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    • 3. 发明授权
    • Decahydro-8H-isoquino(2,1-g)(1,6)naphthyridine derivatives and related
compounds
    • 十氢-8H-异喹啉(2,1-g)(1,6)萘啶衍生物和相关化合物
    • US4956365A
    • 1990-09-11
    • US257372
    • 1988-10-12
    • Robin D. ClarkAndrew T. KilpatrickMichael Spedding
    • Robin D. ClarkAndrew T. KilpatrickMichael Spedding
    • C07D471/14C07D491/22
    • C07D471/14
    • Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;W is oxygen or sulfur; andZ is --R.sup.1, --OR.sup.2 or --NR.sup.3 R.sup.4, whereinR.sup.1 is lower alkyl, lower haloalkyl, cycloalkyl, optionally substituted phenyl or phenyl lower alkyl, or heteroaryl;R.sup.2 is lower alkyl, optionally substituted phenyl or phenyl lower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --(CH.sub.2).sub.m, --N(R.sup.5)-- or oxygen, in which m is an integer of 0-2 and R.sup.5 is hydrogen or lower alkyl;or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers.
    • (1)和(2)的化合物:其中:X和Y独立地是氢,羟基,低级烷基,低级烷氧基或卤素,或X和Y一起是 亚甲二氧基或亚乙基-1,2-二氧基; W是氧或硫; 且Z为-R1,-OR2或-NR3R4,其中R1为低级烷基,低级卤代烷基,环烷基,任选取代的苯基或苯基低级烷基或杂芳基; R2是低级烷基,任意取代的苯基或苯基低级烷基; R3和R4独立地是氢,烷基,任选取代的苯基或苯基低级烷基; 或者R 3和R 4与它们所连接的氮一起代表下式的杂环:其中A是 - (CH 2)m,-N(R 5) - 或氧,其中m是整数0 -2和R5是氢或低级烷基; 或其药学上可接受的盐可用作α2-受体阻滞剂。