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68 条记录 (耗时 0.034 秒)

    2'-FLUORONUCLEOSIDES
    5.
    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
    6.
    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
    9.
    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
    10.
    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。