957133-21-0Relevant academic research and scientific papers
The discovery of pyridone and pyridazone heterocycles as γ-secretase modulators
Huang, Xianhai,Aslanian, Robert,Zhou, Wei,Zhu, Xiaohong,Qin, Jun,Greenlee, William,Zhu, Zhaoning,Zhang, Lili,Hyde, Lynn,Chu, Inhou,Cohen-Williams, Mary,Palani, Anandan
scheme or table, p. 184 - 187 (2010/10/21)
A series of novel pyridazone and pyridone compounds as γ-secretase modulators were discovered. Starting from the initial lead, structure?activity relationship studies were carried out in which an internal hydrogen bond was introduced to conformationally fix the side chain, and compounds with improved in vitro Aβ42 inhibition activity and good Aβtotal/Aβ42 selectivity were quickly discovered. Compound 35 displayed very good in vitro activity and excellent selectivity with good in vivo efficacy in both CRND8 mouse and nontransgenic rat models. This compound displayed a good overall profile in terms of rat pharmacokinetics and ancillary profile. No abnormal behavior and side effects were observed in all of the studies.
GAMMA SECRETASE MODULATORS
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Page/Page column 409; 417-418, (2009/04/25)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formul
Synthesis of regiospecifically polysubstituted pyridazinones
de Araújo-Júnior, Jo?o X.,Schmitt, Martine,Antheaume, Cyril,Bourguignon, Jean-Jacques
, p. 7817 - 7820 (2008/03/11)
Desymmetrization of pyridazine-3,6-diones by the use of N-benzyl protective groups leads to useful starting materials for building polysubstituted pyridazine libraries in a regioselective manner.
