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    C-PHENYL 1-THIOGLUCITOL COMPOUND
    1.
    发明公开
    C-PHENYL 1-THIOGLUCITOL COMPOUND 有权
    C-苯基1-硫代胡萝卜醇化合物

    公开(公告)号：EP2036901A1

    公开(公告)日：2009-03-18

    申请号：EP07767824.1

    申请日：2007-06-28

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： KAKINUMA, Hiroyuki ,  OI, Takahiro ,  KOBASHI, Yohei ,  HASHIMOTO, Yuko ,  TAKAHASHI, Hitomi

    IPC分类号： C07D335/02 ,  A61K31/382 ,  A61P3/10 ,  A61P43/00

    CPC分类号： C07D335/02 ,  C07H7/04

    摘要： C-phenyl 1-thioglucitol compounds of the following formula (I) or pharmaceutically acceptable salts thereof or hydrates thereof:

    [wherein
    X represents a hydrogen atom or a C 1-6 alkyl group,
    Y represents a C 1-6 alkylene group or -O-(CH 2 )n- (wherein n represents an integer of 1 to 5), and
    Z represents -CONHR A or -NHCONHR B (provided that when Z represents -NHCONHR B , n is not 1),
    wherein
    R A represents a C 1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and -CONH 2 , and
    R B represents a hydrogen atom or a C 1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and -CONH 2 ] are useful as prophylactic or therapeutic agents for diabetes, because of their suppressive effect on sugar (e.g., glucose) absorption through inhibition of SGLT1 activity, or alternatively, because of their suppressive effect on sugar (e.g., glucose) absorption and excretory effect on urinary sugars through inhibition of both SGLT1 and SGLT2 activities.

    摘要翻译： 下式（I）的C-苯基1-硫代葡萄糖醇化合物或其药学上可接受的盐或其水合物：[其中X代表氢原子或C1-6烷基，Y代表C1-6亚烷基或-O- （CH 2）n - （式中，n表示1〜5的整数），Z表示-CONHRA或-NHCONHRB（条件是当Z表示-NHCONHRB时，n不为1），其中RA表示C1-6烷基取代 具有1至3个选自羟基和-CONH 2的取代基，RB表示氢原子或被1至3个选自羟基和-CONH 2的取代基取代的C 1-6烷基] 由于它们通过抑制SGLT1活性而抑制糖（例如葡萄糖）的吸收，或者由于它们对糖（例如葡萄糖）的吸收和对泌尿的排泄效果的抑制作用，因此可用作糖尿病的预防剂或治疗剂 糖通过抑制剂 SGLT1和SGLT2活动。

    4 -ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS
    5.
    发明公开
    4 -ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS 有权
    4-异丙基苯基硫酸酯化合物作为SGLT1抑制剂

    公开(公告)号：EP2398786A1

    公开(公告)日：2011-12-28

    申请号：EP10708391.7

    申请日：2010-02-23

    申请人： Taisho Pharmaceutical Co., Ltd.

    发明人： KAKINUMA, Hiroyuki ,  KOBASHI, Yohei ,  CHONAN, Tomomichi ,  OI, Takahiro ,  SHIOZAWA, Fumiyasu ,  IWATA, Yuki ,  KAWABE, Kenichi

    IPC分类号： C07D309/10 ,  A61K31/351 ,  A61P3/10

    CPC分类号： C07D309/10

    摘要： The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases. A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: [Chem. 1] wherein R
    1 represents a hydrogen atom, etc., R
    2 represents a methyl group, etc., R
    3 represents a C
    1-4 alkyl group substituted with an amino group(s), etc., and R
    4 represents a hydrogen atom, etc.

    摘要翻译： 本发明提供了4-异丙基苯基葡萄糖醇化合物，其没有倾向于在体内累积并抑制SGLT1活性以通过抑制小肠中的葡萄糖吸收来抑制餐后高血糖（或葡萄糖耐量降低），由此该化合物，例如， 可以抑制糖尿病和代谢综合征的发作或可以治疗这些疾病。 由下式（I）表示的4-异丙基苯基山梨醇化合物或其药学上可接受的盐： 1]式中，R 1表示氢原子等，R 2表示甲基等，R 3表示被氨基取代的C 1-4烷基等，R 4表示 氢原子等

    1-THIO-D-GLUCITOL DERIVATIVES
    6.
    发明公开
    1-THIO-D-GLUCITOL DERIVATIVES 有权
    1-硫代-D-山梨醇衍生物

    公开(公告)号：EP1845095A1

    公开(公告)日：2007-10-17

    申请号：EP06711505.5

    申请日：2006-01-10

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： KAKINUMA, Hiroyuki ,  HASHIMOTO, Yuko ,  OI, Takahiro ,  HIRANO, Hitomi

    IPC分类号： C07D335/00

    CPC分类号： C07D409/14 ,  A61K31/382 ,  A61K31/7004 ,  A61K45/06 ,  C07D335/02 ,  C07D409/04 ,  C07D409/10 ,  C07D417/10 ,  C07D495/04 ,  A61K2300/00

    摘要： The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.

    摘要翻译： 本发明提供下式的1-硫代-D-葡萄糖醇化合物，其显示了抑制SGLT2，该化合物的药学上可接受的盐或该化合物或盐的水合物的活性的作用; 以及含有该化合物作为有效成分的药物，特别是用于预防或治疗糖尿病，糖尿病相关疾病或糖尿病并发症的药物。 本发明还提供了生产1-硫代-D-葡萄糖醇化合物及其中间体的方法。