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1. 发明申请

US20100152165A1 CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：羧酸衍生物
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。

2. 发明授权

US07968552B2 Oxadiazolidinedione compound 有权
标题翻译：恶二唑烷二酮化合物
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。

3. 发明申请

US20090186909A1 Oxadiazolidinedione Compound 有权
标题翻译：恶二唑烷二酮化合物
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。

4. 发明申请

US20100267775A1 OXADIAZOLIDINEDIONE COMPOUND 审中-公开
标题翻译：氧化杂环化合物
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。

5. 发明申请

US20120035196A1 CARBOXYLIC ACID COMPOUND 审中-公开
标题翻译：羧酸化合物
公开(公告)号：US20120035196A1
公开(公告)日：2012-02-09
申请号：US13265781
申请日：2010-04-21
申请人： Kenji Negoro , Kei Ohnuki , Yasuhiro Yonetoku , Kazuyuki Kuramoto , Yasuharu Urano , Hideyuki Watanabe
发明人： Kenji Negoro , Kei Ohnuki , Yasuhiro Yonetoku , Kazuyuki Kuramoto , Yasuharu Urano , Hideyuki Watanabe
IPC分类号： A61K31/505 , C07C63/36 , A61K31/216 , A61K31/192 , C07D239/34 , C07D305/06 , A61K31/337 , C07D207/46 , A61K31/4015 , C07D309/10 , A61K31/351 , C07D317/18 , A61K31/341 , A61P3/10 , C07C69/616
CPC分类号： C07D207/06 , A61K31/40 , A61K31/4015 , C07C49/417 , C07C59/68 , C07C59/72 , C07C69/732 , C07C69/734 , C07C229/42 , C07C233/18 , C07C235/20 , C07C255/37 , C07C271/30 , C07C311/04 , C07C2603/18 , C07C2603/94 , C07D207/27 , C07D239/34 , C07D305/06 , C07D307/94 , C07D309/06 , C07D309/10 , C07D317/22 , C07D319/06 , C07D405/12
摘要： [Problem]The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes.[Means for Solution]The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.
摘要翻译：本发明的目的是提供具有GPR40激动活性的化合物，其可用作药物组合物，胰岛素分泌促进剂或糖尿病预防/治疗剂。 [解决方案]本发明人广泛研究了具有GPR40激动活性的化合物，结果发现本发明的化合物（I）或其药学上可接受的盐，其中羧酸为通过亚甲基键合到双环或三环部分，此外，被单环6元芳环取代的苯环通过-O-亚甲基或-NH-亚甲基与双环或三环部分连接，具有优异的GPR40激动活性。他们还发现该化合物具有优异的胰岛素分泌促进作用，并且强烈地抑制葡萄糖负荷后血糖的增加，从而完成本发明。

6. 发明授权

US07960562B2 Propane-1,3-dione derivative or salt thereof 有权
标题翻译：丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US07960562B2
公开(公告)日：2011-06-14
申请号：US11887384
申请日：2006-03-30
申请人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号： A61K31/4184 , C07D235/12
CPC分类号： C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译：旨在提供可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙烷-1,3-二酮衍生物。结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

7. 发明授权

US08076367B2 Benzimidazolylidene propane-1,3-dione derivative or salt thereof 失效
标题翻译：苯并咪唑基丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US08076367B2
公开(公告)日：2011-12-13
申请号：US12726506
申请日：2010-03-18
申请人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
发明人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
IPC分类号： A01N43/52
CPC分类号： C07D401/06
摘要： Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.
摘要翻译：提供了可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙-1,3-二酮衍生物，结果确认了具有2-（1,3-二氢-2H-苯并咪唑-2-亚基）的丙-1,3-二酮或化合物其具有被衍生自1-羟甲基的基团取代的苯或噻吩环，除了其优异的GnRH受体拮抗作用外，显示出优异的可利用性，从而完成本发明。由于本发明的化合物显示出优异的可利用性，除了其强的GnRH受体拮抗作用外，可以预期其在生物体中具有优异的药物作用，并且可用于治疗性激素依赖性疾病如前列腺癌，乳腺癌，子宫内膜异位症，子宫平滑肌瘤，良性前列腺肥大等。此外，由于本发明的化合物在人体中的代谢稳定性优异，药物相互作用也较少，因此作为上述疾病的药物具有更优选的特性。

8. 发明授权

US07709519B2 Benzimidazolylidene propane-1,3 dione derivative or salt thereof 失效
标题翻译：苯并咪唑基丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US07709519B2
公开(公告)日：2010-05-04
申请号：US10588485
申请日：2005-06-02
申请人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
发明人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
IPC分类号： A01N43/52
CPC分类号： C07D401/06
摘要： Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.
摘要翻译：提供了可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙-1,3-二酮衍生物，结果确认了具有2-（1,3-二氢-2H-苯并咪唑-2-亚基）的丙-1,3-二酮或化合物其具有被衍生自1-羟甲基的基团取代的苯或噻吩环，除了其优异的GnRH受体拮抗作用外，显示出优异的可利用性，从而完成本发明。由于本发明的化合物显示出优异的可利用性，除了其强的GnRH受体拮抗作用外，可以预期其在生物体中具有优异的药物作用，并且可用于治疗性激素依赖性疾病如前列腺癌，乳腺癌，子宫内膜异位症，子宫平滑肌瘤，良性前列腺肥大等。此外，由于本发明的化合物在人体中的代谢稳定性优异，药物相互作用也较少，因此作为上述疾病的药物具有更优选的特性。

9. 发明申请

US20100173946A1 BENZIMIDAZOLYLIDENE PROPANE-1,3-DIONE DERIVATIVE OR SALT THEREOF 失效
标题翻译：苯并咪唑啉酮1,3-丙二醇衍生物或其盐
公开(公告)号：US20100173946A1
公开(公告)日：2010-07-08
申请号：US12726506
申请日：2010-03-18
申请人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
发明人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
IPC分类号： A61K31/4439 , C07D405/10 , A61K31/4184 , C07D407/14 , A61P13/08 , A61P35/00
CPC分类号： C07D401/06
摘要： Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.
摘要翻译：提供了可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙-1,3-二酮衍生物，结果确认了具有2-（1,3-二氢-2H-苯并咪唑-2-亚基）的丙-1,3-二酮或化合物其具有被衍生自1-羟甲基的基团取代的苯或噻吩环，除了其优异的GnRH受体拮抗作用外，显示出优异的可利用性，从而完成本发明。由于本发明的化合物显示出优异的可利用性，除了其强的GnRH受体拮抗作用外，可以预期其在生物体中具有优异的药物作用，并且可用于治疗性激素依赖性疾病如前列腺癌，乳腺癌，子宫内膜异位症，子宫平滑肌瘤，良性前列腺肥大等。此外，由于本发明的化合物在人体中的代谢稳定性优异，药物相互作用也较少，因此作为上述疾病的药物具有更优选的特性。

10. 发明申请

US20090181964A1 Propane-1,3-Dione Derivative or Salt Thereof 有权
标题翻译：丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US20090181964A1
公开(公告)日：2009-07-16
申请号：US11887384
申请日：2006-03-30
申请人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahisa , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahisa , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号： A61K31/5377 , C07D235/04 , A61K31/4184 , C07D401/02 , A61K31/4439 , C07D403/02 , A61K31/496 , C07D413/14 , A61K31/506 , A61K31/501 , A61P35/00
CPC分类号： C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译：旨在提供可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙烷-1,3-二酮衍生物。结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

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