1433663-33-2Relevant academic research and scientific papers
Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators
Zhao, Zhiqiang,Pissarnitski, Dmitri A.,Huang, Xianhai,Palani, Anandan,Zhu, Zhaoning,Greenlee, William J.,Hyde, Lynn A.,Song, Lixin,Terracina, Giuseppe,Zhang, Lili,Parker, Eric M.
, p. 1002 - 1006 (2017/10/18)
The design and synthesis of a new series of tetrahydrobenzisoxazoles as modulators of γ-secretase activity and their structure-activity relationship (SAR) will be detailed. Several compounds are active γ-secretase modulators (GSMs) with good to excellent selectivity for the reduction of Aβ42 in the cellular assay. Compound 14a was tested in vivo in a nontransgenic rat model and was found to significantly reduce Aβ42 in the CNS compartment compared to vehicle-treated animals (up to 58% reduction of cerebrospinal fluid Aβ42 as measured 3 h after an acute oral dosing at 30 mg/kg).
GAMMA SECRETASE MODULATORS
-
Page/Page column 24; 30, (2013/05/22)
Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and use of the compounds in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
