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    Therapeutic nucleosides
    2.
    发明申请
    Therapeutic nucleosides 审中-公开
    治疗核苷

    公开(公告)号：US20060229327A1

    公开(公告)日：2006-10-12

    申请号：US11442489

    申请日：2006-05-26

    申请人： Dennis Liotta

    发明人： Dennis Liotta

    IPC分类号： A01N43/54

    CPC分类号： A61K9/2018 ,  A45F3/24 ,  A61K9/2059 ,  A61K9/4858 ,  A61K9/5047 ,  A61K31/513 ,  A61K47/02 ,  A61K47/10

    摘要： The use of a 1,3-oxathiolane nucleoside analogue and pharmaceutically acceptable derivatives thereof for the treatment of hepatitis B virus infections is disclosed. Pharmaceutical formulations are also provided.

    摘要翻译： 公开了1,3-氧硫杂环戊烷核苷类似物及其药学上可接受的衍生物用于治疗乙型肝炎病毒感染的用途。 还提供药物制剂。

    FLUORESCENT NUCLEOSIDE ANALOGUES
    4.
    发明申请
    FLUORESCENT NUCLEOSIDE ANALOGUES 审中-公开
    荧光核苷类似物

    公开(公告)号：US20100112561A1

    公开(公告)日：2010-05-06

    申请号：US12310455

    申请日：2007-08-27

    申请人： Stefan Lutz ,  Dennis Liotta ,  Yongfeng Li

    发明人： Stefan Lutz ,  Dennis Liotta ,  Yongfeng Li

    IPC分类号： C12Q1/68 ,  C07H19/06 ,  C07H19/00 ,  C07H19/22

    CPC分类号： C07H23/00

    摘要： Briefly described, embodiments of the present disclosure include novel fluorescent nucleoside analogs (fNAs) including a fluorescent nucleobase, selected from a purine and a pyrimidine base or analog thereof, and a modified sugar moiety that differs in structure from a sugar moiety of a naturally occurring nucleoside. In embodiments, the fNAs of the present disclosure are analogues of NA prodrugs used to treat viral disorders. Embodiments of the present disclosure also include methods of making the novel fNAs of the present disclosure.

    摘要翻译： 简要描述，本公开的实施方案包括新的荧光核苷类似物（fNA），其包括选自嘌呤和嘧啶碱基或其类似物的荧光核碱基，以及结构上与天然存在的糖部分不同的修饰的糖部分 核苷。 在实施方案中，本公开的fNA是用于治疗病毒性疾病的NA前药的类似物。 本公开的实施方案还包括制备本公开的新型fNA的方法。

    Novel curcuminoid-factor VIIa constructs as suppressors of tumor growth and angiogenesis
    6.
    发明申请
    Novel curcuminoid-factor VIIa constructs as suppressors of tumor growth and angiogenesis 审中-公开
    新型姜黄素因子VIIa构建成肿瘤生长和血管生成抑制因子

    公开(公告)号：US20060229239A9

    公开(公告)日：2006-10-12

    申请号：US10383898

    申请日：2003-03-07

    申请人： Mamoru Shoji ,  James Snyder ,  Dennis Liotta ,  Aiming Sun

    发明人： Mamoru Shoji ,  James Snyder ,  Dennis Liotta ,  Aiming Sun

    IPC分类号： A61K38/17

    CPC分类号： C12Y304/21021 ,  A61K47/64 ,  A61K47/6425 ,  C07D213/63 ,  C12N9/6437

    摘要： The fluorinated curcuminoid (3,5-bis-(2-fluorobenzylidene)-piperidin-4-one-acetate is about ten times more effective at arresting the growth of tumor cells than cisplatin. The present invention provides methods to deliver a cytotoxic compound, such as a curcuminoid, specifically to cancer cells and to the vascular endothelial cells that nourish solid tumors. The method involves tethering the drug to a protein such as in factor VIIa that retains high affinity for the surface protein tissue factor. Upon complexation, the resulting heterodimer is endocytosed and the drug is subsequently liberated inside the target cell via proteolytic cleavage. The present invention further provides for the synthesis of novel curcuminoid-tether-linker-factor VIIa compositions and for methods of delivery of effective doses of the novel compositions to target tumor or endothelial cells in a patient

    摘要翻译： 氟化姜黄素（3,5-双 - （2-氟亚苄基） - 哌啶-4-酮乙酸酯在阻止肿瘤细胞生长方面比顺铂高约十倍。本发明提供递送细胞毒性化合物的方法， 例如姜黄素，特别是癌细胞和滋养实体瘤的血管内皮细胞，该方法涉及将药物系在蛋白质上，例如对表面蛋白组织因子保持高亲和力的因子VIIa，在复合后，产生 异二聚体被内吞，并且药物随后通过蛋白水解切割在靶细胞内释放。本发明还提供了新型姜黄素 - 连接子 - 连接因子VIIa组合物的合成和用于将有效剂量的新组合物递送至靶 肿瘤或内皮细胞

    Antiviral activity and resolution of 2-hydroxymethyl-5- (5-fluorocytosin-1-yl)-1, 3-oxathiolane
    7.
    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：US20050215527A1

    公开(公告)日：2005-09-29

    申请号：US11125943

    申请日：2005-05-09

    申请人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    发明人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    IPC分类号： C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  A61K31/675 ,  A61K31/513 ,  C07D49/04

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    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 ，包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 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。

    Novel Curcuminoid-Factor VIIA Constructs as Suppressors of Tumor Growth and Angiogenesis
    8.
    发明申请
    Novel Curcuminoid-Factor VIIA Constructs as Suppressors of Tumor Growth and Angiogenesis 审中-公开
    新型Curcuminoid因子VIIA构建体作为肿瘤生长抑制因子和血管发生

    公开(公告)号：US20090011991A1

    公开(公告)日：2009-01-08

    申请号：US12035995

    申请日：2008-02-22

    申请人： Mamoru Shoji ,  James Synder ,  Dennis Liotta ,  Aiming Sun

    发明人： Mamoru Shoji ,  James Synder ,  Dennis Liotta ,  Aiming Sun

    IPC分类号： A61K38/36 ,  A61P35/00

    CPC分类号： C12Y304/21021 ,  A61K47/6425 ,  C07D213/63 ,  C07D213/64 ,  C12N9/6437

    摘要： The fluorinated curcuminoid (3,5-bis-(2-fluorobenzylidene)-piperidin-4-one-acetate is about ten times more effective at arresting the growth of tumor cells than cisplatin. Conjugates for delivering a cytotoxic compound, such as a curcuminoid, specifically to cancer cells and to the vascular endothelial cells that nourish solid tumors, and methods of making and using thereof are described herein. The conjugate contains a cytotoxic compound bound to a protein such as in factor VIIa that retains high affinity for the surface protein tissue factor. The cytotoxic compound is bound to the protein via a linker and a hydrolyzable bond. Upon complexation, the resulting heterodimer is endocytosed and the drug is subsequently liberated inside the target cell via proteolytic cleavage.

    摘要翻译： 氟化姜黄素（3,5-双 - （2-氟亚苄基） - 哌啶-4-酮乙酸酯在阻止肿瘤细胞生长方面比顺铂高约十倍。用于递送细胞毒性化合物如姜黄素的缀合物 具体涉及癌细胞和滋养实体瘤的血管内皮细胞，本文描述了制备和使用它们的方法，该缀合物含有与蛋白质结合的细胞毒性化合物，例如对表达蛋白保持高亲和力的因子VIIa 细胞毒性化合物通过接头和可水解键与蛋白质结合，络合时，得到的异源二聚体被内吞，然后通过蛋白水解切割将药物释放到靶细胞内。

    HIV-1 mutations selected for by beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine
    9.
    发明申请
    HIV-1 mutations selected for by beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine 失效
    由β-2'，3'-二脱氢-2'，3'-二脱氧-5-氟胞苷选择的HIV-1突变

    公开(公告)号：US20070025964A1

    公开(公告)日：2007-02-01

    申请号：US11542044

    申请日：2006-10-03

    申请人： Raymond Schinazi ,  Jennifer Hammond ,  John Mellors ,  Dennis Liotta

    发明人： Raymond Schinazi ,  Jennifer Hammond ,  John Mellors ,  Dennis Liotta

    IPC分类号： A61K38/21 ,  A61K31/7076 ,  A61K31/7072 ,  A61K31/522 ,  A61K31/538 ,  A61K31/513

    CPC分类号： A61K31/513 ,  A61K31/522 ,  A61K31/538 ,  A61K31/7072 ,  A61K31/7076 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention discloses a method for treating HIV that includes administering β-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using β-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. β-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.

    摘要翻译： 本发明公开了一种治疗艾滋病毒的方法，其包括向需要治疗的人组合或交替给予β-D-D4FC或其药学上可接受的盐或前药，所述药物在其它位置诱导HIV-1中的突变 比70（K至N），90或反转录酶区域的172个密码子。 还公开了将β-D-D4FC用作对其他抗HIV药物具有耐药性的患者的“补救疗法”的方法。 一般来说，β-D-D4FC可用于任何对在70（K至N），90或172个密码子以外诱导突变的药物具有抗性的患者的补救疗法。

    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 有权
    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：US20060276492A1

    公开(公告)日：2006-12-07

    申请号：US11390861

    申请日：2006-03-28

    申请人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    发明人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    IPC分类号： A61K31/513 ,  C07D409/04

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    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 ，包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 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。