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    • 10. 发明授权
    • 3(2H)pyridazinone, process for its preparation and anti-allergic agent
containing it
    • 3(2H)吡咯烷酮,其制备方法和含有其的抗过敏剂
    • US5098900A
    • 1992-03-24
    • US180599
    • 1988-04-11
    • Motoo MutsukadoKeizo TanikawaKen-ichi ShikadaRyozo Sakoda
    • Motoo MutsukadoKeizo TanikawaKen-ichi ShikadaRyozo Sakoda
    • A61K31/50A61K31/535A61P11/00A61P11/08A61P27/16A61P37/08C07D237/00C07D237/14C07D237/22C07D317/00C07D405/12
    • C07D405/12C07D237/22Y10S514/826
    • A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is C.sub.2 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, chlorine or bromine; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --(CH.sub.2).sub.l A [wherein A is substituted amino of the formula --N(R.sub.4) (R.sub.5) (wherein each of R.sub.4 and R.sub.5 which may be the same or different, is C.sub.1 -C.sub.4 alkyl, or R.sub.4 and R.sub.5 together form C.sub.4 -C.sub.6 alkylene), morpholino, 4-R.sub.6 -piperazin-1-yl (wherein R.sub.6 is C.sub.1 -C.sub.3 alkyl) or --OR.sub.7 (wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.3 alkyl), and l is an integer of 0 to 3], --OR.sub.8 [wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.5 alkenyl, benzyl or --(CH.sub.2).sub.q --R.sub.9 [wherein R.sub.9 is CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CONHR.sub.3 (wherein R.sub.3 is as defined above) or --CH.sub.2 OR.sub.7 (wherein R.sub.7 is as defined above), and q is an integer of 1 to 5]], --CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CON(R.sub.10) (R.sub.11) [wherein each of R.sub.10 and R.sub.11 which may be the same or different, is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.5 alkenyl, or R.sub.10 and R.sub.11 together form C.sub.4 -C.sub.6 alkylene, --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 N(R.sub.6)(CH.sub.2).sub.2 -- (wherein R.sub.6 is as defined above)], --CONH(CH.sub.2).sub.m A (wherein A is as defined above, and m is an integer of 2 to 4), --CH.dbd.CHCOR.sub.12 (wherein R.sub.12 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --N(R.sub.13) (CH.sub.2).sub.n CO.sub.2 R.sub.3 (wherein R.sub.13 is hydrogen, C.sub.1 -C.sub.6 alkyl or cycloalkyl, R.sub.3 is as defined above, and n is an integer of 1 to 4)), --SR.sub.14 (wherein R.sub.14 is C.sub.1 -C.sub.4 alkyl), --CN or ##STR2## wherein R.sub.3 is as defined above), or two of Y.sub.1, Y.sub.2 and Y.sub.3 together form ##STR3## (wherein p is an integer of 1 or 2), and a pharmaceutically acceptable salt thereof.
    • 具有下式的3(2H)哒嗪酮:其中R 1是C 2 -C 5烷基; R2是氢,C1-C3烷基,氯或溴; R3是氢或C1-C4烷基; 并且可以相同或不同的Y 1,Y 2和Y 3各自为氢,C 1 -C 8烷基,C 2 -C 8烯基,卤素, - (CH 2)l A [其中A为式-N(R 4) (R 5)(其中可以相同或不同的R 4和R 5各自为C 1 -C 4烷基,或R 4和R 5一起形成C 4 -C 6亚烷基),吗啉代,4-R 6 - 哌嗪-1-基(其中R 6 是C 1 -C 3烷基)或-OR 7(其中R 7是氢或C 1 -C 3烷基),l是0-3的整数],-OR 8 [其中R8是氢,C1-C8烷基,C3-C5链烯基, 苄基或 - (CH 2)q -R 9 [其中R 9是CO 2 R 3(其中R 3如上定义),-CONHR 3(其中R 3如上定义)或-CH 2 OR 7(其中R 7如上所定义),q是整数 1〜5]],-CO 2 R 3(其中R 3如上定义),-CON(R 10)(R 11)[其中R 10和R 11可以相同或不同,为氢,C 1 -C 4烷基或C 3 (CH 2)2 O(CH 2)2 - 或 - (CH 2)2 N(R 6)(CH 2)2 - (其中R 6如上所定义)], - (C 1 -C 6)烷基,或者R 10和R 11一起形成C 1 -C 6亚烷基, CONH(CH2)mA(其中 在A中如上所定义,m为2〜4的整数),-CH = CHCOR 12(其中,R 12为羟基,C 1〜C 4烷氧基或-N(R 13)(CH 2)n CO 2 R 3(式中,R 13为氢, C6烷基或环烷基,R3如上所定义,n是1至4的整数)),-SR 14(其中R 14是C 1 -C 4烷基),-CN或其中R 3如上定义),或 Y1,Y2和Y3中的两个一起形成(其中p为1或2的整数)及其药学上可接受的盐。