公开(公告)号：US06579868B1

公开(公告)日：2003-06-17

申请号：US09582840

申请日：2000-07-05

申请人： Osamu Asano ,  Hitoshi Harada ,  Yorihisa Hoshino ,  Seiji Yoshikawa ,  Takashi Inoue ,  Tatsuo Horizoe ,  Nobuyuki Yasuda ,  Kaya Nagata ,  Junsaku Nagaoka ,  Manabu Murakami ,  Seiichi Kobayashi

发明人： Osamu Asano ,  Hitoshi Harada ,  Yorihisa Hoshino ,  Seiji Yoshikawa ,  Takashi Inoue ,  Tatsuo Horizoe ,  Nobuyuki Yasuda ,  Kaya Nagata ,  Junsaku Nagaoka ,  Manabu Murakami ,  Seiichi Kobayashi

IPC分类号： C07D47334

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

摘要： The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, —CH═CH— or —C≡C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc. which maybe substituted with a lower alkyl group, etc.; R3 is a cycloalkyl group, an optionally substituted aryl group, etc.; and R4 is a lower alkyl group etc.

摘要翻译： 本发明提供了基于腺苷A2受体拮抗作用的新型糖尿病和糖尿病并发症的预防或治疗剂。由式（I）表示的嘌呤化合物，其药理学上可接受的盐或其水合物具有 腺苷A2受体拮抗作用，可用于预防或治疗糖尿病和糖尿病并发症。 此外，与上述化合物例如KW6002具有不同结构的腺苷A2受体拮抗剂对于预防或治疗糖尿病和糖尿病并发症也是有效的。在该式中，W是-CH 2 CH 2 - ， - CH = CH - 或-C = C-; R1为（式中，X为氢原子，羟基，低级烷基，低级烷氧基等），R5和R6彼此相同或不同，分别表示氢原子，低级 烷基，环烷基等）等; R2是可被低级烷基取代的氨基等; R3是环烷基，任选取代的芳基等; R4为低级烷基等。