公开(公告)号：US06211158B1

公开(公告)日：2001-04-03

申请号：US07908513

申请日：1992-06-26

申请人： Frank Seela ,  Heinz-Peter Muth ,  Klaus Kaiser ,  Werner Bourgeois ,  Klaus Mühlegger ,  Herbert Von der Eltz ,  Hans-Georg Batz

发明人： Frank Seela ,  Heinz-Peter Muth ,  Klaus Kaiser ,  Werner Bourgeois ,  Klaus Mühlegger ,  Herbert Von der Eltz ,  Hans-Georg Batz

IPC分类号： A01N4304

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20

摘要： The present invention provides desazapurine-nucleoside derivatives of the general formula: wherein X is a nitrogen atom or a methine radical, W is a nitrogen atom or a C—R4 radical, R1, R2, R3 and R4, which can be the same or different, are hydrogen or halogen atoms, hydroxyl or mercapto groups, lower alkyl, lower alkylthio, lower alkoxy, aralkyl, aralkoxy or aryloxy radicals or amino groups optionally substituted once or twice, R5 is a hydrogen atom or a hydroxyl group, R6 and R7 are each hydrogen atoms or one of them is a halogen atom or a cyano or azido group or an amino group optionally substituted once or twice, whereby one of R6 and R7 can also be a hydroxyl group when X is a methine radical and, in addition, R5 and R7 can together also represent a further valency bond between C-2′ and C-3′ and Y is a hydrogen atom or a mono-, di- or tri-phosphate group.

摘要翻译： 本发明提供了以下通式的脱氮嘌呤 - 核苷衍生物：其中X是氮原子或次甲基，W是氮原子或C-R 4基团，R 1，R 2，R 3和R 4可以相同或 不同的是氢或卤素原子，羟基或巯基，低级烷基，低级烷硫基，低级烷氧基，芳烷基，芳烷氧基或芳氧基或任选取代一次或两次的氨基，R5是氢原子或羟基，R6和R7 各自为氢原子或其中一个为卤素原子或氰基或叠氮基或任选取代一次或两次的氨基，其中当X为次甲基时，R6和R7中的一个也可为羟基，另外 ，R 5和R 7一起也代表C-2'和C-3'之间的进一步的价键，Y是氢原子或一，二或三磷酸基。