- Investigation of 4-piperidinols as novel H3 antagonists
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Compounds containing a substituted 4-piperidinol core have been found to be potent antagonists of the human H3 receptor. The compounds exhibited up to a 60-fold preference for inhibiting the human H3 receptor over the mouse and showed a low binding affinity for the hERG channel.
- Anderson, James T.,Campbell, Michael,Wang, Jianmin,Brunden, Kurt R.,Harrington, John J.,Stricker-Krongrad, Alain,Song, Jianping,Doucette, Chris,Murphy, Steven,Bennani, Youssef L.
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- 4-PIPERIDINOL TERTIARY AMINES AS HISTAMINE 3 RECEPTOR INHIBITORS FOR THE TREATMENT OF OBESITY AND OTHER CNS DISORDERS
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This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain non-imidazole tertiary amine derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.
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Page/Page column 15-16
(2008/06/13)
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- SYNTHESIS OF 4-SUBSTITUTED 1-METHYL(BENZYL)-2,5-DIMETHYL-4-R-AMINOPIPERIDINES
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Schiff base derivatives of 1-methyl(benzyl)-2,5-dimethylpiperidin-4-ones with phenyl, α-pyridyl, benzyl, and β-hydroxyethyl substituents attached to the imine nitrogen atom react with organometallic compounds to give analogously substituted piperidine bases with methyl, allyl, phenyl, and benzyl substituents in the the 4-position.Pure individual geometric isomers of these newly synthetised compound have been isolated and their structures determined.
- Kuznetsov, V. V.,Gaivoronskaya, L. A.,Romero, R. M.,Stashenko, E. E.,Zakharov, P. I.,Prostatkov, N. S.
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p. 783 - 786
(2007/10/02)
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- ASYMMETRIC SYNTHESIS AND ABSOLUTE CONFIGURATION OF 1-α-PHENYLETHYL-2,5-DIMETHYL-4-PIPERIDONE ISOMERS
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Reaction of the methyl iodide of trans-1,2-5-trimethyl-4-piperidone with S-α-phenylethylamine proceeds asymmetrically and leads in 66percent optical yield to the formation of the cis- and trans-diastereomeric pair of 1-(α-phenylethyl)-2,5-dimethyl-4-piperidone, in which the new asymmetric centers possess the 2S,5S- and 2S,5R-configurations, respectively.According to x-ray structural analysis, the minor trans-1-(α-phenylethyl)-2,5-dimethyl-4-piperidone component possesses the 2R,5S-configuration.The occurrence of asymmetric synthesis accompanying transamination was confirmed via the preparation of enantiomers of trans-2,5- and trans-1,2,5-trimethyl-4-piperidones.
- Grishina, G. V.,Potapov, V. M.,Abdulganeeva, S. A.,Gudasheva, T. A.,Karapetyan, A. A.,et al.
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p. 1327 - 1333
(2007/10/02)
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