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91 条记录 (耗时 0.143 秒)

    9-substituted adenine derivatives as prodrug regulators of cell and tissue function
    58.
    发明授权
    9-substituted adenine derivatives as prodrug regulators of cell and tissue function 失效
    9-取代的腺嘌呤衍生物作为细胞和组织功能的前体调节剂

    公开(公告)号：US07045309B2

    公开(公告)日：2006-05-16

    申请号：US10332314

    申请日：2001-07-06

    申请人： Roger A. Johnson ,  Praveen Pande ,  Wolfgang Laux ,  Gilles Gosselin

    发明人： Roger A. Johnson ,  Praveen Pande ,  Wolfgang Laux ,  Gilles Gosselin

    IPC分类号： G01N33/53 ,  C07H19/20

    CPC分类号： C07H19/20

    摘要： The present invention relates to 9-substituted adenine derivatives represented by formula (I) wherein W is selected from the group consisting of H, halogen, azido and amino group; X is selected from the group consisting of O, S, N(H), CH2, CH and C; Y is selected from the group consisting of H, hydroxy, C1-4 alkyl, C1-4 alkoxy and halogen; R is selected from the group consisting of H, hydroxymethyl, C1-4 alkyl, and C1-4 alkoxy; R1is selected from the group consisting of O, NH and CH2; R2represents a radical selected from the group consisting of —(CH2)n—S—C(O)—R4 and —(CH2)n—S—S—R4, where n=1-4 and R4is a C1-4-alkyl or aryl group and R4 is optionally substituted with a halogen, amino, N-alkylamino, N, N-dialkylamino or C1-4 alkoxy group and wherein each of the R2radicals may be the same or different; and R3is O or S. The derivatives are useful as prodrugs for inhibiting adenylyl cyclase and lowering 3′:5′-cAMP in cells, thereby inhibiting adenylyl cyclase dependent effects within cells.

    摘要翻译： 本发明涉及由式（I）表示的9-取代腺嘌呤衍生物，其中W选自H，卤素，叠氮基和氨基; X选自O，S，N（H），CH 2，CH和C; Y选自H，羟基，C 1-4烷基，C 1-4烷氧基和卤素; R选自H，羟甲基，C 1-4烷基和C 1-4烷氧基; R 1选自O，NH和CH 2; R 2表示选自以下的基团： - （CH 2）n --SC（O）-R 4 其中n = 1-4和R 4 和 - （CH 2）2 - >是C 1-4烷基或芳基，R 4任选被卤素，氨基，N-烷基氨基，N，N-二烷基氨基或C 其中每个R 2个基团可以相同或不同; R 3为O或S.该衍生物可用作抑制腺苷酸环化酶和降低细胞中3'：5-cAMP的前药，从而抑制细胞内腺苷酸环化酶依赖性作用。

    5-Aza-7-deazapurine derivatives for treating Flaviviridae
    59.
    发明申请
    5-Aza-7-deazapurine derivatives for treating Flaviviridae 审中-公开
    用于治疗黄病毒科的5-氮杂-7-脱氮嘌呤衍生物

    公开(公告)号：US20060040944A1

    公开(公告)日：2006-02-23

    申请号：US11166498

    申请日：2005-06-23

    申请人： Gilles Gosselin ,  Frank Seela ,  Paolo La Colla ,  Richard Storer ,  David Dukhan ,  Frederic Leroy

    发明人： Gilles Gosselin ,  Frank Seela ,  Paolo La Colla ,  Richard Storer ,  David Dukhan ,  Frederic Leroy

    IPC分类号： A61K31/53 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/52 ,  A61K31/522 ,  A61K31/53 ,  C07D519/00

    摘要： This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and/or pestivirus, comprising administering to that host an effective amount of an anti-flavivirus or anti-pestivirus, biologically active compound has a 5-aza-7-deazapurine moiety. The 5-aza-7-deazapurine moiety may be substituted or unsubstituted, and may comprise a nucleoside analogue, or a salt or prodrug thereof. The compound of the present invention may be administered alone or in combination with another anti-hepatitis C, anti-flavivirus and/or anti-pestivirus agent.

    摘要翻译： 本发明涉及用于治疗感染丙型肝炎，黄病毒和/或瘟病毒的宿主，特别是人的方法，包括向该宿主施用有效量的抗黄病毒或抗瘟病毒，生物活性化合物具有 5-氮杂-7-脱氮嘌呤部分。 5-氮杂-7-脱氮嘌呤部分可以是取代或未取代的，并且可以包含核苷类似物或其盐或前药。 本发明的化合物可以单独施用或与另一种抗丙型肝炎，抗黄病毒和/或抗瘟病毒剂组合施用。