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：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。

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：US07375113B2

公开(公告)日：2008-05-20

申请号：US10591757

申请日：2005-03-03

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 ,  C07D498/02 ,  C07D513/02

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, analkenyl 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试剂 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，其中R 1表示H，任选取代的烷基，断链基等; R 2表示H，卤素原子或烷基; R 3和R 4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E H表示H，F或OH;以及E < 表示H，F，甲基等），以及含有它们的药物组合物及其药物用途

公开(公告)号：US20070191289A1

公开(公告)日：2007-08-16

申请号：US10591757

申请日：2005-03-03

申请人： Nobuhiko Fushimi ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Shigeru Yoneku ,  Fumiaki Ito ,  Masayuki Isaji

发明人： Nobuhiko Fushimi ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Shigeru Yoneku ,  Fumiaki Ito ,  Masayuki Isaji

IPC分类号： A61K31/7052 ,  C07H15/02

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, analkenyl 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，其中R 1表示H，任选取代的烷基，断链基等; R 2表示H，卤素原子或烷基; R 3和R 4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E H表示H，F或OH;以及E < 表示H，F，甲基等），以及含有它们的药物组合物及其药物用途。

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。

公开(公告)号：US08022192B2

公开(公告)日：2011-09-20

申请号：US11908693

申请日：2006-03-16

申请人： Kiyoshi Kasai ,  Tetsuji Ozawa ,  Nobuhiko Fushimi ,  Hidetoshi Isawa ,  Ken Kikuchi ,  Masahiro Kobayashi ,  Junichi Sonehara ,  Minoru Kubota

发明人： Kiyoshi Kasai ,  Tetsuji Ozawa ,  Nobuhiko Fushimi ,  Hidetoshi Isawa ,  Ken Kikuchi ,  Masahiro Kobayashi ,  Junichi Sonehara ,  Minoru Kubota

IPC分类号： C07H17/02 ,  A61K31/7056

CPC分类号： C07H17/02

摘要： The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R1, R2, R3, R4 and R5 may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R6 is an alkyl group, for example R7 is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PG1 is a pivaloyl group or the like, as an example, X1 is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.

摘要翻译： 本发明涉及一种制备吡喃葡萄糖氧吡唑衍生物的方法，其可用作预防或治疗与糖尿病，糖尿病并发症，肥胖症等高血糖相关的疾病的药剂。 吡喃葡萄糖氧吡唑衍生物可以容易且有效地制备，其中R 1，R 2，R 3，R 4和R 5可以相同或不同，例如氢原子，卤原子 或烷基，烷氧基，芳基甲氧基等，R6是烷基，例如R7是氢原子或烷基，烷氧基，芳基甲氧基等，与通式表示的化合物反应：其中作为 作为实例，PG1是新戊酰基等，作为实例，X1是溴原子等，因此本发明作为制备药物化合物的方法是非常有用的。

公开(公告)号：US20090325900A1

公开(公告)日：2009-12-31

申请号：US12089674

申请日：2006-10-17

申请人： Kohsuke Ohno ,  Takashi Miyagi ,  Tomonaga Ozawa ,  Nobuhiko Fushimi

发明人： Kohsuke Ohno ,  Takashi Miyagi ,  Tomonaga Ozawa ,  Nobuhiko Fushimi

IPC分类号： A61K31/695 ,  C07D215/58 ,  C07D211/72 ,  C07D311/02 ,  A61K31/47 ,  A61K31/44 ,  C07D223/16 ,  A61K31/55 ,  A61P5/24

CPC分类号： C07D495/04

摘要： The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O— (alkylene)-Y, —O-Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.

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药剂的化合物。 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，含有该杂环衍生物的药物组合物，其医药用途等。 在式（I）中，环A表示5元环状不饱和烃或5元杂芳基; 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表示芳基或杂芳基; RB代表卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2表示氧原子等; U表示单键或亚烷基; X表示Y表示的基团，-SO 2 -Y，-O-（亚烷基）-Y，-O-Z，Y表示Z，氨基等; Z表示环烷基，杂环烷基，芳基，杂芳基等; 或类似物。

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。