21 results about "Donepezil" patented technology

The use of glutamate 2b receptor antagonists and sigma receptor agonists as antitussives to treat or prevent a cough is disclosed. In preferred embodiments, the glutamate 2b receptor antagonist is ifenprodil or radiprodil. Preferred sigma receptor agonists include fluvoxamine, fluoxetine, excitalpram, and donepezil.

The application discloses application of a drug composition of bacosol and donepezil in preparation of a drug for treating Alzheimer's disease. The application first discovers that bacosol has double-target point inhibitory activity on BACE1 and AChE. Through cell and animal model verification, the bacosol single drug and the composition can exert an anti-AD effect through a multi-target point mechanism, and the composition with a molar ratio of 1:1 to 1:10 has a significant synergistic effect, wherein the synergistic effect is the most significant when the molar ratio is 1:1. The application provides a new treatment method for Alzheimer's disease.

The present invention relates to a donepezil and tadalafil combination therapy for the prevention, treatment or amelioration of Alzheimer's disease or cognitive dysfunction. The combined administration of donepezil and tadalafil according to the present invention has an improvement effect on Alzheimer's disease or cognitive impairment superior to that of the individual administration of donepezil, and thus can be effectively used as a therapeutic or complexing agent or the like for Alzheimer's disease or cognitive impairment.

The use of glutamate 2b receptor antagonists and sigma receptor agonists as antitussives to treat or prevent a cough is disclosed. In preferred embodiments, the glutamate 2b receptor antagonist is ifenprodil or radiprodil. Preferred sigma receptor agonists include fluvoxamine, fluoxetine, excitalpram, and donepezil.

The invention provides an application of a donepezil or gardenia jasminoides ellis-phellodendron amurense component in preparation of a cholinergic regulation-based immune liver injury resisting medicine, and belongs to the technical field of biological medicines. The pharmaceutical composition for resisting immunological liver injury is a donepezil component or a gardenia jasminoides ellis-phellodendron amurense component. The invention solves the problems of single action target and incomplete regulation and control mechanism of the existing immunological liver injury treatment medicine, provides a treatment scheme with anti-inflammatory, anti-oxidation, liver cell apoptosis inhibition and cholinergic system regulation and control functions, explores a brand new medical application of donepezil, verifies the liver protection effect of donepezil in immunological liver injury, and provides a new application of donepezil in immunological liver injury. The application limitation is broken through; the treatment effect of the Jashima component in an immune liver injury model induced by concanavalin A is defined, a dual regulation mechanism of inhibiting AChE expression and increasing alpha7 nAChR expression is disclosed, and the application scene is expanded; a multi-dimensional regulation and control network of cholinergic anti-inflammatory pathway-NF-kappa B inflammatory pathway-hepatocyte apoptosis is constructed, and a more efficient and comprehensive treatment strategy is provided for immunological liver injury.

The invention relates to application of a phenyl pyrimidone compound, in particular to application of the phenyl pyrimidone compound shown in a formula (I) or tautomers, pharmaceutically acceptable salts, solvates or isotope labels of the phenyl pyrimidone compound in preparation of drugs for improving or treating cognitive impairment and / or improving or treating brain vascular diseases. Through cell model and animal model test research, compared with a clinically available drug donepezil on the market and a clinically researched drug mironafil, the compound disclosed by the invention has remarkable treatment characteristics and substantive technical progress in the aspects of protecting nerve cells, improving cognitive impairment, improving brain vascular diseases, improving degenerative diseases such as Parkinson's disease and the like.

Use of a phenylpyrimidinone compound. The present invention specifically relates to use of a phenylpyrimidinone compound represented by formula (I) or a tautomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or an isotopically labelled compound thereof in the preparation of a drug for ameliorating or treating cognitive impairment, and / or ameliorating or treating cerebrovascular diseases. Studies using cell and animal models have shown that compared to the commercially available clinical drug donepezil and the investigational clinical drug mirodenafil, the compound has demonstrated significant therapeutic characteristics and substantial technical advancements in terms of protecting nerve cells, ameliorating cognitive impairment, ameliorating cerebrovascular diseases, and ameliorating degenerative diseases such as Parkinson's disease.

The invention provides compositions comprising a topical formulation of donepezil and methods of use thereof for intradermal applications.

The invention provides application of apoptin combined peptide to treatment of Alzheimer's disease. The apoptin combined peptide used in the invention has the following amino acid sequences: MetGlyArg, LysLysArg, Arg, GIn, Arg, Arg, LeuLysProProSerLysLysArgleArgleGlyleAlaGlyleThrLeuSerLeuArg, ProArg, Thr, AlaLysArg, ArgleArg, Leu and the like. The apoptin combined peptide provided by the invention has the following amino acid sequences: MetGlyArg, LysLysLysArg, Arg, Arg and Leu. Various animal model experiments prove that after the polypeptide drug is administered through intravenous injection (with the dosage of 1mg / kg to 3mg / kg), cognitive impairment, spatial learning and memory ability of model animals with Alzheimer's disease, vascular dementia and senile dementia can be remarkably improved, and the treatment effect is superior to that of donepezil. The action mechanism comprises reduction of oxidative damage, inhibition of APP and BACE1 pathological protein expression, increase of neuron number and nissl body content, inhibition of cell apoptosis and the like. The polypeptide medicine is high in safety and remarkable in curative effect, and a new effective medicine is provided for treating the Alzheimer's disease.

This invention discloses a traditional Chinese medicine composition for treating vascular cognitive impairment, its preparation method, and its application, belonging to the field of traditional Chinese medicine technology. It includes the following raw materials: stir-fried Atractylodes macrocephala, Fritillaria thunbergii, Ligusticum chuanxiong, Salvia miltiorrhiza, Curcuma longa, Acorus tatarinowii, Polygala tenuifolia, Cornus officinalis, Cistanche deserticola, Rehmannia glutinosa, Scrophularia ningpoensis, and borneol. Preparation method: First, the volatile oil is extracted by steam distillation and encapsulated with β-cyclodextrin; then, the lipid-soluble components in Salvia miltiorrhiza and Fritillaria thunbergii are extracted with ethanol; finally, the residue is combined with the remaining medicinal materials and decocted in water for extraction. Through the combination of Fritillaria thunbergii and borneol, the dual functions of "clearing inflammation + opening the blood-brain barrier" are achieved, increasing the brain concentration of lipid-soluble components such as tanshinone IIA. It significantly improves the learning and memory abilities of rats with vascular cognitive impairment, with efficacy superior to the Western medicine donepezil, and exhibits synergistic effects on multiple targets such as inhibiting NLRP3 inflammasomes and upregulating BDNF. This invention has a simple process, is suitable for industrial production, and has significant clinical application value.

The present application relates to the salt of donepezil derivative and its application in medicine, specifically, the present application relates to the salt of compound shown in formula (I), the salt of the compound can play the role of long-acting inhibition of acetylcholinesterase expression, thereby more long-acting prevention and / or treatment of Alzheimer's disease, wherein R 1 has the meaning described in the present application.

The invention discloses a method for detecting related substances in a memantine hydrochloride donepezil preparation. The detection method comprises the following steps: preparing and measuring a test solution and a reference solution by adopting a GC (Gas Chromatography) method, measuring a solvent acetonitrile, and respectively injecting into a gas chromatograph; and recording a chromatogram and calculating by peak area according to an external standard method. The detection method can be used for simultaneously detecting memantine impurity E, memantine impurity F, memantine impurity G, memantine impurity H and memantine impurity I in the memantine hydrochloride donepezil preparation. The method has the advantages of good sensitivity, durability, system applicability, specificity and accuracy, and qualified recovery rate.

Provided herein are methods for promoting biostasis or preservation of a cell, tissue or organ during cancer treatment or for transplantation comprising contacting the cell, tissue or organ with an agonist of the δ-opioid receptor, SNC-80, an or Donepezil. Further provided herein is a method of treating a hematological neoplastic disease.

The invention provides compositions comprising a topical formulation of donepezil and methods of use thereof for intradermal applications.

The present invention relates to a novel low-dose daily administration regimen of donepezil and its derivatives, or pharmaceutically acceptable salts and / or solvates thereof, for the prevention and / or treatment of obsessive-compulsive disorders, particularly eating disorders. The present invention also relates to a unit dosage form containing 0.25 to 2.5 mg of donepezil, its derivatives, or pharmaceutically acceptable salts and / or solvates thereof, for use in the prevention and / or treatment of obsessive-compulsive disorders, particularly eating disorders.

A percutaneous absorption preparation for the treatment of dementia wherein the drug-containing layer contains donepezil or a pharmaceutically acceptable salt thereof as an active ingredient and a stabilizer that is either (i) a mixture of a thiocyanate salt and a compound selected from the group consisting of tea catechin, (+)-catechin, epigallocatechin gallate, ascorbic acid, and isoascorbic acid, or (ii) a mixture of monothioglycerol and a compound selected from the group consisting of tea catechin, (+)-catechin, epigallocatechin gallate, and ascorbic acid is disclosed. The percutaneous absorption preparation meets the criteria of Procedure 1 and Procedure 2 of the U.S. Pharmacopoeia in short-term stress test (70° C. 48 hours storage), long-term accelerated test 1 (40° C. relative humidity 75% 1 month storage), and long-term accelerated test 2 (40° C. relative humidity 75% 3 months storage), and exhibits improved stability for long-term preservation.

The present invention relates to combination of donepezil or a pharmaceutically acceptable salt thereof and cevimeline or a pharmaceutically acceptable salt thereof for use in the treatment of Alzheimer´s disease. Furthermore, a pharmaceutical formulation containing donepezil or a pharmaceutically acceptable salt thereof, cevimeline or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient is provided.

The invention provides a transdermal patch containing donepezil and a preparation method of the transdermal patch. The transdermal patch comprises a backing layer, a drug-containing matrix layer and a stripping layer, wherein the medicine-containing matrix layer comprises donepezil or pharmaceutically acceptable salt of donepezil, a pressure-sensitive adhesive and a permeation enhancing agent group; the penetration enhancing agent group comprises at least three of lauryl lactate, laurel sorbitan, triethyl citrate, propylene glycol, sorbitol laurate and isopropyl myristate. The donepezil or the pharmaceutically acceptable salt of the donepezil in the transdermal patch can maintain the blood concentration for a long time, the permeation efficiency of the transdermal patch can be improved, the bioavailability can be improved, the adhesion of the transdermal patch can be improved, and the use comfort of a patient can be improved.

The invention discloses an application of a scopolamine model in an acetylcholin esterase inhibitor, and relates to the technical field of medicines.The application comprises the steps that S1, the learning memory of the scopolamine model is improved through a compound; s2, the inhibition effect of the compound on acetylcholin esterase is verified, and the compound is specifically (5S)-1-(3, 4-dihydroxyphenyl)-5-hydroxy-7-(4-hydroxy-3-methoxyphenyl) heptyl-3-ketone. A plurality of groups of experiments are designed to prove that the compound can remarkably improve the learning and memory dysfunction of AD model mice induced by scopolamine and has dose dependence, an enzyme activity inhibition experiment shows that the compound has strong inhibitory activity on AChE, the half inhibitory concentration (IC50) of the compound reaches 5.5 nM and is more remarkable than that of a clinical first-line anti-AD drug donepezil (IC50 = 12.2 nM), and the compound can be applied to preparation of anti-AD drugs. As the AChE activity increase is a key factor of cholinergic system injury in the AD pathological process, the compound is speculated to reduce hydrolysis of acetylcholine by inhibiting the AChE activity, and further improve the learning and memory ability of model animals.

The invention discloses a forskolin derivative as well as a preparation method and application thereof, and relates to the technical field of biological medicine, the molecular formula of the forskolin derivative is C32H39N3O9, the molecular weight is 609.67600, and the specific structural formula is shown in the specification. The forskolin derivative prepared by the invention has excellent druggability and pharmacological activity, has a better neuroprotective effect, shows a stronger neuroprotective effect than donepezil and forskolin in an A beta25-35 induced PC12 cell injury model, and has lower toxicity to PC12 cells, so that the forskolin derivative can be used for preparing a neuroprotective drug. The compound can be applied to preparation of Alzheimer's disease medicines in the later period, and is of great significance to prevention and treatment of Alzheimer's disease.