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    1-substituted-3-β-D-glucopyranosylated nitrogenous hetero-cyclic compounds and medicines containing the same
    1.
    发明授权
    1-substituted-3-β-D-glucopyranosylated nitrogenous hetero-cyclic compounds and medicines containing the same 失效
    1-取代-3-吡喃葡糖基氮杂环化合物和含有它们的药物

    公开(公告)号：US07750145B2

    公开(公告)日：2010-07-06

    申请号：US11719201

    申请日：2005-11-17

    申请人： Shigeru Yonekubo ,  Nobuhiko Fushimi

    发明人： Shigeru Yonekubo ,  Nobuhiko Fushimi

    IPC分类号： C07H7/06 ,  A01N43/04 ,  A61K31/70

    CPC分类号： A61K45/06 ,  A61K31/404 ,  A61K31/4166 ,  C07D405/04 ,  A61K2300/00

    摘要： A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.

    摘要翻译： 具有SGLT1和/或SGLT2抑制活性的化合物，其可用作预防或治疗糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症，肥胖症等的药剂。它是1-取代-3 - （＆bgr ; D-吡喃葡糖基）含氮杂环化合物或其药学上可接受的盐，或其水合物或溶剂化物; 含有其的SGLT抑制剂; 含有它们的药物组合物和它们的组合药剂。 在该式中，A表示亚烷基或亚烯基; B表示单键，-O - ， - S-或-NH-; C表示任选取代的芳基或杂芳基; Q独立地表示氢原子或取代基结合的碳原子或氮原子。

    1-substituted-7-(β-D-glycopyranosyloxy)(aza)indole compound and pharmaceutical containing the same
    2.
    发明授权
    1-substituted-7-(β-D-glycopyranosyloxy)(aza)indole compound and pharmaceutical containing the same 有权
    1-取代-7 - （＆bgr-D-糖吡喃糖基氧基）（氮杂）吲哚化合物和含有它们的药物

    公开(公告)号：US07749972B2

    公开(公告)日：2010-07-06

    申请号：US11816056

    申请日：2006-02-14

    申请人： Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Kohsuke Ohno

    发明人： Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Kohsuke Ohno

    IPC分类号： A61K31/70 ,  A01N43/04 ,  C07H17/02

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

    摘要： The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like.It is a 1-substituted-7-(β-D-glycopyranosyloxy)(aza)-indole compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof: wherein R1 represents a halogen atom or the like; n represents j an integer number from 0 to 3; R2 represents a hydrogen atom or the like; X represents a carbon atom which a hydrogen atom or the like binds to, or a nitrogen atom; Q represents an alkylene group or an alkenylene group each of which may have an oxygen atom or a sulfur atom in the chain; and A represents an aryl or heteroaryl group which may have a substituent.

    摘要翻译： 本发明提供具有SGLT1和/或SGLT2抑制活性的化合物，其可用作预防或治疗糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症，肥胖症等。 它是由通式（I）表示的1-取代-7 - （＆bgr-D-吡喃葡萄糖基氧基）（氮杂） - 吲哚化合物，其前体药物或其药学上可接受的盐，或其水合物或溶剂化物： 其中R1表示卤素原子等; n表示j为0〜3的整数; R2表示氢原子等; X表示与氢原子等结合的碳原子或氮原子; Q表示可以在链中具有氧原子或硫原子的亚烷基或亚烯基; A表示可以具有取代基的芳基或杂芳基。

    GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES
    4.
    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。

    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
    5.
    发明申请
    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof 有权
    吡唑衍生物，含有该吡唑衍生物的药物组合物，其医药用途及其生产用中间体

    公开(公告)号：US20060166899A1

    公开(公告)日：2006-07-27

    申请号：US10523820

    申请日：2003-08-07

    申请人： Hirotaka Teranishi ,  Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Kazuo Shimizu ,  Toshihide Shibazaki ,  Masayuki Isaji

    发明人： Hirotaka Teranishi ,  Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Kazuo Shimizu ,  Toshihide Shibazaki ,  Masayuki Isaji

    IPC分类号： A61K31/7056 ,  C07H17/02

    CPC分类号： C07H17/02

    摘要： The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

    摘要翻译： 本发明提供由以下通式表示的吡唑衍生物：其中R 1表示H，任选取代的C 1-6烷基等; Q和T之一表示由通式表示的基团或由通式表示的基团：而另一个表示任选取代的C 1-6烷基等; R 2表示H，卤素原子，OH，任选取代的C 1-6烷基等; X表示单键，O或S; Y表示单键，C 1-6亚烷基等; Z表示CO或SO 2; R 4和R 5表示H，任选取代的C 1-6烷基等; R 3，R 6和R 7表示H，卤素原子等，其药学上可接受的盐或其前药，其表现出 在人SGLT1中具有优异的抑制活性，并且可用作预防或治疗与糖尿病，糖尿病并发症或肥胖症等高血糖相关的疾病的药剂，以及含有该疾病的药物组合物，其药学用途及其生产用中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    6.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US07053060B2

    公开(公告)日：2006-05-30

    申请号：US10432905

    申请日：2001-11-20

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/00 ,  C07H17/00

    CPC分类号： C07H15/203

    摘要： The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物：其中R 1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（低级烷基 ）基团，取代或未取代的（低级烷氧基）基团等; R 2表示氢原子或低级烷基; 和R 3表示取代或未取代的（低级烷基）基团，取代或未取代的（低级烷氧基）基团，取代或未取代的（低级烷硫基）等，或其药学上可接受的盐，其中 在人SGLT2中具有抑制活性，并且可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂，包含其的药物组合物及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    7.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US20050059614A1

    公开(公告)日：2005-03-17

    申请号：US10978413

    申请日：2004-11-02

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07H15/203 ,  A61K31/70 ,  C07H5/04 ,  C07H5/06

    CPC分类号： C07H15/203

    摘要： The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted(lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖基 - 氧苄基苯衍生物：其中R 1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（低级烷基） 取代或未取代的（低级烷氧基）等。 R 2表示氢原子或低级烷基; 和R 3表示具有抑制活性的取代或未取代的（低级烷基）基团，取代或未取代的（低级烷氧基）基团，取代或未取代的（低级烷硫基）等，或其药学上可接受的盐 人SGLT2，并且可用作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，包含其的药物组合物及其中间体。

    Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof
    8.
    发明授权
    Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof 有权
    稠合杂环衍生物，含有它们的药物组合物及其医药用途

    公开(公告)号：US09040693B2

    公开(公告)日：2015-05-26

    申请号：US12089674

    申请日：2006-10-17

    申请人： Kohsuke Ohno ,  Takashi Miyagi ,  Tomonaga Ozawa ,  Nobuhiko Fushimi

    发明人： Kohsuke Ohno ,  Takashi Miyagi ,  Tomonaga Ozawa ,  Nobuhiko Fushimi

    IPC分类号： C07D495/04

    CPC分类号： C07D495/04

    摘要： The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.

    摘要翻译： 本发明提供了可用作预防或治疗性激素依赖性疾病等的药剂的化合物。 也就是说，本发明提供由以下通式（I）表示的稠合杂环衍生物，含有该杂环衍生物的药物组合物，其医药用途等。 在式（I）中，环A表示5元环状不饱和烃或5元杂芳基; 烷基，烯基，炔基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; 环B表示芳基或杂芳基; RB代表卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2表示氧原子等; U表示单键或亚烷基; X表示Y表示的基团，-SO 2 -Y，-O-（亚烷基）-Y，-O-Z，Y表示Z，氨基等; Z表示环烷基，杂环烷基，芳基，杂芳基等; 或类似物。

    Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs
    9.
    发明授权
    Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs 有权
    含氮稠环衍生物，含有衍生物的药物组合物及其作为药物的用途

    公开(公告)号：US07998975B2

    公开(公告)日：2011-08-16

    申请号：US12032411

    申请日：2008-02-15

    申请人： Nobuhiko Fushimi ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Shigeru Yonekubo ,  Fumiaki Ito ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Shigeru Yonekubo ,  Fumiaki Ito ,  Masayuki Isaji

    IPC分类号： A61K31/44 ,  A61K31/405 ,  A01N43/38

    CPC分类号： A61K31/7056 ,  A61K31/706 ,  C07H17/02

    摘要： The present invention provides nitrogen-containing fused-ring 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 R1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which 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环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疾病的药剂 与糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症或肥胖症等高血糖相关，在式R 1中表示H，任选取代的烷基，烯基等; R2表示H，卤素原子或烷基; R3和R4代表H，OH，卤素原子，任选取代的烷基等; Y表示CH或N; Q表示亚烷基，亚烯基等; 环A表示芳基或杂芳基; G表示由以下通式（G-1）或（G-2）表示的基团（其中E1表示H，F或OH; E2表示H，F，甲基等）和药物组合物 包括它们的药物用途。