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    Synthesis and use of 2′-substituted-N6 -modified nucleosides
    1.
    发明授权
    Synthesis and use of 2′-substituted-N6 -modified nucleosides 有权
    2'-取代-N6修饰核苷的合成与应用

    公开(公告)号：US07799908B2

    公开(公告)日：2010-09-21

    申请号：US10542235

    申请日：2004-01-15

    申请人： Haoyun An ,  Kanda Ramasamy ,  Stephanie Shaw

    发明人： Haoyun An ,  Kanda Ramasamy ,  Stephanie Shaw

    IPC分类号： C07H19/167 ,  C07H19/173

    CPC分类号： C07H19/16

    摘要： An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.

    摘要翻译： 制备糖改性核苷类似物的改进方法包括其中在对应的羰基的亲核改性之前糖的羟基被选择性脱保护和氧化的方案。 然后将修饰的糖偶联到杂环基，其在另外的步骤中用双重亲核试剂修饰，其提供具有高立体选择性的N6-修饰的腺苷类似物。

    4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS
    3.
    发明申请
    4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS 失效
    作为艾滋病毒抗体的4-氰基亚氨基取代的双环杂环化合物

    公开(公告)号：US20080176871A1

    公开(公告)日：2008-07-24

    申请号：US11938101

    申请日：2007-11-09

    申请人： Jean-Luc Girardet ,  Zhi Hong ,  Stephanie Shaw ,  Yung-hyo Koh

    发明人： Jean-Luc Girardet ,  Zhi Hong ,  Stephanie Shaw ,  Yung-hyo Koh

    IPC分类号： A61K31/519 ,  C07D519/00 ,  A61P31/12

    CPC分类号： C07D495/04

    摘要： This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

    摘要翻译： 本申请涉及式I的某些4-氰基苯基氨基取代的双环杂环，其中虚线表示可以位于A和C（V）之间或C（V）和D之间的双键，其中A是S或C（ Z）; D为S或C（W）; A和D中只有一个是S; 其中T是NH，O或S; 并且其中其它取代基在本文中定义。 这些化合物是非核苷逆转录酶抑制剂，具有抗HIV治疗的潜力。

    SYNTHESIS AND USE OF 2'-SUBSTITUTED-N6-MODIFIED NUCLEOSIDES
    5.
    发明申请
    SYNTHESIS AND USE OF 2'-SUBSTITUTED-N6-MODIFIED NUCLEOSIDES 有权
    2'-取代N6修饰的核苷酸的合成和用途

    公开(公告)号：US20110196144A1

    公开(公告)日：2011-08-11

    申请号：US12876997

    申请日：2010-09-07

    申请人： Haoyun An ,  Kanda Ramasamy ,  Stephanie Shaw

    发明人： Haoyun An ,  Kanda Ramasamy ,  Stephanie Shaw

    IPC分类号： C07H21/00 ,  C07H19/167

    CPC分类号： C07H19/16

    摘要： An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.

    摘要翻译： 制备糖改性核苷类似物的改进方法包括其中在对应的羰基的亲核改性之前糖的羟基被选择性脱保护和氧化的方案。 然后将修饰的糖偶联到杂环基，其在另外的步骤中用双重亲核试剂修饰，其提供具有高立体选择性的N6-修饰的腺苷类似物。

    2-Beta-modified-6-substituted adenosine analogs and their use as antiviral agents
    6.
    发明申请
    2-Beta-modified-6-substituted adenosine analogs and their use as antiviral agents 有权
    2-β-改性-6-取代的腺苷类似物及其作为抗病毒剂的用途

    公开(公告)号：US20060183706A1

    公开(公告)日：2006-08-17

    申请号：US10530627

    申请日：2002-10-23

    申请人： An Haoyun ,  Yili Ding ,  Stephanie Shaw ,  Zhi Hong

    发明人： An Haoyun ,  Yili Ding ,  Stephanie Shaw ,  Zhi Hong

    IPC分类号： A61K31/7076 ,  C07H19/22

    CPC分类号： C07H19/22

    摘要： Various 2′-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.

    摘要翻译： 通过常规和组合文库方法制备各种2'-β-甲基-6-取代的腺苷类似物（包括2,6-二取代的腺苷，8-氮杂-6-取代的腺苷和2-氮杂-6-取代的腺苷）。 考虑的化合物特别可用作治疗剂，特别是作为抗病毒剂。

    Substituted Thienol[2,3-d] pyrimidines as HIV Inhibitors
    8.
    发明申请
    Substituted Thienol[2,3-d] pyrimidines as HIV Inhibitors 失效
    取代的噻吩并[2,3-d]嘧啶作为HIV抑制剂

    公开(公告)号：US20120225894A1

    公开(公告)日：2012-09-06

    申请号：US13470119

    申请日：2012-05-11

    申请人： Jean-Luc GIRARDET ,  Zhi HONG ,  Stephanie SHAW ,  Yung-hyo KOH

    发明人： Jean-Luc GIRARDET ,  Zhi HONG ,  Stephanie SHAW ,  Yung-hyo KOH

    IPC分类号： C07D495/04 ,  A61P31/18 ,  C12N5/00 ,  A61K31/519 ,  C12N7/06

    CPC分类号： C07D495/04

    摘要： This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

    摘要翻译： 本申请涉及式I的某些4-氰基苯基氨基取代的双环杂环，其中虚线表示可以位于A和C（V）之间或C（V）和D之间的双键，其中A是S或C（ Z）; D为S或C（W）; A和D中只有一个是S; 其中T是NH，O或S; 并且其中其它取代基在本文中定义。 这些化合物是非核苷逆转录酶抑制剂，具有抗HIV治疗的潜力。

    Substituted thieno[3,2-d]pyrimidines as HIV inhibitors
    9.
    发明授权
    Substituted thieno[3,2-d]pyrimidines as HIV inhibitors 失效
    取代噻吩并[3,2-d]嘧啶作为HIV抑制剂

    公开(公告)号：US08211898B2

    公开(公告)日：2012-07-03

    申请号：US12504566

    申请日：2009-07-16

    申请人： Jean-Luc Girardet ,  Zhi Hong ,  Stephanie Shaw ,  Yung-hyo Koh

    发明人： Jean-Luc Girardet ,  Zhi Hong ,  Stephanie Shaw ,  Yung-hyo Koh

    IPC分类号： C07D495/04 ,  C07D403/12 ,  A61K31/502 ,  A61K31/519 ,  A61P31/14

    CPC分类号： C07D495/04

    摘要： This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

    摘要翻译： 本申请涉及式I的某些4-氰基苯基氨基取代的双环杂环，其中虚线表示可以位于A和C（V）之间或C（V）和D之间的双键，其中A是S或C（ Z）; D为S或C（W）; A和D中只有一个是S; 其中T是NH，O或S; 并且其中其它取代基在本文中定义。 这些化合物是非核苷逆转录酶抑制剂，具有抗HIV治疗的潜力。

    4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS
    10.
    发明申请
    4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS 失效
    作为艾滋病毒抗体的4-氰基亚氨基取代的双环杂环化合物

    公开(公告)号：US20090281124A1

    公开(公告)日：2009-11-12

    申请号：US12504566

    申请日：2009-07-16

    申请人： Jean-Luc Girardet ,  Zhi Hong ,  Stephanie Shaw ,  Yung-hyo Koh

    发明人： Jean-Luc Girardet ,  Zhi Hong ,  Stephanie Shaw ,  Yung-hyo Koh

    IPC分类号： A61K31/519 ,  A61P31/12

    CPC分类号： C07D495/04

    摘要： This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

    摘要翻译： 本申请涉及式I的某些4-氰基苯基氨基取代的双环杂环，其中虚线表示可以位于A和C（V）之间或C（V）和D之间的双键，其中A是S或C（ Z）; D为S或C（W）; A和D中只有一个是S; 其中T是NH，O或S; 并且其中其它取代基在本文中定义。 这些化合物是非核苷逆转录酶抑制剂，具有抗HIV治疗的潜力。