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    GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES
    11.
    发明申请
    GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES 有权
    葡萄糖醛酰氧基吡唑衍生物及其在药物中的应用

    公开(公告)号：US20090093419A1

    公开(公告)日：2009-04-09

    申请号：US12169882

    申请日：2008-07-09

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A61K31/7056

    CPC分类号： A61K45/06 ,  A61K31/7056 ,  C07H17/02 ,  A61K2300/00

    摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团; Q和T之一表示由通式表示的基团：（其中P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作 用于预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。

    Benzimidazole derivatives and medical uses thereof
    12.
    发明授权
    Benzimidazole derivatives and medical uses thereof 失效
    苯并咪唑衍生物及其医疗用途

    公开(公告)号：US07547680B2

    公开(公告)日：2009-06-16

    申请号：US11473957

    申请日：2006-06-23

    申请人： Norihiko Kikuchi ,  Yoshinori Nonaka ,  Kazuya Tatani ,  Masahiro Hiratochi ,  Yu Kuramochi ,  Masayuki Isaji ,  Kazuo Shimizu ,  Takashi Miyagi

    发明人： Norihiko Kikuchi ,  Yoshinori Nonaka ,  Kazuya Tatani ,  Masahiro Hiratochi ,  Yu Kuramochi ,  Masayuki Isaji ,  Kazuo Shimizu ,  Takashi Miyagi

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07H19/052

    摘要： The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like.In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.

    摘要翻译： 本发明提供由下式（I）表示的苯并咪唑衍生物或其药学上可接受的盐或其前药，其对钠依赖性核苷转运蛋白2具有抑制活性，并且可用于与血浆尿酸异常有关的疾病 水平。 本发明的化合物可用于预防或治疗痛风，高尿酸血症，尿结石病，高尿酸性肾病等。 在该式中，n为1或2; R 1和R 2是H，卤素原子，氰基，任选取代的烷基，任选取代的芳基等; R3是H，卤素原子，任选取代的烷基等; R 4和R 5是H，卤素原子，OH等; R6和RX是H或OH：RY是F或OH。

    Glucopyranosyloxypyrazole derivatives and medicinal use thereof
    13.
    发明授权
    Glucopyranosyloxypyrazole derivatives and medicinal use thereof 有权
    吡喃葡萄糖氧吡唑衍生物及其医药用途

    公开(公告)号：US07294618B2

    公开(公告)日：2007-11-13

    申请号：US10469140

    申请日：2002-02-26

    申请人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H17/00

    CPC分类号： C07H17/02 ,  Y10S514/866

    摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1, R2 and R3 represent a hydrogen atom or a halogen atom; R4 represents a lower alkyl group or a halo(lower alkyl) group; and R5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R 1，R 2和R 3表示氢原子或卤素原子 ; R 4表示低级烷基或卤代（低级烷基）基团; 和R 5表示氢原子，低级烷基，低级烷氧基，低级烷硫基等，其药学上可接受的盐或其前药，其具有优异的抑制活性 在人SGLT2中，因此可用作预防或治疗与高血糖相关疾病如糖尿病，糖尿病并发症或肥胖症的药物，其药学上可接受的盐或其前药，其生产中间体及其药学用途。

    Phenol derivative, medicinal composition containing the same, and medicinal use thereof
    14.
    发明申请
    Phenol derivative, medicinal composition containing the same, and medicinal use thereof 审中-公开
    苯酚衍生物，含有该酚衍生物的药物组合物及其医药用途

    公开(公告)号：US20070185197A1

    公开(公告)日：2007-08-09

    申请号：US10599444

    申请日：2005-03-30

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Masayuki Isaji

    IPC分类号： A61K31/295

    CPC分类号： C07H15/203 ,  A61K31/7034

    摘要： The present invention provides phenol derivatives represented by the following general formula or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like, and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof. In the chemical structure, R1 and R2 represent H, OH, NH2, etc.; R3and R4represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G); E1 represents H or F; and E2 represents H, F, or a methyl group, etc.

    摘要翻译： 本发明提供由以下通式表示的酚衍生物或其药学上可接受的盐或其前药，其在人SGLT中表现出抑制活性，并且可用作预防或治疗与高血糖相关的疾病如糖尿病， 餐后高血糖，葡萄糖耐量降低，糖尿病并发症，肥胖症等，以及含有该糖尿病并发症的药物组合物及其药物用途。 在化学结构中，R 1和R 2代表H，OH，NH 2等; R 3和R 4代表H，OH，卤素原子，任选取代的烷基等; 环A表示芳基或杂芳基; G表示由以下通式（G）表示的基团。 E 1表示H或F; 并且E 2表示H，F或甲基等。

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    17.
    发明授权
    Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
    吡喃葡萄糖氧吡唑衍生物及其在药物中的应用

    公开(公告)号：US07989424B2

    公开(公告)日：2011-08-02

    申请号：US12169882

    申请日：2008-07-09

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： A61K45/06 ,  A61K31/7056 ,  C07H17/02 ,  A61K2300/00

    摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团; Q和T之一表示由通式表示的基团：（其中P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作 用于预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。

    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
    18.
    发明授权
    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof 有权
    稠合的杂环衍生物，含有它们的药物组合物及其医药用途

    公开(公告)号：US07732596B2

    公开(公告)日：2010-06-08

    申请号：US10591403

    申请日：2005-03-03

    申请人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Masayuki Isaji

    IPC分类号： C07H7/06 ,  C07H7/04 ,  A61K31/7042

    CPC分类号： C07H17/00

    摘要： The present invention provides nitrogen-containing fused cyclic derivatives represented by the following general formula or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula one of R1 and R4 represents a group represented by the following general formula (S) (in which R5 and R6 represent H, OH, a halogen atom, etc.; Q represents an alkylene group etc.; and ring A represents an aryl group etc.), and the other represents H, OH, an amino group, etc.; R2 and R3 represent H, OH, an amino group, a halogen atom, and an optionally substituted alkyl group, etc.; A1 represents O, S, etc.; A2 represents CH or N; G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的含氮稠合环状衍生物或其药学上可接受的盐或其前药，其在人SGLT中表现出优异的抑制活性，并且可用作预防或治疗与 R 1和R 4的式1中的糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症或肥胖症等高血糖代表由以下通式（S）表示的基团（其中R 5和R 6表示H，OH，卤素 原子等; Q表示亚烷基等;环A表示芳基等），另外表示H，OH，氨基等; R2和R3表示H，OH，氨基，卤素原子和任选取代的烷基等; A1代表O，S等; A2表示CH或N; G表示由以下通式（G-1）或（G-2）表示的基团（E1表示H，F或OH; E2表示H，F，甲基等），以及包含 相同的药物用途。

    Glucopyranosyloxyprazole derivatives and use thereof in medicines
    20.
    发明申请
    Glucopyranosyloxyprazole derivatives and use thereof in medicines 有权
    吡喃葡萄糖基吡唑衍生物及其在药物中的应用

    公开(公告)号：US20060035847A1

    公开(公告)日：2006-02-16

    申请号：US11247356

    申请日：2005-10-12

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A61K31/7056 ,  C07H17/02

    CPC分类号： A61K45/06 ,  A61K31/7056 ,  C07H17/02 ,  A61K2300/00

    摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo (lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团; Q和T之一表示由通式表示的基团：（其中P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R 2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作 用于预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。