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    Hydroxypyrimidinone derivatives having inhibitory activity against HIV integrase
    6.
    发明授权
    Hydroxypyrimidinone derivatives having inhibitory activity against HIV integrase 有权
    具有对HIV整合酶的抑制活性的羟基嘧啶酮衍生物

    公开(公告)号：US07745453B2

    公开(公告)日：2010-06-29

    申请号：US10583796

    申请日：2004-12-21

    申请人： Hidenori Mikamiyama ,  Minamo Iwata ,  Yoshiyuki Taoda

    发明人： Hidenori Mikamiyama ,  Minamo Iwata ,  Yoshiyuki Taoda

    IPC分类号： A61K31/505 ,  C07D239/02 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

    CPC分类号： C07D417/14 ,  C07D401/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D487/04

    摘要： Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S(═O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.

    摘要翻译： 式（1）的化合物，含有它们的药物，特别是具有抗病毒活性的抗HIV剂，特别是针对HIV整合酶的抑制活性，其中X表示以下基团之一：（其中，C环为含氮芳族杂环 环中与原子相邻的原子中的至少一个原子与嘧啶环结合是未取代的氮原子; R 10是氢或低级烷基; D环是芳基或杂芳基），Z 1和Z 3各自独立地是单键，O，S， S（ΟO）或SO2; Z2是单键，低级亚烷基或低级亚烯基; Ar是任选取代的芳基或任选取代的杂芳基; R 1是低级烷基，取代的低级烷基等; R2是氢原子或任选取代的低级烷基; 或者R 1和R 2可以与相邻原子一起形成任选取代的杂环，其药学上可接受的盐或溶剂合物。

    Hydroxypyrimidinone derivatives having inhibitory activity against hiv integrase
    7.
    发明申请
    Hydroxypyrimidinone derivatives having inhibitory activity against hiv integrase 有权
    对hiv整合酶具有抑制活性的羟基嘧啶酮衍生物

    公开(公告)号：US20070149556A1

    公开(公告)日：2007-06-28

    申请号：US10583796

    申请日：2004-12-21

    申请人： Hidenori Mikamiyama ,  Minamo Iwata ,  Yoshiyuki Taoda

    发明人： Hidenori Mikamiyama ,  Minamo Iwata ,  Yoshiyuki Taoda

    IPC分类号： A61K31/513 ,  C07D403/02

    CPC分类号： C07D417/14 ,  C07D401/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D487/04

    摘要： Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S (═O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.

    摘要翻译： 式（1）的化合物，含有它们的药物，特别是具有抗病毒活性的抗HIV剂，特别是针对HIV整合酶的抑制活性，其中X表示以下基团之一：（其中，C环为含氮芳族杂环 环中与原子相邻的原子中至少一个原子与嘧啶环结合是未取代的氮原子; R 10是氢或低级烷基; D环是芳基或杂芳基） / SUP>和Z 3各自独立地为单键O，S，S（-O）或SO 2; Z 2是单键，低级亚烷基或低级亚烯基; Ar是任选取代的芳基或任选取代的杂芳基; R 1是低级烷基，取代的低级烷基等; R 2是氢原子或任选取代的低级烷基; 或R 1和R 2可以与相邻原子一起形成任选取代的杂环，其药学上可接受的盐或溶剂合物。

    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
    10.
    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。