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1.发明申请Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same 失效吡唑衍生物，含有该吡唑衍生物的药物组合物，其药学用途及其制造中间体公开(公告)号：US20060128635A1
公开(公告)日：2006-06-15
申请号：US10529895
申请日：2003-09-30
IPC分类号： A61K31/7052 , C07H17/02
CPC分类号： C07D405/04 , A61K31/7056 , C07D231/20 , C07D401/04 , C07D409/04 , C07H17/02 , Y10S514/866
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 selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), 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之一表示选自以下基团的基团：另一个表示 - （CH 2）n Ar -Ar其中Ar表示任选取代的C 1 -C 6烷基， 6-10芳基或任选取代的C 1-19杂芳基; 并且n表示0至2的整数，任选取代的C 1-6烷氧基，任选取代的氨基，任选取代的C 2-9杂环烷基 或任选取代的杂环稠合的苯基; 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，其药学上可接受的盐或其前药，其表现出优异的 在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中的抑制活性，并且可用作预防，抑制与至少一种选自葡萄糖，果糖和甘露糖的碳水化合物过量摄取相关的疾病进展或治疗的药剂 或与高血糖相关的疾病（例如，糖尿病并发症，糖尿病等），以及包含该疾病的药物组合物，其药学用途和用于生产的中间体。
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2.发明申请PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE IN PRODUCING THE SAME 失效吡唑衍生物，含有该药物的药物组合物，在其生产中的药物用途及其中间体公开(公告)号：US20100029919A1
公开(公告)日：2010-02-04
申请号：US12534452
申请日：2009-08-03
IPC分类号： C07H17/02
CPC分类号： C07D405/04 , A61K31/7056 , C07D231/20 , C07D401/04 , C07D409/04 , C07H17/02 , Y10S514/866
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 selected from the following groups: , and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), 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中的一个表示选自以下基团的基团：另一个表示 - （CH 2）n -Ar，其中Ar表示任选取代的C 6-10芳基或任选取代的C 1-8杂芳基; n表示0〜2的整数，可以具有取代基的C 1-6烷氧基，可以具有取代基的氨基，可以具有取代基的C2-9杂环烷基或任意取代的杂环稠合苯基; 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，其药学上可接受的盐或其前体药物，其在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中表现出优异的抑制活性， 可用作预防，抑制与选自葡萄糖，果糖和甘露糖中的至少一种碳水化合物或与高血糖相关疾病（例如，糖尿病并发症，糖尿病等）的过量摄取相关疾病进展或治疗的药剂。 ），以及包含该药物组合物的药物组合物，其药学用途及其生产用中间体。
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3.发明申请Pyrazole derivative, drug composition containing the same and production intermediate therefor 失效吡唑衍生物，含有它们的药物组合物及其制备中间体公开(公告)号：US20070060531A1
公开(公告)日：2007-03-15
申请号：US10561217
申请日：2004-06-15
IPC分类号： A61K31/7052 , C07H15/00
CPC分类号： C07D231/32 , A61K31/7056 , A61K31/706 , C07D231/52 , Y10S514/866
摘要： The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl, etc.; one of Q and T represents a group selected from the following: , and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.; R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium/glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.
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中的一个表示选自以下的基团：另一个表示-Z-Ar，其中Z表示-O-，-S-等; Ar表示任选取代的C 6-10芳基等; 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，其药学上可接受的盐及其前药，其表现出优异的 在人钠/葡萄糖协同转运蛋白（SGLT）中的抑制活性，并且可用作预防，抑制与选自葡萄糖，果糖和甘露糖中的至少一种碳水化合物的过量摄取相关的疾病的进展或治疗的药剂（糖尿病， 餐后高血糖，葡萄糖耐量降低，糖尿病并发症等），含有该组合物的药物组合物，其医药用途和用于其生产的中间体。
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4.发明授权Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same 失效吡唑衍生物，含有该吡唑衍生物的药物组合物，其药学用途及其制造中间体公开(公告)号：US07888487B2
公开(公告)日：2011-02-15
申请号：US12534452
申请日：2009-08-03
CPC分类号： C07D405/04 , A61K31/7056 , C07D231/20 , C07D401/04 , C07D409/04 , C07H17/02 , Y10S514/866
摘要： 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 selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents a substituted C6-10 aryl group, etc., and n represents 0 to 2, R represents an optionally substituted C3-8 cycloalkyl group, etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates from glucose, fructose and mannose or a disease associated with hyperglycemia and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
摘要翻译： 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之一表示选自以下基团的基团：另一个表示 - （CH 2）n -Ar，其中Ar表示取代的C 6-10芳基等，n表示0至2，R表示任选地 取代的C3-8环烷基等，其药学上可接受的盐或其前体药物，其在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中表现出优异的抑制活性，并且可用作预防，抑制进展或治疗 与来自葡萄糖，果糖和甘露糖的至少一种碳水化合物的过量摄取相关的疾病或与高血糖相关的疾病以及包含其的药物组合物，其药学用途及其生产用中间体。
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5.发明授权Pyrazole derivative, drug composition containing the same and production intermediate therefor 失效吡唑衍生物，含有它们的药物组合物及其制备中间体公开(公告)号：US07576064B2
公开(公告)日：2009-08-18
申请号：US10561217
申请日：2004-06-15
CPC分类号： C07D231/32 , A61K31/7056 , A61K31/706 , C07D231/52 , Y10S514/866
摘要： The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl, etc.; one of Q and T represents a group selected from the following: and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.; R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium/glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.
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中的一个表示选自以下的基团：另一个表示-Z-Ar，其中Z表示-O-，-S-等; Ar表示任选取代的C 6-10芳基等。 R表示在人钠/葡萄糖共转运体（SGLT）中表现出优异抑制活性的可任选取代的C 3-8环烷基，任选取代的C 6-10芳基等，其药学上可接受的盐及其前药，并且可用作试剂 用于预防，抑制与选自葡萄糖，果糖和甘露糖（糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症等）中的至少一种碳水化合物的过量摄取相关的疾病的进展或治疗，以及药物 含有该组合物的组合物，其医药用途和用于其生产的中间体。
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6.发明授权Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same 失效吡唑衍生物，含有该吡唑衍生物的药物组合物，其药学用途及其制造中间体公开(公告)号：US07576063B2
公开(公告)日：2009-08-18
申请号：US10529895
申请日：2003-09-30
CPC分类号： C07D405/04 , A61K31/7056 , C07D231/20 , C07D401/04 , C07D409/04 , C07H17/02 , Y10S514/866
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 selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), 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之一表示选自以下基团的基团：另一个表示 - （CH 2）n -Ar，其中Ar表示任选取代的C 6-10芳基或任选取代的C 1-8杂芳基; n表示0〜2的整数，可以具有取代基的C 1-6烷氧基，可以具有取代基的氨基，可以具有取代基的C2-9杂环烷基或任意取代的杂环稠合苯基; 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，其药学上可接受的盐或其前体药物，其在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中表现出优异的抑制活性， 可用作预防，抑制与选自葡萄糖，果糖和甘露糖中的至少一种碳水化合物或与高血糖相关疾病（例如，糖尿病并发症，糖尿病等）的过量摄取相关疾病进展或治疗的药剂。 ），以及包含该药物组合物的药物组合物，其药学用途及其生产用中间体。
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7.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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8.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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9.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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10.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：US07129381B2
公开(公告)日：2006-10-31
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）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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