公开(公告)号：US20060035844A1

公开(公告)日：2006-02-16

申请号：US10537495

申请日：2003-12-04

申请人： Fumiaki Ito ,  Toshihide Shibazaki ,  Masaki Tomae ,  Nobuhiko Fushimi ,  Masayaki Isajo

发明人： Fumiaki Ito ,  Toshihide Shibazaki ,  Masaki Tomae ,  Nobuhiko Fushimi ,  Masayaki Isajo

IPC分类号： A61K31/70

CPC分类号： A61K31/7056 ,  A61K31/706

摘要： The present invention provides pharmaceutical compositions comprising as an active ingredient a selective SGLT1 inhibitor (e.g., an SGLT1 inhibitor substantially showing no GLUT2 and/or GLUT5 inhibitory effect), which have a wider range of inhibitory effect on carbohydrate absorption and a hypoglycemic effect caused by fructose ingestion at regular diets and therefore can exhibit a marked hypoglycemic effect, and which are suitable as agents for the prevention or treatment of diseases associated with hyperglycemia (e.g., diabetes, impaired glucose tolerance, diabetic complications, obesity).

摘要翻译： 本发明提供药物组合物，其包含作为活性成分的选择性SGLT1抑制剂（例如，基本上不显示GLUT2和/或GLUT5抑制作用的SGLT1抑制剂），其具有对碳水化合物吸收的更宽范围的抑制作用和由 因此可以显示明显的降血糖作用，适合作为预防或治疗与高血糖相关疾病（如糖尿病，葡萄糖耐量减低，糖尿病并发症，肥胖症）的药剂。

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。

公开(公告)号：US20090203633A1

公开(公告)日：2009-08-13

申请号：US12421236

申请日：2009-04-09

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

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

IPC分类号： A61K31/7056

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。

公开(公告)号：US08324176B2

公开(公告)日：2012-12-04

申请号：US12421236

申请日：2009-04-09

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 ,  C07H17/02

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。

公开(公告)号：US20050272669A1

公开(公告)日：2005-12-08

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： A61K31/00 ,  A61K31/10 ,  A61K31/205 ,  A61K31/37 ,  A61K31/4166 ,  A61K31/7056 ,  A61K31/7072 ,  A61K31/737 ,  A61K38/18 ,  A61K38/28 ,  A61K45/00 ,  A61K45/06 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/48 ,  A61P7/10 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P19/06 ,  A61P43/00 ,  C07H17/02 ,  A61K31/7052

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表示任选取代的C 1-6亚烷基等; Z表示-R B，C，C，C等。 其中R B表示任选取代的C 1-6烷基等; 且R C表示任选取代的C 1-6烷基等; R 4表示H，任选取代的C 1-6烷基等; R 3，R 5和R 6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，葡萄糖耐量降低，空腹血糖受损，糖尿病并发症或肥胖症相关的高血糖疾病的药剂，以及与血液半乳糖水平升高有关的疾病 例如半乳糖血症，以及包含其的药物组合物，其药学用途及其生产用中间体。