Initial Optimization of
a New Series of γ‑Secretase
Modulators Derived from a Triterpene Glycoside
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Abstract
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