TY - PAT
T1 - Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators.
AU - Gillen, Kevin James
AU - Jamieson, Craig
AU - Maclean, John Kinnaird Ferguson
AU - Moir, Elizabeth Margaret
AU - Rankovic, Zoran.
N1 - M1 - Copyright (C) 2011 American Chemical Society (ACS). All Rights Reserved.
CAPLUS AN 2008:42505(Patent)
PY - 2008/1/10
Y1 - 2008/1/10
N2 - 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)]
AB - 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)]
M3 - Patent
M1 - WO2008003452A1
ER -