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    Prodrugs of herpes TK inhibitors
    5.
    发明授权
    Prodrugs of herpes TK inhibitors 失效
    疱疹TK抑制剂的前药

    公开(公告)号：US5663175A

    公开(公告)日：1997-09-02

    申请号：US353475

    申请日：1994-12-09

    申请人： Richard L. Tolman ,  John D. Karkas ,  Derek Von Langen ,  Malcolm MacCoss

    发明人： Richard L. Tolman ,  John D. Karkas ,  Derek Von Langen ,  Malcolm MacCoss

    IPC分类号： C07D473/00 ,  C07F9/6561 ,  A61K31/52

    CPC分类号： C07D473/00 ,  C07F9/65616 ,  Y10S514/931 ,  Y10S514/934

    摘要： Certain prodrugs such as ##STR1## are useful in the inhibition of herpes virus thymidine kinase, the prevention or treatment of recurrent infection by herpes virus, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating recurrent infection by herpes virus are also described.

    摘要翻译： 某些前药如“IMAGE”可用于抑制疱疹病毒胸苷激酶，预防或治疗疱疹病毒的复发性感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其它抗病毒药物组合， 免疫调节剂，抗生素或疫苗。 还描述了预防或治疗疱疹病毒复发性感染的方法。

    N-alkylguanine acyclonucleosides as antiviral agents
    7.
    发明授权
    N-alkylguanine acyclonucleosides as antiviral agents 失效
    N-烷基鸟嘌呤非循环核苷作为抗病毒剂

    公开(公告)号：US4579849A

    公开(公告)日：1986-04-01

    申请号：US597785

    申请日：1984-04-06

    申请人： Malcolm MacCoss ,  Richard L. Tolman ,  Robert A. Strelitz

    发明人： Malcolm MacCoss ,  Richard L. Tolman ,  Robert A. Strelitz

    IPC分类号： C07D473/18 ,  A61K31/52 ,  A61K31/522 ,  A61K31/675 ,  A61P31/12 ,  A61P31/22 ,  C07D473/00 ,  C07F9/6561

    CPC分类号： C07D473/00 ,  C07F9/65616

    摘要： Disclosed are compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.1 and R.sup.2 are independently alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, each having 1 to 19 carbon atoms, or R.sup.2 is hydrogen; R.sup.3 is hydrogen, alkyl having 1 to 6 carbon atoms or hydroxyalkyl having 1 to 6 carbon atoms; R.sup.4 is hydrogen, halogen, amino or alkyl having 1 to 4 carbon atoms; R.sup.5, R.sup.6 and R.sup.7 are independently selected from hydrogen, hydroxy, alkyl having 1 to 6 carbon atoms, acyloxy having 1 to 8 carbon atoms, alkoxy having 1 to 6 carbon atoms, hydroxyalkyl having 1 to 6 carbon atoms, acyloxyalkyl having 1 to 12 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms and --PO.sub.3.sup.=, or two of R.sup.5, R.sup.6 and R.sup.7 taken together form a group --OPO.sub.2 O.sup.- --, --CH.sub.2 OPO.sub.2 O.sup.- --, --CH.sub.2 OPO.sub.2 OPO.sub.2 O.sup.= --, or --OPO.sub.2 OPO.sub.2 O.sup.= --; A is O, S or CH.sub.2 and X is a pharmaceutically acceptable anion. The compounds have antiviral activity, especially against viruses of the herpes class.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中R 1和R 2独立地为烷基，卤代烷基，烯基，卤代烯基，炔基或卤代炔基，各自具有1至19个碳原子，或R 2为氢; R3是氢，具有1至6个碳原子的烷基或具有1至6个碳原子的羟烷基; R4是氢，卤素，氨基或具有1至4个碳原子的烷基; R5，R6和R7独立地选自氢，羟基，具有1至6个碳原子的烷基，具有1至8个碳原子的酰氧基，具有1至6个碳原子的烷氧基，具有1至6个碳原子的羟烷基，具有1至12个碳原子的酰氧基烷基 碳原子，氨基，1至6个碳原子的烷基氨基和-PO 3 =，或者R 5，R 6和R 7中的两个一起形成基团-OPO 2 O - ， - CH 2 OPO 2 - + 13，-CH 2 OPO 2 OPO 2 - =或 - - ; A是O，S或CH 2，X是药学上可接受的阴离子。 这些化合物具有抗病毒活性，特别是抗疱疹病毒。

    Cyclic monophosphates of purine and pyrimidine acyclonucleosides as anti-retroviral agents
    8.
    发明授权
    Cyclic monophosphates of purine and pyrimidine acyclonucleosides as anti-retroviral agents 失效
    作为抗逆转录病毒剂的嘌呤和嘧啶环己基核苷的环磷酸单磷酸酯

    公开(公告)号：US4966895A

    公开(公告)日：1990-10-30

    申请号：US305234

    申请日：1989-02-02

    申请人： Richard L. Tolman ,  Malcolm MacCoss

    发明人： Richard L. Tolman ,  Malcolm MacCoss

    IPC分类号： A61K31/675

    CPC分类号： A61K31/675

    摘要： The present invention relates to a method for treating mammals having acquired immuno-deficiency syndrome (AIDS) or AIDS-related complex or who are infected with other retroviruses, which comprises the administration of a therapeutically effective amount of a cyclic monophosphate derivative of a purine or pyrimidine acyclonucleoside. Process for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及一种用于治疗具有获得性免疫缺陷综合征（AIDS）或AIDS相关复合物或被其他逆转录病毒感染的哺乳动物的方法，其包括施用治疗有效量的嘌呤的环状单磷酸酯衍生物或 嘧啶阿昔洛韦。 还公开了制备这些化合物的方法和含有其活性成分的化合物的组合物。

    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
    10.
    发明申请
    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase 审中-公开
    核苷衍生物作为rna依赖性rna病毒聚合酶的抑制剂

    公开(公告)号：US20060234962A1

    公开(公告)日：2006-10-19

    申请号：US10517294

    申请日：2003-06-23

    申请人： David Olsen ,  Malcolm MacCoss ,  Balkrishen Bhat ,  Anne Eldrup

    发明人： David Olsen ,  Malcolm MacCoss ,  Balkrishen Bhat ,  Anne Eldrup

    IPC分类号： A61K31/7076 ,  C07H19/16 ,  C07H19/22

    CPC分类号： C07H19/22 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20

    摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

    摘要翻译： 本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。 这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。 本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。 还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。