2'-FLUORONUCLEOSIDES
    4.
    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

    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。

    CXCR4 antagonists including diazine and triazine structures for the treatment of medical disorders
    5.
    发明授权
    CXCR4 antagonists including diazine and triazine structures for the treatment of medical disorders 有权
    CXCR4拮抗剂包括用于治疗医学疾病的二嗪和三嗪结构

    公开(公告)号:US08080659B2

    公开(公告)日:2011-12-20

    申请号:US11776476

    申请日:2007-07-11

    摘要: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors or for the treatment of viral infections. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis, or for reducing entry of HIV in to a cell while not reducing the capacity of the stem cells to proliferate. The compounds may be useful for long term treatment regimes.

    摘要翻译: 本发明提供化合物,药物组合物和使用作为趋化因子CXCR4受体的拮抗剂的某些化合物用于治疗由CXCR4受体介导的增殖性病症或用于治疗病毒感染的化合物,药物组合物和方法。 所提供的化合物干扰SDF1与受体的结合。 这些化合物特别可用于通过抑制转移或减少HIV进入细胞而不降低干细胞增殖的能力来治疗或降低过度增殖性疾病的严重性。 这些化合物可用于长期治疗方案。

    Branched Diepoxide Compounds for the Treatment of Inflammatory Disorders
    6.
    发明申请
    Branched Diepoxide Compounds for the Treatment of Inflammatory Disorders 审中-公开
    支链二环化合物治疗炎性疾病

    公开(公告)号:US20100324133A1

    公开(公告)日:2010-12-23

    申请号:US12831672

    申请日:2010-07-07

    申请人: Dennis C. Liotta

    发明人: Dennis C. Liotta

    CPC分类号: C07D303/08 C07D303/32

    摘要: The present invention provides certain diepoxide carbocyclic compounds wherein at least one carbocyclic ring carbon includes two non-epoxide substituents, and pharmaceutical compositions containing the same, for the treatment or prophylaxis of inflammatory, autoimmune and hyper- or abnormally proliferative diseases and disorders.

    摘要翻译: 本发明提供某些二环氧化物碳环化合​​物,其中至少一个碳环碳包括两个非环氧化物取代基,和含有它们的药物组合物,用于治疗或预防炎性,自身免疫性和异常增殖性疾病和病症。

    Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane
    10.
    发明申请
    Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane 审中-公开
    2-羟甲基-5(5-氟胞嘧啶-1-基)-1,3-氧硫杂环戊烷的抗病毒活性和拆分

    公开(公告)号:US20090048190A1

    公开(公告)日:2009-02-19

    申请号:US12150964

    申请日:2008-05-02

    摘要: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

    摘要翻译: 公开了用于治疗人体中HIV和HBV感染的方法和组合物,其包括给予有效量的2-羟甲基-5-(5-氟胞嘧啶-1-基)-1,3-氧硫杂环戊烷,其药学上可接受的衍生物 ,包括5'或N4烷基化或酰化衍生物或其药学上可接受的盐在药学上可接受的载体中。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法,其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。