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1. 发明申请

US20090093419A1 GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES 有权
标题翻译：葡萄糖醛酰氧基吡唑衍生物及其在药物中的应用
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。

2. 发明授权

US07053060B2 Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
标题翻译：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：US07053060B2
公开(公告)日：2006-05-30
申请号：US10432905
申请日：2001-11-20
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： A01N43/04 , A61K31/70 , C07H15/00 , C07H17/00
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。

3. 发明申请

US20050059614A1 Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
标题翻译：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：US20050059614A1
公开(公告)日：2005-03-17
申请号：US10978413
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 , A61K31/70 , C07H5/04 , C07H5/06
CPC分类号： C07H15/203
摘要： The present invention relates to glucopyranosyl-oxybenzylbenzene 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基 - 氧苄基苯衍生物：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）取代或未取代的（低级烷氧基）等。 R 2表示氢原子或低级烷基; 和R 3表示具有抑制活性的取代或未取代的（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人SGLT2，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。

4. 发明授权

US07294618B2 Glucopyranosyloxypyrazole derivatives and medicinal use thereof 有权
标题翻译：吡喃葡萄糖氧吡唑衍生物及其医药用途
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。

5. 发明申请

US20070185197A1 Phenol derivative, medicinal composition containing the same, and medicinal use thereof 审中-公开
标题翻译：苯酚衍生物，含有该酚衍生物的药物组合物及其医药用途
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。

6. 发明授权

US07989424B2 Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
标题翻译：吡喃葡萄糖氧吡唑衍生物及其在药物中的应用
公开(公告)号：US07989424B2
公开(公告)日：2011-08-02
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： 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。

7. 发明授权

US07732596B2 Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof 有权
标题翻译：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：US07732596B2
公开(公告)日：2010-06-08
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： C07H7/06 , C07H7/04 , A61K31/7042
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中的糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症或肥胖症等高血糖代表由以下通式（S）表示的基团（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），另外表示H，OH，氨基等; R2和R3表示H，OH，氨基，卤素原子和任选取代的烷基等; A1代表O，S等; A2表示CH或N; 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; E2表示H，F，甲基等），以及包含相同的药物用途。

8. 发明授权

US07393838B2 Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
公开(公告)号：US07393838B2
公开(公告)日：2008-07-01
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： A01N43/04 , A61K31/70 , C07H17/00
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.

9. 发明申请

US20060035847A1 Glucopyranosyloxyprazole derivatives and use thereof in medicines 有权
标题翻译：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。

10. 发明申请

US20050113315A1 Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 审中-公开
标题翻译：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。

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