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39 results about "Dihydrotetrabenazine" patented technology

Dihydrotetrabenazine or DTBZ is an organic compound with the chemical formula C₁₉H₂₉NO₃. It is a close analog of tetrabenazine. DTBZ and its derivatives, when labeled with positron emitting isotopes such as carbon-11 and fluorine-18, are used as PET radioligands for examining VMAT2.

Dihydrotetrabenazines And Pharmaceutical Compositions Containing Them

The invention provides novel isomers of dihydrotetrabenazine, individual enantiomers and mixtures thereof wherein the dihydrotetrabenazine is a 3,11 b-cis-dihydrotetrabenazine. Also provided are methods for the preparation of the novel isomers, pharmaceutical compositions containing them and their use in treating hyperkinetic movement disorders such as Huntington's disease, hemiballismus, senile chorea, tic, tardive dyskinesia and Tourette's syndrome.
Owner:VALEANT INT BARBADOS

Methods and compositions for modulating insulin secretion and glucose metabolism

InactiveUS20100204258A1Treating and ameliorating effectTreating and preventing hyperglycemiaBiocideHydroxy compound active ingredientsAcute hyperglycaemiaMetabolite
The present invention relates to methods and compositions for treating or ameliorating the effects of diabetes. In addition, the present invention relates to methods and compositions for treating or preventing hyperglycemia, as well as modulating monoamine levels, islet β-cell insulin secretion, insulin and / or glucagon levels in a patient. In certain preferred embodiments, such methods include administering to a patient an effective amount of a vesicular monoamine transporter type 2 (VMAT2) antagonist, such as tetrabenazine (TBZ), dihydrotetrabenazine (DTBZ), tetrahydroberberine (THB), reserpine, emetine, Compound 6, or enantiomers, optical isomers, diastereomers, N-oxides, crystalline forms, hydrates, metabolites or pharmaceutically acceptable salts thereof.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK

Preparation method of (2r,3r,11br)-dihydrotetrabenazine and related compounds

The invention relates to a preparation method of (2R, 3R, 11bR)-dihydrotetrabenazine (formula I), (2S, 3S, 11bS)-dihydrotetrabenazine (formula II) and (+_)-alpha-dihydrotetrabenazine. The preparation method comprises the following steps of: adopting borane or various borane complexes, carrying out three-dimensional selective reduction on (3R, 11bR)-tetrabenazine under low temperature, and obtaining the (2R, 3R, 11bR)-dihydrotetrabenazine; and adopting the same method to carry out reduction on the (3R, 11bS)-tetrabenazine and tetrabenazine racemic modification, and respectively preparing the (2S, 3S, 11bS)-dihydrotetrabenazine and the (+_)-alpha-dihydrotetrabenazine. In the preparation method, the three-dimensional selection and the chemical yield of the reduction reaction are greatly improved, so that the very fussy column chromatography purification is avoided, so that the preparation method can be applicable to industrial production.
Owner:JIANGSU VCARE PHARMATECH

Pharmaceutical compounds

This application describes method of treating dementia and cognitive deficits associated with dementia that involve administration of dihydrotetrabenazine, and isomers and / or pharmaceutically acceptable salts thereof.
Owner:VALEANT INT BARBADOS

Pharmaceutical compounds

This application describes methods of treatment and / or prophylaxis of asthma that involve administration of dihydrotetrabenazine, and isomers and / or pharmaceutically acceptable salts thereof.
Owner:VALEANT INT BARBADOS

Pharmaceutical compounds

This application describes method of treating dementia and cognitive deficits associated with dementia that involve administration of dihydrotetrabenazine, and isomers and / or pharmaceutically acceptable salts thereof.
Owner:VALEANT INT BARBADOS

Method for synthesizing (+/-)-9-O-demethyl-alpha-dihydrotetrabenazine

The invention discloses a method for synthesizing (+ / -)-9-O-demethyl-alpha-dihydrotetrabenazine, which comprises the following steps of: adding sodium hydride and hexamethylphosphoramide into dimethylbenzene, heating to the temperature of between 90 and 100 DEG C, dripping N-methylaniline, and stirring for 15 to 20 minutes; dripping dimethylbenzene suspension of (+ / -)-alpha-dihydrotetrabenazine into the mixed solution, after dripping, continuously stirring the reaction suspension at the temperature of between 90 and 100 DEG C for 48 to 50 hours; slowly adding aqueous solution of sodium hydroxide into the reaction suspension, separating out an aqueous phase, neutralizing the aqueous phase by using aqueous solution of hydrochloric acid until the pH value is 7 to 9, extracting by using diethyl ether, concentrating an organic phase under reduced pressure to obtain a light brown solid; and purifying the light brown solid by using column chromatography technology to obtain the target product. By optimizing the reaction conditions of the prior art and improving posttreatment and purification technology, the method has the advantages of low preparation cost, high repeatability and high yield.
Owner:JIANGSU INST OF NUCLEAR MEDICINE

Dihydrotetrabenanzine for the treatment of anxiety

InactiveUS20110190333A1Prevention and alleviation and reductionShortness of breathBiocideNervous disorderClinical psychologyDihydrotetrabenazine
The invention provides a 3,11b-cis-dihydrotetrabenazine of the formula (Ib): or a pharmaceutically acceptable salt thereof for use in the prophylaxis or treatment of anxiety.
Owner:VALEANT INT BARBADOS

Synthesis method of 9-demethyl-(+)-alpha-dihydrotetrabenazine

The invention relates to a synthesis method of 9-demethyl-(+)-alpha-dihydrotetrabenazine. The synthesis method comprises the following steps: 9-benzyloxy-(+)-alpha-dihydrotetrabenazine serves as a raw material and experiences reactions for at least 10min in a polar protonic solvent at room temperature under the catalysis of hydrobromic acid to obtain the reaction liquid of a crude product of 9-demethyl-(+)-alpha-dihydrotetrabenazine, wherein the polar protonic solvent is at least one of C1-C10 monohydric alcohols. The synthesis method has the advantages of relatively low preparation cost, relatively mild reaction conditions, relatively short reaction time, relatively simple reaction operation and relatively high reaction yield, facilitates the large-scale industrial production of 9-demethyl-(+)-alpha-dihydrotetrabenazine and lays a foundation for the large-scale industrial production of a development drug 11C-(+)-alpha-DTBZ and a development drug 18F-FP-(+)-alpha-DTBZ.
Owner:JIANGSU INST OF NUCLEAR MEDICINE

Pharmaceutical compositions

The invention provides (+)-α-dihydrotetrabenazine succinate salt.Also provided are (+)-α-dihydrotetrabenazine succinate salt for use in medicine, pharmaceutical compositions comprising (+)-α-dihydrotetrabenazine succinate salt and a pharmaceutically acceptable excipient and the uses of (+)-α-dihydrotetrabenazine succinate salt as a VMAT2 receptor antagonist and in the treatment of a movement disorder such as Tourette's syndrome.The invention further provides a method for preparing the (+)-α-dihydrotetrabenazine succinate salt.
Owner:ADEPTIO PHARMA

Pharmaceutical compositions

The invention provides (+)-α-dihydrotetrabenazine succinate salt.Also provided are (+)-α-dihydrotetrabenazine succinate salt for use in medicine, pharmaceutical compositions comprising (+)-α-dihydrotetrabenazine succinate salt and a pharmaceutically acceptable excipient and the uses of (+)-α-dihydrotetrabenazine succinate salt as a VMAT2 receptor antagonist and in the treatment of a movement disorder such as Tourette's syndrome.The invention further provides a method for preparing the (+)-α-dihydrotetrabenazine succinate salt.
Owner:ADEPTIO PHARMA

Esters of dihydrotetrabenazine

The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof.wherein R1 is —C(═O)O-alkyl, carbonate ester, or —C(═O)-alkyl, ester, or —C(═O)N-alkyl, carbamate ester and wherein R2 is —CH3 or —CD3. The alkyl ester can contain saturated or unsaturated C12 to C26 alkyl carbon. The alkyl carbon chain can have either a straight, branched, noncyclic, cyclic, unsubstituted or substituted structure.
Owner:FORESEE PHARMA CO LTD

Method of preparing tetrabenazine and dihydrotetrabenazine

The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.
Owner:KOREA INST OF SCI & TECH

Esters of dihydrotetrabenazine

The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof.wherein R1 is —C(═O)O-alkyl, carbonate ester, or —C(═O)-alkyl, ester, or —C(═O)N-alkyl, carbamate ester and wherein R2 is —CH3 or —CD3. The alkyl ester can contain saturated or unsaturated C12 to C26 alkyl carbon. The alkyl carbon chain can have either a straight, branched, noncyclic, cyclic, unsubstituted or substituted structure.
Owner:FORESEE PHARMA CO LTD

Pharmaceutical compositions

This invention relates to the use of (+)-beta-dihydrotetrabenazine and combinations of (+)-alpha-dihydrotetrabenazine, (-)-alpha-dihydrotetrabenazine and / or (+)-beta-dihydrotetrabenazine, for the treatment of movement disorders, such as Tourette's syndrome. The invention also provides dosage forms containing said dihydrotetrabenazine isomers.
Owner:ADEPTIO PHARMA

Use of 3, 11b-cis-dihydrotetrabenazine in the treatment of multiple sclerosis and autoimmune myelitis

InactiveUS20110039877A1Avoids chromatographic separationAvoid separationBiocideSenses disorderMyelitisDihydrotetrabenazine
The invention provides a compound for use in treating multiple sclerosis wherein the compound is a 3, 11b-cis-dihydrotetrabenazine of the formula (Ia): or a pharmaceutically acceptable salt thereof.
Owner:VALEANT INT BARBADOS

Separation and determination method for 9-demethylation-alpha-dihydrotetrabenazine and impurities thereof

The invention belongs to the field of pharmaceutical analysis and in particular relates to a separation and determination method for 9-demethylation-alpha-dihydrotetrabenazine and impurities thereof. The separation and determination method provided by the invention has the advantages that complete separation of 9-DM-alpha-DTBZ and impurities thereof, namely alpha-DTBZ and N-methyl phenylamine, can be realized, contents of the 9-DM-alpha-DTBZ and the impurities thereof, namely alpha-DTBZ and N-methyl phenylamine, can be determined at the same time, and a simple, quick and sensitive detection method is provided for determination of content of 9-demethylation-alpha-dihydrotetrabenazine in 9-demethylation-alpha-dihydrotetrabenazine raw materials and the determination of the content of related substances, so that quality control on the 9-DM-alpha-DTBZ raw materials can be realized, and further the purity and labeling efficiency of a PET imaging drug 11C-alpha-DTBZ are guaranteed, and effective and safe application of the PET imaging drug 11C-alpha-DTBZ are facilitated.
Owner:JIANGSU INST OF NUCLEAR MEDICINE
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