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    Bicyclic Carbamoylpyridone Derivative Having Hiv Integrase Inhibitory Activity
    3.
    发明申请
    Bicyclic Carbamoylpyridone Derivative Having Hiv Integrase Inhibitory Activity 有权
    具有Hiv整合酶抑制活性的双环氨甲酰吡哆醇衍生物

    公开(公告)号：US20080161271A1

    公开(公告)日：2008-07-03

    申请号：US11884686

    申请日：2006-02-20

    申请人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Yoshiyuki Taoda

    发明人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Yoshiyuki Taoda

    IPC分类号： A61K31/675 ,  C07D241/36 ,  A61K31/4985 ,  A61P31/18 ,  C07D295/00 ,  A61K31/5377

    CPC分类号： C07D471/04 ,  C07F9/6561

    摘要： [Object] Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent. [Solving means] A compound represented by the formula: (wherein Z1 is NR4 (R4 is hydrogen, optionally substituted lower alkyl etc.), O or CH2; Z2 is optionally substituted lower alkylene or optionally substituted lower alkenylene, each may be intervened by a heteroatom group selected from group consisting O, S, SO, SO2, NR5 (R5 is selected independently from the same substituent group of R4)—N═ and ═N—; R1 is hydrogen or lower alkyl; X is a single bond, a heteroatom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted alkyl group etc.)

    摘要翻译： 本发明提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物和药剂，特别是抗HIV剂。 [解决方案]由下式表示的化合物（其中Z 1是NR 4）（R 4）是氢，任选取代的低级烷基等 。），O或CH 2; Z 2是任选取代的低级亚烷基或任选取代的低级亚烯基，各自可以被选自O，S SO，SO 2，NR 5（R 5）独立地选自与R 4相同的取代基， ）-N-和-N-; R 1是氢或低级烷基; X是单键，选自O，S，SO，SO 2的杂原子基团; 和NH，或低级亚烷基或低级亚烯基各自可以被杂原子基团插入; R 2是任选取代的芳基; R 3是氢，卤素，羟基，任选取代的 烷基等）

    Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
    4.
    发明授权
    Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity 有权
    具有HIV整合酶抑制活性的双环氨基甲酰吡啶酮衍生物

    公开(公告)号：US07858788B2

    公开(公告)日：2010-12-28

    申请号：US11884686

    申请日：2006-02-20

    申请人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Yoshiyuki Taoda

    发明人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Yoshiyuki Taoda

    IPC分类号： C07D413/00 ,  C07D471/00

    CPC分类号： C07D471/04 ,  C07F9/6561

    摘要： Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent.A compound represented by the formula: (wherein Z1 is NR4 (R4 is hydrogen, optionally substituted lower alkyl etc.), O or CH2; Z2 is optionally substituted lower alkylene or optionally substituted lower alkenylene, each may be intervened by a heteroatom group selected from group consisting O, S, SO, SO2, NR5 (R5 is selected independently from the same substituent group of R4) —N═ and ═N—; R1 is hydrogen or lower alkyl; X is a single bond, a heteroatom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted alkyl group etc.)

    摘要翻译： 是提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物和药剂，特别是抗HIV剂。 由下式表示的化合物（其中Z 1为NR 4（R 4为氢，任选取代的低级烷基等），O或CH 2; Z 2为任选取代的低级亚烷基或任选取代的低级亚烯基，各自可以被选自 来自由O，S，SO，SO 2，NR 5组成的基团（R 5独立地选自与R 4相同的取代基组）-N =和N - ; R 1是氢或低级烷基; X是单键， O，S，SO，SO 2和NH，或低级亚烷基或低级亚烯基各自可以被杂原子基团插入; R2是任选取代的芳基; R 3是氢，卤素，羟基，任选取代的烷基等）

    Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
    5.
    发明授权
    Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity 有权
    具有HIV整合酶抑制活性的多环氨基甲酰吡啶酮衍生物

    公开(公告)号：US08188271B2

    公开(公告)日：2012-05-29

    申请号：US12084128

    申请日：2006-10-26

    申请人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Teruhiko Taishi ,  Yoshiyuki Taoda

    发明人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Teruhiko Taishi ,  Yoshiyuki Taoda

    IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/53 ,  A61P31/18

    CPC分类号： C07F9/6561 ,  C07D471/04 ,  C07D471/14 ,  C07D471/20 ,  C07D498/14

    摘要： Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line. When B2 is NR22, R4 and R22 may be connected together to form an optionally substituted heterocycle;When B2 is CHR21, R4 and R21 may be connected together to form an optionally substituted heterocycle.Alternatively, B1 and B2 are independently C, CR23 or N and, in this case, B1 and B2 may be taken together to form a heterocycle.R20, R21, R22 and R23 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl etc.)

    摘要翻译： 提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物，以及药物组合物，特别是抗HIV剂。 （其中R1为氢或低级烷基; X为低级亚烷基等; R2为任选取代的芳基; R3为氢，卤素，羟基，任选取代的低级烷基等; R4为氢，任选取代的低级烷基，任选取代的环烷基， 任选取代的环烷基低级烷基，任选取代的芳基，任选取代的芳基低级烷基，任选取代的杂环基，任选取代的杂环低级烷基等;虚线表示存在或不存在键; B1和B2使得任何一个 它们是CR20R21，另一个是NR22，在这种情况下没有虚线，当B2是NR22时，R4和R22可以连接在一起形成任选取代的杂环;当B2是CHR21时，R4和R21可以是 连接在一起形成任选取代的杂环，或者B1和B2独立地为C，CR23或N，在这种情况下，B1和B2可以一起形成杂环R 20，R 21，R 22 和R 23独立地是氢，任选取代的低级烷基，任选取代的环烷基，任选取代的环烷基低级烷基等）

    Polycylclic Carbamoylpyridone Derivative Having HIV Integrase Inhibitory Acitvity
    6.
    发明申请
    Polycylclic Carbamoylpyridone Derivative Having HIV Integrase Inhibitory Acitvity 有权
    具有HIV整合酶抑制作用的聚酰胺酰吡啶酮衍生物

    公开(公告)号：US20090143356A1

    公开(公告)日：2009-06-04

    申请号：US12084128

    申请日：2006-10-26

    申请人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Teruhiko Taishi ,  Yoshiyuki Taoda

    发明人： Hiroshi Yoshida ,  Takashi Kawasuji ,  Teruhiko Taishi ,  Yoshiyuki Taoda

    IPC分类号： A61K31/553 ,  C07D487/04 ,  A61K31/53 ,  C07D413/06 ,  C07D498/14 ,  C07D498/12 ,  A61K31/5383 ,  A61K31/5377 ,  C07D487/14 ,  A61K31/551

    CPC分类号： C07F9/6561 ,  C07D471/04 ,  C07D471/14 ,  C07D471/20 ,  C07D498/14

    摘要： Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line. When B2 is NR22, R4 and R22 may be connected together to form an optionally substituted heterocycle;When B2 is CHR21, R4 and R21 may be connected together to form an optionally substituted heterocycle.Alternatively, B1 and B2 are independently C, CR23 or N and, in this case, B1 and B2 may be taken together to form a heterocycle.R20, R21, R22 and R23 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl etc.)

    摘要翻译： 提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物，以及药物组合物，特别是抗HIV剂。 （其中R1为氢或低级烷基; X为低级亚烷基等; R2为任选取代的芳基; R3为氢，卤素，羟基，任选取代的低级烷基等; R4为氢，任选取代的低级烷基，任选取代的环烷基， 任选取代的环烷基低级烷基，任选取代的芳基，任选取代的芳基低级烷基，任选取代的杂环基，任选取代的杂环低级烷基等;虚线表示存在或不存在键; B1和B2使得任何一个 它们是CR20R21，另一个是NR22，在这种情况下没有虚线，当B2是NR22时，R4和R22可以连接在一起形成任选取代的杂环;当B2是CHR21时，R4和R21可以是 连接在一起形成任选取代的杂环，或者B1和B2独立地为C，CR23或N，在这种情况下，B1和B2可以一起形成杂环R 20，R 21，R 22 和R 23独立地是氢，任选取代的低级烷基，任选取代的环烷基，任选取代的环烷基低级烷基等）

    Substituted 9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydor-1H-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazines
    8.
    发明授权
    Substituted 9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydor-1H-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazines 有权
    取代的9,11-二氧代-2,3,4a，5,9,11,13,13a-八氢-1H-吡啶并[1,2-a]吡咯并[1'，2'：3,4]咪唑并[1 ，2-d]吡嗪

    公开(公告)号：US08183372B2

    公开(公告)日：2012-05-22

    申请号：US13055046

    申请日：2009-07-23

    申请人： Brian Alvin Johns ,  Yasunori Aoyama ,  Hiroshi Yoshida ,  Yoshiyuki Taoda

    发明人： Brian Alvin Johns ,  Yasunori Aoyama ,  Hiroshi Yoshida ,  Yoshiyuki Taoda

    IPC分类号： C07D241/36

    CPC分类号： C07D471/14

    摘要： The present invention is directed to a process for the preparation of a compound of formula 1b which compound is useful as a prodrug of HIV integrase inhibitors and therefore is useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. The process includes the steps of a) brominating a compound of formula P-7 to form a compound of formula P-8, b) treating a compound of formula P-8 with NaIO4 to form a compound of formula P-9, c) reacting a compound of formula P-9 with [(2R)-pyrrolidinylmethyl]amine of formula to form a compound of formula P-10, d) reacting a compound of formula P-10 with 2, 4-difluorobenzylamine to form a compound of formula P-11, e) treating a compound of P-11 with palladium on carbon and ammonium hydroxide to form a compound of formula 1a, and f) treating a compound of formula 1a with NaOH and ethanol to form a compound of formula 1b. The structures of the above mentioned compounds are disclosed in the specification.

    摘要翻译： 本发明涉及一种制备式1b化合物的方法，该化合物可用作HIV整合酶抑制剂的前药，因此可用于抑制HIV复制，预防和/或治疗HIV感染， 和治疗艾滋病和/或ARC。 该方法包括以下步骤：a）将式P-7化合物溴化以形成式P-8的化合物，b）用NaIO 4处理式P-8的化合物以形成式P-9的化合物，c） 使式P-9的化合物与式的[（2R） - 吡咯烷基甲基]胺反应形成式P-10的化合物，d）使式P-10的化合物与2,4-二氟苄胺反应，形成化合物 式P-11，e）用钯碳和氢氧化铵处理P-11化合物以形成式1a化合物，和f）用NaOH和乙醇处理式1a化合物以形成式1b化合物。 上述化合物的结构在说明书中公开。

    Assistance device of network system
    9.
    发明授权
    Assistance device of network system 有权
    网络系统辅助装置

    公开(公告)号：US09596124B2

    公开(公告)日：2017-03-14

    申请号：US14005324

    申请日：2011-03-23

    申请人： Hiromi Sasaki ,  Hiroshi Yoshida ,  Takeshi Jinkawa ,  Masaki Namie ,  Hirohito Mizumoto ,  Yutaka Tahara ,  Shigenori Sawada

    发明人： Hiromi Sasaki ,  Hiroshi Yoshida ,  Takeshi Jinkawa ,  Masaki Namie ,  Hirohito Mizumoto ,  Yutaka Tahara ,  Shigenori Sawada

    IPC分类号： G06F15/16 ,  H04L12/24 ,  H04L12/40 ,  H04L12/403 ,  H04L29/12

    CPC分类号： H04L41/04 ,  H04L12/40006 ,  H04L12/403 ,  H04L41/0853 ,  H04L41/0866 ,  H04L41/12 ,  H04L41/145 ,  H04L61/2038

    摘要： A design assistance device includes: a design information storage section configured to store design information containing at least information of slave devices and information of a topology in a network system in accordance with a design created by a user; an actual configuration information generation section configured to generate actual configuration information containing at least the information of the slave devices and the information of the topology in the actual network system; a comparison section configured to compare the design information and the actual configuration information; and an output section configured to generate a comparison screen indicating the respective configurations of the designed network system and the actual network system along with their commonalities and differences and outputting the comparison screen to a display device. Thus, a technology can be provided which assists the user to easily compare the designed network configuration and the actual machine's network configuration.

    摘要翻译： 设计辅助装置包括：设计信息存储部分，被配置为根据由用户创建的设计，在网络系统中存储至少包含从设备信息和拓扑信息的设计信息; 实际配置信息生成部，被配置为生成至少包含所述从设备的信息和所述实际网络系统中的拓扑的信息的实际配置信息; 配置为比较设计信息和实际配置信息的比较部分; 以及输出部，其被配置为生成指示所设计的网络系统和实际网络系统的各自配置及其共同点和差异的比较屏幕，并将比较屏幕输出到显示设备。 因此，可以提供一种技术，其帮助用户容易地比较设计的网络配置和实际机器的网络配置。