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    • 6. 发明授权
    • Substituted 5H-pyrimido[5,4-b]indoles
    • 取代的5H-嘧啶并[5,4-b]吲哚
    • US4564610A
    • 1986-01-14
    • US562248
    • 1983-12-16
    • Dieter RahtzAndreas HuthRalph SchmiechenDieter SeidelmannWolfgang KehrHerbert H. SchneiderClaus T. Braestrup
    • Dieter RahtzAndreas HuthRalph SchmiechenDieter SeidelmannWolfgang KehrHerbert H. SchneiderClaus T. Braestrup
    • A61K31/505A61P25/00C07D209/42C07D487/04C07F9/6561
    • C07D487/04C07D209/42C07F9/6561
    • Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.2 wherein R is C.sub.1-5 -alkyl, exhibit strong affinity for binding to benzodiazepine receptors.The novel compounds are suitable for use in psychopharmaceutical preparations.
    • 取代的式I的5H-嘧啶并[5,4-b]吲哚其中R 2是卤素; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; C 1-5 - 烷基,环烷基,芳烷基或芳基; ORI,nn为0,1或2,或其中R 1为氢,C 1-5 - 烷基,环烷基,芳烷基或芳基的SO nRI; 其中RII和RIII是氢,C1-5-烷基,C3-5-烯基,环烷基,芳烷基,芳基,或具有连接的N-原子的5-或6-元杂环; RA为氢; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; 卤素,硝基,ORI,nn为0,1或2的SO nRI,其中R 1为氢,C 1-5 - 烷基,环烷基,芳烷基或芳基; 其中RII和RIII是氢,C1-5烷基,环烷基,C3-5-烯基,芳烷基,芳基,或具有连接的N-原子的5或6元杂环; 或其中R为C 1-5 - 烷基的PO(OR)2表现出对苯并二氮杂受体结合的强亲合力。 新型化合物适用于精神药物制剂。