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公开(公告)号:US07547680B2
公开(公告)日:2009-06-16
申请号:US11473957
申请日:2006-06-23
申请人: Norihiko Kikuchi , Yoshinori Nonaka , Kazuya Tatani , Masahiro Hiratochi , Yu Kuramochi , Masayuki Isaji , Kazuo Shimizu , Takashi Miyagi
发明人: Norihiko Kikuchi , Yoshinori Nonaka , Kazuya Tatani , Masahiro Hiratochi , Yu Kuramochi , Masayuki Isaji , Kazuo Shimizu , Takashi Miyagi
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是H,卤素原子,氰基,任选取代的烷基,任选取代的芳基等; R3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; R6和RX是H或OH:RY是F或OH。
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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。
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