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    GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES
    2.
    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 in producing the same
    3.
    发明申请
    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same 失效
    吡唑衍生物，含有该吡唑衍生物的药物组合物，其药学用途及其制造中间体

    公开(公告)号：US20060128635A1

    公开(公告)日：2006-06-15

    申请号：US10529895

    申请日：2003-09-30

    申请人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

    IPC分类号： A61K31/7052 ,  C07H17/02

    CPC分类号： C07D405/04 ,  A61K31/7056 ,  C07D231/20 ,  C07D401/04 ,  C07D409/04 ,  C07H17/02 ,  Y10S514/866

    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 selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), 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之一表示选自以下基团的基团：另一个表示 - （CH 2）n Ar -Ar其中Ar表示任选取代的C 1 -C 6烷基， 6-10芳基或任选取代的C 1-19杂芳基; 并且n表示0至2的整数，任选取代的C 1-6烷氧基，任选取代的氨基，任选取代的C 2-9杂环烷基 或任选取代的杂环稠合的苯基; R表示任选取代的C 3-8环烷基，任选取代的C 6-10芳基等，其药学上可接受的盐或其前药，其表现出优异的 在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中的抑制活性，并且可用作预防，抑制与至少一种选自葡萄糖，果糖和甘露糖的碳水化合物过量摄取相关的疾病进展或治疗的药剂 或与高血糖相关的疾病（例如，糖尿病并发症，糖尿病等），以及包含该疾病的药物组合物，其药学用途和用于生产的中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    4.
    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
    5.
    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 AND USE THEREOF FOR MEDICAL PURPOSES
    7.
    发明申请
    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 审中-公开
    熔融杂环衍生物及其用于医疗用途的方法

    公开(公告)号：US20110201815A1

    公开(公告)日：2011-08-18

    申请号：US13124336

    申请日：2009-10-14

    申请人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

    发明人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

    IPC分类号： C07D401/10 ,  C07D417/10

    CPC分类号： C07D401/04 ,  A61K31/427 ,  A61K31/443 ,  A61K31/4439 ,  C07D405/04 ,  C07D417/04

    摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

    摘要翻译： 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠合杂环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前体药物，其盐或类似物 。 在式（I）中，T代表三氟甲基，硝基或氰基; 环Q表示杂芳基; X1和X2独立地表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

    PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE IN PRODUCING THE SAME
    9.
    发明申请
    PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE IN PRODUCING THE SAME 失效
    吡唑衍生物，含有该药物的药物组合物，在其生产中的药物用途及其中间体

    公开(公告)号：US20100029919A1

    公开(公告)日：2010-02-04

    申请号：US12534452

    申请日：2009-08-03

    申请人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

    IPC分类号： C07H17/02

    CPC分类号： C07D405/04 ,  A61K31/7056 ,  C07D231/20 ,  C07D401/04 ,  C07D409/04 ,  C07H17/02 ,  Y10S514/866

    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 selected from the following groups: , and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), 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中的一个表示选自以下基团的基团：另一个表示 - （CH 2）n -Ar，其中Ar表示任选取代的C 6-10芳基或任选取代的C 1-8杂芳基; n表示0〜2的整数，可以具有取代基的C 1-6烷氧基，可以具有取代基的氨基，可以具有取代基的C2-9杂环烷基或任意取代的杂环稠合苯基; R表示任选取代的C 3-8环烷基，任选取代的C 6-10芳基等，其药学上可接受的盐或其前体药物，其在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中表现出优异的抑制活性， 可用作预防，抑制与选自葡萄糖，果糖和甘露糖中的至少一种碳水化合物或与高血糖相关疾病（例如，糖尿病并发症，糖尿病等）的过量摄取相关疾病进展或治疗的药剂。 ），以及包含该药物组合物的药物组合物，其药学用途及其生产用中间体。

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    10.
    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：US07465713B2

    公开(公告)日：2008-12-16

    申请号：US11247216

    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： 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。