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    • 1. 发明授权
    • Halo substituted aminotetralins
    • 卤代替氨基四氢化萘
    • US5225596A
    • 1993-07-06
    • US721532
    • 1991-07-08
    • Per A. E. CarlssonHakan V. WikstromKjell A. I. SvenssonBengt R. AnderssonBarbro A. EkmanNils P. StjernlofNils A. Svensson
    • Per A. E. CarlssonHakan V. WikstromKjell A. I. SvenssonBengt R. AnderssonBarbro A. EkmanNils P. StjernlofNils A. Svensson
    • C07C211/42C07C217/74
    • C07C211/42C07C217/74C07C2101/02C07C2102/10
    • This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein X.sub.1 is halogen, CF.sub.3, --OR.sub.3, or --SR.sub.4 ; wherein R.sub.3 is alkyl(C.sub.1 -C.sub.8); alkenyl(C.sub.1 -C.sub.8); --CH.sub.2 -cycloalkyl(C.sub.3 -C.sub.8) or benzyl; wherein R.sub.4 is alkyl(C.sub.1 -C.sub.3); wherein X.sub.2 is hydrogen, CF.sub.3 or halogen; wherein R.sub.7 is hydrogen or methyl; wherein R.sub.1 is hydrogen, alkyl(C.sub.1 -C.sub.3), or cyclopropylmethyl; wherein R.sub.2 is --CH.sub.2 -cycloalkyl(C.sub.3 -C.sub.8), alkyl(C.sub.1 -C.sub.8), --(CH.sub.2).sub.q --R.sub.5 or --CH.sub.2 CH.sub.2 --Z--(CH.sub.2).sub.r CH.sub.3 ; wherein R.sub.5 is phenyl, 2-thiophene or 3-thiophene; wherein Z is oxygen or sulfur; and wherein p is one or 2, q is 2 or 3, and r is zero to 3; with the provisos that (1) when X.sub.1 is --OR.sub.3, X.sub.2 is halogen or CF.sub.3 ; and (2) when X.sub.1 is halogen, X.sub.2 is hydrogen, and p is 2, X.sub.1 is in a position other than the 8-position. These compounds are useful to treat central nervous system disorders.
    • 本发明是治疗上有用的式Ⅰ化合物及其药学上可接受的酸式加成盐,其中X 1是卤素,CF 3,-OR 3或-SR 4; 其中R3是烷基(C1-C8); 烯基(C1-C8); -CH 2 - 环烷基(C 3 -C 8)或苄基; 其中R4是烷基(C1-C3); 其中X 2是氢,CF 3或卤素; 其中R7是氢或甲基; 其中R1是氢,烷基(C1-C3)或环丙基甲基; 其中R2是-CH2-环烷基(C3-C8),(C1-C8)烷基, - (CH2)q-R5或-CH2CH2-Z-(CH2)rCH3; 其中R5是苯基,2-噻吩或3-噻吩; 其中Z是氧或硫; 并且其中p是1或2,q是2或3,并且r是0-3; 条件是(1)当X1为-OR3时,X2为卤素或CF3; 和(2)当X1为卤素时,X2为氢,p为2,X1为8位以外的位置。 这些化合物可用于治疗中枢神经系统疾病。