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)]
LanguageEnglish
Patent numberWO2008003452A1
Publication statusPublished - 10 Jan 2008

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Thiophenes
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Salts
Modulation
Psychiatry
alkoxyl radical

Cite this

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).
Gillen, Kevin James (Inventor) ; Jamieson, Craig (Inventor) ; Maclean, John Kinnaird Ferguson (Inventor) ; Moir, Elizabeth Margaret (Inventor) ; Rankovic, Zoran. (Inventor). / Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators. Patent No.: WO2008003452A1.
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title = "Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators.",
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)]",
author = "Gillen, {Kevin James} and Craig Jamieson and Maclean, {John Kinnaird Ferguson} and Moir, {Elizabeth Margaret} and Zoran. Rankovic",
note = "M1 - Copyright (C) 2011 American Chemical Society (ACS). All Rights Reserved. CAPLUS AN 2008:42505(Patent); WO2008003452A1",
year = "2008",
month = "1",
day = "10",
language = "English",
type = "Patent",

}

Gillen, KJ, Jamieson, C, Maclean, JKF, Moir, EM & Rankovic, Z 2008, Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators., Patent No. WO2008003452A1.

Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators. / Gillen, Kevin James (Inventor); Jamieson, Craig (Inventor); Maclean, John Kinnaird Ferguson (Inventor); Moir, Elizabeth Margaret (Inventor); Rankovic, Zoran. (Inventor).

Patent No.: WO2008003452A1.

Research output: Patent

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 -

Gillen KJ, Jamieson C, Maclean JKF, Moir EM, Rankovic Z, inventors. Preparation of pyrazolealkanamide substituted thiophenes as AMPA potentiators. WO2008003452A1. 2008 Jan 10.