2'-FLUORONUCLEOSIDES
    32.
    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。

    Branched Diepoxide Compounds for the Treatment of Inflammatory Disorders
    33.
    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
    36.
    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。

    [5-carboxamido or 5-fluoro]-[2',3'-unsaturated or 3'-modified]-pyrimidine nucleosides
    37.
    发明申请
    [5-carboxamido or 5-fluoro]-[2',3'-unsaturated or 3'-modified]-pyrimidine nucleosides 审中-公开
    [5-甲酰氨基或5-氟] - [2',3'-不饱和或3'-修饰] - 嘧啶核苷

    公开(公告)号:US20080293668A1

    公开(公告)日:2008-11-27

    申请号:US12220609

    申请日:2008-07-25

    摘要: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2′,3′-dideoxy-2′,3′-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3′-modified-pyrimidine nucleoside, or a mixture or 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.

    摘要翻译: 公开了用于治疗人和其他宿主动物中的HIV和HBV感染的方法和组合物,其包括给予有效量的[5-甲酰氨基或5-氟] -2',3'-二脱氧-2' ,3'-二脱氢嘧啶核苷或[5-甲酰氨基或5-氟] -3'-修饰的嘧啶核苷或其混合物或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。