Simon Ward - Discovery of N-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamid e, a Novel Clinical AMPA Receptor Positive Modulator

Version 1

      Publication Details (including relevant citation   information):

      J. Med. Chem., 2010, 53 (15), pp 5801–5812
      DOI: 10.1021/jm1005429
      Publication Date (Web): July 8, 2010

      Abstract:

      A series of AMPA receptor positive allosteric modulators has been   optimized from poorly penetrant leads to identify molecules with   excellent preclinical pharmacokinetics and CNS penetration. These   discoveries led to 17i, a potent, efficacious   CNS penetrant molecule with an excellent pharmacokinetic profile   across preclinical species, which is well tolerated and is also   orally bioavailable in humans.

      Address (URL): http://pubs.acs.org/doi/full/10.1021/jm1005429