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    C-phenyl glycitol compound
    3.
    发明授权
    C-phenyl glycitol compound 有权
    C-苯基甘氨醇化合物

    公开(公告)号：US07973012B2

    公开(公告)日：2011-07-05

    申请号：US12301463

    申请日：2007-05-18

    申请人： Hiroyuki Kakinuma ,  Yohei Kobashi ,  Yuko Hashimoto ,  Takahiro Oi ,  Hitomi Takahashi ,  Hideaki Amada ,  Yuki Iwata

    发明人： Hiroyuki Kakinuma ,  Yohei Kobashi ,  Yuko Hashimoto ,  Takahiro Oi ,  Hitomi Takahashi ,  Hideaki Amada ,  Yuki Iwata

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H1/00 ,  C07H5/04

    CPC分类号： C07D405/10 ,  C07D309/12

    摘要： Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, —O—(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is —NHC(═NH)NH2 or —NHCON(RB)RC, n is not 1, Z is —CONHRA, —NHC(═NH)NH2 or —NHCON(RB)RC,

    摘要翻译： 提供了可以通过抑制SGLT1活性和SGLT2活性而作为糖尿病的预防或治疗剂的新颖的C-苯基糖醇化合物，从而表现出葡萄糖吸收抑制作用和尿葡萄糖排泄作用。 由下式（I）表示的C-苯基糖醇化合物或其药学上可接受的盐或其水合物，其中R 1和R 2相同或不同，表示氢原子，羟基，C 1-6烷基， C 1-6烷氧基或卤原子，R 3为氢原子，C 1-6烷基，C 1-6烷氧基或卤素原子，Y为C 1-6亚烷基，-O-（CH 2）n - （n为1〜4的整数）或C 2-6亚烯基，条件是当Z为-NHC（= NH）NH 2或-NHCON（RB）RC时，n不为1，Z为-CONHRA， - NHC（= NH）NH 2或-NHCON（RB）RC，

    4-ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS
    5.
    发明申请
    4-ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS 有权
    4-ISOPROPYLPHENYL GLUCITOL化合物作为SGLT1抑制剂

    公开(公告)号：US20110306759A1

    公开(公告)日：2011-12-15

    申请号：US13202523

    申请日：2010-02-23

    申请人： Hiroyuki Kakinuma ,  Yohei Kobashi ,  Tomomichi Chonan ,  Takahiro Oi ,  Fumiyasu Shiozawa ,  Yuki Iwata ,  Kenichi Kawabe

    发明人： Hiroyuki Kakinuma ,  Yohei Kobashi ,  Tomomichi Chonan ,  Takahiro Oi ,  Fumiyasu Shiozawa ,  Yuki Iwata ,  Kenichi Kawabe

    IPC分类号： C07H7/04 ,  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: wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.

    摘要翻译： 本发明提供了通过抑制小肠中的葡萄糖吸收而不具有积累在体内的倾向而抑制SGLT1活性来抑制餐后高血糖（或葡萄糖耐量降低）的4-异丙基苯基甘醇醇化合物，其中， 可以抑制糖尿病和代谢综合征的发病，或者可以治疗这些疾病。 由下式（I）表示的4-异丙基苯基硬糖醇化合物或其药学上可接受的盐：其中R1表示氢原子等，R2表示甲基等，R3表示被 氨基等，R4表示氢原子等。

    AMINOTHIAZOLE DERIVATIVE
    8.
    发明申请
    AMINOTHIAZOLE DERIVATIVE 失效
    氨基噻唑衍生物

    公开(公告)号：US20120220767A1

    公开(公告)日：2012-08-30

    申请号：US13502636

    申请日：2010-10-04

    申请人： Tetsuya Yabuuchi ,  Yusuke Oka ,  Shoichi Kuroda ,  Takahiro Oi ,  Yoshinori Sekiguchi

    发明人： Tetsuya Yabuuchi ,  Yusuke Oka ,  Shoichi Kuroda ,  Takahiro Oi ,  Yoshinori Sekiguchi

    IPC分类号： C07D417/14

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which has a PI3 kinase γ inhibitory effect and is useful as a prophylactic or therapeutic agent for articular rheumatism, Crohn's disease, irritable colitis, Sjoegren's syndrome, multiple sclerosis, systemic lupus erythematosus, asthma, atopic dermatitis, arteriosclerosis, organ transplant rejection, cancer, retinopathy, psoriasis, arthrosis deformans, age-related macular degeneration, type II diabetes, insulin resistance, obesity, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hyperlipemia, etc.

    摘要翻译： 由式（1）表示的化合物或其药学上可接受的盐，其具有PI3激酶γ抑制作用，并且可用作关节风湿病，克罗恩病，过敏性结肠炎，Sjoegren综合征，多发性硬化症，系统性红斑狼疮的预防或治疗剂 红斑狼疮，哮喘，特应性皮炎，动脉硬化，器官移植排斥，癌症，视网膜病变，牛皮癣，变形性关节炎，年龄相关性黄斑变性，II型糖尿病，胰岛素抵抗，肥胖，非酒精性脂肪性肝病（NAFLD），非酒精性 脂肪性肝炎（NASH），高脂血症等

    4-isopropylphenyl glucitol compounds as SGLT1 inhibitors
    10.
    发明授权
    4-isopropylphenyl glucitol compounds as SGLT1 inhibitors 有权
    4-异丙基苯基葡糖醇化合物作为SGLT1抑制剂

    公开(公告)号：US08466113B2

    公开(公告)日：2013-06-18

    申请号：US13202523

    申请日：2010-02-23

    申请人： Hiroyuki Kakinuma ,  Yohei Kobashi ,  Tomomichi Chonan ,  Takahiro Oi ,  Fumiyasu Shiozawa ,  Yuki Iwata ,  Kenichi Kawabe

    发明人： Hiroyuki Kakinuma ,  Yohei Kobashi ,  Tomomichi Chonan ,  Takahiro Oi ,  Fumiyasu Shiozawa ,  Yuki Iwata ,  Kenichi Kawabe

    IPC分类号： C07H5/04 ,  C07H5/06 ,  A01N43/04 ,  A61K31/70

    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: wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.

    摘要翻译： 本发明提供了通过抑制小肠中的葡萄糖吸收而不具有积累在体内的倾向而抑制SGLT1活性来抑制餐后高血糖（或葡萄糖耐量降低）的4-异丙基苯基甘醇醇化合物，其中， 可以抑制糖尿病和代谢综合征的发病，或者可以治疗这些疾病。 由下式（I）表示的4-异丙基苯基硬糖醇化合物或其药学上可接受的盐：其中R1表示氢原子等，R2表示甲基等，R3表示被 氨基等，R4表示氢原子等。