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)]