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    • 5. 发明申请
    • INDOLOQUINONE DERIVATIVES AS BIOREDUCTIVE AGENTS
    • 吲哚喹啉衍生物作为生物降解剂
    • WO1997023456A1
    • 1997-07-03
    • PCT/GB1996003176
    • 1996-12-20
    • BRITISH TECHNOLOGY GROUP LTD.STRATFORD, Ian, JamesNAYLOR, Matthew, AlexanderJAFFAR, MohammedADAMS, Gerald, Edward
    • BRITISH TECHNOLOGY GROUP LTD.
    • C07D209/42
    • C07D209/12A61K31/404
    • Use of a compound of general formula (I) or salt thereof wherein R and R are independently selected from hydrogen, halogen and C1-6 alkyl or haloalkyl, C2-6 alkenyl or haloalkenyl, C1-6 alkoxy, phenoxy, C1-6 alkylthio, phenylthio, primary and secondary amino or hydroxy groups and R is hydrogen, hydroxy, a C1-6 alkyl or haloalkyl, C2-6 alkenyl or haloalkenyl or C1-6 alkoxy or haloalkoxy group is provided for the manufacture of a medicament for the treatment of neoplasms, particularly solid cancerous tumours characterised in that R is selected from a C1-6 alkyl or haloalkyl group, -CO2R where R is hydrogen or a C1-6 alkyl or haloalkyl group, or a group -CH2-X where X is selected from groups of formula -S-R , -O-R , and (a) where R is a hydrogen or a leaving group, the acid HR6 of which has a pKa of 10 or less and R and R are the same or different and are selected from C1-6 alkyl or haloalkyl or together with the interjacent nitrogen form a heterocyclic ring of 5 to 7 atoms optionally substituted by C1-4 alkyl or haloalkyl and R is selected from hydrogen, C1-4 alkyl and haloalkyl or groups-(CH2)nCHR R of more than four carbon atoms where n is an integer of 0 to 2 and R and R are independently selected from a C1-4 alkyl or haloalkyl group, or R and R together with the interjacent carbon atom form a C3-7 cycloalkyl or cycloalkenyl ring optionally substituted with one or more C1-4 alkyl or haloalkyl, or C2-4 alkenyl or haloalkenyl groups.
    • 使用通式(I)的化合物或其盐,其中R和R 4独立地选自氢,卤素和C 1-6烷基或卤代烷基,C 2-6烯基或卤代烯基,C 1-6烷氧基,苯氧基,C 1 -6烷硫基,苯硫基,伯和仲氨基或羟基,R 3为氢,羟基,C 1-6烷基或卤代烷基,C 2-6烯基或卤代链烯基或C 1-6烷氧基或卤代烷氧基,用于制备 用于治疗肿瘤,特别是固体癌性肿瘤的药物,其特征在于R 1选自C 1-6烷基或卤代烷基,-CO 2 R 5,其中R 5是氢或C 1-6烷基 或卤代烷基,或基团-CH 2 -X(其中X选自式-SR 6,-OR 6)和(a)其中R 6为氢或离去基团的基团,该酸 HR6的pKa为10以下,R 7和R 8相同或不同,选自C 1-6烷基或卤代烷基,或与中间的氮一起形成杂环 任选被C 1-4烷基或卤代烷基取代的5至7个原子,R 2选自氢,C 1-4烷基和卤代烷基或多于四个碳原子的基团 - (CH 2)n CHR 9 R 10,其中 n为0〜2的整数,R 9和R 10独立地选自C 1-4烷基或卤代烷基,或R 9和R 10与中间碳原子一起形成C 3 -7环烷基或环烯基,任选被一个或多个C 1-4烷基或卤代烷基取代,或C 2-4链烯基或卤代烯基。