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    DIAZEPINEDIONE DERIVATIVE
    4.
    发明申请
    DIAZEPINEDIONE DERIVATIVE 有权

    公开(公告)号：US20110319610A1

    公开(公告)日：2011-12-29

    申请号：US13148728

    申请日：2010-02-15

    申请人： Shogo Sakuma ,  Toshihiro Takahashi ,  Masatoshi Ushioda ,  Toshiyasu Imai ,  Kazuhide Inoue

    发明人： Shogo Sakuma ,  Toshihiro Takahashi ,  Masatoshi Ushioda ,  Toshiyasu Imai ,  Kazuhide Inoue

    IPC分类号： C07D403/10 ,  C07D413/10

    CPC分类号： C07D243/10 ,  C07D403/10 ,  C07D413/10

    摘要： A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.

    摘要翻译： 作为P2X4受体拮抗剂，使用式（I）表示的二氮平二酮衍生物或其药理学上可接受的盐，其中，R1表示氢原子，碳原子数为1〜8的烷基等，R2，R3表示 氢原子，碳原子数1〜8的烷基，卤素原子等，R4和R5表示氢原子，碳原子数1〜8的烷基等，W表示四唑等 。

    Diazepinedione derivative
    5.
    发明授权
    Diazepinedione derivative 有权
    二氮杂二酮衍生物

    公开(公告)号：US08470814B2

    公开(公告)日：2013-06-25

    申请号：US13148728

    申请日：2010-02-15

    申请人： Shogo Sakuma ,  Toshihiro Takahashi ,  Masatoshi Ushioda ,  Toshiyasu Imai ,  Kazuhide Inoue

    发明人： Shogo Sakuma ,  Toshihiro Takahashi ,  Masatoshi Ushioda ,  Toshiyasu Imai ,  Kazuhide Inoue

    IPC分类号： C07D403/10 ,  A61K31/5513 ,  A61P25/04

    CPC分类号： C07D243/10 ,  C07D403/10 ,  C07D413/10

    摘要： A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.

    摘要翻译： 作为P2X4受体拮抗剂，使用式（I）表示的二氮平二酮衍生物或其药理学上可接受的盐，其中，R1表示氢原子，碳原子数为1〜8的烷基等，R2，R3表示 氢原子，碳原子数1〜8的烷基，卤素原子等，R4和R5表示氢原子，碳原子数1〜8的烷基等，W表示四唑等 。

    PPAR delta activators
    7.
    发明授权
    PPAR delta activators 有权
    PPARδ激活剂

    公开(公告)号：US06787552B2

    公开(公告)日：2004-09-07

    申请号：US10344496

    申请日：2003-02-11

    申请人： Shogo Sakuma ,  Tsuyoshi Endo ,  Atsushi Tendo ,  Toshihiro Takahashi ,  Shinichi Yoshida ,  Kunio Kobayashi ,  Nobutaka Mochizuki ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    发明人： Shogo Sakuma ,  Tsuyoshi Endo ,  Atsushi Tendo ,  Toshihiro Takahashi ,  Shinichi Yoshida ,  Kunio Kobayashi ,  Nobutaka Mochizuki ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    IPC分类号： A61K31421

    CPC分类号： C07D413/04 ,  C07D263/32 ,  C07D277/24

    摘要： Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.

    摘要翻译： 通式（I）的化合物或其盐和含有化合物或其盐作为活性成分的PPARdta（过氧化物酶体增殖物活化受体δ）的活化剂：其中R 1和R 2各自为氢，C 1-8 烷基，可被取代的芳基或杂环基等; A是氧，硫等; X 1和X 2各自为自由价，氧，S（O）p（其中p为0至2的整数），C（= O），C（= O）NH，NHC（= O），CH = CH等; Y是任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基，条件是当X 1是自由价时，X 2不是O或S（O）p，而当X 1是C（O） = O）NH，X 2不是自由价。

    Morphinan derivative
    8.
    发明授权
    Morphinan derivative 有权
    吗啡衍生物

    公开(公告)号：US08952030B2

    公开(公告)日：2015-02-10

    申请号：US14343218

    申请日：2012-09-07

    申请人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

    发明人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

    IPC分类号： A61K31/485 ,  C07D491/18 ,  C07D487/08 ,  C07F7/18

    CPC分类号： C07D491/18 ,  C07D471/08 ,  C07D471/22 ,  C07D487/08 ,  C07D491/22 ,  C07F7/1804

    摘要： A morphinan derivative represented by the following general formula (I): (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

    摘要翻译： 由以下通式（I）表示的吗啡喃衍生物：（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子） ，芳烷基（芳基部分具有6〜10个碳原子，亚烷基部分具有1〜5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基，C 6-10芳基，芳烷基（ 芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 3，R 4和R 5表示氢，羟基，氨基甲酰基，C 1-6烷氧基，C 6-10芳氧基等，R 6a ，R6b，R7，R8，R9和R10表示氢等，X表示O或CH2，Y表示C = O，SO2，原子键等）或其酸加成盐作为 镇痛药

    MORPHINAN DERIVATIVE
    9.
    发明申请
    MORPHINAN DERIVATIVE 有权
    莫宁衍生物

    公开(公告)号：US20140343015A1

    公开(公告)日：2014-11-20

    申请号：US14343218

    申请日：2012-09-07

    申请人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

    发明人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

    IPC分类号： C07D491/18 ,  C07F7/18 ,  C07D487/08

    CPC分类号： C07D491/18 ,  C07D471/08 ,  C07D471/22 ,  C07D487/08 ,  C07D491/22 ,  C07F7/1804

    摘要： A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like,R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like,X represents O or CH2, andY represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

    摘要翻译： 由以下通式（I）表示的吗啡喃衍生物（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子） 芳烷基（芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基，C 6-10芳基，芳烷基（芳基 部分具有6至10个碳原子，并且亚烷基部分具有1至5个碳原子）等，R3，R4和R5表示氢，羟基，氨基甲酰基，C1-6烷氧基，C6-10芳氧基等，R6a， R6b，R7，R8，R9和R10表示氢等，X表示O或CH2，Y表示C = O，SO2，原子键等）或其酸加成盐作为止痛剂 。

    GPR119 AGONIST
    10.
    发明申请
    GPR119 AGONIST 审中-公开

    公开(公告)号：US20120245344A1

    公开(公告)日：2012-09-27

    申请号：US13392961

    申请日：2010-08-30

    申请人： Tsuyoshi Endo ,  Hiroto Tanaka ,  Toshihiro Takahashi ,  Toshihiro Kunigami

    发明人： Tsuyoshi Endo ,  Hiroto Tanaka ,  Toshihiro Takahashi ,  Toshihiro Kunigami

    IPC分类号： C07D401/14 ,  C07D471/04

    CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

    摘要： A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: wherein each of R23, R24, and R25 is hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylsulfonyl, or the like; each of Q0 and T0 is CH2 or the like, or Q0 and T0 are combined to form CH═CH or the like; A0 is (CH2)p, C(O), or a bond; B0 is a bond or the like; one of U0 and V0 is N, and the other is CR31 or the like; each of X0 and Y0 is CH2CH2 or the like; Z0 is C(O)OR32 or the like; and each of R21 and R22 is hydrogen, a halogen atom, hydroxyl, C1-8 alkyl, or the like.

    摘要翻译： 由式（II）表示的化合物是GPR119激动剂，用作治疗糖尿病的药剂：其中R23，R24和R25各自为氢，卤素，C1-8烷基，C1-8烷氧基，C1- 8烷基磺酰基等; Q0和T0各自为CH2等，或Q0和T0组合形成CH = CH等; A0为（CH2）p，C（O）或键; B0是键或类似物; U0和V0之一是N，另一个是CR31等; X 0和Y 0各自为CH 2 CH 2等; Z 0是C（O）OR 32等; R 21和R 22各自为氢，卤素原子，羟基，C 1-8烷基等。