公开(公告)号：US20080139484A1

公开(公告)日：2008-06-12

申请号：US11576204

申请日：2005-09-28

申请人： Hirotaka Teranishi ,  Norihiko Kikuchi ,  Kohsuke Ohno

发明人： Hirotaka Teranishi ,  Norihiko Kikuchi ,  Kohsuke Ohno

IPC分类号： A61K31/7056 ,  C07H17/02 ,  A61P3/10 ,  A61P3/06 ,  A61P3/00

CPC分类号： A61K31/7056 ,  A61K31/706 ,  A61K45/06 ,  C07H19/04 ,  A61K2300/00

摘要： A compound having SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-(β-D-glycopyranosyl)-3-substituted nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a medicinal use thereof. In the formula, ring A represents optionally substituted aryl or heteroaryl; Q1 to Q5 independently represent a carbon atom having a hydrogen atom or substituent bonded thereto or a nitrogen atom; E represents a single bond, alkylene, —O—, —S— or —NH—; and R represents methyl, ethyl, fluoromethyl or hydroxymethyl.

摘要翻译： 具有SGLT1和/或SGLT2抑制活性的化合物，其可用作预防或治疗糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症，肥胖症等的药物。它是1-（β-D-糖吡喃糖基） 由通式（I）表示的3-取代的含氮杂环化合物，其前体药物或其药学上可接受的盐，或其水合物或溶剂化物; 含有其的SGLT抑制剂; 含有该组合物的药物组合物及其药物用途。 在该式中，环A表示任选取代的芳基或杂芳基; Q 1至Q 5独立地表示具有与其键合的氢原子或取代基的碳原子或氮原子; E表示单键，亚烷基，-O - ， - S-或-NH-; R代表甲基，乙基，氟甲基或羟甲基。

公开(公告)号：US20050119192A1

公开(公告)日：2005-06-02

申请号：US10507611

申请日：2003-03-04

申请人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

发明人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

IPC分类号： A61K31/7034 ,  A61P3/04 ,  A61P3/10 ,  C07H15/203 ,  A61K31/7028 ,  C07H11/04

CPC分类号： C07H15/203 ,  A61K31/7034

摘要： The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-β-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.

摘要翻译： 本发明提供2-（4-甲氧基苄基）苯基6-O-乙氧基羰基-β-D-吡喃葡萄糖苷的晶体，含有该结晶的药物组合物及其用途，其表现出优异的SGLT2抑制活性，可用于治疗或预防疾病 与高血糖相关。

公开(公告)号：US07371730B2

公开(公告)日：2008-05-13

申请号：US10507611

申请日：2003-03-04

申请人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

发明人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/00 ,  C07H15/24

CPC分类号： C07H15/203 ,  A61K31/7034

摘要： The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-β-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.

摘要翻译： 本发明提供2-（4-甲氧基苄基）苯基6-O-乙氧基羰基-β-D-吡喃葡萄糖苷的晶体，含有该结晶的药物组合物及其用途，其表现出优异的SGLT2抑制活性，可用于治疗或预防疾病 与高血糖相关。

公开(公告)号：US20060166899A1

公开(公告)日：2006-07-27

申请号：US10523820

申请日：2003-08-07

申请人： Hirotaka Teranishi ,  Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Kazuo Shimizu ,  Toshihide Shibazaki ,  Masayuki Isaji

发明人： Hirotaka Teranishi ,  Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Kazuo Shimizu ,  Toshihide Shibazaki ,  Masayuki Isaji

IPC分类号： A61K31/7056 ,  C07H17/02

CPC分类号： C07H17/02

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 a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 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, diabetic complications or obesity, 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表示单键，C 1-6亚烷基等; Z表示CO或SO 2; R 4和R 5表示H，任选取代的C 1-6烷基等; R 3，R 6和R 7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，糖尿病并发症或肥胖症等高血糖相关的疾病的药剂，以及含有该疾病的药物组合物，其药学用途及其生产用中间体。

公开(公告)号：US07998975B2

公开(公告)日：2011-08-16

申请号：US12032411

申请日：2008-02-15

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

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, an alkenyl 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，在式R 1中表示H，任选取代的烷基，烯基等; R2表示H，卤素原子或烷基; R3和R4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E1表示H，F或OH; E2表示H，F，甲基等）和药物组合物 包括它们的药物用途。

公开(公告)号：US07566699B2

公开(公告)日：2009-07-28

申请号：US10551648

申请日：2004-03-24

申请人： Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Hideyuki Muranaka ,  Hiroaki Shiohara ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Fumiaki Ito ,  Masayuki Isaji

发明人： Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Hideyuki Muranaka ,  Hiroaki Shiohara ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Fumiaki Ito ,  Masayuki Isaji

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/00 ,  C07H17/00

CPC分类号： C07H15/203 ,  C07H17/00 ,  C07H17/02 ,  C07H17/04

摘要： The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents 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, 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稠合杂环衍生物：其中R1表示H，卤素，OH等; R2表示H，卤素或烷基; R3和R4代表H，OH，卤素等; Q表示亚烷基等。 环A表示芳基或杂芳基; 和G表示其药学上可接受的盐或其前体药物，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高血糖相关的疾病如糖尿病，餐后高血糖，葡萄糖耐量异常，糖尿病 并发症或肥胖症，包含其的药物组合物及其药物用途。

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：US20080188426A1

公开(公告)日：2008-08-07

申请号：US12032411

申请日：2008-02-15

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： A61K31/7056 ,  C07H19/01 ,  A61P3/10

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, an alkenyl 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的R 1表示H，任选取代的烷基，烯基等; 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：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