利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

27 条记录 (耗时 0.046 秒)

    N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
    5.
    发明授权
    N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors 失效
    可用作HIV整合酶抑制剂的N-（取代苄基）-8-羟基-1,6-萘啶-7-甲酰胺

    公开(公告)号：US07323460B2

    公开(公告)日：2008-01-29

    申请号：US10508094

    申请日：2003-03-12

    申请人： Melissa Egbertson ,  H. Marie Langford ,  Jeffrey Y. Melamed ,  John S. Wai ,  Wei Han ,  Debbie S. Perlow ,  Linghang Zhuang ,  Mark Embrey

    发明人： Melissa Egbertson ,  H. Marie Langford ,  Jeffrey Y. Melamed ,  John S. Wai ,  Wei Han ,  Debbie S. Perlow ,  Linghang Zhuang ,  Mark Embrey

    IPC分类号： C07D401/02 ,  A61K31/4375

    CPC分类号： C07D471/04

    摘要： N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R2′ and R3′ are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

    摘要翻译： N-（取代的苄基）-8-羟基-1,6-萘啶-7-甲酰胺是HIV整合酶和HIV复制抑制剂的抑制剂。 萘啶甲酰胺具有式（I）：其中R 1，R 2，R 3和R 3'在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

    HIV INTEGRASE INHIBITORS
    7.
    发明申请
    HIV INTEGRASE INHIBITORS 审中-公开
    艾滋病毒整合抑制剂

    公开(公告)号：US20130178468A1

    公开(公告)日：2013-07-11

    申请号：US13606929

    申请日：2012-09-07

    申请人： Joseph P. Vacca ,  John S. Wai ,  Linda S. Payne ,  Richard C. A. Isaccs ,  Wei Han ,  Melissa Egbertson ,  Richard Pracitto

    发明人： Joseph P. Vacca ,  John S. Wai ,  Linda S. Payne ,  Richard C. A. Isaccs ,  Wei Han ,  Melissa Egbertson ,  Richard Pracitto

    IPC分类号： C07D471/14 ,  C07D498/14

    CPC分类号： C07D471/14 ,  A61K31/4353 ,  A61K31/4375 ,  C07D498/14

    摘要： Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

    摘要翻译： 式I的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中键A，环A，R 1，R 2和R 3在本文中定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

    Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
    9.
    发明授权
    Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors 失效
    可用作HIV整合酶抑制剂的羟基萘啶酮甲酰胺

    公开(公告)号：US07279487B2

    公开(公告)日：2007-10-09

    申请号：US10500972

    申请日：2003-01-13

    申请人： Melissa Egbertson ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  Steven D. Young

    发明人： Melissa Egbertson ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  Steven D. Young

    IPC分类号： A61K31/44 ,  C07F5/02 ,  C07D471/02

    CPC分类号： C07D471/04 ,  A61K31/4353 ,  A61K45/06 ,  A61K2300/00

    摘要： Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b, R3, R4, and R5 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

    摘要翻译： 下式的羟基萘啶酮甲酰胺被描述为HIV整合酶的抑制剂和HIV复制抑制剂，其中L，R 1a，R 1b，R 1c， R 2a，R 2b，R 3，R 4和R 5，以及R 5， >在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

    NOVEL TRPA1 ANTAGONISTS
    10.
    发明申请
    NOVEL TRPA1 ANTAGONISTS 有权
    新一代TRPA1 ANTAGONISTS

    公开(公告)号：US20120196894A1

    公开(公告)日：2012-08-02

    申请号：US13499844

    申请日：2010-09-28

    申请人： Mark T. Bilodeau ,  Melissa Egbertson ,  Ahren Green ,  John C. Hartnett ,  Yiwei Li

    发明人： Mark T. Bilodeau ,  Melissa Egbertson ,  Ahren Green ,  John C. Hartnett ,  Yiwei Li

    IPC分类号： A61K31/136 ,  C07D215/38 ,  A61K31/47 ,  C07C255/59 ,  A61K31/4706 ,  C07D311/74 ,  A61K31/352 ,  A61P29/00 ,  C07D215/44 ,  C07C211/48 ,  A61K31/277

    CPC分类号： C07C215/20 ,  A61K31/133 ,  C07C25/02 ,  C07C211/34 ,  C07C215/44 ,  C07C255/58 ,  C07C2602/10 ,  C07D215/38 ,  C07D215/44 ,  C07D311/74 ,  C07D311/76 ,  C07D405/04 ,  C07D405/06

    摘要： The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.

    摘要翻译： 本发明涉及调节至少一种TRP家族成员的组合物和方法。 具体地说，本发明涉及新型TRPA1拮抗剂及其用于治疗慢性炎性和神经性疼痛等疼痛的用途。 可以调节一种或多种TRPA1功能的化合物在许多方面是有用的，包括但不限于维持钙稳态; 维持钠稳态; 调节细胞内钙含量; 调节膜极化（膜电位）; 调节阳离子水平; 和/或治疗或预防与钙稳态相关的疾病，病症或病症，钠稳态，钙或钠血管平衡，或膜极化/超极化（包括低钠和过度兴奋性）和/或治疗或预防与疾病，病症或病症相关 与TRPA1表达或功能调节或失调。 本发明还涉及拮抗TRPA1的功能和一种或多种另外的TRP通道的功能的方法和组合物。