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    Combined systemic and topical treatment of disordered tissues
    57.
    发明授权
    Combined systemic and topical treatment of disordered tissues 有权
    组合系统和局部治疗无序组织

    公开(公告)号：US09545408B2

    公开(公告)日：2017-01-17

    申请号：US14823830

    申请日：2015-08-11

    申请人： QUADEX PHARMACEUTICALS, LLC

    发明人： B. Ron Johnson

    IPC分类号： A01N43/04 ,  A61K31/70 ,  A61K31/522 ,  A61K31/14 ,  A61K31/7072 ,  A61K9/00 ,  A61K45/06 ,  A61K31/52 ,  A61K31/662 ,  A61K31/675 ,  A61K31/7125 ,  A61K31/7052 ,  A61K31/7076 ,  A61K31/706 ,  A61K31/7064

    CPC分类号： A61K31/522 ,  A61K9/0014 ,  A61K31/14 ,  A61K31/52 ,  A61K31/662 ,  A61K31/675 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7125 ,  A61K45/06 ,  A61K2300/00 ,  A61K31/375

    摘要： Kits and methods for treating disordered or infected tissue caused by a virus in a mammal involve co-administering a systemic anti-virus drug and topically administered anti-infective composition. The systemic anti-virus drug is internally administered and disrupts or inhibits virus replication systemically within the mammal. Examples include nucleoside analogs, nucleoside analog precursors, and nucleotide analogs. The topically administered anti-infective composition includes at least one anti-infective agent, such as an organohalide (e.g., benzalkonium chloride), and is formulated to penetrate below the skin surface and allow the anti-infective agent to kill viruses at the infected tissue site. The topical anti-infective composition renders the systemic anti-virus drug more efficacious and reduces the time and/or number of dosages otherwise required for the systemic anti-virus drug to treat the disordered tissue. In some cases, the topical anti-infective composition is more beneficial than the systemic anti-virus drug in killing viruses and can reduce or eliminate post-herpetic neuralgia.

    摘要翻译： 用于治疗由哺乳动物病毒引起的无序或感染组织的试剂盒和方法涉及共同施用全身性抗病毒药物和局部施用的抗感染组合物。 全身性抗病毒药物在内部施用，并且在哺乳动物内全面地破坏或抑制病毒复制。 实例包括核苷类似物，核苷类似物前体和核苷酸类似物。 局部施用的抗感染组合物包括至少一种抗感染剂，例如有机卤化物（例如苯扎氯铵），并配制成渗入皮肤表面以下，并允许抗感染剂在感染组织中杀死病毒 现场。 局部抗感染组合物使全身性抗病毒药物更有效，并且减少了全身性抗病毒药物治疗无序组织所需的剂量的时间和/或剂量。 在一些情况下，局部抗感染组合物比全身性抗病毒药物在杀死病毒中更有益，并且可以减少或消除疱疹后神经痛。

    Anti-viral pyrimidine nucleoside derivatives
    59.
    发明授权
    Anti-viral pyrimidine nucleoside derivatives 有权
    抗病毒嘧啶核苷衍生物

    公开(公告)号：US09427447B2

    公开(公告)日：2016-08-30

    申请号：US14482125

    申请日：2014-09-10

    申请人： UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED ,  K.U. LEUVEN RESEARCH AND DEVELOPMENT

    发明人： Christopher McGuigan ,  Jan Balzarini ,  Marco Migliore

    IPC分类号： A01N43/04 ,  A61K31/70 ,  A61K31/7068 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7052

    CPC分类号： A61K31/7068 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.

    摘要翻译： 用于治疗或预防病毒感染的化合物，例如由水痘带状疱疹病毒引起的水痘或带状疱疹，所述具有通式（II）的化合物：其中X是O，S，NH或CH 2，Y 是O，S或NH，Z是O，S或CH 2，R 1是C 1-6烷基，优选正烷基，例如正戊基或正己基，R 2和R 3之一是OH，另一个是 R3和R2是中性的，非极性的氨基酸部分，或其药学上可接受的盐或水合物。 所述中性，非极性氨基酸部分R 2或R 3可以是（Ⅳ）：其中R 4，R 5，R 6和R 7各自独立地为H或C 1-2烷基。 在优选的实施方案中，R2或R3之一是缬氨酸，亮氨酸，异亮氨酸或丙氨酸，特别是缬氨酸。