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    Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
    1.
    再颁专利
    Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes 失效
    嘌呤衍生物和腺苷A2受体拮抗剂作为糖尿病的预防药物/治疗药物

    公开(公告)号：USRE39112E1

    公开(公告)日：2006-05-30

    申请号：US11057854

    申请日：1998-12-24

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

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

    IPC分类号： C07D473/34 ,  C07D473/30 ,  C07D473/00 ,  A61K31/52 ,  A61K31/522

    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 antagonist 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—, or —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受体拮抗剂作用的糖尿病新型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受体拮抗剂对于糖尿病和糖尿病并发症的预防或治疗也是有效的。 在该式中，W是-CH 2 CH 2 - ，或-CH-CH-或-C≡C-; R 1是：（在该式中，X是氢原子，羟基，低级烷基，低级烷氧基等; R 5和R 5， SUP> 6 <！ - SIPO - >相同或不同，各自表示氢原子，低级烷基，环烷基等）等; R 2是可以被低级烷基等取代的氨基等; R 3是环烷基，任选取代的芳基等; R 4是低级烷基等。

    Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
    2.
    发明授权
    Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes 有权
    嘌呤衍生物和腺苷A2受体拮抗剂作为糖尿病的预防药物/治疗药物

    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。

    Concomitant drug as therapeutic agent for inflammatory bowel disease
    9.
    发明申请
    Concomitant drug as therapeutic agent for inflammatory bowel disease 审中-公开
    伴随药物作为炎症性肠病的治疗剂

    公开(公告)号：US20060177444A1

    公开(公告)日：2006-08-10

    申请号：US10549321

    申请日：2004-03-18

    申请人： Tatsuo Horizoe

    发明人： Tatsuo Horizoe

    IPC分类号： A61K38/22 ,  A61K39/395 ,  A61K31/60 ,  A61K31/573 ,  A61K31/198

    CPC分类号： C07K16/241 ,  A61K31/00 ,  A61K38/13 ,  A61K45/06 ,  A61K2300/00

    摘要： An object of the present invention is to provide a medicament efficacious for an inflammatory bowel disease such as ulcerative colitis or Crohn's disease. Specifically, it provides a therapeutic agent for inflammatory bowel diseases comprising active ingredient (a) consisting of at least one compound having inflammatory inhibiting activity selected from the group consisting of an aminosalicylic acid derivative, an antiinflammatory glucocorticoid, an immunosuppressive compound, an anti-TNFα antibody, a neurohypophysial hormone and an antiinfective compound, combined with active ingredient (b) consisting of at least one compound having PPARγ agonistic activity, wherein the agent is so configured that the compound (a) and the compound (b) are used simultaneously, separately or every scheduled time.

    摘要翻译： 本发明的目的是提供一种对炎症性肠病如溃疡性结肠炎或克罗恩病有效的药物。 具体地说，本发明提供了一种炎症性肠病治疗剂，其含有由至少一种具有炎性抑制活性的化合物组成的活性成分（a），所述化合物具有选自氨基水杨酸衍生物，抗炎性糖皮质激素，免疫抑制化合物，抗TNFα 与由至少一种具有PPARγ激动活性的化合物组成的活性成分（b）组合，其中所述试剂配置成使得化合物（a）和化合物（b）同时使用， 分别或每个预定的时间。