- Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists
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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.
- Becknell, Nadine C.,Lyons, Jacquelyn A.,Aimone, Lisa D.,Huang, Zeqi,Gruner, John A.,Raddatz, Rita,Hudkins, Robert L.
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experimental part
p. 3880 - 3886
(2012/08/27)
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- PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
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Page/Page column 29; 47
(2009/10/30)
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- SUBSTITUTED PYRIDAZINONE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS
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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
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Page/Page column 65-66
(2009/12/27)
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- DIAMINO-PYRIDINE, PYRIMIDINE, AND PYRIDAZINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
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Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
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Page/Page column 208-209
(2010/01/07)
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- Pyridizinone derivatives
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The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.
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Page/Page column 78
(2008/06/13)
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- Pyridazine derivatives. Part 39: Reactivity of 5-iodopyridazin-3(2H)-ones in palladium-catalysed reactions
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In the search for novel antiplatelet agents, convenient and efficient methods for the preparation of 2,5-disubstituted pyridazin-3(2H)-ones are reported that utilise palladium-catalysed cross-coupling reactions. A post-coupling base-promoted isomerisation
- Coelho, Alberto,Sotelo, Eddy,Novoa, Héctor,Peeters, Oswald M.,Blaton, Norbert,Ravi?a, Enrique
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p. 12177 - 12189
(2007/10/03)
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