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    • 3. 发明授权
    • 2,6-Diamino-benzo[1,2-d:5,4-d']bisthiazoles and salts thereof
    • 2,6-二氨基 - 苯并[1,2-d:5,4-d']二联体及其盐
    • US4344946A
    • 1982-08-17
    • US182077
    • 1980-08-28
    • Ernest CullenGenus PossanzaPatrick B. Stewart
    • Ernest CullenGenus PossanzaPatrick B. Stewart
    • A61K31/425A61K31/428A61K31/429A61K31/445A61K31/495A61K31/535A61K31/54A61P19/02A61P29/00C07D513/04C07D521/00
    • C07D513/04Y10S514/825
    • Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.1 ', which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 2 carbon atoms;R.sub.2 and R.sub.2 ', which may be identical to or different from each other, are each hydrogen or ##STR2## but other than both hydrogen at the same time, where A is alkylene of 1 to 2 carbon atoms,R.sub.5 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;R.sub.6 is hydrogen, lower alkyl, lower alkylamino-lower alkyl or lower alkoxy-lower alkyl; orR.sub.5 and R.sub.6, 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; andR.sub.3 and R.sub.4, 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.
    • 其中R 1和R 1'可以彼此相同或不同的化合物分别为氢或1至2个碳原子的烷基; R 2和R 2'可以彼此相同或不同,各自为氢或不同于氢,但不是同时为氢,其中A为1至2个碳原子的亚烷基,R5为氢,低级烷基 低级烷基氨基 - 低级烷基,低级烷氧基 - 低级烷基,羟基羰基 - 低级烷基,5-8个碳原子的环烷基,5-8个碳原子的低级烷基 - 环烷基,苯基或吗啉代; R6是氢,低级烷基,低级烷基氨基 - 低级烷基或低级烷氧基 - 低级烷基; 或R 5和R 6彼此连接并与它们相连的氮原子形成5-,6-或7-元杂环,其中5-或6-元环可以包含另外的硫或氮杂原子 在后一种情况下,所述杂环可任选地具有一个或两个低级烷基取代基,低级烷氧基 - 羰基,低级烷氧基 - 羰基 - 甲基,羟基 - 低级烷基,三氟乙基,环烷基,低级烷基 - 环烷基 ,环己基甲基,苄基,吡啶基,哌啶子基,苯基,氟 - 苯基,氯 - 苯基,三氟甲基 - 苯基或与其连接的乙酰基 - 苯基取代基; 可以相同或不同的R 3和R 4各自为氢,氯,溴,低级烷基,低级烷氧基,低级烷酰基,羟基羰基,低级烷氧基 - 羰基,氨基 - 羰基,苯基,三氟甲基,硝基, 氰基或氨基; 和无毒的,药学上可接受的酸加成盐。 化合物以及盐可用作抗关节炎和抗风湿剂。