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    Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
    3.
    发明授权
    Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase 有权
    核苷衍生物作为RNA依赖性RNA病毒聚合酶的抑制剂

    公开(公告)号：US07202224B2

    公开(公告)日：2007-04-10

    申请号：US11496338

    申请日：2006-07-31

    申请人： Anne B. Eldrup ,  Marija Prhavc ,  Phillip Dan Cook ,  Steven S. Carroll ,  David B. Olsen

    发明人： Anne B. Eldrup ,  Marija Prhavc ,  Phillip Dan Cook ,  Steven S. Carroll ,  David B. Olsen

    IPC分类号： A61K31/70 ,  C07H19/14

    CPC分类号： C07H19/16 ,  A61K9/4858 ,  A61K31/7056 ,  A61K31/7064 ,  A61K31/7076 ,  A61K38/21 ,  A61K45/06 ,  C07D473/00 ,  C07D487/04 ,  C07H19/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/12 ,  C07H19/14 ,  C07H19/20 ,  Y02P20/582 ,  A61K2300/00

    摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

    摘要翻译： 本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。 这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。 本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。 还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

    Nucleobase heterocyclic combinatorialization
    4.
    发明授权
    Nucleobase heterocyclic combinatorialization 失效
    核碱基杂环组合

    公开(公告)号：US06893815B1

    公开(公告)日：2005-05-17

    申请号：US08884873

    申请日：1997-06-30

    申请人： Phillip Dan Cook

    发明人： Phillip Dan Cook

    IPC分类号： C07B61/00 ,  C07D473/00 ,  C07H19/16 ,  C12Q1/68

    CPC分类号： C07D473/00 ,  C07H19/16 ,  C40B40/00

    摘要： Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally through employment of a tether moiety. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.

    摘要翻译： 提供化合物的混合物具有抗菌和其他效用。 混合物优选在溶液相中由嘌呤或嘧啶杂环支架与一组相关的化学取代基的反应形成，任选地通过使用系链部分。 根据本发明形成的图书馆本身具有效用，并且是商品。 它们可用于筛选农药，药物和其他生物活性化合物。

    Peptide nucleic acid combinatorial libraries and improved methods of synthesis
    6.
    发明授权
    Peptide nucleic acid combinatorial libraries and improved methods of synthesis 失效
    肽核酸组合文库和改进的合成方法

    公开(公告)号：US06756199B1

    公开(公告)日：2004-06-29

    申请号：US08466395

    申请日：1995-06-06

    申请人： Phillip Dan Cook ,  John Kiely ,  Kelly Sprankle

    发明人： Phillip Dan Cook ,  John Kiely ,  Kelly Sprankle

    IPC分类号： C12Q168

    CPC分类号： C07K14/003 ,  B01J2219/00592 ,  B01J2219/00729 ,  C07K7/02

    摘要： New sub-monomer synthetic methods for the preparation of peptide nucleic acid oligomeric structures are disclosed that provide for the synthesis of both predefined sequence peptide nucleic acid oligomers as well as random sequence peptide nucleic acid oligomers. Further these methods also provide for the incorporation of peptide nucleic acid units or strings of such units with amino acids or strings of amino acids in chimeric peptide nucleic acid-amino acid compounds. Further disclosed are method of making random libraries of peptide nucleic acids using the fully preformed monomers. Chimeric oligomers and libraries of the same are also disclosed.

    摘要翻译： 公开了用于制备肽核酸低聚结构的新的亚单体合成方法，其提供预定义的序列肽核酸寡聚体以及随机序列肽核酸寡聚体的合成。 此外，这些方法还提供了嵌合肽核酸 - 氨基酸化合物中肽核酸单元或这些单元的串与氨基酸或氨基酸序列的结合。 进一步公开的是使用完全预制的单体制备肽核酸的随机文库的方法。 也公开了嵌合低聚物和其文库。

    Compositions and methods for non-parenteral delivery of oligonucleotides
    7.
    发明授权
    Compositions and methods for non-parenteral delivery of oligonucleotides 失效
    用于非肠胃外递送寡核苷酸的组合物和方法

    公开(公告)号：US06747014B2

    公开(公告)日：2004-06-08

    申请号：US10029598

    申请日：2001-12-21

    申请人： Ching-Leou Teng ,  Phillip Dan Cook ,  Lloyd Tillman ,  Gregory E. Hardee ,  David J. Ecker ,  Muthiah Manoharan

    发明人： Ching-Leou Teng ,  Phillip Dan Cook ,  Lloyd Tillman ,  Gregory E. Hardee ,  David J. Ecker ,  Muthiah Manoharan

    IPC分类号： A61K3170

    CPC分类号： A61K48/0075 ,  A61K9/0014 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/28 ,  A61K48/00 ,  C07H21/00 ,  Y10S514/946

    摘要： The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.

    摘要翻译： 本发明涉及通过非肠胃外给药途径增强寡核苷酸和核酸的局部和全身摄取和递送的组合物和方法。 包含本文公开的寡核苷酸的药物组合物包括用于全身递送的乳液和微乳液制剂用于各种应用和口服剂型。 还令人惊讶地发现，可以用简单的溶液，例如纯的或盐水，通过直肠灌肠剂和栓剂将寡核苷酸局部递送至结肠部位。 寡核苷酸的这种药物组合物可以进一步包括一种或多种用于将寡核苷酸和其它核酸转移穿过粘膜的渗透增强剂。 本发明的组合物和方法用于对动物进行口服，口腔，直肠或阴道施用反义寡核苷酸，以调节动物中基因在调查，治疗，姑息或预防目的中的表达。