公开(公告)号：US20060128635A1

公开(公告)日：2006-06-15

申请号：US10529895

申请日：2003-09-30

申请人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

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。

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。

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。

公开(公告)号：US20120289506A1

公开(公告)日：2012-11-15

申请号：US13494380

申请日：2012-06-12

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/40 ,  C07D231/14 ,  A61K31/415 ,  C07D405/10 ,  C07D231/22 ,  A61P13/12 ,  A61K31/4439 ,  A61K31/454 ,  C07D413/06 ,  A61K31/5377 ,  A61P19/06 ,  C07D207/34 ,  C07D401/04

CPC分类号： A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  A61K2300/00

摘要： 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.

摘要翻译： 具有黄嘌呤氧化酶抑制活性的通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病或其前药或其盐的药剂。 在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。

公开(公告)号：US08227500B2

公开(公告)日：2012-07-24

申请号：US12595437

申请日：2008-04-10

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/405 ,  C07D207/00

CPC分类号： A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, -N(-D-L-M)2 and the like, in the formula, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常相关疾病，其前药或盐类的药物 其中。 在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，式中，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。

公开(公告)号：US20110230454A1

公开(公告)日：2011-09-22

申请号：US13116389

申请日：2011-05-26

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/56 ,  C07D209/14 ,  A61K31/405 ,  C07D409/12 ,  C07D401/10 ,  A61K31/4439 ,  C07D413/10 ,  A61K31/5377 ,  C07D498/04 ,  A61K31/407 ,  C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P19/00 ,  A61P13/12

CPC分类号： C07D209/30 ,  A61K31/165 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/42 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐 其中。 在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

公开(公告)号：US07888487B2

公开(公告)日：2011-02-15

申请号：US12534452

申请日：2009-08-03

申请人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Norihiko Kikuchi ,  Shigeki Tazawa ,  Tokuhisa Yamato ,  Masayuki Isaji

IPC分类号： C07G3/00 ,  C07H17/00

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。

公开(公告)号：US20100227864A1

公开(公告)日：2010-09-09

申请号：US12595437

申请日：2008-04-10

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/5377 ,  C07D231/10 ,  A61K31/4155 ,  C07D413/06 ,  C07D401/04 ,  A61K31/4412 ,  A61P43/00

CPC分类号： A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, -N(-D-L-M)2 and the like, in the formula, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常相关疾病，其前药或盐类的药物 其中。 在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，式中，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。

公开(公告)号：US07108044B2

公开(公告)日：2006-09-19

申请号：US10789185

申请日：2004-02-27

申请人： Yutaka Miyamoto ,  Norihiko Kikuchi

发明人： Yutaka Miyamoto ,  Norihiko Kikuchi

IPC分类号： B22C19/04

CPC分类号： B21D37/20

摘要： A method and an apparatus for machining a mold material to produce a mold. By casting based on a cast mold model (15), a mold material (20) is produced in a form having a work margin. Thereafter, a shape of the mold material (20) is measured by a measuring device (16), and measurement data and an envelope model (M2) generated based on the measurement data are stored in a storage unit (12A) of a computer (12). Thereafter, a mold model (M1) based on mold design data and an envelope model (M2) are displayed on a display unit (12C), and the envelope model (M2) is linearly moved in direction of three axes X, Y and Z orthogonal to one another respectively and rotated around the three axes to bring a product forming plane (M2B) of the envelope model (M2) into close proximity of a product forming plane (M1B) of the mold model (M1). Thereby, a state in which a work amount of a product forming plane (20B) of the mold material (20) is reduced is found, and a reference plane (20A) and a product forming plane (20B) of the mold material 20 are cut by a mold working machine (18) controlled by the computer (12).

摘要翻译： 一种用于加工模具材料以制造模具的方法和装置。 通过基于铸造模型（15）的铸造，以具有工作余量的形式制造模具材料（20）。 此后，通过测量装置（16）测量模具材料（20）的形状，并且将基于测量数据生成的测量数据和包络模型（M 2）存储在存储单元（12A）中 电脑（12）。 此后，在显示单元（12C）上显示基于模具设计数据和包络模型（M 2）的模具模型（M 1），并且包络模型（M2）在三个轴线X的方向上线性移动 ，Y和Z分别彼此正交并围绕三个轴线旋转，以使包络模型（M2）的产品形成平面（M 2 B）紧邻模具的产品形成平面（M 1 B） 型号（M 1）。 因此，发现了模具材料（20）的产品形成平面（20B）的加工量减少的状态，并且模具的参考平面（20A）和产品形成平面（20B） 材料20被由计算机（12）控制的模具加工机（18）切割。

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。