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    ANTIVIRAL NUCLEOSIDE ANALOGUES CONTAINING A SUBSTITUTED BENZIMIDAZOLE BASE ATTACHED TO A CARBOCYCLIC RING
    2.
    发明公开
    ANTIVIRAL NUCLEOSIDE ANALOGUES CONTAINING A SUBSTITUTED BENZIMIDAZOLE BASE ATTACHED TO A CARBOCYCLIC RING 失效
    抗病毒药NUKELOSIDANALOGE其中一个取代的苯并咪唑与链接甲碳环INCLUDED

    公开(公告)号：EP0779885A1

    公开(公告)日：1997-06-25

    申请号：EP95934402.0

    申请日：1995-09-11

    申请人： THE WELLCOME FOUNDATION LIMITED ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN

    发明人： TOWNSEND, Leroy, B. ,  DALUGE, Susan, Mary

    IPC分类号： A61K31 ,  A61P31 ,  C07D235 ,  C07D403

    CPC分类号： C07D403/04 ,  C07D235/30

    摘要： Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue. In formulae (I) and (I-1), R1 is H, CH¿3? or CH2OH; R?2¿ is H or OH; R3 is H or OH; or R?2 and R3¿ together form a bond; R4 is amino, cyclopropylamino, cyclobutylamino, isopropylamino, tert-butylamino or -NR8R9 where R?8 and R9¿ together with the nitrogen atom to which they are attached form a 4, 5 or 6-membered heterocyclic ring; R5 is H and R?6 and R7¿ are Cl, excluding the compound (±)-(1R*, 2S*, 3S*, 5S*)-5-[5,6-Dichloro-2-(cyclopropylamino)-1H-benzimidazol-1-yl]-3-(hydroxymethyl)-1,2-cyclopentanediol and provided that at least one of R?1, R2 and R3¿ is or contains OH. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.

    LYXOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS
    4.
    发明公开
    LYXOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS 失效
    LYX非呋喃酰基苯并咪唑作为抗病毒药物

    公开(公告)号：EP1000080A1

    公开(公告)日：2000-05-17

    申请号：EP98937254.5

    申请日：1998-07-29

    申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  GLAXO GROUP LIMITED

    发明人： TOWNSEND, Leroy, B. ,  DRACH, John, C. ,  BIRON, Karen,K. ,  BOYD, Frank,L. Jr.

    IPC分类号： C07H19/052 ,  A61K31/70

    CPC分类号： C07H19/052 ,  Y02P20/55

    摘要： The present invention pertains to D- and L-lyxofuranosyl benzimidazole compounds. In one embodiment, the present invention pertains to D- and L-lyxofuranosyl benzimidazole compounds selected from the group consisting of compounds having a formula selected from the following: (beta-D), (beta-L), (alpha-L) and (alpha-D) wherein R?2, R4, R5, R6, and R7¿ are independently the same or different and independently selected from the group consisting of: -H, -F, -Cl, -Br, -I, -NO¿2?, -N(R?8)¿2, -OR?8, -SR12¿, and -CF¿3?, wherein R?8¿ is independently -H or an alkyl group having 1-6 carbon atoms and wherein R12 is independently -H or a hydrocarbyl group having 1-10 carbon atoms; and R?9, R10 and R11¿ are independently the same or different and are H or a hydroxyl protecting group; anomeric and optical isomers thereof; and pharmaceutically acceptable salts and prodrug derivatives thereof. The present invention also pertains to antiviral compositions using these compounds, methods of treating a viral infection using these compounds, and the use of these compounds in the preparation of a medicament for use in the treatment of a viral infection.

    摘要翻译： 本发明涉及D-和L-左旋呋喃糖基苯并咪唑化合物。 在一个实施方案中，本发明涉及选自具有选自以下结构式的化合物的D-和L-来苏呋喃糖基苯并咪唑化合物：（β-D），（β-L），（α-L）和 （α-D）其中R 2，R 4，R 5，R 6和R 7'独立地相同或不同并且独立地选自：-H，-F，-Cl，-Br，-I， - -N（R 8）2，-OR 8，-SR 12和-CF 3，其中R 8独立地为-H或具有1-6个碳原子的烷基 并且其中R 12独立地为-H或具有1-10个碳原子的烃基; R9，R10和R11独立地是相同或不同的，并且是H或羟基保护基; 它们的端基异构体和光学异构体; 及其药学上可接受的盐和前药衍生物。 本发明还涉及使用这些化合物的抗病毒组合物，使用这些化合物治疗病毒感染的方法，以及这些化合物在制备用于治疗病毒感染的药物中的用途。

    PYRROLO(2,3-D)PYRIMIDINE DERIVATIVES AS ANTIVIRALS
    5.
    发明公开
    PYRROLO(2,3-D)PYRIMIDINE DERIVATIVES AS ANTIVIRALS 失效
    吡咯并（2,3-d）嘧啶衍生物作为抗病毒化合物

    公开(公告)号：EP0746559A1

    公开(公告)日：1996-12-11

    申请号：EP95911092.0

    申请日：1995-02-23

    申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

    发明人： TOWNSEND, Leroy, B. ,  DRACH, John, C. ,  RENAU, Thomas, E.

    IPC分类号： A61K31 ,  A61P31 ,  C07D487

    CPC分类号： C07D487/04

    摘要： This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and superior antiviral activity than known nucleoside, non-nucleoside, and non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidine derivatives, particularly against human DNA viruses such as cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1). These compounds are represented by formula (I) wherein R4 is -NH¿2? or -NHCH3; R?5¿ is -CN, -CSNH¿2?, or -CSeNH2; R?6¿ is -H or -NH¿2?; and R?7¿ is selected from the group consisting of aryls and aralkyls having 6 to 30 carbon atoms; aliphatic oxy-hydrocarbyls having 2 to 15 carbon atoms, lacking free hydroxyl groups and further lacking acyl or acyl derivatized groups; and oxy-hydrocarbyls having 6 to 30 carbon atoms, at least one aryl or aralkyl group, and only one oxy-group; with the proviso that if R5 is -CN and R6 is -H, then R4 is -NH¿2? and R?7¿ is -CH¿2?C6H4-2-CH3.

    5'-SUBSTITUTED-RIBOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS
    8.
    发明授权
    5'-SUBSTITUTED-RIBOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS 失效
    5'-取代的呋喃核糖基的苯并咪唑作为抗病毒药。

    公开(公告)号：EP0845001B1

    公开(公告)日：2002-11-13

    申请号：EP96928176.5

    申请日：1996-08-16

    申请人： The Regents of The University of Michigan

    发明人： TOWNSEND, Leroy, B. ,  DRACH, John, C.

    IPC分类号： C07H19/052 ,  A61K31/70

    CPC分类号： C07H19/052

    摘要： The present invention relates to polysubstituted benzimidazoles, having formula (I), wherein Q is substituted benzimidazole group attached at the benzimidazole 1-position; R is a halogen or atomic number 9 to 53, inclusive (i.e., -F, -Cl, -Br, or -I); azido (i.e., -N3); or -X-R1, wherein X is a chalcogen of atomic number 8 to 16, inclusive (i.e., -O- or -S-), and R1 may be straight or branched chain alkyl of 1 to 8 carbon atoms; and R2 and R3 may be the same or different and are separately -O-C(=O)CH3 (i.e., -OAc) or hydroxy (i.e., -OH); and pharmaceutically acceptable salts and operative combinations thereof. Also provided by this invention are compositions comprising a polysubstituted benzimidazoles as defined above and methods of use thereof.

    MODIFIED BENZIMIDAZOLE NUCLEOSIDES AS ANTIVIRAL AGENTS
    9.
    发明公开
    MODIFIED BENZIMIDAZOLE NUCLEOSIDES AS ANTIVIRAL AGENTS 失效
    改进的苯并咪唑核苷AS抗病毒药物

    公开(公告)号：EP1019425A1

    公开(公告)日：2000-07-19

    申请号：EP97902982.4

    申请日：1997-01-22

    申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  GLAXO GROUP LIMITED

    发明人： TOWNSEND, Leroy, B. ,  DRACH, John, C. ,  FREEMAN, George, A.

    IPC分类号： C07H19/052 ,  A61K31/70

    CPC分类号： C07D471/04 ,  C07H7/06 ,  C07H9/04 ,  C07H11/00 ,  C07H19/052

    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.

    5'-SUBSTITUTED-RIBOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS
    10.
    发明公开
    5'-SUBSTITUTED-RIBOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS 失效
    5'-取代基 - 呋喃糖基苯并咪唑烷基硫脲。

    公开(公告)号：EP0845001A1

    公开(公告)日：1998-06-03

    申请号：EP96928176.0

    申请日：1996-08-16

    申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

    发明人： TOWNSEND, Leroy, B. ,  DRACH, John, C.

    IPC分类号： C07H19 ,  A61K31 ,  A61P31

    CPC分类号： C07H19/052

    摘要： The present invention relates to polysubstituted benzimidazoles, having formula (I), wherein Q is substituted benzimidazole group attached at the benzimidazole 1-position; R is a halogen or atomic number 9 to 53, inclusive (i.e., -F, -Cl, -Br, or -I); azido (i.e., -N3); or -X-R1, wherein X is a chalcogen of atomic number 8 to 16, inclusive (i.e., -O- or -S-), and R1 may be straight or branched chain alkyl of 1 to 8 carbon atoms; and R2 and R3 may be the same or different and are separately -O-C(=O)CH3 (i.e., -OAc) or hydroxy (i.e., -OH); and pharmaceutically acceptable salts and operative combinations thereof. Also provided by this invention are compositions comprising a polysubstituted benzimidazoles as defined above and methods of use thereof.