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    • 4. 发明授权
    • 2,3(1H,4H)quinoxalinedione
    • 2,3(1H,4H)喹喔啉二酮
    • US5714489A
    • 1998-02-03
    • US512282
    • 1995-08-08
    • Wilfried LubischBerthold BehlHans Peter Hofmann
    • Wilfried LubischBerthold BehlHans Peter Hofmann
    • A61K31/495A61K31/498A61P25/00A61P25/08A61P25/20A61P25/22A61P25/24A61P25/26C07D241/44C07D241/52C07D401/04C07D403/04C07D487/12C07D487/14C07D403/10
    • C07D403/04C07D241/52C07D487/14
    • 2,3(1H,4H)-quinoxalinediones of the formula I ##STR1## where R.sup.1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R.sup.3, --CO--O--R.sup.3 or --CO--NH--R.sup.3, where R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R.sup.1 can have up to three of the following substituents: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R.sup.3 and --CO--NH--R.sup.3 ; R.sup.2 is 1-pyrrolyl which can have up to two of the following substituents: C.sub.1 -C.sub.4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R.sup.3, --CO--NH--R.sup.3, --CH.sub.2 --O--R.sup.3, --O--R.sup.3 and --CH.dbd.NO--R.sup.3 R radicals are identical or different and are the following: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R.sup.3 and --CO--NH--R.sup.3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' ##STR2## where R.sup.1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.
    • 式I的2,3(1H,4H) - 喹喔啉,其中R 1是氢,具有至多12个碳原子并且可以被下列之一取代的脂族基团:苯基,环戊基,环己基或-CO -R 3,-CO-O-R 3或-CO-NH-R 3,其中R 3是氢,C 1 -C 4烷基,苯基,苄基或1-苯基乙基,具有至多12个碳的脂环族基团或苯基, R1中的基团可以具有多达三个以下取代基:C 1 -C 4 - 烷基,C 1 -C 4 - 卤代烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 卤代烷氧基,卤素,硝基,氰基,-CO-O-R 3和 -CO-NH-R3; R2是可以具有至多两个以下取代基的1-吡咯基:C 1 -C 4烷基,苯基,苯基磺酰基,硝基,氰基和-CO-O-R 3,-CO-NH-R 3,-CH 2 -O-R 3 ,-O-R3和-CH = NO-R3R基团是相同或不同的,如下:C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,三氟甲基,三氯甲基,三氟甲氧基,三氯甲氧基,氟,氯,溴,碘 ,硝基,氰基和-CO-O-R 3和-CO-NH-R 3以及稠合的苯环; n为0-3,并且具有所述含义的2,3(1H,4H) - 喹喔啉酮I',其中R 1具有所述含义,适合作为治疗神经变性疾病和中枢神经系统的神经毒性紊乱的药物。
    • 8. 发明授权
    • 2,3(1H,4H)-quinoxalinediones
    • 2,3(1H,4H) - 喹喔啉
    • US5852017A
    • 1998-12-22
    • US880507
    • 1997-06-23
    • Wilfried LubischBerthold BehlHans Peter Hofmann
    • Wilfried LubischBerthold BehlHans Peter Hofmann
    • A61K31/495A61K31/498A61P25/00A61P25/08A61P25/20A61P25/22A61P25/24A61P25/26C07D241/44C07D241/52C07D401/04C07D403/04C07D487/12C07D487/14
    • C07D403/04C07D241/52C07D487/14
    • 2,3(1H,4H)-quinoxalinediones of the formula I ##STR1## where R.sup.1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R.sup.3, --CO--O--R.sup.3 or --CO--NH--R.sup.3, where R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R.sup.1 can have up to three of the following substituents: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R.sup.3 and --CO--NH--R.sup.3 ; R.sup.2 is 1-pyrrolyl which can have up to two of the following substituents: C.sub.1 -C.sub.4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R.sup.3, --CO--NH--R.sup.3, --CH.sub.2 --O--R.sup.3, --O--R.sup.3 and --CH.dbd.NO--R.sup.3 R radicals are identical or different and are the following: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R.sup.3 and --CO--NH--R.sup.3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' ##STR2## where R.sup.1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.
    • 式I的2,3(1H,4H) - 喹喔啉,其中R 1是氢,具有至多12个碳原子并且可以被下列之一取代的脂族基团:苯基,环戊基,环己基或-CO -R 3,-CO-O-R 3或-CO-NH-R 3,其中R 3是氢,C 1 -C 4烷基,苯基,苄基或1-苯基乙基,具有至多12个碳的脂环族基团或苯基, R1中的基团可以具有多达三个以下取代基:C 1 -C 4 - 烷基,C 1 -C 4 - 卤代烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 卤代烷氧基,卤素,硝基,氰基,-CO-O-R 3和 -CO-NH-R3; R2是可以具有至多两个以下取代基的1-吡咯基:C 1 -C 4烷基,苯基,苯基磺酰基,硝基,氰基和-CO-O-R 3,-CO-NH-R 3,-CH 2 -O-R 3 ,-O-R3和-CH = NO-R3R基团是相同或不同的,如下:C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,三氟甲基,三氯甲基,三氟甲氧基,三氯甲氧基,氟,氯,溴,碘 ,硝基,氰基和-CO-O-R 3和-CO-NH-R 3以及稠合的苯环; n为0-3,并且具有所述含义的2,3(1H,4H) - 喹喔啉酮I',其中R 1具有所述含义,适合作为治疗神经变性疾病和中枢神经系统的神经毒性紊乱的药物。