55 results about "Quinidine" patented technology

Pharmaceutical compositions and methods for treating depression, anxiety, and neurodegenerative diseases and cognitive disorders, such as dementia and Alzheimer's disease, by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.

Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.

During clinical trials on patients suffering from neurological disorders, it has been observed that some patients obtain dramatic improvements in motor control and/or higher mental functioning, when they receive a combination of dextromethorphan and quinidine, at suitable dosages. Improved motor control has been exemplified to date by improved ability to swallow and/or speak, among victims of stroke, head injury, or ALS. Improved higher mental functioning has been exemplified better job performance, increased ability to analyze and solve problems, and increased ability to have successful and satisfying interactions with other people. These types of effects can be seen in a relatively brief time period, such as within several days to a week.

The invention discloses a preparation method of an alpha-hydroxy-beta-dicarbonyl compound using a cinchona alkaloid derivative as a catalyst. In the condition that the cinchona alkaloid derivative is used as the catalyst, a compound is caused to be in contact with oxidants including oxygen, hydrogen peroxide, and alkyl hydroperoxide; the compound and the oxidant in contact are mixed and stirred in an inert solvent for reaction; after the reaction is ended, the alpha-hydroxy-beta-dicarbonyl compound is obtained by separation, wherein the inert solvent comprises halogenated hydrocarbon, aromatic hydrocarbon, alkane and the like; the dosage molar ratio of the peroxide, which is used as the oxidant, to a beta-dicarbonyl compound is 1-30; the dosage of the catalyst III is 0.5-50mol%; the reaction temperature is minus 78 to 50 DEG C. According to the novel preparation method of the alpha-hydroxy-beta-dicarbonyl compound using the cinchona alkaloid derivative as the catalyst disclosed by the invention, cinchona alkaloid quinine and cinchona alkaloid quinindium, which are main alkaloids in the bark of cinchona and congener, are widely applied to organic unsymmetrical catalytic reaction.

The invention discloses a cinchona alkaloids compound with a new macrocyclic structure, and a preparation method thereof. The cinchona alkaloids compound is prepared with cinchona alkaloids quinidine as a substrate. According to the preparation method, quinidine is subjected to a halogen cyclization reaction, such that the new macrocyclic structure is obtained. Related derivatives can be obtained through the changes on the C11-locus. The cinchona alkaloids compound provided by the invention can be used as a novel chiral catalyst or a ligand. The preparation method is simple, and yield is high.

One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the invention relates to a method of preparing a derivatized quinine-based or quinidine-based catalyst comprising 1) reacting quinine or quinidine with base and a compound that has a suitable leaving group, and 2) converting the ring methoxy group to a hydroxy group. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone, comprising the step of: reacting a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone with a nucleophile in the presence of a catalyst; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized quinine or quinidine. Another aspect of the present invention relates to a method of kinetic resolution, comprising the step of: reacting racemic chiral alkene with a nucleophile in the presence of a derivatized quinine or quinidine.

A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

The present invention provides gero-protective pharmaceutical compositions and methods, the compositions being adapted to enhance at least one of cell survival and cell metabolism in a mammalian subject, the pharmaceutical compositions include at least two of Withaferin a or its structural analogs, coumestrol, ginsenoside, quinidine, silymarin, licochalcone a, lipoic acid and apigenin, in a pharmaceutically effective amount.

The invention discloses a method for synthesizing a gamma-aminobutyric acid chiral compound. The method comprises the following steps of: adding nitroolefin and malonate to a solvent in the presence of a catalyst A and an additive; carrying out conjugate addition reaction on nitroolefin and malonate to selectively obtain a compound V; carrying out hydrogenation reduction reaction on the compound V under the action of a catalyst B and hydrogen, decarboxylation and amidation to obtain a compound II; carrying out acidolysis on the compound II to obtain a compound I. According to the method, a gamma-aminobutyric acid chiral drug prepared by taking a low-cost easily-prepared quinidine derivative as a catalyst and alkali as an additive is high in yield and high in enantioselectivity. The method disclosed by the invention is moderate in reaction condition and easy to operate and is a green synthesis process for synthesizing gamma-aminobutyric acid chiral drugs.

The invention belongs to the technical field of organic chemistry, and specifically relates to a synthetic method for 2-hydroxyl-1-indanone compounds. The method uses an indanone compound as a raw material, a peroxide as an oxidant and a quinidine or a quinine derivative as a catalyst, in the presence of a solvent, the indanone compound and the peroxide are subjected to an asymmetric hydroxylation, and therefore the 2-hydroxyl-1-indanone compounds with stereoselectivity are obtained. Compared with a previous method, the method provided by the invention has the advantages that the catalyst canbe quantitatively recovered, the reaction conditions are mild, the costs are low, the yield is high, and the stereoselectivity is strong, and is suitable for industrialized production.

The invention discloses a method for preparing quinindium and cinchonine. The method comprises the following steps: separating out quinine from a total alkaloid of Peruvian bark through a sulfate precipitation method so as to obtain a filtrate containing other alkaloids; basifying the filtrate until the pH value is not less than 10, collecting the obtained precipitate and drying the precipitate so as to obtain a raw material A; dissolving the raw material A with an organic solvent, filtering, separating an indissoluble substance from the filtrate; dissolving the indissoluble substance with a proper amount of alcohol solvent, adding activated carbon for decoloring, and then carrying out filtration and crystallization so as to obtain the cinchonine; and concentrating the filtrate until the volume of filtrate is 1/5-1/10 of the original volume, standing until a solid is separated out, dissolving the solid with a proper amount of alcohol solvent, adding the activated carbon for decoloring, and then carrying out filtration and crystallization so as to obtain the quinindium. The method is economical, simple and convenient and is in favor of amplification production; and the yield is high.

Pharmaceutical compositions and methods for treating neurological disorders by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine. This invention also provides methods of reducing CNS and gastrointestinal side effects associated with a long term, dextromethorphan/low-dose quinidine combination therapy.

The invention discloses a method for preparing serial cinchona alkaloid with effects of malaria resistance, arrhythmia resistance and the like by adopting cinchona bark as a raw material. The method utilizes advanced ultrasonic cell disruption and extraction, simple extraction separation and high-purity column purification process to generate quinine sulfate, quinidine, cinchonidine and cinchonine, of which the purities are all higher than 99.5%. Compared with the traditional method, the method has higher extraction recovery and environment-friendly and low-carbon process flow, and is better applicable to industrial mass production of active ingredients at the grade of GMP (Good Manufacturing Practice and food additives).

The invention discloses a method of the solvent-free synthesis of cinchona alkaloid derivatives by adopting microwave radiation with the catalysis of a phase transfer catalyst. According to the method of the invention, 1, 4-dichloro-2, 3-naphthyridine, 3, 6-dichloropyridazine, 4, 6-dichloropyrimidines, 2, 5-diphenyl-4, 6-dichloropyrimidines or phthalic acid can react with quinine, hydroquinine, quinidine, dihydro quinidine, cinchonine or cinchonidine according to a mol ratio of 1:3 to 3:1 to obtain the cinchona alkaloid derivatives. Under the action of microwave, the synthetic process of the cinchona alkaloid derivatives can become simple and safe in operation, short in reaction time, and mild in reaction condition; more particularly, toxic organic solvents such as methylbenzene and DMF with a high boiling point, etc. are not adopted in the course of the reaction, thus being in line with the megatrend of green chemistry, furthermore, monosubstituted products and disubstituted products can be obtained with high yield by the control of reaction time and power.

Process for the formation of MeO-Peg-protected dihydroquinine or dihydro quinindine derivatives, new dihydroquinine-or dihyroquinidine derivatives as well as the use thereof. It is known that dihydroquinine or dihydroquinidine derivatives can be successfully used as ligands in the enantioselective dihydroxylation. The new disclosed ligand systems based on dihydroquinine/quinidine, unlike the prior art ligands, can be recycled after enantioselective dihydroxylation by precipitating and filtering the reaction medium, and be reused in the reaction medium. Also disclosed are the ligand systems (I) and (IV), process for preparing the same and their use in the enantioselective dihydroxiation of double bonds.

The present invention discloses a class of chiral alpha-amino phosphonate ester compounds having anti-virus activity and containing benzothiazole heterocycle, preparation and applications thereof, wherein the structure of the compound is represented by the following general formula (I). According to the present invention, thiourea or thiourea quinidine is adopted as a chiral catalyst, a 4A molecular sieve is adopted as a cocatalyst, and dichloromethane is adopted as solvent to rapidly synthesize the high yield and high optical activity chiral alpha-amino phosphonate ester compound containing benzothiazole heterocycle at a room temperature; and especially treatment, protection and activity passivation of the compound R-4h on cucumber mosaic virus are superior to the commercial agent ningnanmycin, treatment, protection and activity passivation of the compound R-4q on tobacco mosaic virus are superior to the commercial agent ningnanmycin, and the compounds R-4h and R-4q provide good inhibition effects on tobacco mosaic virus (TMV), cucumber mosaic virus (CMV), Southern rice black-streaked dwarf virus (SRBSDV) and the like, have good universality, and can be used for anti-plant virus chiral pesticide preparation. The formula (1) is defined in the specification.

The invention discloses the use of CaH2 in synthesizing cinchona alkaloid ligand, wherein the ligand has a structure disclosed in the specification. CaH2 can be used as the acid binder in synthesizing cinchona alkaloid ligand. monosubstituted product or disubstituted product including hydroquinine, Quinidine, Dihydroquinidine and their derivatives.

This invention relates to quinidine derivatives and immunogenic conjugates and reporter conjugates prepared therefrom. The immunogenic conjugates and reporter conjugates are useful for eliciting antibodies and for performing immunoassays for quinidine. A particle agglutination immunoassay for quinidine is also provided.