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Positive allosteric modulators of AMPA receptors naftotiazina (paarm)

机译:AMPA受体naftotiazina(paarm)的正构构调节剂

摘要

1.- Compounds of the general formula (I) in which R1 means a radical chosen from the group consisting of hydrogen, a C1-C6 alkyl group optionally substituted with one or more halogen atoms, -SO2H, -SO2- -C1-C6 alkyl , -SO-C1-C6-alkyl, -CO-C1-C6-alkyl, -O, phenyl-C1-C4-alkyl, -C1-C4-alkyl-NR6R7 and -C1-C4-alkyl-C1-C4-alkyl, and cycloalkyl C3-C6, R2, R3, the same or different, mean a radical chosen from the group consisting of hydrogen, a C1-C6 alkyl group optionally substituted with one or more halogen, halogen, -NO2, -SO2H, -SO2-alkyl atoms C1-C6, -SO-C1-C6-alkyl, -CO-C1-C6-alkyl, -OH, -O-C1-C6-alkyl, -S-C1-C6-alkyl,C 1 -C 4 -alkyl-NR6R7 and -C 1 -C 4 -alkyl-O-C 1 -C 4 -alkyl, and C3-C6-cycloalkyl, oR1 and R2, together, mean a C4-C6, R6, R7 alkylene bridge, the same or different, mean hydrogen, C1-C4 alkyl or -CO-C1-C4 alkyl, R4, the same or different, means a radical chosen from the group consisting of a C1-C6 alkyl group optionally substituted with one or more halogen atoms, phenyl-C1- alkyl C4, halogen, -CN, -NO2, -SO2H, -SO3H, -SO2-C1-C6-alkyl, -SO-C1-C6-alkyl, -SO2-NR6R7, -COOH, -CO-C1-C6-alkyl, TO- CO-C1-C4-alkyl, -CO-O-C1-C4-alkyl, -O-CO-O-C1-C4-alkyl, -CO-NR6R7, -OH, -O-C1-C6-alkyl, -S-C1-alkyl -C6, -NR6R7 and an aryl radical, optionally substituted,once or several times, with halogen atoms, -NO2, -SO2H or C1-C4 alkyl, R5, the same or different, means a radical chosen from the group consisting of a C1-C6 alkyl group optionally substituted with one or more atoms of halogen, phenyl-C1-C4-alkyl, halogen, -CN, -NO2, -SO2H, -SO3H, -SO2-C1-C6-alkyl, -SO-C1-C6-alkyl, -SO2-NR6R7, -COOH, -CO- C1-C6-alkyl, -O-CO-C1-C4-alkyl, -CO-O-C1-C4-alkyl, -O-CO-O-C1-C4-alkyl, -CO-NR6R7, -OH, -O-C1-alkyl -C6, -S-C1-C6-alkyl, -NR6R7 and an aryl radical, optionally substituted, once or several times, with halogen atoms, -NO2, -SO2H or C1-C4-alkyl, and n, m, the same or different , mean 0, 1,2 or 3, provided that [1, 8-de] - 2, 3-dihydro-1, 1-sulfur dioxide-1, 2-tiazina is not included, and may take the form of its corresponding isomer and symmetric isomer, as well as its salts with safety characteristics.
机译:1.-通式(I)的化合物,其中R 1表示选自氢,任选被一个或多个卤素原子取代的C 1 -C 6烷基,-SO 2 H,-SO 2 --C 1 -C 6的基团。烷基,-SO-C1-C6-烷基,-CO-C1-C6-烷基,-O,苯基-C1-C4-烷基,-C1-C4-烷基-NR6R7和-C1-C4-烷基-C1-C4 -烷基和C 3 -C 6的环烷基,R 2,R 3相同或不同,是指选自氢,任选被一个或多个卤素,卤素,-NO 2,-SO 2 H取代的C 1 -C 6烷基组成的组的基团。 ,-SO2-烷基原子C1-C6,-SO-C1-C6-烷基,-CO-C1-C6-烷基,-OH,-O-C1-C6-烷基,-S-C1-C6-烷基,C 1 -C 4-烷基-NR 6 R 7和-C 1 -C 4-烷基-OC 1 -C 4-烷基和C 3 -C 6环烷基,o 1和R 2一起表示C 4 -C 6,R 6,R 7亚烷基桥相同或不同的R 4表示氢,C 1 -C 4烷基或-CO-C 1 -C 4烷基,R 4相同或不同,是指选自由C 1 -C 6烷基任选地被一个或多个取代的基团卤素原子,苯基-C 1-烷基C4,卤素,-CN,-NO2,-SO2H,-SO3H,-SO2-C1-C6-烷基,-SO-C1-C6-烷基,-SO2-NR6R7,-COOH,-CO-C1- C6-烷基,TO-CO-C1-C4-烷基,-CO-O-C1-C4-烷基,-O-CO-O-C1-C4-烷基,-CO-NR6R7,-OH,-O-C1 -C6-烷基,-S-C1-烷基-C6,-NR6R7和一个或多个被卤素原子取代的芳基,-NO2,-SO2H或C1-C4烷基,R5相同或不同,是指选自由任选地被一个或多个卤素,苯基-C1-C4-烷基,卤素,-CN,-NO2,-SO2H,-SO3H,-SO2的一个或多个原子取代的C1-C6烷基的基团。 -C1-C6-烷基,-SO-C1-C6-烷基,-SO2-NR6R7,-COOH,-CO-C1-C6-烷基,-O-CO-C1-C4-烷基,-CO-O-C1 -C4-烷基,-O-CO-O-C1-C4-烷基,-CO-NR6R7,-OH,-O-C1-烷基-C6,-S-C1-C6-烷基,-NR6R7和芳基(n,m表示相同或不同的n,m表示0、1、2或3,前提是[1、8, -de]-不包含2,3-二氢-1,1-二氧化硫-1,2-噻嗪并可以采取其相应的异构体和对称异构体的形式,以及具有安全特性的盐。

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