-
公开(公告)号:US20100152165A1
公开(公告)日:2010-06-17
申请号:US12517033
申请日:2007-11-29
申请人: Kenji Negoro , Kei Ohnuki , Toshio Kurosaki , Fumiyoshi Iwasaki , Yasuhiro Yonetoku , Kazuyuki Tsuchiya , Norio Asai , Shigeru Yoshida , Takatoshi Soga , Daisuke Suzuki
发明人: Kenji Negoro , Kei Ohnuki , Toshio Kurosaki , Fumiyoshi Iwasaki , Yasuhiro Yonetoku , Kazuyuki Tsuchiya , Norio Asai , Shigeru Yoshida , Takatoshi Soga , Daisuke Suzuki
IPC分类号: A61K31/55 , C07D215/20 , A61K31/47 , C07D223/16 , C07D279/16 , A61K31/5415 , A61K31/4375 , C07D471/02
CPC分类号: C07D471/04 , C07D209/08 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/227 , C07D215/26 , C07D215/38 , C07D215/40 , C07D215/58 , C07D265/36 , C07D279/16 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/12
摘要: [Problem] To provide a pharmaceutical, particularly a compound which can be used as an insulin secretion promoter or a preventive or therapeutic agent for diabetes mellitus and the like diseases in which GPR40 is concerned.[Means for resolution] It was found that novel carboxylic acid derivatives or salts thereof, characterized in that carboxylic acid is linked to a 6-membered monocyclic aromatic ring via two atoms and said aromatic ring is linked to a nitrogen-containing bicyclic ring via a linker, have excellent GPR40 receptor agonist action. In addition, since the carboxylic acid derivatives of the invention showed excellent insulin secretion promoting action and blood glucose reducing action, they are useful as an insulin secretion promoter and a preventive or therapeutic agent for diabetes mellitus.
摘要翻译: [问题]提供可以用作胰岛素分泌促进剂的药物,特别是涉及GPR40的糖尿病等的预防或治疗剂的化合物。 [解决方法]发现新的羧酸衍生物或其盐,其特征在于羧酸通过两个原子与6元单环芳香环连接,所述芳环经由含氮双环通过 接头,具有优异的GPR40受体激动作用。 此外,由于本发明的羧酸衍生物显示出优异的胰岛素分泌促进作用和降血糖作用,因此它们可用作糖尿病的胰岛素分泌促进剂和预防或治疗剂。
-
公开(公告)号:US07968552B2
公开(公告)日:2011-06-28
申请号:US12298522
申请日:2007-04-23
申请人: Kenji Negoro , Fumiyoshi Iwasaki , Kei Ohnuki , Toshio Kurosaki , Yasuhiro Yonetoku , Norio Asai , Shigeru Yoshida , Takatoshi Soga
发明人: Kenji Negoro , Fumiyoshi Iwasaki , Kei Ohnuki , Toshio Kurosaki , Yasuhiro Yonetoku , Norio Asai , Shigeru Yoshida , Takatoshi Soga
IPC分类号: A61K31/506 , A61K31/4439 , A61K31/4245 , C07D413/12 , C07D271/07
CPC分类号: C07D271/06 , C07D271/07 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided.It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.
摘要翻译: 可以提供可用作药物的化合物,特别是胰岛素分泌促进剂或用于预防/治疗其中涉及GPR40的疾病如糖尿病等的化合物。 已经发现,具有通过在恶二唑烷二酮环2位上的连接体与环状基团结合的苄基等取代基的恶二唑烷二酮化合物或其药学上可接受的盐具有优异的GPR40激动剂作用 。 此外,由于本发明的恶二唑烷二酮化合物显示出优异的胰岛素分泌促进作用和血糖降低作用,因此可用作胰岛素分泌促进剂或糖尿病的预防/治疗剂。
-
公开(公告)号:US20090186909A1
公开(公告)日:2009-07-23
申请号:US12298522
申请日:2007-04-23
申请人: Kenji Negoro , Fumiyoshi Iwasaki , Kei Ohnuki , Toshio Kurosaki , Yasuhiro Yonetoku , Norio Asai , Shigeru Yoshida , Takatoshi Soga
发明人: Kenji Negoro , Fumiyoshi Iwasaki , Kei Ohnuki , Toshio Kurosaki , Yasuhiro Yonetoku , Norio Asai , Shigeru Yoshida , Takatoshi Soga
IPC分类号: A61K31/506 , A61K31/4439 , A61K31/4245 , C07D413/12 , C07D271/07
CPC分类号: C07D271/06 , C07D271/07 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided.[Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.
摘要翻译: 可以提供可用作药物的化合物,特别是胰岛素分泌促进剂或用于预防/治疗其中涉及GPR40的疾病如糖尿病等的化合物。 [解决方法]已经发现,恶二唑烷二酮化合物或其药学上可接受的盐,其特征在于具有通过在恶二唑烷二酮环的2位上的连接基与环状基团结合的苄基等取代基, 具有优异的GPR40激动作用。 此外,由于本发明的恶二唑烷二酮化合物显示出优异的胰岛素分泌促进作用和血糖降低作用,因此可用作胰岛素分泌促进剂或糖尿病的预防/治疗剂。
-
公开(公告)号:US20100267775A1
公开(公告)日:2010-10-21
申请号:US12739501
申请日:2008-10-22
申请人: Kenji Negoro , Fumiyoshi Iwasaki , Kei Ohnuki , Toshio Kurosaki , Kazuyuki Tsuchiya , Kazuyuki Kuramoto , Shigeru Yoshida , Takatoshi Soga
发明人: Kenji Negoro , Fumiyoshi Iwasaki , Kei Ohnuki , Toshio Kurosaki , Kazuyuki Tsuchiya , Kazuyuki Kuramoto , Shigeru Yoshida , Takatoshi Soga
IPC分类号: A61K31/4439 , C07D271/07 , A61K31/4245 , A61P3/10 , C07D413/12
CPC分类号: C07D271/06 , C07D271/07 , C07D413/12
摘要: A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.
摘要翻译: 具有GPR40受体激动作用的药剂,特别是可用作胰岛素促分泌剂的化合物或用于预防和/或治疗糖尿病的药剂。 本发明人已经研究了具有GPR40受体激动作用的化合物,证实了通过2-位的连接基与诸如苯基等取代基连接的具有苄基等取代基的恶二唑烷二酮化合物等 的恶二唑烷二酮环或其药学上可接受的盐具有优异的GPR40激动活性,从而完成了本发明。 恶二唑烷二酮化合物具有优异的胰岛素促分泌作用和抗高血糖作用,因此可用作胰岛素促分泌素或预防和/或治疗糖尿病的药剂。
-
公开(公告)号:US20070161787A1
公开(公告)日:2007-07-12
申请号:US11710434
申请日:2007-02-26
申请人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号: A61K31/7052 , C07H17/00
CPC分类号: C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
-
公开(公告)号:US20090069252A1
公开(公告)日:2009-03-12
申请号:US12173614
申请日:2008-07-15
申请人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号: A61K31/7042 , C07H7/06
CPC分类号: C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译: 本发明提供C-糖苷衍生物及其盐,其中B环通过-X-与A环结合,A环与葡萄糖残基直接结合,可用作Na + - 葡萄糖共转运蛋白抑制剂,尤其用于 胰岛素依赖性糖尿病(1型糖尿病)和胰岛素依赖性糖尿病(2型糖尿病)等糖尿病治疗剂和/或预防剂,以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
-
公开(公告)号:US20060122126A1
公开(公告)日:2006-06-08
申请号:US10541615
申请日:2004-03-12
申请人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号: C07H23/00 , A61K31/7052
CPC分类号: C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译: 本发明提供C-糖苷衍生物及其盐,其中B环通过-X-与A环键合,并且A环直接键合到葡萄糖残基,并且其可用作Na + 葡萄糖共转运蛋白抑制剂,特别是用于糖尿病的治疗和/或预防剂,例如胰岛素依赖性糖尿病(1型糖尿病)和不依赖胰岛素的糖尿病(2型糖尿病),以及糖尿病相关疾病如胰岛素抵抗 疾病和肥胖。
-
公开(公告)号:US07977466B2
公开(公告)日:2011-07-12
申请号:US12173614
申请日:2008-07-15
申请人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号: A61K31/7034 , C07H7/04
CPC分类号: C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译: 本发明提供C-糖苷衍生物及其盐,其中B环通过-X-与A环结合,A环与葡萄糖残基直接结合,可用作Na + - 葡萄糖共转运蛋白抑制剂,尤其用于 胰岛素依赖性糖尿病(1型糖尿病)和胰岛素依赖性糖尿病(2型糖尿病)等糖尿病治疗剂和/或预防剂,以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
-
公开(公告)号:US07772407B2
公开(公告)日:2010-08-10
申请号:US11710434
申请日:2007-02-26
申请人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号: A61K31/7034 , A61K31/381 , C07H7/04 , C07D333/34 , C07D495/00
CPC分类号: C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译: 本发明提供C-糖苷衍生物及其盐,其中B环通过-X-与A环结合,A环与葡萄糖残基直接结合,可用作Na + - 葡萄糖共转运蛋白抑制剂,尤其用于 胰岛素依赖性糖尿病(1型糖尿病)和胰岛素依赖性糖尿病(2型糖尿病)等糖尿病治疗剂和/或预防剂,以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
-
公开(公告)号:US07202350B2
公开(公告)日:2007-04-10
申请号:US10541615
申请日:2004-03-12
申请人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人: Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
CPC分类号: C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译: 本发明提供C-糖苷衍生物及其盐,其中B环通过-X-与A环键合,并且A环直接键合到葡萄糖残基,并且其可用作Na + 葡萄糖共转运蛋白抑制剂,特别是用于糖尿病的治疗和/或预防剂,例如胰岛素依赖性糖尿病(1型糖尿病)和不依赖胰岛素的糖尿病(2型糖尿病),以及糖尿病相关疾病如胰岛素抵抗 疾病和肥胖。
-
-
-
-
-
-
-
-
-