Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators.

Gillen, Kevin James (2008) Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators. WO2008003452A1.

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Abstract

The title compds. I [wherein m = 1-4; R1 = CN or (un)substituted alkyl; R2 = acyl, (un)substituted alkyl, or alkoxy; R3 = H or (un)substituted Me; or R2 and R3 form a ring; R4 = CH2OH, CO2H, or (un)substituted CONH2; R5 and R6 = independently H or (cyclo)alkyl; or R5 and R6 form a ring], or pharmaceutically acceptable salts or solvates thereof were prepd. as AMPA potentiators. For example, II was prepd. in a multi-step synthesis. II gave an EC50 of 2.2 μM in pos. modulation of the AMPA (GluR1) receptor. The compds. ae useful in the treatment or prevention of psychiatric diseases, including schizophrenia, depression, and Alzheimer's disease (no data). [on SciFinder(R)]

Creators(s): Gillen, Kevin James, Jamieson, Craig ORCID logoORCID: https://orcid.org/0000-0002-6567-8272, Maclean, John Kinnaird Ferguson, Moir, Elizabeth Margaret and Rankovic, Zoran.;
Item type:Patent
ID code:33924
Notes:M1 - Copyright (C) 2011 American Chemical Society (ACS). All Rights Reserved. CAPLUS AN 2008:42505(Patent)
Subjects:UNSPECIFIED
Department:Faculty of Science > Pure and Applied Chemistry
Depositing user: Pure Administrator
Date deposited:20 Oct 2011 15:37
Last modified:04 Nov 2020 04:49
URI:https://strathprints.strath.ac.uk/id/eprint/33924
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