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

  • Bioorg Med Chem Lett. 2011 Jan 15;21(2):664-9. doi: 10.1016/j.bmcl.2010.12.012.
Jun Qin  1 ,  Pawan Dhondi ,  Xianhai Huang ,  Mihirbaran Mandal ,  Zhiqiang Zhao ,  Dmitri Pissarnitski ,  Wei Zhou ,  Robert Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  John Clader ,  Lili Zhang ,  Mary Cohen-Williams ,  Nicholas Jones ,  Lynn Hyde ,  Anandan Palani
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]
PMID: 21195610 DOI: 10.1016/j.bmcl.2010.12.012
Abstract

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