发明公开
- 专利标题: MODIFIED BENZIMIDAZOLE NUCLEOSIDES AS ANTIVIRAL AGENTS
- 专利标题(中): 改进的苯并咪唑核苷AS抗病毒药物
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申请号: EP97902982.4申请日: 1997-01-22
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公开(公告)号: EP1019425A1公开(公告)日: 2000-07-19
- 发明人: TOWNSEND, Leroy, B. , DRACH, John, C. , FREEMAN, George, A.
- 申请人: THE REGENTS OF THE UNIVERSITY OF MICHIGAN , GLAXO GROUP LIMITED
- 申请人地址: 3003 S. State StreetWolverine Tower, Room 2071 Ann ArborMichigan 48109-1280 US
- 专利权人: THE REGENTS OF THE UNIVERSITY OF MICHIGAN,GLAXO GROUP LIMITED
- 当前专利权人: THE REGENTS OF THE UNIVERSITY OF MICHIGAN,GLAXO GROUP LIMITED
- 当前专利权人地址: 3003 S. State StreetWolverine Tower, Room 2071 Ann ArborMichigan 48109-1280 US
- 代理机构: Goldin, Douglas Michael
- 优先权: US10463P 19960123
- 国际公布: WO9727204 19970731
- 主分类号: C07H19/052
- IPC分类号: C07H19/052 ; A61K31/70
摘要:
This invention pertains to nucleoside analogs which have antiviral activity and improved metabolic stability. More specifically, this invention pertains to modified sugar benzimidazole nucleosides, as exemplified by compounds such as benzimidazole nucleosides possessing a fluorinated sugar-like moiety (for example, a 2'-fluoro-furanosyl moiety or a 3'-fluoro-furanosyl moiety), and may be represented by formula (I) wherein R1 is a fluorinated sugar-like moiety; and R?2, R4, R5, R6 and R7¿ are benzimidazole substituents, such as -H, halogens (e.g., -F, -C1, -Br, -I), -NO¿2?, -NR2 (where R is independently -H or an alkyl group having 1-6 carbon atoms), -OR (where R is -H or an alkyl group having 1-6 carbon atoms), -SR (where R is -H or a hydrocarbyl of 1-10 carbon atoms), and -CF3. In one embodiment, R?1¿ is 2'-fluoro-furanosyl or 3'-fluoro-furanosyl; R2 is -H, -F, -C1, -Br, -I, or -NR¿2?, wherein R is independently -H or an alkyl group having 1-6 carbon atoms; R?4, R5, R6 and R7¿ are independently -H, -F, -C1, -Br, or -I.
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