825633-94-1Relevant articles and documents
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists
Becknell, Nadine C.,Lyons, Jacquelyn A.,Aimone, Lisa D.,Huang, Zeqi,Gruner, John A.,Raddatz, Rita,Hudkins, Robert L.
experimental part, p. 3880 - 3886 (2012/08/27)
A novel series of 4-pyridazin-3-one and 5-pyridazin-3-one analogues were designed and synthesized as H3R antagonists. Structure-activity relationship revealed the 5-pyridazin-3-ones 8a and S-methyl 8b had excellent human and rat H3R affinities, and acceptable pharmacokinetic properties. In vivo evaluation of 8a showed potent activity in the rat dipsogenia model and robust wake-promoting activity in the rat EEG/EMG model.
SUBSTITUTED PYRIDAZINONE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS
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Page/Page column 65-66, (2009/12/27)
The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII; their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof
Pyridizinone derivatives
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Page/Page column 78, (2008/06/13)
The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.