Purine analog nucleoside and nucleotide compounds
    2.
    发明授权
    Purine analog nucleoside and nucleotide compounds 失效
    嘌呤类似物核苷和核苷酸化合物

    公开(公告)号:US5446139A

    公开(公告)日:1995-08-29

    申请号:US809506

    申请日:1992-02-21

    CPC分类号: C07H19/04

    摘要: The invention concerns nucleoside derivatives of the formula I ##STR1## in which Ba signifies an indolyl (A), benzimidazolyl (B), pyrrolopyridinyl (C), imidazopyridinyl (D), triazolopyrimidinyl (E), imidazotriazinyl (F) or imidazopyrimidinyl (G) group substituted by R.sup.1, R.sup.2 and R.sup.3, in which R.sup.1, R.sup.2 and R.sup.3, which can be the same or different, signify hydrogen, halogen, a C.sub.1 -C.sub.7 -alkyl, C.sub.2 -C.sub.7 -alkenyl, hydroxy, mercapto, C.sub.1 -C.sub.7 -alkylthio, C.sub.1 -C.sub.7 -alkoxy, C.sub.2 -C.sub.7 -alkenyloxy, ar-C.sub.1 -C.sub.5 -alkyl, ar-C.sub.2 -C.sub.5 -alkenyl, ar-C.sub.1 -C.sub.5 -alkoxy, ar-C.sub.2 -C.sub.5 -alkenyloxy, aryloxy, nitro, amino-C.sub.1 -C.sub.7 -alkyl, C.sub.1 -C.sub.7 -alkylamino-C.sub.1 -C.sub.7 -alkyl, di-C.sub.1 -C.sub.7 -alkylamino-C.sub.1 -C.sub.7 -alkyl, amino, a substituted amino group --NMR.sup.4 or --N(R.sup.4).sub.2 or an imino group --N.dbd.CH--R.sup.4, and R.sup.4 has the meaning given in the description, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 each signify hydrogen or one or two of the radicals R.sup.5, R.sup.6, R.sup.7 and R.sup.8 a hydroxyl, halogen, cyano, azido or a substituted amino group --NHR.sup.4 or --N(R.sup.4).sub.2 or R.sup.5 and R.sup.7 can together represent a further bond between C-2' and C-3' and Y represents hydrogen or a C.sub.1 -C.sub.7 -alkylcarbonyl, monophosphate, diphosphate or triphosphate group, whereby "aryl" signifies a phenyl or naphthyl group and "hetaryl" a furanyl, thienyl or pyridyl group, as well as their possible anomers, N.sup.7 - or N.sup.9 -regioisomers (purine nomenclature), tautomers and salts.

    摘要翻译: PCT No.PCT / EP90 / 00650 Sec。 一九九二年二月二十一日 102(e)日期1992年2月21日PCT提交1990年4月23日PCT公布。 第WO91 / 01325号公报 1991年2月7日,本发明涉及式Ⅰ(I)的核苷衍生物,其中Ba表示吲哚基(A),苯并咪唑基(B),吡咯并吡啶基(C),咪唑并吡啶基(D),三唑并嘧啶基(E ),被R1,R2和R3取代的咪唑并吡嗪基(F)或咪唑并嘧啶基(G)基团,其中可以相同或不同的R 1,R 2和R 3表示氢,卤素,C 1 -C 7 - 烷基, C7-烯基,羟基,巯基,C1-C7-烷硫基,C1-C7-烷氧基,C2-C7-烯氧基,芳基-C1-C5-烷基,ar-C2-C5-烯基,ar-C1-C5-烷氧基, 芳基氧基,硝基,氨基-C 1 -C 7 - 烷基,C 1 -C 7 - 烷基氨基-C 1 -C 7 - 烷基,二-C 1 -C 7 - 烷基氨基-C 1 -C 7 - 烷基,氨基,取代的 氨基-NMR4或-N(R4)2或亚氨基-N = CH-R4,R4具有说明书中给出的含义,R5,R6,R7和R8各自表示氢或一个或两个基团R 5 ,R6,R7和R8是羟基,卤素,氰基,叠氮基或取代的氨基-NHR4或-N(R4)2或R5和R7可以一起代表另一个b C-2'和C-3'之间,Y表示氢或C1-C7-烷基羰基,一磷酸,二磷酸或三磷酸基,其中“芳基”表示苯基或萘基,“杂芳基”是呋喃基,噻吩基或吡啶基 组,以及它们可能的端基异构体,N7-或N9-区域异构体(嘌呤命名法),互变异构体和盐。