发明申请
US20110166151A1 GLUCOCORTICOID RECEPTOR AGONIST COMPRISING 1,2,3,4-TETRAHYDROQUINOXALINE DERIVATIVES CONTAINING PHENYL GROUP HAVING SULFONIC ACID ESTER STRUCTURE INTRODUCED THEREIN AS SUBSTITUENT
失效
包含具有作为替代物引入的磺酸酯结构的苯基的1,2,3,4-四氢喹啉衍生物的GLUCOCORTICOID受体激动剂
- 专利标题: GLUCOCORTICOID RECEPTOR AGONIST COMPRISING 1,2,3,4-TETRAHYDROQUINOXALINE DERIVATIVES CONTAINING PHENYL GROUP HAVING SULFONIC ACID ESTER STRUCTURE INTRODUCED THEREIN AS SUBSTITUENT
- 专利标题(中): 包含具有作为替代物引入的磺酸酯结构的苯基的1,2,3,4-四氢喹啉衍生物的GLUCOCORTICOID受体激动剂
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申请号: US13063186申请日: 2009-09-11
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公开(公告)号: US20110166151A1公开(公告)日: 2011-07-07
- 发明人: Masatomo Kato , Miwa Takai , Takahiro Matsuyama , Tatsuji Kurose , Yumi Hagiwara , Kenji Oki , Mamoru Matsuda , Toshiyuki Mori
- 申请人: Masatomo Kato , Miwa Takai , Takahiro Matsuyama , Tatsuji Kurose , Yumi Hagiwara , Kenji Oki , Mamoru Matsuda , Toshiyuki Mori
- 申请人地址: JP Osaka
- 专利权人: Santen Pharmaceutical Co., Ltd.
- 当前专利权人: Santen Pharmaceutical Co., Ltd.
- 当前专利权人地址: JP Osaka
- 优先权: JP2008234105 20080912
- 国际申请: PCT/JP2009/065888 WO 20090911
- 主分类号: A61K31/498
- IPC分类号: A61K31/498 ; C07D241/38 ; A61P37/02
摘要:
The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye). R1 represents a group represented by general formula (2a), (3a), (4a) or (5a); R2 represents a lower alkyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, or the like; R3 represents a lower alkyl group; R4, R5, R6 or R7 represent a halogen atom, a lower alkyl group which may have a substituent, a hydroxy group, a lower alkoxy group which may have a substituent, or the like; and m, n, p or q represents a number of 0, 1 or 2.
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