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    2'-FLUORONUCLEOSIDES
    2.
    发明申请
    2'-FLUORONUCLEOSIDES 审中-公开
    2'-氟核苷酸

    公开(公告)号：US20130157971A1

    公开(公告)日：2013-06-20

    申请号：US13437676

    申请日：2012-04-02

    申请人： RAYMOND F. SCHINAZI ,  Dennis C. Liotta ,  Chung K. Chu ,  J. Jeffrey McAtee

    发明人： RAYMOND F. SCHINAZI ,  Dennis C. Liotta ,  Chung K. Chu ,  J. Jeffrey McAtee

    IPC分类号： A61K31/708 ,  A61K31/7064 ,  A61K31/7076 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/7072

    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： 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, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy; R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 公开了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，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; R2是H，磷酸盐或稳定的磷酸盐前药; 酰基或其它药学上可接受的苄基，脂质，氨基酸，肽或胆固醇; 烷基，磷酸酯或其它药学上可接受的离去基团; 或其药学上可接受的盐。

    2′-Fluoronucleosides
    3.
    发明授权
    2′-Fluoronucleosides 有权
    2'-氟核苷

    公开(公告)号：US07307065B2

    公开(公告)日：2007-12-11

    申请号：US10796529

    申请日：2004-03-08

    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： A61K38/00 ,  A01N61/00 ,  C07H1/00 ,  C07G3/00

    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, loweralkylamino, 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 arylalkyl 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 N ，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; R 2是H，磷酸盐，包括单磷酸盐，二磷酸盐，三磷酸盐或稳定化的磷酸盐前药; 酰基或其它药学上可接受的离去基团，其当在体内施用时能够提供其中R 2是H或磷酸酯的化合物; 磺酸酯，包括烷基或芳基烷基磺酰基，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，如上述芳基定义中所述，脂质，氨基酸，肽或胆固醇; 并且R 3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，其能够被切割成母体化合物或其药学上可接受的盐。

    3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents
    6.
    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。

    Process for the preparation of enantiomerically pure .beta.-D-(-)-dioxolane-nucleosides
    8.
    发明授权
    Process for the preparation of enantiomerically pure .beta.-D-(-)-dioxolane-nucleosides 失效
    制备完全纯度（BETA）-D - （ - ） - 二氧杂环己烷的方法

    公开(公告)号：US5179104A

    公开(公告)日：1993-01-12

    申请号：US622762

    申请日：1990-12-05

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

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

    IPC分类号： C07D473/18 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/52 ,  A61K31/522 ,  A61K31/53 ,  A61K31/675 ,  A61K31/7076 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D497/08

    CPC分类号： A61K31/675 ,  C07D405/04

    摘要： An asymmetric process for the preparation of enantiomerically pure .beta.-D-(-)-dioxolane-nucleosides. The enantiomerically pure dioxolane nucleosides are active HIV agents, that are significantly more effective than the prior prepared racemic mixtures of the nucleosides. The anti-viral activity of the compounds is surprising in light of the generally accepted theory that moieties in the endo conformation, including these dioxolanes, are not effective antiviral agents. The toxicity of the enantiomerically pure dioxolane nucleosides is lower that that of the racemic mixture of the nucleosides, because the nonnaturally occurring .alpha.-isomer is not included.The product can be used as a research tool to study the inhibition of HIV in vitro or can be administered in a pharmaceutical composition to inhibit the growth of HIV in vivo.

    摘要翻译： 用于制备对映体纯的β-D（ - ） - 二氧戊环 - 核苷的不对称方法。 对映体纯的二氧戊环核苷是活性的HIV试剂，其显着比先前制备的核苷的外消旋混合物更有效。 根据普遍接受的理论，化合物的抗病毒活性是令人惊讶的，内在构象中的部分（包括这些二氧戊环）不是有效的抗病毒剂。 由于不包含非天然存在的α-异构体，对映体纯的二氧杂环戊烷核苷的毒性低于核苷的外消旋混合物的毒性。 该产品可用作研究HIV体外抑制的研究工具，或可以在药物组合物中施用以抑制体内HIV生长。

    5'-diphosphohexose nucleoside pharmaceutical compositions
    9.
    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：US5118672A

    公开(公告)日：1992-06-02

    申请号：US551548

    申请日：1990-07-11

    申请人： Raymond F. Schinazi ,  Jean-Pierre Sommadossi ,  Chung K. Chu ,  William M. Shafer

    发明人： Raymond F. Schinazi ,  Jean-Pierre Sommadossi ,  Chung K. Chu ,  William M. Shafer

    IPC分类号： C07H19/10 ,  C07H19/20

    CPC分类号： C07H19/10 ,  C07H19/20

    摘要： This invention provides compounds and pharmaceutical compositions that include compounds of the formula: ##STR1## in which 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, W is O or S; X is O, S, or CH.sub.2 ; Y is a purine or pyrimidine base, Z is C, S, or O, and wherein when Z is S or O, A and C are not present. The compounds of this inverntion have enhanced pharmaceutical or biological activity or increased intracellular absorption compared to the corresponding parent nucleoside as a function of the 5'-diphosphohexose moiety. Many of these compounds have antiviral, including anti-HIV, activity. Others have antibacterial activity. In one embodiment, the invention is a method to treat HIV infection and opportunistic infections concomitantly.

    摘要翻译： 本发明提供了包括下式的化合物的化合物和药物组合物：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，己二酰胺或N-乙酰基己糖胺，W是O或S; X是O，S或CH 2; Y是嘌呤或嘧啶碱，Z是C，S或O，并且其中当Z是S或O时，不存在A和C。 与相应的亲本核苷作为5'-二磷酸己糖部分的函数相比，该反应的化合物具有增强的药物或生物活性或增加的细胞内吸收。 这些化合物中的许多具有抗病毒，包括抗HIV，活性。 其他有抗菌活性。 在一个实施方案中，本发明是一种同时治疗HIV感染和机会性感染的方法。

    3'-Azido-2',3'-dideoxyuridine anti-retroviral composition
    10.
    发明授权
    3'-Azido-2',3'-dideoxyuridine anti-retroviral composition 失效
    3'-叠氮基-2'，3'-二脱氧尿苷抗逆转录病毒组合物

    公开(公告)号：US4916122A

    公开(公告)日：1990-04-10

    申请号：US104438

    申请日：1987-10-02

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

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

    IPC分类号： C07H1/00 ,  A61K20060101 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P31/12 ,  C07H19/06 ,  C07H19/073 ,  C07H19/10

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

    摘要： Compositions for the treatment of AIDS and ARC having the following compound as an active ingredient: ##STR1## where R.sup.1 is OH, monophosphate, diphosphate, or triphosphate; or a pharmacologically acceptable salt thereof.The primary advantage of this compound is its highly selective anti-retroviral activity, i.e., it significantly decreases viral replication as measured as reverse transcriptase activity while demonstrating orders of magnitude less cytotoxicity than other anti-viral compounds such as AZT.In a preferred embodiment, the compound is present in an amount sufficient to inhibit the HIV reverse transcriptase activity but not significantly inhibit human DNA polymerase activity. Also included within the scope of this invention are 3'-azido-2',3'-dideoxyuridine mono-, di-, and triphosphate and compositions containing these compounds as the active agent.

    摘要翻译： 用于治疗AIDS和ARC的组合物，其具有以下化合物作为活性成分：其中R 1为OH，单磷酸酯，二磷酸酯或三磷酸酯; 或其药理学上可接受的盐。 该化合物的主要优点是其高度选择性的抗逆转录病毒活性，即如通过逆转录酶活性测量的那样显着降低病毒复制，同时显示比其它抗病毒化合物如AZT更小的数量级的细胞毒性。 在优选的实施方案中，化合物以足以抑制HIV逆转录酶活性但不显着抑制人DNA聚合酶活性的量存在。 也包括在本发明范围内的是3'-叠氮基-2'，3'-二脱氧尿苷单 - ，二 - 和三磷酸，以及含有这些化合物作为活性剂的组合物。