33347-88-5Relevant academic research and scientific papers
4-Phenoxypiperidine pyridazin-3-one histamine H3 receptor inverse agonists demonstrating potent and robust wake promoting activity
Hudkins, Robert L.,Zulli, Allison L.,Dandu, Reddeppa Reddy,Tao, Ming,Josef, Kurt A.,Aimone, Lisa D.,Haltiwanger, R. Curtis,Huang, Zeqi,Lyons, Jacquelyn A.,Mathiasen, Joanne R.,Raddatz, Rita,Gruner, John A.
scheme or table, p. 1504 - 1509 (2012/04/04)
Structure-activity relationships for a series of phenoxypiperidine pyridazin-3-one H3R antagonists/ inverse agonists are disclosed. The search for compounds with improved hERG and DAT selectivity without the formation of in vivo active metaboli
Iodine-mediated facile dehydrogenation of dihydropyridazin-3(2H)one
Humne, Vivek T.,Konda, Shankaraiah G.,Hasanzadeh, Kamal,Lokhande, Pradeep D.
, p. 1435 - 1438 (2012/06/01)
A new protocol for the dehydrogenation of dihydropyridazin-3(2H)-one has been carried out by catalytic amount of iodine in dimethyl sulphoxide in good yield with easy workup.
Amine-constrained pyridazinone histamine H3 receptor antagonists
Sundar, Babu G.,Bailey, Thomas,Bacon, Edward,Aimone, Lisa,Huang, Zeqi,Lyons, Jacquelyn,Raddatz, Rita,Hudkins, Robert
scheme or table, p. 5543 - 5546 (2011/10/12)
Pyridazinone 1 was recently reported as a potent H3R antagonist with good drug-like properties and in vivo activity. A series of constrained amine analogs of 1 was synthesized to identify compounds with improved pharmacokinetic profiles. From these efforts, a new class of (S)-2-pyrrolidin-1-ylmethyl-1-pyrrolidinyl amides was identified.
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl) propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): A potent, selective histamine H3 receptor inverse agonist
Hudkins, Robert L.,Raddatz, Rita,Tao, Ming,Mathiasen, Joanne R.,Aimone, Lisa D.,Becknell, Nadine C.,Prouty, Catherine P.,Knutsen, Lars J. S.,Yazdanian, Mehran,Moachon, Gilbert,Ator, Mark A.,Mallamo, John P.,Marino, Michael J.,Bacon, Edward R.,Williams, Michael
experimental part, p. 4781 - 4792 (2011/09/21)
Optimization of a novel series of pyridazin-3-one histamine H3 receptor (H3R) antagonists/inverse agonists identified 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (8a, CEP-26401; irdabisant) as a lead candid
Pyridizinone derivatives
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Page/Page column 36, (2008/06/13)
The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.
