38 results about "Dihydrotetrabenazine" patented technology

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.

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.

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.

This invention relates to the use of low doses of (+)-α-dihydrotetrabenazine for the treatment of movement disorders, such as Tourette's syndrome.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

This invention relates to pharmaceutical compositions containing (−)-β-dihydrotetrabenazine, processes for making them and their therapeutic uses.

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.

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.

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.