METHOD OF MAKING THE 2,6-BIS(AMINOACYLAMINO)-BENZO-1,2-D:5,4-D-BISTHIAZOLE AND 2-AMINO-6-(AMINOACYLAMINO)-BENZO 1,2-D:5,4-D-BISTHIAZOLE DERIVATIVES

摘要

Compounds of the formula IMAGE wherein R1 and R1', which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 2 carbon atoms; R2 and R2', which may be identical to or different from each other, are each hydrogen or IMAGE but other than both hydrogen at the same time, where A is alkylene of 1 to 2 carbon atoms, R5 is hydrogen, lower alkyl, lower alkylamino-lower alkyl, lower alkoxy-lower alkyl, hydroxycarbonyl-lower alkyl, cycloalkyl of 5 to 8 carbon atoms, lower alkyl-cycloalkyl of 5 to 8 carbon atoms, phenyl or morpholino; R6 is hydrogen, lower alkyl, lower alkylamino-lower alkyl or lower alkoxy-lower alkyl; or R5 and R6, together with each other and the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring, where a 5- or 6-membered ring may comprise an additional sulfur or nitrogen heteroatom, and in the latter case said heterocyclic ring may optionally have one or two lower alkyl substituents, a lower alkoxy-carbonyl, a lower alkoxy-carbonyl-methyl, a hydroxy-lower alkyl, a trifluoroethyl, a cycloalkyl, a lower alkyl-cycloalkyl, a cyclohexylmethyl, a benzyl, a pyridyl, a piperidino, a phenyl, a fluoro-phenyl, a chloro-phenyl, a trifluoromethyl-phenyl, or an acetyl-phenyl substituent attached thereto; and R3 and R4, which may be identical to or different from each other, are each hydrogen, chlorine, bromine, lower alkyl, lower alkoxy, lower alkanoyl, hydroxycarbonyl, lower alkoxy-carbonyl, amino-carbonyl, phenyl, trifluoromethyl, nitro, cyano or amino; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as antiarthritics and antirheumatics.