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44 results about "Dihydrotetrabenazine" patented technology
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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
Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents
ActiveUS20080050312A1Nervous disorderIn-vivo radioactive preparationsDihydrotetrabenazineImaging agent
This invention relates to a method of imaging vesicular monoamine transporters and to labeled compounds and pharmaceutical compositions thereof, and methods of making labeled compounds useful in imaging vesicular monoamine transporters. This invention also relates to compounds, and methods of monitoring progression of a disease related to vesicular monoamine transporters.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA +2
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
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:BIOVAIL LAB INT BARBADOS
Pharmaceutical compositions
This invention relates to the use of low doses of (+)-α-dihydrotetrabenazine for the treatment of movement disorders, such as Tourette's syndrome.
Owner:ADEPTIO PHARMA
3,11 b-cis-Dihydrotetrabenazine for the Treatment of a Proliferative Disease or an Inflammatory Disease
InactiveUS20090275605A1Inhibiting and preventing proliferationAvoid separationBiocideAntipyreticDiseaseDihydrotetrabenazine
The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a proliferative disease or an inflammatory disease, the compound being 3,11b-cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof.
Owner:VALEANT INT BARBADOS
Preparation method of (2r,3r,11br)-dihydrotetrabenazine and related compounds
ActiveCN102285984AHigh stereoselectivityHigh yieldAsymmetric synthesesDihydrotetrabenazineSelective reduction
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
ActiveCN101985446AThe steps are well designedSimple and fast operationOrganic chemistryDiethyl etherMethyl group
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
Pharmaceutical compositions
This invention relates to pharmaceutical compositions containing (+)-β-dihydrotetrabenazine and their therapeutic uses, in particular in their use in the treatment of movement disorders, such as Tourette's syndrome.
Owner:ADEPTIO PHARMA
Pharmaceutical compositions
InactiveUS20190111035A1Reduce biological side-effectsEasy to operateNervous disorderAmine active ingredientsDihydrotetrabenazineS syndrome
This invention relates to the use of low doses of (+)-α-dihydrotetrabenazine for the treatment of movement disorders, such as Tourette's syndrome.
Owner:ADEPTIO PHARMA
3 , llb-cis-dihydrotetrabenazine for the treatment of a proliferative disease or an inflammation
The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a proliferative disease or an inflammatory disease, the compound being 3,1lb-cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof.
Owner:BIOVAIL LAB INT BARBADOS
Pharmaceutical compositions
This invention relates to the use of combinations of stereoisomers of dihydrotetrabenazine for the treatment of movement disorders, such as Tourette's syndrome.
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
Synthesis method of 9-demethyl-(+)-alpha-dihydrotetrabenazine
ActiveCN105732613AConducive to large-scale industrial productionReduce manufacturing costOrganic chemistryAlcoholSynthesis methods
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
ActiveUS20180280375A1Organic active ingredientsNervous disorderDihydrotetrabenazineNK1 receptor antagonist
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
ActiveUS20200246324A1Organic active ingredientsNervous disorderDihydrotetrabenazinePharmaceutical drug
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
ActiveUS11306082B2Good physical and chemical stabilityAcceptable ester hydrolysis rateOrganic active ingredientsNervous disorderCarbamateCarbonate ester
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
ActiveUS8993766B2Simple and short processOrganic active ingredientsSilicon organic compoundsAlkyl transferTrimethylsilyl
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
Method for synthesizing (+/-)-9-O-demethyl-alpha-dihydrotetrabenazine
ActiveCN101985446BThe steps are well designedSimple and fast operationOrganic chemistryDiethyl etherMethyl group
Owner:JIANGSU INST OF NUCLEAR MEDICINE
Combination dosage forms and administration thereof
This disclosure relates to methods of administering bupropion, such as S-bupropion or R-bupropion, in conjunction with tetrabenazine, alpha-dihydrotetrabenazine, or beta-dihydrotetrabenazine to a human being. Dosage forms, drug delivery systems, and methods related to tetrabenazine, alpha-dihydrotetrabenazine, or beta-dihydrotetrabenazine and bupropion, such as S-bupropion or R-bupropion, are also disclosed.
Owner:AXSOME THERAPEUTICS INC
Esters of dihydrotetrabenazine
ActiveUS20200270241A1Improve securityLow water solubilityOrganic active ingredientsNervous disorderCarbamateCarbonate ester
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
Dihydrotetrabenazine for the treatment of anxiety and psychoses
This invention relates to pharmaceutical compositions containing (−)-β-dihydrotetrabenazine, processes for making them and their therapeutic uses.
Owner:ADEPTIO PHARMA
Crystalline dihydrotetrabenazine and the method thereof
PCT designated stageWO2025264950A1Isotope introduction to organic compoundsHeterocyclic compound active ingredientsCrystallographyMedicine
Described herein are crystalline dihydrotetrabenazine, methods for obtaining such crystalline forms, pharmaceutical compositions comprising the crystalline dihydrotetrabenazine, as well as methods of using the crystalline dihydrotetrabenazine in the treatment of hyperkinetic disorders.
Owner:FORESEE PHARMA CO LTD +1
Preparation method of alpha-type 2-amino-dihydrotetrabenazine
PendingCN120987939AIsotope introduction to heterocyclic compoundsRadioactive preparation carriersEthylic acidSilica gel
The invention provides a preparation method of alpha-type 2-amino-dihydrotetrabenazine, which comprises the following steps: 1) reacting raw materials containing tetrabenazine, ammonium acetate and sodium cyanoborohydride, and post-treating a reaction mixed solution to obtain a crude product; (2) carrying out column chromatography on the crude product in the step (1), and separating to obtain alpha-type 2-amino-dihydrotetrabenazine; a stationary phase used by the column chromatography is silica gel; the diameter-height ratio of the stationary phase is 1: (6-8), a mixed solution of dichloromethane and methanol is adopted as an elution system, and the volume ratio of dichloromethane to methanol is (9-11): 1; the elution flow rate is 4 to 6 mL / min. Radioactive labeling of the alpha-type 2-amino-dihydrotetrabenazine is realized through a fluorine [< 18 > F] labeling technology, a key technical support is provided for development of a novel positron emission tomography (PET) specific tracing probe based on a molecular skeleton, and an important technical foundation is laid for development of a novel VMAT2 targeted tracing probe based on a compound skeleton.
Owner:JIANGSU INST OF NUCLEAR MEDICINE
Pharmaceutical compositions
PendingCN110691596AOrganic active ingredientsNervous disorderDihydrotetrabenazinePharmaceutical drug
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
InactiveCN101932323AOrganic active ingredientsSenses disorderDihydrotetrabenazinePharmaceutical medicine
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:BIOVAIL LAB INT BARBADOS