1 research outputs found
Initial Optimization of a New Series of γ‑Secretase Modulators Derived from a Triterpene Glycoside
The discovery of a new series of γ-secretase modulators
is
disclosed. Starting from a triterpene glycoside γ-secretase
modulator that gave a very low brain-to-plasma ratio, initial SAR
and optimization involved replacement of a pendant sugar with a series
of morpholines. This modification led to two compounds with significantly
improved central nervous system (CNS) exposure