公开(公告)号：US08822503B2

公开(公告)日：2014-09-02

申请号：US13081201

申请日：2011-04-06

申请人： Takanori Kawaguchi ,  Kengo Watatani ,  Keiko Fusegi ,  Masahiro Bohno ,  Hajime Asanuma ,  Shoichi Kuroda ,  Yudai Imai ,  Tomomichi Chonan ,  Nagaaki Sato ,  Shigeru Tokita ,  Shigetada Sasako ,  Takumi Okada ,  Keishi Hayashi ,  Shin Itoh ,  Noriko Saito ,  Rui Jibiki ,  Seishi Ishiyama ,  Hirofumi Ota

发明人： Takanori Kawaguchi ,  Kengo Watatani ,  Keiko Fusegi ,  Masahiro Bohno ,  Hajime Asanuma ,  Shoichi Kuroda ,  Yudai Imai ,  Tomomichi Chonan ,  Nagaaki Sato ,  Shigeru Tokita ,  Shigetada Sasako ,  Takumi Okada ,  Keishi Hayashi ,  Shin Itoh ,  Noriko Saito ,  Rui Jibiki ,  Seishi Ishiyama ,  Hirofumi Ota

IPC分类号： A61K31/4439 ,  C07D401/06

CPC分类号： C07D401/10 ,  C07D213/64 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14

摘要： A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.

摘要翻译： 由式[1]表示的2-吡啶酮化合物：其中，在式[1]中，由A表示的环表示苯环或吡啶环，X表示由式[3]表示的任何结构 V表示单键或低级亚烷基，W表示单键，醚键或低级亚烷基（其中低级亚烷基可以含有醚键）}，化合物的互变异构体或立体异构体， 其药学上可接受的盐或其溶剂合物是具有优异的GK活化作用并可用作药物的化合物。

公开(公告)号：US20110213143A1

公开(公告)日：2011-09-01

申请号：US13126685

申请日：2009-10-28

申请人： Hideaki Amada ,  Daisuke Matsuda ,  Masahiro Bohno ,  Shiuji Saito ,  Ayako Bohno

发明人： Hideaki Amada ,  Daisuke Matsuda ,  Masahiro Bohno ,  Shiuji Saito ,  Ayako Bohno

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D471/14

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein A is a benzene ring or a pyridine ring; X is the formula —(CH2)—, the formula —(CH2)2—, an oxygen atom, a nitrogen atom or a single bond; Y is the formula —(CH2)3—NH—R3, the formula —(CH2)4—NH—R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula —CO2R4; R4 is a C1-6 alkyl group, the formula —CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; m and n are each an integer of zero or one.

摘要翻译： 提供具有优异TAFIa抑制活性的化合物。 具体地，提供由下式（I）表示的化合物或其药学上可接受的盐：其中A是苯环或吡啶环; X是式 - （CH 2） - ，式 - （CH 2）2 - ，氧原子，氮原子或单键; Y是式 - （CH2）3-NH-R3，式 - （CH2）4-NH-R3或2-氨基吡啶基; R 3是氢原子，C 1-6烷基或式-CO 2 R 4; R4是C1-6烷基，式-CHR5OC（O）R6或具有由下式Ia表示的结构的取代基; R5是C1-6烷基; R6是C1-6烷基，C3-8环烷基或苯基; R7是C1-6烷基或苯基; R1是氢原子，卤素原子，被1-3个卤素原子取代的C1-4烷基，C1-10烷基，C1-8烷氧基，C3-8环烷基，C3-8环烷氧基 基团，C4-14环烷基烷基或苯基; R2是CO2R8或四唑基; R8是氢原子，C1-10烷基或具有由下式Ib或Ic表示的结构的取代基; m和n分别为0或1的整数。