- Cinnamic amides of (S)-2-(aminomethyl)pyrrolidines are potent H3 antagonists
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New imidazole-free H3 antagonists have been found in a series of cinnamic amides of (S)-(aminomethyl)pyrrolidines. The influence of the substituent on the aromatic moiety on the potency and the inhibition of three cytochrome P450 subtypes are also described.
- Peschke, Bernd,Bak, Sonja,Hohlweg, Rolf,Pettersson, Ingrid,Frolund Refsgaard, Hanne Hoffmann,Viuff, Dorthe,Rimvall, Karin
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p. 2603 - 2616
(2007/10/03)
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- Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes
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Novel amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
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