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110 条记录 (耗时 0.055 秒)

    3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents
    31.
    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
    32.
    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。

    AZIDO PURINE NUCLEOSIDES FOR TREATMENT OF VIRAL INFECTIONS
    36.
    发明申请
    AZIDO PURINE NUCLEOSIDES FOR TREATMENT OF VIRAL INFECTIONS 审中-公开
    用于治疗病毒感染的AZIDO嘌呤核苷

    公开(公告)号：US20100279969A1

    公开(公告)日：2010-11-04

    申请号：US12599951

    申请日：2008-05-14

    申请人： Raymond F. Schinazi ,  John W. Mellors ,  Nicolas Paul Sluis-Cremer ,  Frank Amblard ,  Steven J. Coats ,  Junxing Shi ,  Richard Anthony Whitaker

    发明人： Raymond F. Schinazi ,  John W. Mellors ,  Nicolas Paul Sluis-Cremer ,  Frank Amblard ,  Steven J. Coats ,  Junxing Shi ,  Richard Anthony Whitaker

    IPC分类号： A61K31/70 ,  C07H19/16 ,  C07D473/00 ,  A61K31/522 ,  A61P31/18

    CPC分类号： C07H19/173 ,  C07D473/16 ,  C07D473/18 ,  C07D473/34

    摘要： The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, HBV, and HCV, in human patients or other animal hosts. The compounds are 3′-azido-2′,3′-dideoxy purine nucleosides or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 resistance mutants including HIV-1K65R, HTV-1K70E, HIV-1L74V, HIV-1M184V, HIV-1Q151M and inhibitory activity against HIV-1 RT harboring TAMS or insertion mutations including HIV-1AZT3, HIV-1AZT7, HIV-1AZT9, HIV-1Q151M, or HIV-169insertion. In one embodiment, the compounds are 3′-azido-ddA, 3′-azido-ddG, or combinations thereof, administered with one or more additional antiviral agents that select for TAM mutations and/or the M 184V mutation, along with a pharmaceutically acceptable carrier.

    摘要翻译： 本发明涉及在人类患者或其他动物宿主中用于治疗或预防病毒感染，特别是HIV，HBV和HCV的化合物，组合物和方法。 化合物是3'-叠氮基-2'，3'-二脱氧嘌呤核苷或膦酸酯，及其药学上可接受的盐，前药和其它衍生物。 特别地，这些化合物显示针对HIV-1抗性突变体（包括HIV-1K65R，HTV-1K70E，HIV-1L74V，HIV-1M184V，HIV-1Q151M）的有效的抗病毒活性，以及​​对携带TAMS或包括HIV的插入突变的HIV-1RT的抑制活性 -1AZT3，HIV-1AZT7，HIV-1AZT9，HIV-1Q151M或HIV-169插入。 在一个实施方案中，化合物是3位 - 叠氮基-ddA，3'-叠氮基-ddG或其组合，与选择TAM突变和/或M 184V突变的一种或多种另外的抗病毒剂一起，连同药物 可接受的载体

    NOVEL HIV-1 REVERSE TRANSCRIPTASE CODON DELETION AND ITS USE IN THE MANAGEMENT AND TREATMENT OF HIV INFECTIONS
    37.
    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。

    2′-fluoronucleosides
    38.
    发明授权
    2′-fluoronucleosides 有权
    2'-核糖核苷

    公开(公告)号：US07662938B2

    公开(公告)日：2010-02-16

    申请号：US11942551

    申请日：2007-11-19

    申请人： Raymond F. Schinazi ,  Dennis C. Liotta ,  Chung K. Chu ,  J. Jeffrey McAtee ,  Junxing Shi ,  Yongseok Choi ,  Kyeong Lee ,  Joon H. Hong

    发明人： Raymond F. Schinazi ,  Dennis C. Liotta ,  Chung K. Chu ,  J. Jeffrey McAtee ,  Junxing Shi ,  Yongseok Choi ,  Kyeong Lee ,  Joon H. Hong

    IPC分类号： C07G3/00 ,  C07H21/00 ,  C07H21/02 ,  C12Q1/68

    CPC分类号： A61K31/7076 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/708 ,  C07D405/04 ,  C07D473/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16

    摘要： A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formula: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, lower alkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or aryalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 公开了一类可用于治疗乙型肝炎感染，丙型肝炎感染，HIV和异常细胞增殖（包括肿瘤和癌症）的2'-氟 - 核苷化合物。 所述化合物具有以下通式：其中碱是嘌呤或嘧啶碱; R 1是OH，H，OR 3，N 3，CN，卤素，包括F或CF 3，低级烷基，氨基，低级烷基氨基，二（低级）烷基氨基或烷氧基，碱是指嘌呤或嘧啶碱基; R2是H，磷酸盐，包括单磷酸盐，二磷酸盐，三磷酸盐或稳定的磷酸盐前体药物; 酰基或其它药学上可接受的离去基团，其在体内施用时能够提供其中R 2为H或磷酸酯的化合物; 磺酸酯，包括烷基或芳烷基磺酰基，包括甲磺酰基，苄基，其中苯基任选被一个或多个取代基取代，如上文给出的芳基的定义，脂质，氨基酸，肽或胆固醇; 并且R3是酰基，烷基，磷酸酯或其它药学上可接受的离去基团，当其在体内施用时，能够被切割成母体化合物或其药学上可接受的盐。