-
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。
-