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。

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。

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。

公开(公告)号：US07115575B2

公开(公告)日：2006-10-03

申请号：US11191024

申请日：2005-07-28

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/415 ,  C07H17/00 ,  C07D231/20

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

公开(公告)号：US07056892B2

公开(公告)日：2006-06-06

申请号：US11189832

申请日：2005-07-27

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/415 ,  C07H17/00

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to 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吡唑衍生物：其中R 1表示氢原子或低级烷基; Q 1和T 1之一表示由通式表示的基团：而另一个表示低级烷基或卤代（低级烷基）基团; 和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）基或卤素原子或其药学上可接受的盐，它们具有 在人SGLT2中的抑制活性，并且可用作预防或治疗糖尿病，糖尿病并发症或肥胖症的药剂，以及包含其的药物组合物及其中间体。

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。

公开(公告)号：US20070197450A1

公开(公告)日：2007-08-23

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： A61K31/7052 ,  C07H17/02

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 例如糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症或肥胖症，式R 1至R 4代表H，OH，氨基等; R 5和R 6代表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（E 1）表示H，F或OH; E表示H，F，甲基等 ），以及包含其的药物组合物及其药物用途。

公开(公告)号：US20070197449A1

公开(公告)日：2007-08-23

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： A61K31/7052 ,  C07H17/02 ,  A61K38/28 ,  A61K38/22

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中的高血糖症如糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症或肥胖症代表由以下通式表示的基团 （S）（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），另一个表示H，OH，氨基等; R 2和R 3代表H，OH，氨基，卤素原子和任选取代的烷基等; A 表示O，S等; A 2表示CH或N; G表示由以下通式（G-1）或（G-2）表示的基团（E 1）表示H，F或OH;且E 2表示H ，F，甲基等）及其药物组合物及其药物用途。

公开(公告)号：US07087579B2

公开(公告)日：2006-08-08

申请号：US10468454

申请日：2002-02-26

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

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

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

CPC分类号： C07H15/203 ,  C07H17/02

摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., 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.

公开(公告)号：US20060142209A1

公开(公告)日：2006-06-29

申请号：US11358400

申请日：2006-02-22

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

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

IPC分类号： A61K31/7052

CPC分类号： C07H15/203 ,  C07H17/02

摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., 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Q和T之一表示由通式表示的基团，而另一个代表低级烷基或卤代（低级烷基）基团; R 1表示氢原子，任选取代的低级烷基，低级烯基，环状低级烷基等; R 2表示氢原子，任选取代的低级烷基，低级烷氧基，低级烯基，环状低级烷基，环状低级烷氧基等，其具有优异的 因此可用作预防或治疗与糖尿病，糖尿病并发症或肥胖症，糖尿病并发症或肥胖症，糖尿病并发症或肥胖症，其药学上可接受的盐或其前药，与其生产中间体及其药物用途有关的疾病的药物。