some embodiments include venlafaxine in controlled release form in combination with an anti-Alzheimer's or an anti-Parkinson's drug in a rapid release external coat. Memantine is used as an anti-Alzheimer's drug or an anti-Parkinson's drug. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray-coated rather than compression-coated onto the device. The device is useful for the treatment of depression in Alzheimer's and / or Parkinson's patients. The device and method can also be used to treat or ameliorate other symptoms associated with Alzheimer's disease, Parkinson's disease or any other neurological disorder. Other dosage forms that provide a controlled, sustained or extended release of venlafaxine in combination with a rapid or immediate release of memantine are useful in the invention.

In general, the invention relates to novel bioactive pentapeptides from heat stabilized defatted rice bran having anti-cancer, anti-obesity, anti-Alzheimer and other health-promoting activities proteins. The bioactive pentapeptides can be incorporated into pharmaceutical, nutraceuticals and food compositions having at least the bioactive pentapeptide as an active ingredient.

The invention discloses a serial of iridoids compounds with the structural formula (I), the application of the compounds in preparing medicaments applied to the prevention or treatment of nervous system degenerative disorders such as senile dementia and the like, the medical compositions containing the compounds and a preparation method of the compounds. The structural formula is as shown above, wherein, various groups are defined in the instruction.

The invention provides an anti-Alzheimer disease monoclonal antibody which can specifically identify and combine Abeta oligomers and can be used in the preparation of diagnostic reagents and treatment drugs for Alzheimer disease.

The invention relates to establishment and application of a model for screening medicines for treating Alzheimer disease, and aims to provide a transgenic Dosophila melanogaster model for studying molecular pathway of pathogenesis progress of Alzheimer disease and drug screening. The invention obtains stable heritable novel Drosophila melanogaster variety by successive crossing of available transgenic Drosophila melanogaster. The novel disease model can simulate the in vivo generation and metabolism processes of major pathogenic genes of Alzheimer disease, and reproduce the pathogenesis process of the disease. The Drosophila melanogaster model provided by the invention is proven by a variety of indicators closely related to the symptoms of disease, including survive curve, mobility and learning and memory indexes and in vivo experiments, to be distinctly different from other Alzheimer disease Dosophila melanogaster models in all respects.

The invention discloses application of ethyl asterrate in preparation of an anti-alzheimer medicine, and in particular relates to application of diphenyl ether compound ethyl asterrate shown in the structural formula (I) in inhibition of the activity of acetylcholine esterase and preparation of an anti-alzheimer medicine. Experiments prove that the ethyl asterrate can remarkably inhibit the activity of acetylcholine esterase, can remarkably improve the memory and space exploration capability of an alzheimer rat model caused by D-galactose and AlCl3, can be applied to preparation of the anti-alzheimer medicine, and indicates an excellent market application prospect.

The invention belongs to the technical field of nano-medicaments, and discloses a nano-particle for inhibiting aggregation of alpha-beta and metal ion induced alpha-beta, as well as a preparation method and application thereof. The nano-particle is Y-modified nano-ruthenium and / or selenium nano-particle, and Y is at least one of arginine, histidine, glucose, saccharose, vitamin C and gallic acid; the Y-modified nano-particle comprises nano-ruthenium, nano-selenium and composite nano-ruthenium-selenium, can be used for inhibiting spontaneous aggregation of alpha-beta, has the effect of inhibiting aggregation of metal ion induced alpha-beta polypeptide, and can be applied to preparation of anti-alzheimer disease medicaments. According to the nano-particle modified by vitamin C and gallic acid, the vitamin C and the gallic acid are directly used as a reducing agent and a modifying agent, other auxiliary reagents need not to be added in the preparation process, the product system and the operation are simple, the method is simple and easy, and the product can be directly stored and used.

The invention belongs to the fields of pharmaceutical chemistry and pharmacotherapeutics and discloses amide group substituted hesperetin derivatives, a preparation method thereof and an application of the derivatives as AD (Alzheimer's disease) treatment drugs. Study proves that the amide group substituted hesperetin derivatives have strong inhibition property and good inhibition selectivity on acetylcholinesterase, and inhibition capacity of the derivatives on acetylcholinesterase is more than 500 times higher than inhibitory activity on butyrylcholinesterase. The study indicates that the compounds can be developed into the AD treatment drugs.

The invention provides a preparation method of an Ilex kudingcha C.J.Tseng leaf extract, wherein a traditional Chinese medicine Ilex kudingcha C.J.Tseng leaf is crushed, leached, separated and purified to obtain the Ilex kudingcha C.J.Tseng leaf extract, wherein the Ilex kudingcha C.J.Tseng leaf extract comprises active components (A), (b)-(f) and (B)-(E), and active compounds (1)-(5), and the active components (A), (b)-(f) and (B)-(E), and the active compounds (1)-(5) have the significant nerve growth factor simulation activity so as to be used for preparation of drugs and health food for prevention of Alzheimer's disease and other neurodegenerative diseases. According to the present invention, the traditional Chinese medicine Ilex kudingcha C.J.Tseng leaf has characteristics of wide source, easy obtaining and low cost, such that the development of the traditional Chinese medicine Ilex kudingcha C.J.Tseng leaf into the drugs and health food for prevention of Alzheimer's disease and other neurodegenerative diseases has important significance.

The invention discloses a series of compounds having an anti-Alzheimer's disease effect; o-aminobenzoic acid as a raw material is subjected to a reaction with cyclohexanone to obtain 9-chloro-1,2,3,4-tetrahydro acridine, and then 9-chloro-1,2,3,4-tetrahydro acridine is subjected to a reaction with ethylenediamine to obtain 9-(beta-amino ethylenediamine)-1,2,3,4-tetrahydro acridine; then 9-(beta-amino ethylenediamine)-1,2,3,4-tetrahydro acridine is subjected to a reaction with cinnamic acid and derivatives thereof to prepare a series of compounds having the anti-Alzheimer's disease effect; the whole process has the advantages of reasonable design, high yield, fewer by-products, and low cost; the prepared compounds have the advantages of high purity and good anti-Alzheimer's disease effect, and can realize industrialized mass production.

The invention belongs to the field of drug synthesis, and relates to a new method for synthesizing physostigmine, a natural drug against senile dementia, and its derivative, anilinoformate, phenserine. The present invention uses L-tryptophan 3 as raw material, firstly prepares chiral oxazolone intermediate 5, and then through intermolecular asymmetric cyclopropionation-ring-opening-ring and three-step one-pot waterfall reaction, and diazonium Acetate reaction was prepared to obtain optically pure 3-substituted tetrahydropyrroloindole skeleton 6, which was reduced by lithium aluminum hydride to obtain diol-substituted intermediate 7, and intermediate 7 was treated with Raney nickel (Raney-Ni ) after removing the hydroxymethylene group to obtain the intermediate 8 deoxy physostigmine (desoxyeseroline), and the intermediate 8 is obtained by electrophilic bromination reaction, methyl etherification, demethylation and carbonamidation four-step reaction with high yield. Completed the synthesis of physostigmine and its derivative, anilinoformate, physostigmine, a natural drug against Alzheimer's disease. The method has the advantages of high key reaction yield, simple operation, short reaction steps, etc., and has the advantages of solving the problem of raw material source of the marketed drug physostigmine and its derivative anilinoformate phenserine. important practical significance.

The present invention discloses an extracted centella asiatica (l.) urban effective fraction, and further discloses a preparation method for the effective fraction, wherein the effective fraction is prepared by performing a system separation method on centella asiatica (l.) urban. In addition, the present invention discloses an application of the effective fraction in anti-Alzheimer's disease drug preparation.

The invention discloses an alpha, beta-unsaturated carbonyl tetralone derivative and application thereof. The alpha, beta-unsaturated carbonyl tetralone derivative has the following structural formula, wherein R1 represents methylene or -HC-CH3; R2 represents hydrogen atoms or methoxyl; R3 represents hydrogen atoms, chlorine atoms, methoxyl, bromine atoms, fluorine atoms or nitryl; R4 represents hydrogen atoms or methoxyl; R5 represents hydrogen atoms, hydroxyl or methoxyl; R'3 and R'4 respectively represent hydrogen atoms or methoxyl; R'6 represents chlorine atoms or bromine atoms. The synthetic compound has pharmacological activities associated with anti-Alzheimer's disease, and is suitable for serving as a drug that can prevent, treat and diagnose Alzheimer's disease, and has a good potential application prospect. (Please see the formula in the description).

The invention provides a coumarin / pyridine hybrid derivative shown as the formula (I) or the formula (II) and pharmaceutically acceptable salt thereof. The coumarin / pyridine hybrid derivative and thepharmaceutically acceptable salt thereof can be applied in preparation of anti-Alzheimer and antiparkinsonian drugs or drugs for treating other diseases by inhibiting MAOs (monoamine oxidases) or chelating iron ions.

The invention, belonging to the field of drug compound, relates to 40H-GTS-21 compounds of formula (I), a preparation method and applications of the compounds, wherein, R1, R2 and X in the formula (I) are as defined in the description. The 40H-GTS-21 compounds are prepared by using 40H-GTS-21 as a matrix and introducing different glycosyl units in the position of hydroxyl groups of benzene ring. Experiments prove that the compounds disclosed in the invention has obvious stimulation to the excitatory synapse in hippocampal CA1 region, can improve the capability of permeating blood brain barrier (BBB), the bioavailability and the target activity of the drug molecules, and can be further used for preparing anti-Alzheimer drugs.

The invention discloses a compound with anti-alzheimer's disease activity which has a structure in formula (I), and the substituent R of the compound represents C1-C6 alkyl group, cycloalkyl group or aryl group. By structurally transforming the C-5 site of L-685-458, the method is adopted for the first time to successfully prepare the L-685-458, synthesize five types of new L-685-458 analogues, which have the advantages of high yield, easiness in separation, low cost, convenient production expansion and the like. Inferred according to the activity of the compound L-685-458, the five types of new L-685-458 analogues ought to have the anti-alzheimer's disease activity, and therefore have the prospect of being developed into anti-alzheimer's disease medicines.

The invention discloses a preparation method and an application of ethyl 2-(4-hydroxyphenyl)thiazole-4-carboxylate derivatives. The preparation method comprises the following steps: reacting p-hydroxythiobenzamide with ethyl 3-bromopyruvate to synthesize an intermediate ethyl 2-(4-hydroxyphenyl)thiazole-4-carboxylate, respectively reacting the intermediate with 1,3-dibromopropane, 1,4-dibromobutane or 1,5-dibromopentate to synthesize ethyl 2-(4-(3-bromopropoxy)phenyl)thiazole-4-carboxylate, ethyl 2-(4-(4-bromobutoxy)phenyl)thiazole-4-carboxylate or ethyl 2-(4-((5-bromopentyl)oxy)phenyl)thiazole-4-carboxylate, and respectively reacting the ethyl 2-(4-(3-bromopropoxy)phenyl)thiazole-4-carboxylate, ethyl 2-(4-(4-bromobutoxy)phenyl)thiazole-4-carboxylate or ethyl 2-(4-((5-bromopentyl)oxy)phenyl)thiazole-4-carboxylate with an amine to generate the target products. The synthesis method has the advantages of simplicity, safety and small pollution, and the products have a strong inhibition effect on butyrylcholine esterase and / or acetylcholinesterase, and can be used for preparing anti-Alzheimer disease medicines.

The invention belongs to the field of medicines, and relates to an application of a novel compound, which has effects of preventing and treating Alzheimer's disease and is extracted and separated fromdried shells of a plant xanthoceras sorbifolia, which belongs to the Xanthoceras Sapindaceae. In the invention, the novel compound is extracted and separated mainly through a traditional extraction and separation methods with combination of modern instrumental analytic methods, wherein the method mainly includes heating reflux extraction, macroporous adsorption resin column chromatography, silicagel column chromatography, ODS opened column chromatography, and preparative HPLC separation. A pharmacological experiment proves that the compound has excellent nervous protection effect on PC12 cell damage induced by A[beta]25-35; the compound can be used for further development and application of an anti-Alzheimer's disease medicine.

The invention belongs to the technical field of medicinal chemistry, in particular to N-(3,5-dimethyladamantane-1-yl)-N'-substituted phenylurea compounds as well as preparation methods and application thereof. The compounds have the structure shown in the formula I. The compounds are proved that the compounds can improve the image recognition memory, the working and learning memory, the spatial learning and memory ability of model rats and has good anti-alzheimer effects by the new object discrimination experiments, Y-maze experiments, positioning navigation and space exploration experiments in mats. The formula I is shown in the description.

The invention relates to a preparation method and application of a cornu cervi pantotrichum liposome. The preparation method of the cornu cervi pantotrichum liposome is established, and the prepared cornu cervi pantotrichum liposome can improve memory reappearance ability of mice with memory reproduction disorders, has potential anti-Alzheimer's disease activity, can be applied to prevention and treatment of cognitive disorder diseases such as the Alzheimer's disease, and has broad application prospects.

The invention relates to the technical field of microbial culture and discloses a preparation method of functional red yeast rice for preventing Alzheimer's disease. The preparation method includes following steps: 1), preparing a culture medium: smashing rice to obtain rice flour, mixing the rice flour with yam flour, Radix puerariae powder and pearl barley flour and then distilled water to obtain a solid culture medium, and sterilizing and loosening the solid culture medium; B), inoculating: inoculating a Monascus strain; C), culturing, wherein the culturing process is divided into a first stage, a second stage and a third stage, in the first stage, culturing the culture medium at 30-35 DEG C for 3-5 days, in the second stage, culturing at 25-30 DEG C for 5-10 days, and in the third stage, culturing at 20-25 DEG C for 10-20 days; D), drying: drying the solid culture medium to obtain red yeast rice. A special process is adopted, so that the red yeast rice prepared is high in active ingredient content and suitable for preventing and treating the Alzheimer's disease.

The invention discloses a quinoline-indole derivative and application thereof in preparation of a drug used for treating, improving and / or preventing alzheimer disease. The quinoline-indole derivativedisclosed by the invention is a multi-target anti-alzheimer disease active molecule, has the effects of inducing increase of number of neure of nerve cells PC12, neuronal differentiation and antioxidation and inhibiting Abeta aggregation and depolymerization, can promote formation of cerebral hippocampal neuron of an adult mouse and can improve APP / PS1 cognitive capability and spatial memory of an alzheimer disease mouse.

The invention relates to a polypeptide compound pheproserile valgly, which can inhibit the activity of DPP IV, prolylendopeptidase IV,lower blood sugar and fight Alzheimer's disease Argpro, whose amino acid sequence is pheproserievalglyargpro. The polypeptide pheproserievalglyargpro has DPP IV and PEP inhibitory activities, hypoglycemic and memory improving activities. It has a good application prospect as a health care product and drug lead compound for hypoglycemic and memory improvement as well as for the treatment of type II diabetes and anti Alzheimer's disease.

In general, the invention relates to novel bioactive pentapeptides from heat stabilized defatted rice bran having anti-cancer, anti-obesity, anti-Alzheimer and other health-promoting activities proteins. The bioactive pentapeptides can be incorporated into pharmaceutical, nutraceuticals and food compositions having at least the bioactive pentapeptide as an active ingredient.