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公开(公告)号:EP1221444B1
公开(公告)日:2005-08-31
申请号:EP00940909.5
申请日:2000-06-30
申请人: Eisai Co., Ltd.
发明人: ASANO, Osamu , HARADA, Hitoshi , YOSHIKAWA, Seiji , WATANABE, Nobuhisa , INOUE, Takashi , HORIZOE, Tatsuo , YASUDA, Nobuyuki , OHASHI, Kaya , MINAMI, Hiroe , NAGAOKA, Junsaku , MURAKAMI, Manabu , KOBAYASHI, Seiichi , TANAKA, Isao , KAWATA, Tsutomu , SHIMOMURA, Naoyuki , AKAMATSU, Hiroshi , OZEKI, Naoki , SHIMIZU, Toshikazu , HAYASHI, Kenji , HAGA, Toyokazu , NEGI, Shigeto , NAITO, Toshihiko
IPC分类号: C07D473/34 , C07D473/18 , C07D471/08 , C07D473/40 , C07D239/48 , C07D213/73 , C07D213/75 , C07D235/18 , C07D471/04 , C07D487/04 , C07D401/12
CPC分类号: C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
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公开(公告)号:EP1380562A1
公开(公告)日:2004-01-14
申请号:EP02720489.0
申请日:2002-04-18
申请人: Eisai Co., Ltd.
发明人: MATSUURA, Fumiyoshi , EMORI, Eita , SHINODA, Masanobu , CLARK, Richard , KASAI, Shunji , YOSHITOMI, Hideki , YAMAZAKI, Kazuto , INOUE, Takashi , MIYASHITA, Sadakazu , HIHARA, Taro , HARADA, Hitoshi , OHASHI, Kaya
IPC分类号: C07C59/64
CPC分类号: C07D413/12 , C07C59/58 , C07C59/68 , C07C59/72 , C07C233/25 , C07C235/24 , C07C251/48 , C07C251/52 , C07C251/54 , C07C255/37 , C07C255/54 , C07C259/10 , C07C271/14 , C07C271/16 , C07C271/22 , C07C271/28 , C07C271/58 , C07C309/73 , C07C309/75 , C07C311/19 , C07C317/18 , C07C317/22 , C07C323/20 , C07D209/08 , C07D209/18 , C07D209/24 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/75 , C07D215/14 , C07D215/18 , C07D215/26 , C07D235/06 , C07D235/12 , C07D277/56 , C07D295/096 , C07D295/192 , C07D307/79 , C07D317/54 , C07D417/12
摘要: The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them.
Wherein R 1 represents a hydrogen atom, hydroxyl group, halogen, carboxyl group, or a C 1-6 alkyl group etc., each of which may have one or more substituents; L represents a single bond, or a C 1-6 alkylene group, a C 2-6 alkenylene group or a C 2-6 alkynylene group, each of which may have one or more substituents; M represents a single bond, or a C 1-6 alkylene group, a C 2-6 alkenylene group or a C 2-6 alkynylene group, each of which may have one or more substituents; T represents a single bond, or a C 1-3 alkylene group, a C 2-3 alkenylene group or a C 2-3 alkynylene group, each of which may have one or more substituents; W represents a carboxyl group;
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represents a single bond etc. ; X represents a single bond, oxygen atom, a group represented by -NR X1 CQ 1 O- (wherein Q 1 represents an oxygen atom or sulfur atom; and R X1 represents a hydrogen atom, formyl group, or a C 1-6 alkyl group etc., each of which may have one or more substituents), -OCQ 1 NR X1 - (wherein Q 1 and R X1 are as defined above), -CQ 1 NR x1 O- (wherein Q 1 and R X1 are as def ined above), ONR X1 CQ 1 - (wherein Q 1 and R X1 are as defined above), - Q 2 SO 2 - (wherein Q 2 is an oxygen atom or -NR X10 - (wherein R X10 represents a hydrogen atom, formyl group, or a C 1-6 alkyl group etc., each of which may have one or more substituents)) or -SO 2 Q 2 - (wherein Q 2 is as defined above),
(wherein, provided that R X2 and R X3 , and/or R X4 and R X5 may together form a ring, Q 3 and Q 4 are the same as or different from each other and each represents an oxygen atom, (O)S(O) or NR X10 (wherein NR X10 is as defined above)); Y represents a 5- to 14-membered aromatic group etc., which may have one or more substituents and one or more hetero atoms; and the ring Z represents a 5-to 14-membered aromatic group which may have 0 to 4 substituents and one or more hetero atoms, and wherein part of the ring may be saturated.摘要翻译: 本发明提供了可用作胰岛素敏化剂的新型羧酸化合物,其盐或其水合物,以及包含该化合物作为活性成分的药物。 也就是说,本发明提供由下式表示的羧酸化合物,其盐,其酯或它们的水合物。 其中R 1表示氢原子,羟基,卤素,羧基或C 1-6烷基等,其各自可具有一个或多个取代基; L表示可以具有一个或多个取代基的单键或C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基, M表示单键或C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基,其各自可具有一个或多个取代基; T表示可以具有一个或多个取代基的单键或C 1-3亚烷基,C 2-3亚烯基或C 2-3亚炔基, W表示羧基; - - - 代表单一债券等; X表示单键,氧原子,-NR X X1表示的基团,其中Q 1表示氧原子或硫原子,R X1表示氢原子,甲酰基 ,或C 1-6烷基等,其各自可以具有一个或多个取代基),-OCQ 1 NR X1 - (其中Q 1和R X1如上所定义), - CQ <1> NR
O-(其中Q 1和R X 1如上所定义),ONR X1和Q 1 - (其中Q 1和R X1均为 (其中Q 2是氧原子或-NR X 10 - (其中R X 10表示氢原子,甲酰基或C 1-6烷基等) ,其中每个可以具有一个或多个取代基))或-SO 2 Q 2 - (其中Q 2如上所定义),(其中,条件是R X2和R X3,和/或 R X和R X可以一起形成环,Q 3和Q 4彼此相同或不同,并且各自表示氧原子,(O)S(O)或NR X10>(其中NR X10如上所定义)); Y表示可以具有一个或多个取代基和一个或多个杂原子的5至14元芳族基团等; 并且环Z表示可以具有0至4个取代基和一个或多个杂原子的5至14元芳族基团,并且其中部分环可以是饱和的。 -
公开(公告)号:EP1221444A1
公开(公告)日:2002-07-10
申请号:EP00940909.5
申请日:2000-06-30
申请人: Eisai Co., Ltd.
发明人: ASANO, Osamu , HARADA, Hitoshi , YOSHIKAWA, Seiji , WATANABE, Nobuhisa , INOUE, Takashi , HORIZOE, Tatsuo , YASUDA, Nobuyuki , OHASHI, Kaya , MINAMI, Hiroe , NAGAOKA, Junsaku , MURAKAMI, Manabu , KOBAYASHI, Seiichi , TANAKA, Isao , KAWATA, Tsutomu , SHIMOMURA, Naoyuki , AKAMATSU, Hiroshi , OZEKI, Naoki , SHIMIZU, Toshikazu , HAYASHI, Kenji , HAGA, Toyokazu , NEGI, Shigeto , NAITO, Toshihiko
IPC分类号: C07D473/34 , C07D473/18 , C07D471/08 , C07D473/40 , C07D239/48 , C07D213/73 , C07D213/75 , C07D235/18 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/52 , A61K31/522 , A61P3/10 , A61P43/00
CPC分类号: C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
摘要: The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action.
That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I):
(wherein R 1 represents e.g. an amino group which may be substituted with an alkyl group; R 2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R 3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.
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