公开(公告)号：US09051333B2

公开(公告)日：2015-06-09

申请号：US14111262

申请日：2012-04-13

申请人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

发明人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

IPC分类号： C07D498/04 ,  A61K31/5383

CPC分类号： C07D498/04

摘要： The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.

摘要翻译： 本发明提供了对结核杆菌，多重耐药性结核杆菌和非典型抗酸杆菌具有优异的杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。 具体地说，本发明提供由式（1）表示的化合物或其盐，其中R1表示四氢异喹啉基，四氢喹啉基，四氢苯并氮杂基，苯并恶唑基，苯并噻唑基，吲哚基，异吲哚啉基，萘基，喹啉基，苯基，联苯基或吡啶基。 任选被取代的苯基，联苯基和吡啶基，其各自被直接取代或经由具有至少一个选自四氢吡啶基，二氮杂环庚烷基，二氮杂双环庚烷基，四氢三唑并吡嗪基，四氢咪唑并吡嗪基，氮杂双环辛基，恶唑基，哌嗪基，哌啶基 ，噻唑基等，这些基团各自任选被取代; 并且R 2表示氢或低级烷基。 本发明还提供含有上述物质的药物组合物。

公开(公告)号：US20140031342A1

公开(公告)日：2014-01-30

申请号：US14111262

申请日：2012-04-13

申请人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

发明人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

IPC分类号： C07D498/04

CPC分类号： C07D498/04

摘要： The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.

摘要翻译： 本发明提供了对结核杆菌，多重耐药性结核杆菌和非典型抗酸杆菌具有优异的杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。 具体地说，本发明提供由式（1）表示的化合物或其盐，其中R1表示四氢异喹啉基，四氢喹啉基，四氢苯并氮杂基，苯并恶唑基，苯并噻唑基，吲哚基，异吲哚啉基，萘基，喹啉基，苯基，联苯基或吡啶基。 任选被取代的苯基，联苯基和吡啶基，其各自被直接取代或经由具有至少一个选自四氢吡啶基，二氮杂环庚烷基，二氮杂双环庚烷基，四氢三唑并吡嗪基，四氢咪唑并吡嗪基，氮杂双环辛基，恶唑基，哌嗪基，哌啶基 ，噻唑基等，这些基团各自任选被取代; 并且R 2表示氢或低级烷基。 本发明还提供含有上述物质的药物组合物。