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    Novel Cercosporamide Derivative
    1.
    发明申请
    Novel Cercosporamide Derivative 审中-公开
    新型Cercosporamide衍生物

    公开(公告)号：US20090036492A1

    公开(公告)日：2009-02-05

    申请号：US11990289

    申请日：2006-08-08

    申请人： Akihiro Furukawa ,  Jun Ohsumi ,  Tsuyoshi Arita ,  Takehiro Fukuzaki ,  Kazushi Araki ,  Makoto Mori ,  Takayuki Momose ,  Takeshi Honda ,  Masanori Kuroha ,  Ryo Okuyama ,  Susumu Satoh

    发明人： Akihiro Furukawa ,  Jun Ohsumi ,  Tsuyoshi Arita ,  Takehiro Fukuzaki ,  Kazushi Araki ,  Makoto Mori ,  Takayuki Momose ,  Takeshi Honda ,  Masanori Kuroha ,  Ryo Okuyama ,  Susumu Satoh

    IPC分类号： A61K31/443 ,  C07D307/91 ,  C07D405/12 ,  A61K31/343

    CPC分类号： C07D307/91 ,  C07D405/12 ,  C07D407/12

    摘要： The present invention relates to a novel cercosporamide derivative, a pharmacologically acceptable salt thereof or an ester thereof which has an excellent hypoglycemic effect and is useful as a therapeutic and/or prophylactic agent for diabetes.A cercosporamide derivative having the general formula (I): [wherein X represents an oxygen atom or the like, R1 represents a hydrogen atom or a C1-C6 alkyl group, R2 represents a hydrogen atom, a C1-C6 alkyl group or a C1-C6 halogenated alkyl group, R3 represents a hydrogen atom or a C1-C6 alkyl group, R4 represents a C6-C10 aryl group which may be substituted with one to five group(s) independently selected from Substituent Group a, or the like, n represents 1, 2 or 3, and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, a C2-C6 alkenyloxy group, a C2-C6 alkynyloxy group and the like], a pharmacologically acceptable salt thereof or an ester thereof.

    摘要翻译： 本发明涉及一种具有优异的降血糖作用，可用作糖尿病治疗和/或预防剂的新颖的孢子虫素衍生物，其药理学上可接受的盐或其酯。 具有通式（I）的孢孢酰胺衍生物：[其中X表示氧原子等，R 1表示氢原子或C 1 -C 6烷基，R 2表示氢原子，C 1 -C 6烷基或C 1 -C 6卤代烷基，R 3表示氢原子或C 1 -C 6烷基，R 4表示可以被一至五个独立地选自取代基组a的基团取代的C 6 -C 10芳基等， n表示1,2或3，取代基组a表示卤素原子，C1-C6烷基，C1-C6卤代烷基，C2-C6烯基，C2-C6炔基，C1-C6 烷氧基，C1-C6卤代烷氧基，C2-C6链烯氧基，C2-C6炔氧基等]，其药理学上可接受的盐或其酯。

    BENZYLPHENYL GLUCOPYRANOSIDE DERIVATIVE
    2.
    发明申请
    BENZYLPHENYL GLUCOPYRANOSIDE DERIVATIVE 审中-公开
    苯甲酰基吡咯烷酮衍生物

    公开(公告)号：US20090137499A1

    公开(公告)日：2009-05-28

    申请号：US12280510

    申请日：2007-08-03

    申请人： Takeshi Honda ,  Minoru Oguchi ,  Masao Yoshida ,  Ryo Okuyama ,  Tsuneaki Ogata ,  Manabu Abe ,  Kenjiro Ueda ,  Jun Ohsumi ,  Masanori Izumi

    发明人： Takeshi Honda ,  Minoru Oguchi ,  Masao Yoshida ,  Ryo Okuyama ,  Tsuneaki Ogata ,  Manabu Abe ,  Kenjiro Ueda ,  Jun Ohsumi ,  Masanori Izumi

    IPC分类号： A61K31/706 ,  C07G3/00 ,  A61K31/7004 ,  C07H17/02

    CPC分类号： C07H15/203 ,  A61K9/2018 ,  C07H17/02

    摘要： The present invention relates to a benzylphenyl glucopyranoside derivative having an excellent inhibitory effect on human SGLT1 and/or SGLT2 activity. There is provided a compound or a pharmacologically acceptable salt thereof represented by the following general formula (I): wherein R1 represents a hydrogen atom, an amino group, a hydroxy C1-C6 alkyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, etc.; R4 represents a hydrogen atom, a C2-C7 acyl group, etc.; R5, R6, R7, and R8 are the same or different and each represents a hydrogen atom or a C1-C6 alkyl group, provided that R5, R6, R7 and R8 are not hydrogen atoms at the same time; n is 0 to 4; and X is CH or N.

    摘要翻译： 本发明涉及对人SGLT1和/或SGLT2活性具有优异抑制作用的苄基苯基吡喃葡萄糖苷衍生物。 提供由以下通式（I）表示的化合物或其药理学上可接受的盐：其中R1表示氢原子，氨基，羟基C1-C6烷基等; R2表示氢原子等; R3表示C1-C6烷基，羟基C1-C6烷基等; R4表示氢原子，C2-C7酰基等; R5，R6，R7和R8相同或不同，各自表示氢原子或C1-C6烷基，条件是R5，R6，R7和R8不同时为氢原子; n为0〜4; X为CH或N.