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57 条记录 (耗时 0.03 秒)

    Glucopyranosyloxyprazole derivatives and use thereof in medicines
    31.
    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。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    34.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 审中-公开
    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：US20050113315A1

    公开(公告)日：2005-05-26

    申请号：US10978331

    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 ,  A61K31/704 ,  C07H5/04

    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。

    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
    36.
    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：US08058245B2

    公开(公告)日：2011-11-15

    申请号：US10591421

    申请日：2005-03-03

    申请人： Nobuhiko Fushimi ,  Masayuki Isaji ,  Hideki Fujikura

    发明人： Nobuhiko Fushimi ,  Masayuki Isaji ,  Hideki Fujikura

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052

    CPC分类号： C07D405/04 ,  A61K31/351 ,  A61K31/381 ,  A61K31/404 ,  A61K45/06 ,  C07D409/04 ,  A61K2300/00

    摘要： The present invention provides fused heterocyclic derivatives represented by the following general formula (I) 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 or obesity, in the formula R1 to R4 represent H, OH, an amino group, etc.; R5 and R6 represent H, OH, a halogen atom, an option ally substituted alkyl group, etc.; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; the following ring (R1) represents a group represented by the following ring (R2); G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E 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（I）表示的稠合杂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 如糖尿病，餐后高血糖症，葡萄糖耐量减低，糖尿病并发症或肥胖症，式R1至R4表示H，OH，氨基等; R5和R6表示H，OH，卤素原子，选择性烯取代的烷基等; Q表示亚烷基，亚烯基等; 环A表示芳基或杂芳基; 下述环（R1）表示由下述环（R2）表示的基团。 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; E表示H，F，甲基等），以及包含 相同的药物用途。

    Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof
    38.
    发明授权
    Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof 失效
    含氮杂环衍生物，含有该杂环衍生物的医药组合物及其医药用途

    公开(公告)号：US07655633B2

    公开(公告)日：2010-02-02

    申请号：US10540519

    申请日：2003-12-19

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

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

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/24

    CPC分类号： C07H17/02 ,  A61K31/706

    摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents N or CR1; X2 represents N or CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent 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 complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.

    摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X1表示N或CR1; X2表示N或CR2; X3表示N或CR3; X4表示N或CR4; 并且条件是X1至X4中的一个或两个表示N; R代表任选取代的C 3-8环烷基，任选取代的C 6-10芳基等; R1至R4表示H，卤素原子等）或其药学上可接受的盐或其前药，其在人SGLT2中具有优异的抑制活性，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，糖尿病并发症，肥胖症等，包含其的药物组合物及其药用用途。

    Pyrazole derivative, drug composition containing the same and production intermediate therefor
    39.
    发明授权
    Pyrazole derivative, drug composition containing the same and production intermediate therefor 失效
    吡唑衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US07576064B2

    公开(公告)日：2009-08-18

    申请号：US10561217

    申请日：2004-06-15

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

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

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

    CPC分类号： C07D231/32 ,  A61K31/7056 ,  A61K31/706 ,  C07D231/52 ,  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, etc.; one of Q and T represents a group selected from the following: and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.; R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium/glucose cotransporter (SGLT) 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 (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.

    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的基团：另一个表示-Z-Ar，其中Z表示-O-，-S-等; Ar表示任选取代的C 6-10芳基等。 R表示在人钠/葡萄糖共转运体（SGLT）中表现出优异抑制活性的可任选取代的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及其前药，并且可用作试剂 用于预防，抑制与选自葡萄糖，果糖和甘露糖（糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症等）中的至少一种碳水化合物的过量摄取相关的疾病的进展或治疗，以及药物 含有该组合物的组合物，其医药用途和用于其生产的中间体。

    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same
    40.
    发明授权
    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：US07576063B2

    公开(公告)日：2009-08-18

    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： A01N43/04 ,  A61K31/70 ,  C07H17/00

    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之一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。