1-¬bis(hydroxymethyl)-methyl|-2-substituted- isoquinoline...

C - Chemistry – Metallurgy – 07 – D

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C07D 217/24 (2006.01) A61K 31/47 (2006.01) C07D 217/16 (2006.01)

Patent

CA 1265141

Abstract The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), Image (I) wherein R1 and R2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms, the dotted line is an optional double bond in the 1,2-position, R3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or - if there is a single bond in the 1,2-position - represents a group of the formula Image or Image in which X is oxygen if R4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or - 2 - substituted phenyl; or X is oxygen or sulfur if R4 is an -NH2, -NH-C1-4-alkyl, -NH-C3-6-cycloalkyl, -NH-phenyl or -NH-C1-4-alkyl-phenyl group; and R5 and R6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl, and salts thereof. Processes fnr the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.

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