Discovery of fused 5,6-bicyclic heterocycles as gamma-secretase modulators

作者：Qin Jun^*; Dhondi Pawan; Huang Xianhai; Mandal Mihirbaran; Zhao Zhiqiang; Pissarnitski Dmitri; Zhou Wei; Aslanian Robert; Zhu Zhaoning; Greenlee William; Clader John; Zhang Lili; Cohen Williams Mary; Jones Nicholas; Hyde Lynn; Palani Anandan

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(2): 664-669.

DOI：10.1016/j.bmcl.2010.12.012

• Alzheimer's disease
• gamma-Secretase modulator
• Amyloid-beta peptide
• Notch receptor

We herein report the discovery of four series of fused 5,6-bicyclic heterocycles as gamma-secretase modulators. Synthesis and SAR of these series are discussed. These compounds represent a new class of gamma-secretase modulators that demonstrate moderate to good in vitro potency in inhibiting A beta(42) production.

• 出版日期2011-1-15