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110 条记录 (耗时 0.071 秒)

    Porphyrin and phthalocyanine antiviral compositions
    42.
    发明授权
    Porphyrin and phthalocyanine antiviral compositions 失效
    卟啉和酞菁抗病毒组合物

    公开(公告)号：US5281616A

    公开(公告)日：1994-01-25

    申请号：US873415

    申请日：1992-04-24

    申请人： Dabney W. Dixon ,  Raymond F. Schinazi ,  Luigi G. Marzilli

    发明人： Dabney W. Dixon ,  Raymond F. Schinazi ,  Luigi G. Marzilli

    IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/66 ,  A61K33/24 ,  A61K38/21

    CPC分类号： A61K31/44 ,  A61K31/40 ,  A61K31/66 ,  A61K31/70 ,  A61K33/24 ,  A61K38/21 ,  Y10S530/826

    摘要： Compositions for the inhibition of replication of human immunodeficiency virus containing one or more "porphyrins" possessing antiviral activity. As used herein "porphyrins" includes porphyrins, phthalocyanines, chlorins, metallo derivatives thereof, and other porphyrin-like compounds. Examples of natural and synthetic, positively, negatively, and neutrally charged porphyrins, phthalocyanines, and derivatives thereof have been found to exhibit selective anti-HIV activity which is not dependent on the presence of light.

    摘要翻译： 用于抑制含有一种或多种具有抗病毒活性的“卟啉”的人类免疫缺陷病毒复制的组合物。 如本文所用，“卟啉”包括卟啉，酞菁，二氢卟酚，其金属衍生物和其它卟啉样化合物。 已经发现天然和合成，正，负和中性带电的卟啉，酞菁及其衍生物的实例表现出不依赖于光的选择性抗HIV活性。

    3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents
    43.
    发明授权
    3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents 失效
    3'-叠氮基-2'，3'-脱氧嘧啶和相关化合物作为抗病毒剂

    公开(公告)号：US5190926A

    公开(公告)日：1993-03-02

    申请号：US434521

    申请日：1989-11-06

    申请人： Chung K. Chu ,  Raymond F. Schinazi

    发明人： Chung K. Chu ,  Raymond F. Schinazi

    IPC分类号： C07H19/06 ,  C07H19/10

    CPC分类号： A61K31/70 ,  C07H19/06 ,  C07H19/10

    摘要： A pharmaceutical composition in dosage unit form comprising a therapeutically effective HIV inhibitory amount of a compound having the formula: ##STR1## wherein R.sup.1 is selected from the group consisting of OH, C.sub.1-4 acyl, sulfate phosphate, and amino; R.sup.2 is O or NH, and R.sup.3 C or N, or a pharmacologically acceptable acid addition salt thereof, in association with a pharmaceutical carrier.

    摘要翻译： 一种剂量单位形式的药物组合物，其包含治疗有效的HIV抑制量的具有下式的化合物：其中R 1选自OH，C 1-4酰基，硫酸酯磷酸酯和氨基; R2是O或NH，R3C或N，或其药理学上可接受的酸加成盐，与药物载体结合。

    5'-Diphosphohexose nucleoside pharmaceutical compositions
    44.
    发明授权
    5'-Diphosphohexose nucleoside pharmaceutical compositions 失效
    5'-二磷酸己糖核苷药物组合物

    公开(公告)号：US5159067A

    公开(公告)日：1992-10-27

    申请号：US377617

    申请日：1989-07-10

    申请人： Raymond F. Schinazi ,  Jean-Pierre Sommadossi ,  Chum K. Chung

    发明人： Raymond F. Schinazi ,  Jean-Pierre Sommadossi ,  Chum K. Chung

    IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20

    CPC分类号： C07H19/10 ,  A61K31/70 ,  C07H19/06 ,  C07H19/20

    摘要： Compounds of the general formula: ##STR1## wherein A, B, and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, R.sub.1 and R.sub.2 are hydrogen or alkyl groups of from C.sub.1 to C.sub.10 ; W is oxygen or sulfur; X is oxygen, sulfur, or CH.sub.2 ; Y is a purine or pyrimidine base, and Z is carbon, sulfur, or oxygen. Y can be any purine or pyrimidine base, natural or synthetic, which combines with a sugar to form a biologically active nucleoside. In combination with an appropriate pharmaceutical carrier, the compositions have enhanced activity or increased intracellular absorbment over the parent nucleoside as a function of the 5'-O-diphosphosugar. Another embodiment of the present invention is the enhancement of biologically active nucleosides into cells by preparing and administering the 5'-O-diphosphohexose, 5'-diphospho-N-acetylhexosamine or 5'-diphosphohexosamine derivative of the nucleoside. In the preferred embodiment for therapeutic use, the compounds are provided in a pharmaceutical carrier in an amount sufficient to exhibit as known in vitro or in vivo biological activity.

    摘要翻译： 通式的化合物：其中A，B和C是氢，卤素或叠氮基; D是氢，卤素，叠氮基或OH; A和B或C和D可以用双键替换; R是羟基己糖，醛双己糖胺或N-乙酰基己二胺，R1和R2是氢或C1至C10的烷基; W是氧或硫; X是氧，硫或CH 2; Y是嘌呤或嘧啶碱，Z是碳，硫或氧。 Y可以是天然或合成的任何嘌呤或嘧啶碱，其与糖结合以形成生物活性核苷。 与合适的药物载体组合，作为5'-O-二磷磷酸的功能，组合物具有增强的活性或增加的亲核苷的细胞内吸收。 本发明的另一个实施方案是通过制备和施用核苷的5'-二磷酸己糖，5'-二磷酸-N-乙酰基己糖胺或5'-二磷磷酰胺衍生物来增强生物活性核苷进入细胞。 在用于治疗用途的优选实施方案中，化合物以足以显示已知的体外或体内生物活性的量在药物载体中提供。

    NOVEL HIV-1 REVERSE TRANSCRIPTASE CODON DELETION AND ITS USE IN THE MANAGEMENT AND TREATMENT OF HIV INFECTIONS
    46.
    发明申请
    NOVEL HIV-1 REVERSE TRANSCRIPTASE CODON DELETION AND ITS USE IN THE MANAGEMENT AND TREATMENT OF HIV INFECTIONS 有权
    新型HIV-1逆转录酶去除及其在艾滋病毒感染管理与治疗中的应用

    公开(公告)号：US20100130381A1

    公开(公告)日：2010-05-27

    申请号：US12595358

    申请日：2008-04-10

    申请人： Raymond F. Schinazi

    发明人： Raymond F. Schinazi

    IPC分类号： C40B40/08 ,  C07H21/00 ,  C12N7/00 ,  C12Q1/70

    CPC分类号： C12Q1/703 ,  C12N9/1276 ,  G06F19/18 ,  G06F19/28 ,  Y10S435/911

    摘要： The present invention provides an isolated HIV-1 mutant and isolated nucleic acid molecules comprising HIV-RT coding sequences harboring a novel mutation in the S68 codon, and in particular, deletions of the S68 codon. This novel deletion reduces the sensitivity of HIV to various nucleoside reverse transcriptase inhibitors. Methods of using this mutation for selecting effective antiretroviral agents in vitro and in vivo, methods for monitoring infection progression in HIV-infected individuals and methods for avoiding the emergence of and/or to treat individuals infected with HIV comprising mutations at the S68 codon of HIV-RT, e.g., S68del, are provided.

    摘要翻译： 本发明提供了分离的HIV-1突变体和分离的核酸分子，其包含在S68密码子中具有新突变的HIV-RT编码序列，特别是S68密码子的缺失。 这种新的缺失降低了HIV对各种核苷逆转录酶抑制剂的敏感性。 使用该突变在体外和体内选择有效的抗逆转录病毒药物的方法，用于监测HIV感染个体中的感染进展的方法和用于避免HIV感染的个体和/或治疗感染艾滋病病毒的个体的方法，包括在HIV的S68密码子处的突变 -RT，例如S68del。