Bis(substituted methyl)-methyl-isoquinoline derivatives,...

C - Chemistry – Metallurgy – 07 – D

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C07D 217/24 (2006.01) C07D 217/14 (2006.01) C07D 217/16 (2006.01)

Patent

CA 1271761

ABSTRACT OF THE DISCLOSURE Novel bis(substituted methyl)-methyl- isoquinoline derivatives of the formula (I) (I) Image are disclosed wherein R1 and R2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms, R3 is hydrogen, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or a - Image -R4 group, in which R4 is alkyl having from 1 to 5 carbon atoms, phenyl, substituted phenyl or -NH-phenyl, X is oxygen or sulfur, R7 is hydroxyl, halogen or an -O- Image -R9 group, R8 is halogen, alkoxy having from 1 to 4 carbon atoms or an -O- Image -R9 group, in which X has the same meaning as defined above, and R9 independently from R4 may have the same meanings as defined for R4, or is an -NH-(C1- 4-alkyl) or C3-6-cycloalkyl group, and salts thereof. The novel compounds of the invention are biologically active and exhibit immunosuppressive, antidepressive, analgesic, antipyretic, antihypoxial or gastric secretion inhibiting activity. They are also useful as intermediates in the preparation of biologically active azeto-isoquinoline derivatives. Processes for the preparation of the compounds (I) and pharmaceutical compositions containing them are also disclosed.

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