Murali Rajagopalan

TL;DR: In this article, a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds and methods of treatment, prevention, inhibition, or amelioration of one or multiple diseases associated with the central nervous system using such compounds or pharmaceutical compositions are described.

TL;DR: Attachment of the cyclopropylcarbamate group to the piperidine core of gamma-secretase inhibitors leads to a dramatic increase of their in vitro potency.

TL;DR: Development of cis -2,4,6-trisubstituted piperidine N -arylsulfonamides as γ-secretase inhibitors for the potential treatment of Alzheimer’s disease is reported.

TL;DR: The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide gamma-secretase inhibitors is reported, with compounds with less CYP 3A4 liability compared to early leads.

TL;DR: A new class of 2,6-disubstituted morpholine N-arylsulfonamide gamma-secretase inhibitors was designed based on the introduction of a morpholine core in lieu or piperidine in the lead series, resulting in compounds with improved CYP 3A4 profiles.