Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators.

Kevin James Gillen (Inventor), Craig Jamieson (Inventor), John Kinnaird Ferguson Maclean (Inventor), Elizabeth Margaret Moir (Inventor), Zoran. Rankovic (Inventor)

Research output: Patent

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)]
Original languageEnglish
Patent numberWO2008003452A1
Publication statusPublished - 10 Jan 2008

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Gillen, K. J., Jamieson, C., Maclean, J. K. F., Moir, E. M., & Rankovic, Z. (2008). Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators. (Patent No. WO2008003452A1).