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11.发明授权Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效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
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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12.发明申请Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效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
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。
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13.发明申请Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 审中-公开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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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
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.
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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。
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16.发明申请Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof 失效含氮杂环衍生物，含有该杂环衍生物的医药组合物及其医药用途公开(公告)号：US20060035840A1
公开(公告)日：2006-02-16
申请号：US10540519
申请日：2003-12-19
IPC分类号： A61K31/7052 , C07H17/02
CPC分类号： C07H17/02 , A61K31/706
摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents Nor CR1; X2 represents Nor CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent 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 complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.
摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X 1表示Nor CR 1; X <2>表示Nor CR 2; X 3表示N或CR 3; X 4表示N或CR 4; 并且条件是X 1至X 4中的一个或两个表示N; R表示任选取代的C 3-8环烷基，任选取代的C 6-10芳基等; R 1至R 4代表H，卤素原子等）或其药学上可接受的盐或其前药，其在人SGLT2中具有优异的抑制活性，并且为 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，肥胖症等的药剂，其药物组合物及其药物用途。
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17.发明申请Nitrogenous heterocyclic derivative, medicinal composition containing the same, medical use thereof, and intermediate therefor 失效含氮杂环衍生物，含有它们的药物组合物，其医疗用途及其中间体公开(公告)号：US20050049203A1
公开(公告)日：2005-03-03
申请号：US10481013
申请日：2002-06-17
申请人： Toshihiro Nishimura , Hideki Fujikura , Nobuhiko Fushimi , Kazuya Tatani , Kenji Katsuno , Masayuki Isaji
发明人： Toshihiro Nishimura , Hideki Fujikura , Nobuhiko Fushimi , Kazuya Tatani , Kenji Katsuno , Masayuki Isaji
IPC分类号： A61P3/04 , A61P3/10 , A61P43/00 , C07H17/02 , A61K31/7052
CPC分类号： C07H17/02 , Y02P20/55 , Y10S514/866 , Y10S514/909
摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 and X3 independently represent N or CH; X2 represents N or CR2; X4 represents N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 represent N; R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted(lower alkoxy) group, a lower alkoxy(lower alkoxy) -substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A—wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and R3 represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.
摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X 1和X 3独立地表示N或CH; X 2表示N或CR 2; X 4表示N或CR 3; 并且条件是X 1，X 2，X 3和X 4中的一个或两个表示N; R 1表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷氧基） 低级烷氧基（低级烷氧基） - 取代（低级烷基）基团，环状低级烷基，卤代（低级烷基）基团或由通式HO-A表示的基团：其中A表示低级亚烷基， 低级亚烷基氧基或低级亚烷基硫基; R 2表示氢原子，卤素原子，低级烷基，环状低级烷基，低级烷氧基，氨基，（低级酰基）氨基，单（低级烷基）氨基或 二（低级烷基）氨基; R 3表示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症相关疾病的药剂的氢原子或低级烷基或其药学上可接受的盐或其前体药物，药物 含有它们的组合物，及其制药用途和生产中间体。
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18.发明授权Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof 失效含氮杂环衍生物，含有该杂环衍生物的医药组合物及其医药用途公开(公告)号：US07655633B2
公开(公告)日：2010-02-02
申请号：US10540519
申请日：2003-12-19
CPC分类号： C07H17/02 , A61K31/706
摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents N or CR1; X2 represents N or CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent 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 complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.
摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X1表示N或CR1; X2表示N或CR2; X3表示N或CR3; X4表示N或CR4; 并且条件是X1至X4中的一个或两个表示N; R代表任选取代的C 3-8环烷基，任选取代的C 6-10芳基等; R1至R4表示H，卤素原子等）或其药学上可接受的盐或其前药，其在人SGLT2中具有优异的抑制活性，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，糖尿病并发症，肥胖症等，包含其的药物组合物及其药用用途。
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19.发明授权Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor 失效含氮杂环衍生物，含有它们的药物组合物，其医药用途及其中间体公开(公告)号：US07271153B2
公开(公告)日：2007-09-18
申请号：US10481013
申请日：2002-06-17
申请人： Toshihiro Nishimura , Hideki Fujikura , Nobuhiko Fushimi , Kazuya Tatani , Kenji Katsuno , Masayuki Isaji
发明人： Toshihiro Nishimura , Hideki Fujikura , Nobuhiko Fushimi , Kazuya Tatani , Kenji Katsuno , Masayuki Isaji
CPC分类号： C07H17/02 , Y02P20/55 , Y10S514/866 , Y10S514/909
摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 and X3 independently represent N or CH; X2 represents N or CR2; X4 represents N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 represent N; R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group, a lower alkoxy(lower alkoxy)-substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A- wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and R3 represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.
摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X 1和X 3独立地表示N或CH; X 2表示N或CR 2; X 4表示N或CR 3; 并且条件是X 1，X 2，X 3和X 4中的一个或者两个表示N ; R 1表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷基） 低级烷氧基）基团，低级烷氧基（低级烷氧基） - 取代（低级烷基）基团，环状低级烷基基团，卤代（低级烷基）基团或由通式HO-A-表示的基团，其中A表示 低级亚烷基，低级亚烷基氧基或低级亚烷基硫基; R 2表示氢原子，卤素原子，低级烷基，环状低级烷基，低级烷氧基，氨基，（低级酰基）氨基，单（低级） 烷基）氨基或二（低级烷基）氨基; R 3表示氢原子或低级烷基，或其药学上可接受的盐或其前药，其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，包含其的药物组合物及其药物用途和生产中间体。
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公开(公告)号：US07189702B2
公开(公告)日：2007-03-13
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
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。
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