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    • 3. 发明授权
    • Tetrahydronaphthalene derivatives for improving short-term memory
    • 用于改善短期记忆的四氢萘并噻唑衍生物
    • US5120759A
    • 1992-06-09
    • US690408
    • 1991-04-23
    • Urs HengartnerHenri Ramuz
    • Urs HengartnerHenri Ramuz
    • A61K31/215A61K31/357A61K31/36A61P25/28A61P33/02A61P35/00C07C35/52C07C57/58C07C57/76C07C59/48C07C69/732C07C215/42C07C219/24C07C323/52C07D317/58C07D319/18
    • C07C57/76C07C219/24C07C35/52C07C57/58C07D317/58C07D319/18C07C2102/10
    • Novel compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkylthio-lower-alkyl or furyl, R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylenedioxy or ethylenoxy and n is an integer from 1 to 3, have a pronounced activity in counteracting cerebral insufficiency or improving cognitive functions and also reduce the multiple-resistance towards cytostatics in the treatment of tumors or of chloroquine resistance in the treatment of malaria. They can accordingly be used as medicaments, especially for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions. The novel compounds of formula I can be manufactured by O-acylating a likewise novel compound of the formula ##STR2## wherein R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylendioxy or ethylenoxy and n is an integer from 1 to 3.
    • 下式的新型化合物其中R 1为低级烷基,低级烷氧基 - 低级 - 烷基,低级 - 烷硫基 - 低级 - 烷基或呋喃基,R 2为低级烷基,苯基 - 低级 - 烷基或环己基 - 低级 - 烷基,R 3和R 6各自独立地为氢或氟,R 4和R 5各自独立地为氢或低级烷氧基或一起为亚甲二氧基,亚乙二氧基或乙烯氧基,n为1至3的整数,在抵抗脑中具有明显的活性 功能不全或提高认知功能,并且还可减少治疗疟疾时治疗肿瘤或氯喹抗药性细胞抑制剂的多重阻力。 因此,它们可以用作药物,特别是用于控制或预防脑功能不全或改善认知功能。 式I的新化合物可以通过O-酰化类似新颖的式II化合物来制备,其中R 2是低级烷基,苯基 - 低级烷基或环己基 - 低级烷基,R 3和R 6各自独立地是 氢或氟,R 4和R 5各自独立地为氢或低级烷氧基或一起为亚甲二氧基,乙二氧基或亚乙氧基,n为1至3的整数。