New positive allosteric Modulator of AMPA receptors (paarm), processes for their Preparation and their use as medicaments

摘要

Compounds of the general formula (I) EMI FILE = "01007094_1" ID = "1" MFI = JPEG in which A means a sulfur atom, an oxygen atom, NH, or N-C1-C4 alkyl, R1 means a radical selected from the group consisting of hydrogen, of a C1-C6 alkyl group optionally substituted with one or more halogen atoms, as well as of -SO2H, -SO2-C1-C6 alkyl, -SO-C1-C6 alkyl, -CO-C1-C6 alkyl, -O, phenyl-C1-C4 alkyl, C1-C4 alkyl-NR7R8 and C1-C4 alkyl-O-C1-C4 alkyl, or C3-C6, R2, R9 cycloalkyl the same or different , they mean a radical selected from the group consisting of hydrogen,of a C1-C6 alkyl group optionally substituted with one or more halogen atoms, as well as halogen, -NO2, -SO2H, -SO2-C1-C6 alkyl, -SO-C1-C6 alkyl, -CO-C1-alkyl C6, -OH, -O-C1-C6 alkyl, -S-C1-C6 alkyl, C1-C4-NR7R8 alkyl and C1-C4-O-C1-C4 alkyl, or C3-C6 cycloalkyl, oR1 and R2 they mean in common a C2-C6, R7, R8, the same or different alkylene bridge, they mean hydrogen or C1-C4 alkyl, and R3, R4, R5, R6 the same or different, they mean a radical selected from the group consisting of hydrogen, of a C1-C8 alkyl group optionally substituted with one or more halogen atoms, as well as phenyl-C1-C4 alkyl, halogen, -CN, -NO2, -SO2H,-C1-c1-c1-c6 Its different corresponding isomers and non corresponding isomers, as well as the salts which are safe in pharmacology. -2-general (I) compound in characteristic 1, i.e. a refers to sulfur atom, oxygen atom or normal tar C1-C2, R1 refers to radical substance selected from hydrogen group,of a C1-C6 alkyl group optionally substituted with one or several halogen atoms, as well as of -SO2H, -SO2-C1-C6 alkyl, -SO-C1-C6 alkyl, -CO-C1-C6-O alkyl, alkyl C1-C4-NR7R8 and C1-C4-O-alkyl C1-C4 alkyl, or benzyl, R2, R9 the same or different, mean a radical selected from the group consisting of hydrogen, of a C1-C6 alkyl group eventually substituted with one or more halogen atoms, as well as halogen atoms, -NO2, -SO2H, -SO2-C1-C6 alkyl, -SO-C1-C6 alkyl, -CO-C1-C6 alkyl, -OH, -O-alkyl C1-C6, -S-C1-C6 alkyl, C1-C4-NR7R8 alkyl and -C1-C4 alkyl-O-C1-C4 alkyl, oR1 and R2 together mean a C3-C6 alkylene bridge, and R3, R4, R5,R6, the same or different, means a radical selected from the group consisting of hydrogen, of a C1-C4 alkyl group optionally substituted with one or more halogen atoms, as well as C1-C4 alkylene-phenyl, halogen, -CN, - NO2, -SO2H, -SO3H, -SO2CH3, -SOCH3, -CO-C1-C4 alkyl, -OH, -O-C1-C3 alkyl and S-C1-C4 alkyl, possibly in the form of their different enantiomers and diastereoisomers, as well as of its pharmacologically safe salts. Compounds of the general formula (I) according to claim 1 or 2, wherein A means a sulfur atom or C1-C2 N-alkyl, R1, R2, R9 the same or different, means hydrogen, C1-C4 alkyl or benzyl,R1 and R2 together mean a C3-C4 alkylene bridge, and R3, R4, R5, R6, the same or different, mean a radical selected from the group consisting of hydrogen, C1-C4 alkyl, CF3, NO2, benzyl, -SO2 -C1-C4 alkyl, -SO3H and halogen, possibly in the form of their different enantiomers and diastereoisomers, as well as their pharmacologically safe salts. Compounds of the general formula (I) according to claims 1 to 3, wherein A means an atom sulfur or N-CH3, R1, R2, R9 equal or different, mean hydrogen, C1-C4 alkyl, or R1 and R2 together mean a C3-C4, R3, R5, R6 alkylene bridge same or different,They are a radical substance selected from the hydrogen, C1-C4 tar and halogen groups. R4 refers to hydrogen, halogen or C1-C4 tar, which may take the form of different enantiomers and diastereomers, According to one of the 1-4 claims, 1 represents methyl, ethyl, propyl, n-butyl or benzene in kerosene, It may occur in the form of its different enantiomers and diastereomers and their pharmaceutically safe salts: according to the requirements of items 1 to 5, the compound in the trachea is a sulfur atom, R1 represents methyl, R2,R9 represents hydrogen, R3 represents radicals selected from hydrogen, methyl, CN and halon groups, R5 represents radicals selected from hydrogen, methyl and halon groups, R4 represents hydrogen, R6 represents hydrogen or methyl, According to the first requirement, tracheal compound (I) refers to sulfur atom, R1 refers to methyl, R3 refers to hydrogen, fluorine or chlorine, and YR2, R4, R5, R6 and R9 refer to hydrogen, which may refer to the salt with harmless effect.