公开(公告)号：US20120101137A1

公开(公告)日：2012-04-26

申请号：US13380664

申请日：2010-06-26

申请人： Tokuyuki Yamashita ,  Kaori Chikamatsu ,  Naoki Takahashi ,  Hisakazu Iwai ,  Masakazu Kogami ,  Masao Sakairi ,  Nobuhide Watanabe ,  Hiroki Fujieda ,  Daisuke Kataoka ,  Mitsuhiro Makino ,  Noriyasu Kato ,  Toshiyuki Miyazawa ,  Kazushige Nagai ,  Nobuyoshi Kasugai ,  Hiroyo Kataoka ,  Naoki Hiramatsu ,  Nobuaki Tsuruta ,  Yurie Yamada ,  Mika Miyoshi ,  Sei Murakami ,  Izumi Goto ,  Tohru Izuchi ,  Kimie Suzuki ,  Satoko Harada ,  Martin Lang ,  Markus Hans-Juergen Seifert ,  Kristina Kaarina Wolf

发明人： Tokuyuki Yamashita ,  Kaori Chikamatsu ,  Naoki Takahashi ,  Hisakazu Iwai ,  Masakazu Kogami ,  Masao Sakairi ,  Nobuhide Watanabe ,  Hiroki Fujieda ,  Daisuke Kataoka ,  Mitsuhiro Makino ,  Noriyasu Kato ,  Toshiyuki Miyazawa ,  Kazushige Nagai ,  Nobuyoshi Kasugai ,  Hiroyo Kataoka ,  Naoki Hiramatsu ,  Nobuaki Tsuruta ,  Yurie Yamada ,  Mika Miyoshi ,  Sei Murakami ,  Izumi Goto ,  Tohru Izuchi ,  Kimie Suzuki ,  Satoko Harada ,  Martin Lang ,  Markus Hans-Juergen Seifert ,  Kristina Kaarina Wolf

IPC分类号： A61K31/433 ,  A61P3/10 ,  C07D409/04 ,  C07D333/38 ,  A61K31/427 ,  C07D417/14

CPC分类号： A61K31/427 ,  A61K31/433 ,  C07D333/40 ,  C07D409/04 ,  C07D417/14

摘要： The object of the present invention is to provide a compound having a glucokinase-activating effect.A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein X means a nitrogen atom or CR6, wherein R6 means a hydrogen atom or a halogen atom; R1 means a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 alkylthio group; R2 means a hydrogen atom or a fluorine atom; R3 means a hydrogen atom or a C1-C6 alkyl group; and one of R4 and R5 means a hydrogen atom or a C1-C6 alkyl group, and the other means a C1-C6 alkylenecarboxylic acid, a C1-C6 alkylsulfonyl group, a C1-C6 alkylcarbonyl group, or CONH2.

摘要翻译： 本发明的目的是提供具有葡糖激酶活化作用的化合物。 一种药物组合物，其包含由通式（I）表示的化合物或其药学上可接受的盐作为活性成分：其中X表示氮原子或CR 6，其中R 6表示氢原子或卤素原子; R1表示氢原子，C1-C6烷基，C1-C6烷氧基或C1-C6烷硫基; R2表示氢原子或氟原子; R3表示氢原子或C1-C6烷基; R4和R5之一表示氢原子或C1-C6烷基，另一个表示C1-C6亚烷基羧酸，C1-C6烷基磺酰基，C1-C6烷基羰基或CONH2。

公开(公告)号：US20090176841A1

公开(公告)日：2009-07-09

申请号：US12342729

申请日：2008-12-23

申请人： Yukiyasu Asano ,  Koji Maeda ,  Nobuaki Tsuruta ,  Toru Murase

发明人： Yukiyasu Asano ,  Koji Maeda ,  Nobuaki Tsuruta ,  Toru Murase

IPC分类号： A61K31/41 ,  C07D257/04 ,  C07D401/02 ,  A61K31/4439 ,  A61P3/00 ,  A61P35/00 ,  A61P27/06 ,  A61P19/10 ,  A61P25/24 ,  A61P9/00

CPC分类号： C07D209/12 ,  C07D231/56

摘要： An object of the present invention is to provide a medicament as a thyroid hormone receptor ligand which is sufficient in drug efficacy and safety, and has the excellent action as a drug. The present invention provides a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: [wherein [Chemical Formula 2] is a single bond or a double bond; A is —CH2— or —CO—; X, Y, and Z are each independently a nitrogen atom or a carbon atom; R1 is a hydrogen atom or an aralkyl group; R2 is an alkyl group or an aralkyl group, etc.; R3 is a hydrogen atom or an alkyl group, etc.; R4 is a hydrogen atom or an alkyl group; R5 is a hydrogen atom, an alkyl group or a halo lower alkyl group, etc.; R6 is a hydrogen atom or an alkyl group; R7 is a hydrogen atom, etc.; R8 is a hydrogen atom, or an alkyl group, etc.; and E is —NHCO-G-COR12, etc. (wherein G is a single bond or an alkylene group, and R12 is a hydroxy group or an alkoxy group)].

摘要翻译： 本发明的目的是提供一种药物作为甲状腺激素受体配体，其药物功效和安全性足够，作为药物具有优异的作用。 本发明提供由以下通式（I）表示的化合物或其药学上可接受的盐：[其中[化学式2] 是单键或双键; A是-CH2-或-CO-; X，Y和Z各自独立地为氮原子或碳原子; R1是氢原子或芳烷基; R2是烷基或芳烷基等; R3是氢原子或烷基等; R4是氢原子或烷基; R5是氢原子，烷基或卤代低级烷基等; R6是氢原子或烷基; R7是氢原子等; R8是氢原子或烷基等; 并且E是-NHCO-G-COR 12等（其中G是单键或亚烷基，R 12是羟基或烷氧基）]。