397275-42-2Relevant academic research and scientific papers
4-Phenoxypiperidines: Potent, conformationally restricted, non-imidazole histamine H3 antagonists
Dvorak, Curt A.,Apodaca, Richard,Barbier, Ann J.,Berridge, Craig W.,Wilson, Sandy J.,Boggs, Jamin D.,Xiao, Wei,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 2229 - 2238 (2005)
Two new series of 4-(1-alkyl-piperidin-4-yloxy)-benzonitriles and 4-(1-isopropyl-piperidin-4-yloxy)-benzylamines have been prepared. In vitro activity was determined at the recombinant human H3 receptor and several members of these new series were found to be potent H3 antagonists. The present compounds contain a 4-phenoxypiperidine core, which behaves as a conformationally restricted version of the 3-amino-1-propanol moiety common to the many previously described non-imidazole histamine H 3 ligands. One selected member of the new series, 4-[4-(1-isopropyl-piperidin-4-yloxy)-benzyl]-morpholine (13g), was found to be a potent, highly selective H3 receptor antagonist with in vivo efficacy in a rat EEG model of wakefulness at doses as low as 1 mg/kg sc.
NPY ANTAGONISTS, PREPARATION AND USES
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Page/Page column 57, (2009/09/28)
The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
ARYLOXYALKYLAMINE DERIVATES AS H3 RECEPTOR LIGANDS
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Page 27, (2010/02/06)
The present invention relates to novel benzyloxy derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
