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    • 93. 发明授权
    • Chromogenic lactone compounds of benzopyrano-2H-pyrazoles
    • 苯并吡喃-2-基吡唑的显色内酯化合物
    • US4933448A
    • 1990-06-12
    • US343094
    • 1989-04-25
    • Ian J. Fletcher
    • Ian J. Fletcher
    • C07D491/20B41M5/145B41M5/30B41M5/327C07D491/14C09B11/26C09B57/00
    • C07D491/14B41M5/145B41M5/327B41M5/1455B41M5/3275
    • Chromogenic lactone compounds of benzopyrano-2H-pyrazoles of the formula ##STR1## in which Ar is an aryl radical which is unsubstituted or substituted by halogen, nitro, cyano, lower alkyl, lower alkoxy, lower alkylthio, lower alkoxycarbonyl, trifluoromethyl, phenoxy, phenylthio or --NX.sub.3 X.sub.4,R.sub.1 is hydrogen, lower alkyl or lower alkoxy,R.sub.2 is lower alkyl, phenyl, or phenyl which is substituted by halogen, lower alkyl or lower alkoxy, andX.sub.1, X.sub.2, X.sub.3 and X.sub.4, independently of one another, are each hydrogen, alkyl which is unsubstituted or substituted by halogen, hydroxyl, cyano, tetrahydrofuryl or lower alkoxy, or are acyl, cycloalkyl, or aralkyl or aryl, each of which is unsubstituted or substituted by halogen, cyano, nitro, trifluoromethyl, lower alkyl, lower alkoxy or lower alkoxycarbonyl, or the substituent pairs (X.sub.1 and X.sub.2) and (X.sub.3 and X.sub.4), in each case together with the common nitrogen atom, are a 5- or 6-membered, preferably saturated heterocyclic radical, and in which the ring A is unsubstituted or substituted by halogen, nitro, lower alkyl, lower alkoxy, lower alkylthio, lower alkoxycarbonyl, amino, mono(lower alkyl)amino or di(lower alkyl)amino.These novel lactone compounds are particularly suitable as color formers in pressure-sensitive or heat-sensitive recording materials, and give intense yellow, orange or red colorations.
    • 式(1)的苯并吡喃-2H-吡唑的显色内酯化合物,其中Ar是未取代或被卤素,硝基,氰基,低级烷基,低级烷氧基,低级烷硫基,低级烷氧基羰基,三氟甲基 苯氧基,苯硫基或-NX3X4,R1是氢,低级烷基或低级烷氧基,R2是被卤素,低级烷基或低级烷氧基取代的低级烷基,苯基或苯基,X 1,X 2,X 3和X 4独立地是 羟基,氰基,四氢呋喃基或低级烷氧基,或者是酰基,环烷基或芳烷基或芳基,其各自为未取代的或被卤素,氰基,硝基, 三氟甲基,低级烷基,低级烷氧基或低级烷氧基羰基,或取代基对(X1和X2)和(X3和X4)在各种情况下与常见的氮原子一起是5-或6-元,优选饱和的杂环基 ,其中环A i 未取代或被卤素,硝基,低级烷基,低级烷氧基,低级烷硫基,低级烷氧基羰基,氨基,单(低级烷基)氨基或二(低级烷基)氨基取代。 这些新颖的内酯化合物特别适用于压敏或热敏记录材料中的成色剂,并且产生强烈的黄色,橙色或红色着色。
    • 95. 发明授权
    • Isoquinoline derivatives
    • 异喹啉衍生物
    • US4900737A
    • 1990-02-13
    • US250216
    • 1988-09-28
    • Gordon H. PhillippsEsme J. BaileyMichael G. Lester
    • Gordon H. PhillippsEsme J. BaileyMichael G. Lester
    • A61K31/47A61P35/00A61P43/00C07D471/04C07D491/14
    • C07D471/04C07D491/14
    • Compounds of formula (I) ##STR1## (wherein R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 is 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 are a methylenedioxy group;R.sup.4 is a hydrogen or halogen atom or a methyl group;R.sup.5 and R.sup.6 is each a hydrogen atom or a group --OCOCH.sub.2 NR.sup.7 R.sup.8 [where R.sup.7 and R.sup.8, which may be the same or different, each is a hydrogen atom or a C.sub.3-7 cycloalkyl group or a straight or branched C.sub.1-4 alkyl group optionally substituted by a hydroxyl group, or --NR.sup.7 R.sup.8 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring an oxygen or sulphur atom or a group --NH-- or --N(R) where R is a C.sub.1-4 alkyl group optionally substituted by a hydroxyl group] with the proviso that when one of R.sup.5 and R.sup.6 is a hydrogen atom, the other is a group --OCOCH.sub.2 NR.sup.7 R.sup.8) may be prepared by amination of a corresponding compound where R.sup.5 and/or R.sup.6 is a group --OCOCH.sub.2 L wherein L is a displaceable leaving group. The compounds of formula (I) and their physiologically acceptable salts exhibit interesting cancer combatting properties.
    • 式(I)化合物其中R1是氢原子或甲基; R2是氢原子或羟基,C1-4烷氧基或C2-4烷酰氧基; R3是氢原子,或(当 R 2不是氢原子)任选地是羟基,C 1-4烷氧基或C 2-4烷酰氧基,或者R 2和R 3一起是亚甲二氧基; R 4是氢或卤原子或甲基; R 5和R 6各自 氢原子或基团-OCOCH 2 NR 7 R 8 [其中R 7和R 8可以相同或不同,各自为氢原子或C 3-7环烷基或任选被羟基取代的直链或支链C 1-4烷基 或-NR 7 R 8形成饱和杂环氨基,其具有5-7个环成员并且任选地在环中含有氧或硫原子或-NH-或-N(R)基团,其中R是任选的C 1-4烷基 被羟基取代],条件是当R 5和R 6中的一个为氢原子时,另一个为-OCOCH 2 NR 7 R 8基团)可以由上式 其中R5和/或R6是基团-OCOCH2L的相应化合物,其中L是可置换的离去基团。 式(I)化合物及其生理学上可接受的盐表现出有趣的抗癌作用。