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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。

    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
    4.
    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。

    Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs
    5.
    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。

    1-SUBSTITUTED-3-BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO-CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME
    7.
    发明申请
    1-SUBSTITUTED-3-BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO-CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME 失效
    1-取代的3-β-D-吡喃葡糖苷化的氮杂环化合物和含有它们的药物

    公开(公告)号：US20090074738A1

    公开(公告)日：2009-03-19

    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： A61K31/7076 ,  C07H7/06 ,  A61K31/7056

    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-（β -D-糖吡喃糖基）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。

    Nitrogenated fused ring derivative, pharmaceutical composition comprising the same, and use of the same for medical purposes
    8.
    发明授权
    Nitrogenated fused ring derivative, pharmaceutical composition comprising the same, and use of the same for medical purposes 有权
    氮化稠环衍生物，包含其的药物组合物，以及其用于医疗目的

    公开(公告)号：US08217069B2

    公开(公告)日：2012-07-10

    申请号：US12596313

    申请日：2008-04-16

    申请人： Shigeru Yonekubo ,  Takashi Miyagi ,  Kohsuke Ohno ,  Mikie Kambara ,  Nobuhiko Fushimi

    发明人： Shigeru Yonekubo ,  Takashi Miyagi ,  Kohsuke Ohno ,  Mikie Kambara ,  Nobuhiko Fushimi

    IPC分类号： A61K31/415 ,  C07D233/00

    CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/52 ,  C07D473/00 ,  C07D473/04 ,  C07D473/30 ,  C07D473/36 ,  C07D473/40 ,  C07D487/04

    摘要： [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like.[Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

    摘要翻译： [目的]本发明提供可用作预防或治疗性激素依赖性疾病等的药剂的化合物。 [溶液]本发明提供了具有GnRH拮抗活性的下述通式（I）表示的含氮稠环衍生物，前药，盐，含有它们的药物组合物，其药用用途等。 在式（I）中，环A和B独立地为芳基或杂芳基; RA和RB独立地是卤素，氰基，烷基，烷基磺酰基，-OW1，-SW1，-COW2，-NW3W4，-SO2NW3W4，芳基等; RC是H或烷基; E是氧原子等; U是单键或亚烷基; 并且X是Y，-CO-Y，-SO 2 -Y，-S-（亚烷基）-Y，-O-（亚烷基）-Y，-SO 2 - （亚烷基）-Y等; Y是Z或氨基等; Z是环烷基，杂环烷基，芳基，杂芳基等。

    FUSED HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES
    9.
    发明申请
    FUSED HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES 审中-公开
    融合的杂环衍生物，包含衍生物的药物组合物，以及用于医疗用途的组合物的用途

    公开(公告)号：US20100130514A1

    公开(公告)日：2010-05-27

    申请号：US12596301

    申请日：2008-04-16

    申请人： Takashi Miyagi ,  Shigeru Yonekubo ,  Kohsuke Ohno ,  Mikie Kambara ,  Nobuhiko Fushimi

    发明人： Takashi Miyagi ,  Shigeru Yonekubo ,  Kohsuke Ohno ,  Mikie Kambara ,  Nobuhiko Fushimi

    IPC分类号： A61K31/519 ,  C07D495/04

    CPC分类号： C07D495/04 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

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

    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试剂的化合物。 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，含有它们的药物组合物，其药用用途等。 在式（I）中，环A是5元环状不饱和烃或5元杂芳基; RA是卤素，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是芳基或杂芳基; RB是卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2是氧原子等; U是单键或亚烷基; X是由Y，-O-（亚烷基）-Y或-O-Z（其中Y是Z或被Z取代的氨基等）表示的基团; Z是环烷基，杂环烷基，芳基，杂芳基等。

    Pyrazole derivatives, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
    10.
    发明授权
    Pyrazole derivatives, 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：US07635684B2

    公开(公告)日：2009-12-22

    申请号：US10525197

    申请日：2003-08-21

    申请人： Nobuhiko Fushimi ,  Kazuo Shimizu ,  Shigeru Yonekubo ,  Hirotaka Teranishi ,  Masaki Tomae ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Kazuo Shimizu ,  Shigeru Yonekubo ,  Hirotaka Teranishi ,  Masaki Tomae ,  Masayuki Isaji

    IPC分类号： A61K31/7028 ,  A01N43/56 ,  C07H17/02 ,  C07D231/12

    CPC分类号： A61K38/185 ,  A61K31/00 ,  A61K31/10 ,  A61K31/205 ,  A61K31/37 ,  A61K31/4166 ,  A61K31/7056 ,  A61K31/7072 ,  A61K31/737 ,  A61K38/1858 ,  A61K38/28 ,  A61K45/06 ,  C07H17/02 ,  A61K2300/00

    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 an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 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, impaired glucose tolerance, impaired fasting glycemia, diabetic complications or obesity, and a disease associated with the increase of blood galactose level such as galactosemia, 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R1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; R2表示H，卤素原子，OH，任意取代的C 1-6烷基等; X表示单键，O或S; Y表示任选取代的C 1-6亚烷基等; Z表示-RB，-CORC等，其中RB表示任选取代的C 1-6烷基等; 并且RC表示任选取代的C 1-6烷基等; R4代表H，任选取代的C 1-6烷基等; R3，R5和R6表示H，卤素原子等，其药学上可接受的盐或其前药，其在人SGLT1中表现出优异的抑制活性，并且可用作预防或治疗与高血糖相关的疾病的药剂，例如 糖尿病，葡萄糖耐量减低，空腹血糖受损，糖尿病并发症或肥胖症，以及与半乳糖水平升高相关的疾病，以及包含其的药物组合物，其制药用途及其生产用中间体。