公开(公告)号：EP1221444A4

公开(公告)日：2003-05-07

申请号：EP00940909

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

IPC分类号： A61P3/10 ,  A61P43/00 ,  C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D473/40 ,  C07D213/73 ,  C07D213/75 ,  C07D235/18 ,  C07D239/48 ,  C07D401/12 ,  C07D471/08 ,  C07D473/18 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D473/40

摘要： Novel fused imidazole compounds of general formula (I), pharmacologically acceptable salts thereof, or hydrates of both, exhibiting adenosine A2 receptor antagonism and being effective in the prevention and treatment of diabetes mellitus and complications of diabetes; wherein R1 is optionally alkylated amino or the like; R2 is hydrogen, alkyl, or the like; R3 is optionally substituted aryl, a pyridinone group, a pyrimidinone group, or the like; Ar is an optionally sybstituted aryl or heteroaryl group, or the like; and Q and W are each independently N or CH.

摘要翻译： 本发明提供了一种基于腺苷A2受体拮抗剂作用的新型糖尿病和糖尿病并发症的预防或治疗剂。 也就是说，提供了具有腺苷A2受体拮抗剂作用的新颖的缩合咪唑化合物，对预防或治疗糖尿病和糖尿病并发症有效，并且由式（I）表示：其中R 1， 例如可以被烷基取代的氨基; R 2表示例如可以被羟基取代的氢原子，烷基，环烷基或烷基，烯基或炔基等; R 3表示例如任选取代的烷基，烯基，炔基，芳基，杂芳基，吡啶酮基，嘧啶酮基或哌嗪酮基; Ar表示例如任选取代的芳基或杂芳基; Q和W相同 彼此相同或不同，并且各自表示N或CH），其药理学上可接受的盐或其水合物。

公开(公告)号：EP1054012A4

公开(公告)日：2001-12-12

申请号：EP98961528

申请日：1998-12-24

申请人： EISAI CO LTD

发明人： ASANO OSAMU ,  HARADA HITOSHI ,  HOSHINO YORIHISA ,  YOSHIKAWA SEIJI ,  INOUE TAKASHI ,  HORIZOE TATSUO ,  YASUDA NOBUYUKI ,  NAGATA KAYA ,  NAGAOKA JUNSAKU ,  MURAKAMI MANABU ,  KOBAYASHI SEIICHI

IPC分类号： A61K31/52 ,  A61P3/10 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  A61K31/505 ,  A61K45/00 ,  C07D473/04 ,  C07D473/40 ,  C07D487/04 ,  C07D487/14 ,  A61K31/645

CPC分类号： C07D473/30 ,  A61K31/52 ,  C07D473/00 ,  C07D473/34

摘要： Preventives/remedies of a novel type for diabetes and complications thereof based on the adenosine A2 receptor antagonism. Purine derivatives represented by general formula (I), pharmacologically acceptable salts thereof or hydrates of the same have adenosine A2 receptor antagonism and are useful in preventing and treating diabetes and its complications. Moreover, adenosine A2 receptor antagonists being different from the above compounds in structure, for example KW6002 are also useful in preventing and treating diabetes and its complications. In formula (I), W represents -CH2CH2-, -CH=CH- or -C≡C-; and R1 represents KW6002.