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110 条记录 (耗时 0.046 秒)

    Use of (R)-Penciclovir Triphosphate for the Manufacture of a Medicament for the Treatment of Viral Diseases
    3.
    发明申请
    Use of (R)-Penciclovir Triphosphate for the Manufacture of a Medicament for the Treatment of Viral Diseases 审中-公开
    （R） - 普罗昔洛韦三磷酸酯用于制造药物治疗病毒性疾病的用途

    公开(公告)号：US20110092458A1

    公开(公告)日：2011-04-21

    申请号：US12976599

    申请日：2010-12-22

    申请人： Richard Anthony Vere Hodge ,  Raymond F. Schinazi

    发明人： Richard Anthony Vere Hodge ,  Raymond F. Schinazi

    IPC分类号： A61K31/675 ,  A61P31/18

    CPC分类号： A61K31/522 ,  A61K31/661

    摘要： A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.

    摘要翻译： 一种治疗方法：i）哺乳动物，包括人类中的HIV-1感染; 或ii）哺乳动物，包括人类中的HBV感染; 该方法包括向需要这种治疗的人施用有效量的式（A）化合物的三磷酸的（R） - 对映异构体或其药学上可接受的盐; 和用于该方法的化合物。

    POTENT COMBINATIONS OF ZIDOVUDINE AND DRUGS THAT SELECT FOR THE K65R MUTATION IN THE HIV POLYMERASE
    4.
    发明申请
    POTENT COMBINATIONS OF ZIDOVUDINE AND DRUGS THAT SELECT FOR THE K65R MUTATION IN THE HIV POLYMERASE 审中-公开
    在HIV聚合酶中选择K65R突变的ZIDOVUDINE和药物的POTENT组合

    公开(公告)号：US20110053884A1

    公开(公告)日：2011-03-03

    申请号：US12680874

    申请日：2008-09-29

    申请人： Raymond F. Schinazi

    发明人： Raymond F. Schinazi

    IPC分类号： A61K31/7072 ,  A61P31/18 ,  A61P31/14

    CPC分类号： A61K31/505 ,  A61K31/70 ,  A61K31/7072 ,  A61K2300/00

    摘要： Combinations of antiretroviral nucleoside reverse transcriptase inhibitors, and methods for their use in treating retroviral infections, are provided. In one embodiment, the combinations include non-thymidine nucleoside antiretroviral agents, such as tenofovir-DF, abacavir, APD and DAPD, that select for the K65R mutation and relatively low doses of zidovudine (AZT) or other thymidine nucleoside antiretroviral agents. The thymidine nucleoside antiretroviral agents retard development of the K65R mutation, and at the low doses, are less likely to produce side effects. In another embodiment, the combinations include DAPD and AZT. DAPD retards the development of TAMs, and AZT retards the development of the K65R mutation. In a third embodiment, the combinations include adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.

    摘要翻译： 提供抗逆转录病毒核苷逆转录酶抑制剂的组合及其用于治疗逆转录病毒感染的方法。 在一个实施方案中，组合包括选择K65R突变和相对低剂量的齐多夫定（AZT）或其他胸苷核苷抗逆转录病毒剂的非胸苷核苷抗逆转录病毒试剂，如替诺福韦DF，阿巴卡韦，APD和DAPD。 胸苷核苷抗逆转录病毒药物阻碍K65R突变的发展，而在低剂量下，不太可能产生副作用。 在另一个实施方案中，组合包括DAPD和AZT。 DAPD阻碍TAM的发展，AZT阻碍K65R突变的发展。 在第三个实施方案中，组合包括腺嘌呤，胞嘧啶，胸苷和鸟嘌呤核苷抗病毒剂，进一步与至少一种通过不同于核苷类似物的机制起作用的其它抗病毒剂组合。 这种组合有可能在感染患者中消除艾滋病毒的存在。

    Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane
    6.
    发明申请
    Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane 审中-公开
    2-羟甲基-5（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷的抗病毒活性和拆分

    公开(公告)号：US20090048190A1

    公开(公告)日：2009-02-19

    申请号：US12150964

    申请日：2008-05-02

    申请人： Dennis C. Liotta ,  Raymond F. Schinazi ,  Woo-Baeg Choi

    发明人： Dennis C. Liotta ,  Raymond F. Schinazi ,  Woo-Baeg Choi

    IPC分类号： A61K31/506 ,  A61K31/7052 ,  A61P31/12

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    摘要： A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

    摘要翻译： 公开了用于治疗人体中HIV和HBV感染的方法和组合物，其包括给予有效量的2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷，其药学上可接受的衍生物 ，包括5'或N4烷基化或酰化衍生物或其药学上可接受的盐在药学上可接受的载体中。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。

    [5-carboxamido or 5-fluoro]-[2',3'-unsaturated or 3'-modified]-pyrimidine nucleosides
    7.
    发明申请
    [5-carboxamido or 5-fluoro]-[2',3'-unsaturated or 3'-modified]-pyrimidine nucleosides 审中-公开
    [5-甲酰氨基或5-氟] - [2'，3'-不饱和或3'-修饰] - 嘧啶核苷

    公开(公告)号：US20080293668A1

    公开(公告)日：2008-11-27

    申请号：US12220609

    申请日：2008-07-25

    申请人： Raymond F. Schinazi ,  Dennis C. Liotta

    发明人： Raymond F. Schinazi ,  Dennis C. Liotta

    IPC分类号： A61K31/7064 ,  C07H19/06 ,  A61P31/14 ,  A61P31/18

    CPC分类号： A61K31/7068 ,  A61K31/70 ,  A61K45/06 ,  C07H19/06 ,  A61K2300/00

    摘要： A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2′,3′-dideoxy-2′,3′-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3′-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.

    摘要翻译： 公开了用于治疗人和其他宿主动物中的HIV和HBV感染的方法和组合物，其包括给予有效量的[5-甲酰氨基或5-氟] -2'，3'-二脱氧-2' ，3'-二脱氢嘧啶核苷或[5-甲酰氨基或5-氟] -3'-修饰的嘧啶核苷或其混合物或药学上可接受的衍生物，包括5'或N4烷基化或酰化衍生物，或 其药学上可接受的盐在药学上可接受的载体中。

    Enzyme inhibitors, their synthesis, and methods for use
    10.
    再颁专利
    Enzyme inhibitors, their synthesis, and methods for use 失效
    酶抑制剂，它们的合成和使用方法

    公开(公告)号：USRE37623E1

    公开(公告)日：2002-04-02

    申请号：US08980629

    申请日：1997-12-01

    申请人： Mahmoud H. el Kouni ,  Fardos N. M. Naguib ,  Raymond F. Schinazi

    发明人： Mahmoud H. el Kouni ,  Fardos N. M. Naguib ,  Raymond F. Schinazi

    IPC分类号： C07D23936

    CPC分类号： C07D239/24 ,  C07D239/60

    摘要： Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is H or an acyclo tail having the general formula where R2 is H, CH2 OH or CH2 NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.

    摘要翻译： 提供了有效抑制DHUDase或UrdPase活性的新型化合物。 这些化合物具有通式，X是S或Se; Y是 H， I，F，Cl，Br，甲氧基， ，硒基苯基或噻吩基，并且R 1是 H或