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    Arylsulfonyloxy purine intermediates
    3.
    发明授权
    Arylsulfonyloxy purine intermediates 失效
    芳基磺酰氧基嘌呤中间体

    公开(公告)号：US4897479A

    公开(公告)日：1990-01-30

    申请号：US165360

    申请日：1988-02-29

    申请人： Richard L. Tolman ,  Wallace Ashton ,  Malcolm Maccoss

    发明人： Richard L. Tolman ,  Wallace Ashton ,  Malcolm Maccoss

    IPC分类号： C07D473/00 ,  C07F9/6561

    CPC分类号： C07D473/00 ,  C07F9/65616

    摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R.sup.1 is halogen, --SR.sup.4 wherein R.sup.4 is H or alkyl of 1 to 4 carbon atoms, --OCH.sub.3, --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, --NR.sup.4 R.sup.5 wherein R.sup.4 is as defined above and R.sup.5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R.sup.1 is --N(CH.sub.3).sub.3.sup.+ X.sup.-whereinX is halogen or --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms;R.sup.2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl;R.sup.3 is A or B whereinA is ##STR2## and B is ##STR3## wherein R.sup.6 and R.sup.7 are independently selected from H and ##STR4## wherein R.sup.8 and R.sup.9 are independently selected from pharmaceutically acceptable cations and H, or R.sup.6 and R.sup.7 taken together are ##STR5## wherein R.sup.10 is selected from pharmaceutically acceptable cations and H; with the proviso that R.sup.4 is not H when: R.sup.5 is H, R.sup.3 is A, and R.sup.6 and R.sup.7 are H. The compounds have anti-viral activity.

    摘要翻译： 公开了式“IMAGE”的化合物及其药学上可接受的盐。 在这些化合物中，R 1是卤素，-SR 4，其中R 4是H或1-4个碳原子的烷基，-OCH 3，-OSO 2 Ar，其中Ar是苯基或烷基取代的苯基，其中烷基具有1-6个碳原子，-NR4R5其中 R 4如上所定义，R 5为H，具有1至4个碳原子的烷基，氨基，1至8个碳原子的烷酰基，苯甲酰基，甲氧基或羟基或R 1为-N（CH 3）3 + X-，其中X为卤素或 -OSO 2 Ar，其中Ar是苯基或烷基取代的苯基，其中烷基具有1至6个碳原子; R2是H，1-8个碳原子的烷酰基或苯甲酰基; R3是A或B，其中A是，B是，其中R6和R7独立地选自H和IMA，其中R8和R9独立地选自药学上可接受的阳离子，H或R6和R7一起 其中R 10选自药学上可接受的阳离子和H; 条件是当R 5为H，R 3为A且R 6和R 7为H时，R 4不为H。化合物具有抗病毒活性。

    Prodrugs of herpes TK inhibitors
    6.
    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。