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    • 2. 发明授权
    • Isoquinoline derivatives
    • 异喹啉衍生物
    • US4835158A
    • 1989-05-30
    • US120654
    • 1987-11-16
    • Gordon H. PhillippsStanley F. DykeEsme J. BaileyPeter D. HowesDavid I. C. Scopes
    • Gordon H. PhillippsStanley F. DykeEsme J. BaileyPeter D. HowesDavid I. C. Scopes
    • C07D471/04C07D471/14
    • C07D471/04C07D471/14
    • Pharmaceutical compositions for combatting cancer comprising a compound of formula (I) ##STR1## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl group;R.sup.2 represents a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 represents a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together represent a methylenedioxy group;R.sup.4 represents a hydrogen or halogen atom or a C.sub.1-3 alkyl group or a phenyl group optionally substituted by a halogen atom or a hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group; and the ring A represents a group of formula ##STR2## where R.sup.5 and R.sup.6 each represent a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group,R.sup.7 and R.sup.8 each represents a hydrogen atom or a methyl group, and one of X, X.sup.1, X.sup.2 and X.sup.3 represents a nitrogen atom and the others represent --CH-- groups; with the proviso that where Arepresents a group of formula (i) at least one of R.sup.1 to R.sup.6 represents other than a hydrogen atom) together with at least one pharmaceutical carrier or excipient.
    • 包括式(I)化合物(I)(其中R1表示氢原子或C1-4烷基,C2-4烯基或C2-4炔基; R2表示氢原子或 羟基,C 1-4烷氧基或C 2-4烷酰氧基; R 3表示氢原子,或(当R 2不是氢原子时)任选的羟基,C 1-4烷氧基或C 2-4烷酰氧基,或R 2和R 3 一起代表亚甲二氧基; R4代表氢或卤原子或C1-3烷基或任选被卤素原子或羟基,C1-4烷基,C1-4烷氧基或C1-4烷酰氧基取代的苯基; 并且环A表示式为“IMAGE”的基团,其中R 5和R 6各自表示氢原子或羟基,C 1-4烷氧基或C 1-4烷酰氧基,R 7和R 8各自表示氢原子或甲基, X,X 1,X 2和X 3中的一个表示氮原子,其余的表示-CH-基团;条件是其中A代表 (i)R 1至R 6中的至少一个表示除氢原子以外的基团)以及至少一种药物载体或赋形剂。