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1. 发明申请

US20090286751A1 PROGRESSION INHIBITOR FOR DISEASE ATTRIBUTED TO ABNORMAL ACCUMULATION OF LIVER FAT 有权
标题翻译：归因于肝脏异常累积的疾病进展抑制剂
公开(公告)号：US20090286751A1
公开(公告)日：2009-11-19
申请号：US12511654
申请日：2009-07-29
申请人： Kenji KATSUNO , Yoshikazu Fujimori , Masayuki Isaji
发明人： Kenji KATSUNO , Yoshikazu Fujimori , Masayuki Isaji
IPC分类号： A61K31/70 , A61P3/00
CPC分类号： A61K31/7028 , A61K31/155 , A61K31/4427 , A61K31/57 , A61K31/7036
摘要： The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation of liver lipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcoholic fatty liver disease (NAFL), non-alcoholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcoholic fatty liver disease toxic fatty liver or the like.
摘要翻译：本发明提供了可用作抑制与肝脂异常积累相关的疾病进展的药物的药物组合物。特别地，作为活性成分含有钠/葡萄糖共转运体2抑制剂的本发明的药物组合物，作为抑制不仅普通脂肪肝而且还含有非酒精性脂肪性肝病（NAFL），非酒精性脂肪性肝炎（NASH），营养性脂肪肝，糖尿病性脂肪肝，酒精性脂肪肝病毒性脂肪肝等。

2. 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。

3. 发明授权

US07371730B2 Crystals of glucopyranosyloxybenzyl benzene derivative 有权
标题翻译：吡喃葡萄糖氧基苄基苯衍生物的晶体
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。

4. 发明申请

US20080038242A1 Benzimidazole derivatives and medical uses thereof 失效
标题翻译：苯并咪唑衍生物及其医疗用途
公开(公告)号：US20080038242A1
公开(公告)日：2008-02-14
申请号：US11473957
申请日：2006-06-23
申请人： Norhiko Kikuchi , Yoshinori Nonaka , Kazuya Tatani , Masahiro Hiratochi , Yu Kuramochi , Masayuki Isaji , Kazuo Shimizu , Takashi Miyagi
发明人： Norhiko Kikuchi , Yoshinori Nonaka , Kazuya Tatani , Masahiro Hiratochi , Yu Kuramochi , Masayuki Isaji , Kazuo Shimizu , Takashi Miyagi
IPC分类号： A61K38/44 , A61K31/4184 , A61K31/421 , A61K31/426 , A61K31/44 , A61K31/4427 , A61P19/02 , A61P7/00 , C07D221/00 , C07D295/00 , C07D235/04 , C07D213/02 , A61P29/00 , A61K31/4523 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K33/00
CPC分类号： C07H19/052
摘要： The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.
摘要翻译：本发明提供由下式（I）表示的苯并咪唑衍生物或其药学上可接受的盐或其前药，其对钠依赖性核苷转运蛋白2具有抑制活性，并且可用于与血浆尿酸异常有关的疾病水平。本发明的化合物可用于预防或治疗痛风，高尿酸血症，尿结石病，高尿酸性肾病等。在该式中，n为1或2; R 1和R 2均为H，卤素原子，氰基，任选取代的烷基，任选取代的芳基等; R 3是H，卤素原子，任选取代的烷基等; R 4和R 5是H，卤素原子，OH等; R 6和R X是H或OH：R Y是F或OH。

5. 发明申请

US20060166899A1 Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof 有权
标题翻译：吡唑衍生物，含有该吡唑衍生物的药物组合物，其医药用途及其生产用中间体
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。

6. 发明申请

US20060128635A1 Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same 失效
标题翻译：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
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。

7. 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。

8. 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。

9. 发明授权

US07998975B2 Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs 有权
标题翻译：含氮稠环衍生物，含有衍生物的药物组合物及其作为药物的用途
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。

10. 发明授权

US07566699B2 Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof 有权
标题翻译：稠合杂环衍生物，含有它们的药物组合物及其医药用途
公开(公告)号：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。

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