- Sustained-release composition containing tetrahydropyrido[4,3-b]indole derivatives and preparation of the derivatives
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The present invention relates to a sustained-release composition containing 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof as an active ingredient, preparation thereof and the compound. The composition is suitable for oral administration by one time per day, and achieves the peak plasma concentration at 1.0 to 3 hours after oral administration. The composition is suitable for manufacturing a medicament for treatment of cognitive dysfunction syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, or senile dementia.
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- SUSTAINED RELEASE COMPOSITION CONTAINING TETRAHYDROPYRIDO Y4, 3-b¨INDOLE DERIVATIVE AND PREPARATION METHOD OF DERIVATIVE
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The present invention relates to a sustained-release composition containing 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof as an active ingredient, preparation thereof and the compound. The composition is suitable for oral administration by one time per day, and achieves the peak plasma concentration at 1.0 to 3 hours after oral administration. The composition is suitable for manufacturing a medicament for treatment of cognitive dysfunction syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, or senile dementia.
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Page/Page column 7-8; 16
(2012/03/08)
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- [11C]Dimebon, radiosynthesis and lipophilicity of a new potential PET agent for imaging of Alzheimer's disease and Huntington's disease
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[11C]Dimebon (2-[11C]methyl-8-methyl-5-(2-(6-methylpyridin-3-yl)ethyl)-2,3 ,4,5-tetrahydro-1H-pyrido[4,3-b]indole), a new potential PET agent for imaging of Alzheimer's disease and Huntington's disease, was prepared by N-[11C]methylation of desmethyl-Domebon precursor with [11C]CH3OTf and purified with a semi-preparative HPLC method in 30-40% decay corrected radiochemical yield and 222-296 GBq/μmol specific activity at EOB. The measured lipophilicity coefficient (Log P) value of [11C]Dimebon was 2.53.
- Gao, Mingzhang,Wang, Min,Hutchins, Gary D.,Zheng, Qi-Huang
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experimental part
p. 2529 - 2532
(2010/07/10)
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- SYNTHESIS OF 9-(ARYLALKYL)-1,2,3,4-TETRAHYDRO-Υ-CARBOLINE AND ANALOGUES AND INTERMEDIATES
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The present invention pertains generally to methods of preparing certain 9-(arylalkyl)- 1,2,3,4-tetrahydro-Υ-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds.
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Page/Page column 66-67
(2010/07/02)
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- METHODS FOR PREPARING PYRIDYLETHYL-SUBSTITUTED CARBOLINES
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Methods of preparing pyridylethyl-substituted carbolines under reaction conditions that use fewer molar equivalents of MVP to produce the pyridylethyl-substituted carboline as compared to reported methods of preparing pyridylethyl-substituted carbolines using MVP are provided. Also provided are methods of preparing a pyridylethyl-substituted carboline using non-commercial MVP.
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- PYRIDO [3, 4-B] INDOLES AND METHODS OF USE
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This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
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Page/Page column 235-236
(2009/10/22)
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