公开(公告)号：EP2697232B1

公开(公告)日：2016-05-18

申请号：EP12723752.7

申请日：2012-04-13

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： KAWANO, Yoshikazu ,  HARAGUCHI, Yoshikazu ,  SASAKI, Hirofumi ,  UEMATSU, Yukitaka ,  TSUBOUCHI, Hidetsugu ,  YATA, Hiromi ,  SHIMIZU, Hiroshi ,  KOHASHI, Kazuho ,  ITOTANI, Motohiro ,  TAI, Kuninori ,  TAKEMURA, Isao ,  HAYASHI, Mikayo ,  HASHIZUME, Hiroyuki ,  MATSUBA, Miki ,  NAKAMURA, Izuru ,  CHEN, Xiuhao ,  MATSUMOTO, Makoto

IPC分类号： C07D498/04 ,  A61K31/5365 ,  A61P31/04 ,  A61P31/06

CPC分类号： C07D498/04

公开(公告)号：EP2697232A1

公开(公告)日：2014-02-19

申请号：EP12723752.7

申请日：2012-04-13

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： KAWANO, Yoshikazu ,  HARAGUCHI, Yoshikazu ,  SASAKI, Hirofumi ,  UEMATSU, Yukitaka ,  TSUBOUCHI, Hidetsugu ,  YATA, Hiromi ,  SHIMIZU, Hiroshi ,  KOHASHI, Kazuho ,  ITOTANI, Motohiro ,  TAI, Kuninori ,  TAKEMURA, Isao ,  HAYASHI, Mikayo ,  HASHIZUME, Hiroyuki ,  MATSUBA, Miki ,  NAKAMURA, Izuru ,  CHEN, Xiuhao ,  MATSUMOTO, Makoto

IPC分类号： C07D498/04 ,  A61K31/5365 ,  A61P31/04 ,  A61P31/06

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 R
1 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 R
1 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 R
2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.

摘要翻译： 本发明提供了一种对结核杆菌，耐多药结核杆菌和非典型耐酸杆菌具有优异杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。 具体而言，本发明提供式（1）代表的化合物或其盐，其中R 1代表四氢异喹啉基，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， R 1表示的苯基，联苯基和吡啶基各自直接或通过连接基与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，氮杂二环辛基，恶唑基，哌嗪基 ，哌啶基，噻唑基等，这些基团中的每一个任选被取代; 并且R 2代表氢或低级烷基。 本发明进一步提供含有上述的药物组合物。

公开(公告)号：EP3981772A1

公开(公告)日：2022-04-13

申请号：EP20818866.4

申请日：2020-06-05

申请人： Otsuka Pharmaceutical Co., Ltd.

发明人： MIYAJIMA, Rin ,  HAYASHI, Takashi ,  SAKAI, Koji ,  OTANI, Yuki ,  HAYASHI, Mikayo ,  WADATSU, Takashi ,  NAGABUKURO, Akira ,  TANAKA, Masaki ,  NISHIKAWA, Yuki

IPC分类号： C07D495/04 ,  C07K7/06 ,  C12Q1/02 ,  G01N33/53 ,  G01N33/566

摘要： A tetra-functional compound contains a ligand-binding moiety (A) or ligand, a reactive moiety (D), a cleavable moiety (E), and a biotin tag (B), which are linked optionally via a spacer, wherein the ligand-binding moiety (A) is an activated functional group such as an amine-reactive group, or a reactive functional group such as -COOH; the reactive moiety (D) is a group having the structure of a compound such as 2-aryl-5-carboxytetrazole; the cleavable moiety (E) is a group having the structure of a compound such as 1-(4,4-dimethyl-2,6-dioxocyclohex-1-ylidene)ethyl; and the spacer is a group such as a linear or branched alkylene group having one or more carbon atoms, substituted with a crosslinking group.