公开(公告)号：US20100204237A1

公开(公告)日：2010-08-12

申请号：US12662515

申请日：2010-04-21

申请人： Hidenori Mikamiyama ,  Minamo Iwata ,  Yoshiyuki Taoda

发明人： Hidenori Mikamiyama ,  Minamo Iwata ,  Yoshiyuki Taoda

IPC分类号： A61K31/506 ,  A61K31/519 ,  C07D487/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/14 ,  C07D413/14

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.

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。

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。