24 results about "Galantamin" patented technology

The invention discloses a method for extracting galanthamine from snowflake lotus. The method comprises the following steps: S1, cleaning, crushing and drying the snowflake lotus; s2, extracting the dried snow lotus by using an extraction solvent to obtain an extracting solution, and concentrating the extracting solution to obtain a crude extract; s3, adding the crude extract into an aqueous solution of alkali, stirring, layering, extracting an alkali water layer by using an extracting agent, and concentrating an extracting solution to obtain a galanthamine crude product; s4, carrying out column separation on the crude galanthamine, and then concentrating to obtain high-content galanthamine; and S5, crystallizing the high-content galanthamine to obtain the galanthamine. The method provided by the invention is simple to operate, excellent in extraction and separation effect, and high in galanthamine yield and purity.

The invention discloses a preparation method of galanthamine and an intermediate thereof, and belongs to the technical field of organic chemical synthesis. The chemical structural formulas of the intermediates for synthesis of galanthamine are as shown in formulas (I)-(IV). According to the invention, 2-cyclohexenone, acrylic ester, 3-hydroxy-2-halo-4-methoxybenzaldehyde and the like are used as starting raw materials, and the intermediate required for preparing the galanthamine is synthesized in sequence through a plurality of reactions such as Sentian-Bellies-Hilmann reaction, Corey-Barksh-Chai-field reaction, Mitsunobu reaction and the like; and then the galanthamine is synthesized by using the intermediates. The synthesis method is low in raw material and reagent price, low in production cost, short in synthesis route, easy and convenient to operate, high in yield and suitable for large-scale production, and the problems that an existing galanthamine synthesis process is complex, high in cost, low in yield and the like are solved.

Provided is use of galanthamine and a pharmaceutically acceptable salt thereof in the preparation of a drug for treating eye diseases. The present invention pertains to the technical field of pharmaceuticals. In the use of galanthamine and the pharmaceutically acceptable salt thereof in the preparation of the drug for treating eye diseases, galanthamine or an enantiomer thereof, a diastereomer thereof, a racemate thereof or the pharmaceutically acceptable salt thereof, or a solvate thereof is used to prepare the drug for treating eye diseases. The drug can make the pupils contract and ameliorate age-related eye diseases and disorders, providing a new option for preventing, treating, and / or ameliorating presbyopia, cataracts, and other age-related eye diseases.

The present invention relates to a polymer system with a nano-in-micro architecture (fucoidan micromatrix with PLGA nanoparticles incorporated therein) and finds application as a system for controlled delivery of low molecular weight water-soluble medicinal substances (e.g. galantamine hydrobromide, benzydamine hydrochloride, betahistine hydrochloride, etc.). The system includes polylactic-coglycolic acid (PLGA) nanoparticles in a fucoidan matrix, with the PLGA content being from 1% to 10% and fucoidan content being from 90% to 99% in the form of a fucoidan matrix with 100% PLGA nanoparticles incorporated therein, with the microparticles having an average diameter of 2 μm to 10 μm. The polymer system for controlled release of low molecular weight water-soluble drugs, when loaded with low molecular weight water soluble drugs such as galantamine, benzydamine, doxylamine, contains polylactic-co-glycolic acid from 1% to 10% and fucoidan from 90% to 99% in the form of a fucoidan matrix with PLGA nanoparticles incorporated therein, in the form of a fucoidan matrix with PLGA nanoparticles incorporated therein from 94% to 99% and a low molecular weight water-soluble drug from 1% to 6%, wherein the microparticles have an average diameter of 2 μm to 10 μm.

The present application relates to the technical field of medicine and chemical industry solvent recovery, specifically to a galanthamine extraction solvent recovery circulating device, comprising: a base table, a pretreatment assembly comprising pretreatment tanks, high-speed centrifuges and multi-stage filter tanks connected in series through connecting pipes, each connecting pipe is provided with an independently controlled electromagnetic valve, and each connecting pipe is provided with a pump, a feed inlet in the middle of a distillation tower is connected with a discharge outlet of the multi-stage filter tank through a feed pipe, a reboiler is arranged at the lower part of the distillation tower, a condenser is arranged on a steam exhaust pipe, a cooling liquid storage tank is arranged on the liquid outlet of the condenser through a flow guide pipe, a solvent purification unit is detachably arranged on the inner side of the upper part of the cooling liquid storage tank, and a reflux pump is connected with the upper part of the distillation tower through a reflux pipe, which can effectively treat the suspended impurities in the galanthamine extraction waste solvent, recycle and purify the ethanol solvent in the galanthamine waste solution, and improve the recovery purity of the ethanol solvent.

At least one pharmaceutical composition for use in a method of prophylaxis or treatment of COVID wherein the at least one pharmaceutical composition comprises donepezil, rivastigmine or galantamine or one of donepezil, rivastigmine or galantamine combined with one of: Artemether and Lumefantrine; Atazanavir Sulfate; Efavirenz; Fosamprenavir Calcium; Saquinavir; Remdesivir (GS-5734); Digoxin; Memantine; Rivastigmine; Galantamine; Valsartan; Teriflunomide and wherein the method of prophylaxis or treatment of COVID or COVID-19 comprises: providing a subject in need of said prophylaxis or treatment; providing the at least one pharmaceutical composition as defined supra; wherein said components are provided together or separately; wherein said components are administered together or separately; and wherein said components are provided in a pharmaceutically acceptable diluent, adjuvant and / or excipient; and administering a pharmaceutically effective amount of said at least one pharmaceutical composition to said subject; and wherein, in the method, said subject is provided prophylaxis or treatment of COVID and COVID relates to a human coronavirus, mouse hepatitis virus (MHV), or recombinant mouse-adapted SARS-CoV (SARS-CoV MAI 5).

The invention provides a galanthamine hydrolysis crude extraction method. The method comprises the following steps: drying plant raw materials, and crushing the dried plant raw materials to 20-40 meshes; pouring a solvent and the crushed plant raw materials into a hydrolysis tank according to a weight ratio of 1: (10-15); heating and refluxing the stock solution; filtering the refluxed stock solution, and separating residues from hydrolysate; adding a regulator into the hydrolysate, and filtering to form a crude product liquid; adding an extraction liquid to extract the crude product liquid to obtain a purified crude product; concentrating the purified crude product by 5 times, and performing spray drying to obtain a galanthamine crude extract. According to the scheme, the hydrolysis efficiency and the component stability are balanced by optimizing the acid concentration, the temperature and the time. Dichloromethane or ethyl acetate is adopted to improve the extraction efficiency and safety, and finally, the extraction process is monitored through an external TLC or HPLC system by recovering a solvent and reducing waste liquid discharge, so that the purpose of rapid extraction is achieved.

The invention provides application and method of geotrichum galactose yeast NBG001 in improving accumulation of alkaloids for lycoris radiata traditional Chinese medicine, and belongs to the technical field of agricultural production, the geotrichum galactose yeast NBG001 is preserved in China Center for Type Culture Collection on July 7, 2025, and the preservation number is CCTCC NO: M 20251547. By inducing the expression of signal molecules and key genes in the lycoris radiate, the simultaneous accumulation of galanthamine, lycorine and narcissus in the lycoris radiate is remarkably improved.

The present invention relates to a galantamine analog having a cholinesterase inhibitory activity, and a preparation method therefor and the use thereof. The galantamine analog has a general structural formula as shown in formula (IA), (IB) or (IC). In formula (IA), R1 is selected from hydrogen, o-fluoro, m-fluoro, p-fluoro, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorophenyl, m-fluorophenyl, p-fluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl or naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluoro, m-fluoro, p-fluoro, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy or p-methoxy. The galantamine analog of the present invention has a cholinesterase inhibitory activity superior to that of galantamine, and is expected to be used for treating diseases associated with cholinergic dysfunction.

This invention relates to a galantamine analogue with cholinesterase-inhibiting activity, its preparation method, and its application. The general structural formula is shown in formula (IA), (IB), or (IC). In formula (IA), R1 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano, or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorophenyl, m-fluorophenyl, p-fluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl, or a naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy, or p-methoxy. The galantamine analogue of this invention exhibits superior inhibitory activity against cholinesterase compared to galantamine, and holds promise for the treatment of cholinergic dysfunction-related diseases.

The present invention relates to a method for obtaining galantamine mini-tablets, to the mini-tablets obtained by said method, and to the use of these mini-tablets as a sole therapeutic agent or in combination with other active pharmaceutical agents.

The present invention relates to the compound benzene galanthamine (also referred to as alpha-1062 or galanthamine benzoate) or a salt thereof for use in the treatment of symptoms after persistent cerebral concussion. In embodiments, benzene galanthamine is for use in the treatment of persistent post-concussion symptoms from mild traumatic brain injury (mTBI). In embodiments, the symptoms include cognitive impairment. In embodiments, the compositions are administered mucosa, such as intranasal or sublingual. The present invention further relates to a method of treating a symptom after persistent cerebral concussion in a subject comprising administering a therapeutically effective amount of a pharmaceutical composition comprising bengalanthamine or a salt thereof.

The present invention discloses intermediate I and intermediate II that can be used for preparing galanthamine, and its preparation method and a kind of asymmetric total synthesis method of galanthamine and derivatives thereof as shown in structural formula (I) and formula (II) respectively, and a kind of synthetic route is short, high yield galanthamine and its derivatives. The present invention uses simple, cheap and easily available compound 2, vinylcarbamic acid tert-butyl ester and 3 hydroxy 2 iodine 4 methoxybenzaldehyde as starting raw materials, and the intermediate required for preparing galanthamine and its derivatives, i.e. the intermediate shown in formula (I) and formula (II) is synthesized in sequence by multiple reactions such as Suzuki cross-coupling reaction and Mitsunobu reaction, and then galanthamine and its derivatives are prepared using these intermediates. The synthetic route of the preparation method of galanthamine, its derivatives and intermediates provided by the present invention is short, high yield, and it is easy to realize large-scale production.

The application provides an application and method of Galactomyces geotrichum NBG001 in improving accumulation of medicinal alkaloids in Lycoris radiata, and belongs to the technical field of agricultural production. The Galactomyces geotrichum NBG001 is preserved in China Center for Type Culture Collection on July 7, 2025, and the preservation number is CCTCC NO: M 20251547. Through induction of expression of signal molecules and key genes in Lycoris radiata, simultaneous accumulation of galanthamine, lycoramine and narcissus cyclins in Lycoris radiata is significantly improved.

The invention discloses a method for synthesizing a galanthamine key intermediate by a photocatalysis micro-channel method, which comprises the following steps: S1, oxidizing an intermediate II serving as a raw material under illumination by utilizing a photocatalysis micro-channel reactor, a porphyrin compound serving as a photocatalyst and oxygen serving as an oxidant to generate an intermediate I, and performing post-treatment to obtain a crude product of the intermediate I; and S2, recrystallizing and purifying the obtained crude intermediate I to obtain a pure intermediate I product, namely the galanthamine key intermediate. According to the invention, an intermediate II is used as a raw material, under the catalysis of a photocatalyst, a photocatalytic microchannel reactor is utilized, oxygen is used as an oxidant, an intermediate I is generated through oxidation under illumination, an obtained reaction solution is post-treated to obtain a crude product of the intermediate I, and the crude product of the intermediate I is recrystallized and purified to obtain a pure product of the intermediate I. The method has a series of advantages of good process stability, excellent reaction selectivity, high yield, cheap and easily available raw materials, simple operation, high safety, environmental friendliness and the like.

The invention discloses a galanthamine intermediate compound and a synthesis method thereof. The galanthamine intermediate compound is a compound as shown in a formula (I) or a stereoisomer, a tautomer, a solvate and a pharmaceutically acceptable salt of the compound as shown in the formula (I). The galanthamine intermediate compound disclosed by the invention is simple in preparation method, can be prepared without harsh conditions, and has the advantages of low price, easiness in obtaining and the like; moreover, when the galanthamine intermediate compound is used for preparing galanthamine or galanthamine hydrobromide, the preparation process is simple, and the total yield of the prepared galanthamine or galanthamine hydrobromide is high. # imgabs0 #

The invention relates to the field of regulation and control of plant secondary metabolites, in particular to regulation and control of daffodil alkaloid galanthamine. According to the method, the optimal concentration of the yellow narcissus treated by the melatonin, the optimal harvesting period of the narcissus and the tissue with the highest galanthamine content are clearly indicated. According to the technical scheme, the problem that the galanthamine content in the yellow narcissus is too low is solved, the galanthamine content of the narcissus treated with melatonin is increased by 21.7 times compared with that of a control group, the economic benefits of plants are greatly increased, and the method has important significance for increasing the income of farmers and export for earning foreign exchange.

This invention relates to a galantamine analogue with cholinesterase-inhibiting activity, its preparation method, and its application. The general structural formula is shown in formula (IA), (IB), or (IC). In formula (IA), R1 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano, or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorine, m-fluorine, p-fluorine, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl, or a naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy, or p-methoxy. The galantamine analogue of this invention has superior inhibitory activity against cholinesterase compared to galantamine, and is expected to be used to treat cholinergic dysfunction-related diseases.

The present application belongs to the field of medicine and chemical industry, and particularly relates to a galanthamine intermediate compound. The present application obtains a new intermediate compound III through a bromination reaction with compound II as a raw material; the present application simultaneously provides a new method for synthesizing galanthamine by using the intermediate, and the new intermediate compound III is ring-closed to obtain compound IV under the action of an oxidizing agent, and then is subjected to debromination, methylation and reduction to obtain galanthamine. Compared with the prior art, the method solves the problem of poor regioselectivity in the subsequent oxidation and ring-closing step, and in the next step of the oxidation and ring-closing reaction, there is no main impurity, so that the reaction yield is higher, the post-treatment process is simplified, the cost is reduced, and the method is more suitable for industrial production.

The application relates to the field of new medical compounds, in particular to a chiral synthesis method of a key galanthamine hydrobromide impurity, epigalanthamine hydrobromide. The epigalanthamine hydrobromide is synthesized in one step by using an intermediate easy for industrial production as raw material. The synthesis method uses the intermediate in the existing industrial production process, has the advantages of simple steps, low reagent cost, high yield and high optical purity of the product, and greatly facilitates the further development of the impurity preparation of galanthamine and the drug analysis method of galanthamine.

Provided herein is an oral pharmaceutical composition that contains a cholinergic agent, a natural plant alkaloid in particular, selected from the group of lobeline, anabasine, cytisine, galantamine or acceptable salts thereof, in the form of tablets and capsules. The oral pharmaceutical composition is applicable in the treatment of dependency and addiction to nicotine, tobacco products, and alcohol.

The invention provides a method for detecting the purity of benzoyl galanthamine, which comprises the following steps: A) dissolving a benzoyl galanthamine sample to be detected by adding a solvent to obtain a test solution; dissolving a benzoyl galanthamine reference substance in a solvent to obtain a reference substance solution; b) determining the test solution and the reference solution by high performance liquid chromatography to obtain a chromatogram of the test solution and a chromatogram of the reference solution; and performing qualitative and quantitative determination on the benzoyl galanthamine in the chromatogram of the test sample according to the chromatogram of the reference substance, and calculating to obtain the purity of the benzoyl galanthamine. Chromatographic conditions of the high performance liquid chromatography are as follows: a chromatographic column is a C18 column; a mobile phase A is a phosphate methanol buffer solution, a mobile phase B is acetonitrile, and gradient elution is carried out. The method for detecting the purity of the benzoyl galanthamine through liquid chromatography is provided for the first time, and the method is high in specificity, good in operability, good in accuracy, linearity, precision and durability and capable of achieving rapid determination of the purity of the benzoyl galanthamine.

This invention discloses a method for synthesizing a key intermediate of galantamine using a photocatalytic microchannel reactor, comprising the following steps: S1: Using intermediate II as a raw material, porphyrin compounds are used as photocatalysts and oxygen as an oxidant in a photocatalytic microchannel reactor under light irradiation to generate intermediate I. The resulting reaction solution is then post-treated to obtain crude intermediate I, which is then purified by recrystallization to obtain pure intermediate I, i.e., the key intermediate of galantamine. This invention uses intermediate II as a raw material, and under photocatalysis, utilizes a photocatalytic microchannel reactor with oxygen as an oxidant to oxidize intermediate I under light irradiation. The resulting reaction solution is then post-treated to obtain crude intermediate I, which is further purified by recrystallization to obtain pure intermediate I. This method has a series of advantages, including good process stability, excellent reaction selectivity, high yield, and readily available and inexpensive raw materials, simple operation, high safety, and environmental friendliness.