Isatine derivatives, their preparation and use

A - Human Necessities – 61 – K

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167/240, 260/317

A61K 31/40 (2006.01) C07D 209/40 (2006.01) C07D 209/58 (2006.01)

Patent

CA 2031756

A method of employing compounds having the formula (see formula I) wherein R1 is hydrogen, C1-6-alkyl which may be branched, C3-7-cyclo- alkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C1-6-alkoxy, CH2CO2R' wherein R' is hydrogen or C1-6-alkyl which may be branched, CH2CN, CH2CONR IV R V wherein R IV and R V independently are hydrogen or C1-6-alkyl, or CH2C(=NOH)NH2; R2 is hydrogen, benzyl, C1-6-alkyl which may be branched, or C3-7-cycloalkyl; R4, R5, R6, R7 independently are hydrogen, C1-6-alkyl which may be branched, phenyl, halogen, C1-6-alkoxy, NO2, CN, SO2NR''R''' wherein R'' and R''' independently are hydrogen or C1-6-alkyl, or CF3; or R5 and R7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO2, CF3, CN, SO2NR''R''' wherein R'' and R''' independently are hydrogen or C1-6-alkyl, and R4 and R5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions there- of. Certain of the compounds are novel. The compounds and pharmaceutical compositions containing the compounds are useful in antagonizing excitatory amino acids, combating central nervous system disorders, and especially in combating conditions sensitive to excitatory amino acids.

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