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    AZIDO PURINE NUCLEOSIDES FOR TREATMENT OF VIRAL INFECTIONS
    41.
    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
    42.
    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
    43.
    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。

    2'-FLUORONUCLEOSIDES
    46.
    发明申请
    2'-FLUORONUCLEOSIDES 有权
    2'-氟核苷酸

    公开(公告)号：US20080300398A1

    公开(公告)日：2008-12-04

    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： C07H1/00

    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 formulae: 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。

    Nucleoside with anti-hepatitis B virus activity
    49.
    发明授权
    Nucleoside with anti-hepatitis B virus activity 有权
    核苷含抗乙型肝炎病毒活性

    公开(公告)号：US06458773B1

    公开(公告)日：2002-10-01

    申请号：US09435261

    申请日：1999-11-05

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    IPC分类号： A61K3170

    CPC分类号： C07H19/06 ,  C07H19/10

    摘要： Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′is H, acyl, or alkyl.

    摘要翻译： 提供了针对乙型肝炎病毒的化合物和药物组合物，提供了在人和其他宿主动物中治疗乙型肝炎病毒感染的方法，包括施用有效量的β-L-（2'-3'- 叠氮基）-2'，3'-二脱氧-5-氟胞嘧啶R是H，酰基，单磷酸，二磷酸或三磷酸，或稳定的磷酸酯衍生物（形成稳定的核苷酸前药），R'H， 酰基或烷基。

    &bgr;-L nucleosides for the treatment of HIV infection
    50.
    发明授权
    &bgr;-L nucleosides for the treatment of HIV infection 失效
    β-L核苷用于治疗HIV感染

    公开(公告)号：US06407077B1

    公开(公告)日：2002-06-18

    申请号：US09435268

    申请日：1999-11-05

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    IPC分类号： A61K317068

    CPC分类号： A61K31/7068

    摘要： Compounds and pharmaceutical compositions active against HIV are provided, as is a method for the treatment of HIV infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′ or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′ is H, acyl, or alkyl.

    摘要翻译： 提供了对HIV有活性的化合物和药物组合物，如在人和其他宿主动物中治疗HIV感染的方法一样，提供有效量的β-L-（2'或3'-叠氮基）-2 '，3' - 二脱氧-5-氟胞嘧啶R是H，酰基，单磷酸，二磷酸或三磷酸，或稳定的磷酸酯衍生物（形成稳定的核苷酸前药），R'是H，酰基或烷基 。