1005402-20-9Relevant 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.
, 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
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
, 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
Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity
Hudkins, Robert L.,Aimone, Lisa D.,Bailey, Thomas R.,Bendesky, Robert J.,Dandu, Reddeppa Reddy,Dunn, Derek,Gruner, John A.,Josef, Kurt A.,Lin, Yin-Guo,Lyons, Jacquelyn,Marcy, Val R.,Mathiasen, Joanne R.,Sundar, Babu G.,Tao, Ming,Zulli, Allison L.,Raddatz, Rita,Bacon, Edward R.
, p. 5493 - 5497 (2011/10/12)
H3R structure-activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules wi
Amine-constrained pyridazinone histamine H3 receptor antagonists
Sundar, Babu G.,Bailey, Thomas,Bacon, Edward,Aimone, Lisa,Huang, Zeqi,Lyons, Jacquelyn,Raddatz, Rita,Hudkins, Robert
, 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.
Pyridizinone derivatives
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Page/Page column 37, (2008/06/13)
The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.
