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WO2008111632A1 - ２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト - Google Patents

２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト Download PDF

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WO2008111632A1
WO2008111632A1 PCT/JP2008/054568 JP2008054568W WO2008111632A1 WO 2008111632 A1 WO2008111632 A1 WO 2008111632A1 JP 2008054568 W JP2008054568 W JP 2008054568W WO 2008111632 A1 WO2008111632 A1 WO 2008111632A1
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receptor agonist
glucocorticoid receptor
trimethyl
phenyl
represent
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French (fr)
Inventor
Masatomo Kato
Miwa Takai
Takahiro Matsuyama
Tatsuji Kurose
Yumi Hagiwara
Mamoru Matsuda
Toshiyuki Mori
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Santen Pharmaceutical Co Ltd
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Santen Pharmaceutical Co Ltd
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Abstract

　２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト及びそのアゴニストの新たな薬理作用を見出す。 　式（１）で表される化合物又はその塩からなるグルココルチコイド受容体アゴニスト。 ［Ｒ1は下記一般式（２ａ）、（３ａ）、（４ａ）又は（５ａ）を示し； Ｒ2及びＲ3は同一又は異なって、水素原子、ハロゲン原子、低級アルキル基等、Ｒ4は低級アルキル基、Ｒ5、Ｒ6、Ｒ７又はＲ８は、ハロゲン原子、低級アルキル基、低級アルケニル基、低級アルコキシ基等ｍ、ｎ、ｐ又はｑは、０、１又は２を示す。]
PCT/JP2008/054568 2007-03-13 2008-03-13 ２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト Ceased WO2008111632A1 (ja)

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JP2007-063010 2007-03-13
JP2007063010 2007-03-13

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WO2008111632A1 true WO2008111632A1 (ja) 2008-09-18

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WO (1) WO2008111632A1 (ja)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009139361A1 (ja) * 2008-05-12 2009-11-19 参天製薬株式会社 置換オキシ基を有する２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト
WO2010029986A1 (ja) * 2008-09-12 2010-03-18 参天製薬株式会社 スルホン酸エステル構造を導入したフェニル基を置換基として有する新規１，２，３，４－テトラヒドロキノキサリン誘導体からなるグルココルチコイド受容体アゴニスト
EP2085388A4 (en) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd NEW 1,2-DIHYDROCHINOLINE DERIVATIVE WITH SUBSTITUTED PHENYLAMINOENE ALKYL GROUP AND PHENYL GROUP INTRODUCED BY AN ESTER AS SUBSTITUENTS
US8017775B2 (en) 2005-09-14 2011-09-13 Santen Pharmaceutical Co., Ltd. 1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity
US8193187B2 (en) 2007-05-29 2012-06-05 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline compound with a phenyl group substituent having a sulfonic acid ester structure or a sulfonic acid amide structure introduced therein and having glucocorticoid receptor-binding activity
WO2013108921A1 (ja) * 2012-01-20 2013-07-25 参天製薬株式会社 １，２－ジヒドロキノリン誘導体またはその塩の工業的製造方法およびその製造中間体
US8551991B2 (en) 2006-03-14 2013-10-08 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity
WO2018230713A1 (ja) 2017-06-16 2018-12-20 学校法人同志社 カスパーゼ阻害活性を有する化合物、これらの化合物を含む、角膜内皮の症状、障害または疾患を治療または予防するための医薬およびその応用
US11433090B2 (en) 2017-06-16 2022-09-06 The Doshisha mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof

Citations (4)

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JPH10510840A (ja) * 1994-12-22 1998-10-20 リガンド・ファーマシューティカルズ・インコーポレイテッド ステロイド受容体モジュレーター化合物および方法
JP2006504678A (ja) * 2002-08-21 2006-02-09 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用
WO2006019716A1 (en) * 2004-07-14 2006-02-23 Ligand Pharmaceuticals, Inc. Intracellular receptor modulator compounds and methods
WO2007032556A1 (ja) * 2005-09-14 2007-03-22 Santen Pharmaceutical Co., Ltd. グルココルチコイド受容体結合活性を有する新規１，２−ジヒドロキノリン誘導体

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10510840A (ja) * 1994-12-22 1998-10-20 リガンド・ファーマシューティカルズ・インコーポレイテッド ステロイド受容体モジュレーター化合物および方法
JP2006504678A (ja) * 2002-08-21 2006-02-09 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用
WO2006019716A1 (en) * 2004-07-14 2006-02-23 Ligand Pharmaceuticals, Inc. Intracellular receptor modulator compounds and methods
WO2007032556A1 (ja) * 2005-09-14 2007-03-22 Santen Pharmaceutical Co., Ltd. グルココルチコイド受容体結合活性を有する新規１，２−ジヒドロキノリン誘導体

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8017775B2 (en) 2005-09-14 2011-09-13 Santen Pharmaceutical Co., Ltd. 1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity
US8420635B2 (en) 2005-09-14 2013-04-16 Santen Pharmaceutical Co., Ltd. Method for preventing or treating a glucocorticoid receptor-related disease
US8975256B2 (en) 2006-03-14 2015-03-10 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline compounds having glucocorticoid receptor binding activity
US8551991B2 (en) 2006-03-14 2013-10-08 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity
US8440660B2 (en) 2006-11-14 2013-05-14 Santen Pharmaceutical Co., Ltd. Method for treating a disease related to the glucocorticoid receptor
EP2085388A4 (en) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd NEW 1,2-DIHYDROCHINOLINE DERIVATIVE WITH SUBSTITUTED PHENYLAMINOENE ALKYL GROUP AND PHENYL GROUP INTRODUCED BY AN ESTER AS SUBSTITUENTS
US8008498B2 (en) 2006-11-14 2011-08-30 Santen Pharmaceutical Co., Ltd. 1,2-dihydroquinoline derivative having substituted phenylamino lower alkyl group and ester-introduced phenyl group as substituents
US8008496B2 (en) 2006-11-14 2011-08-30 Santen Pharmaceutical Co., Ltd. 1,2-dihydroquinoline derivative having substituted phenylchalcogeno lower alkyl group and ester-introduced phenyl group as substituents
EP2085389A4 (en) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE COMPRISING AS SUBSTITUENTS A LOWER ALKYL-CARBONYLOXY GROUP (PHENYL-SUBSTITUTED OR HETEROCYCLIC SUBSTITUTED) AND A PHENYL GROUP LINKED BY AN ESTER
EP2085387A4 (en) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd NEW 1,2-DIHYDROCHINOLINE DERIVATIVITY WITH SUBSTITUTED PHENYLCHALCOGENONIAL ALKYL GROUP AND PHENYL GROUP INTRODUCED BY AN ESTER AS SUBSTITUENTS
US8008497B2 (en) 2006-11-14 2011-08-30 Santen Pharmaceutical Co., Ltd. 1,2-dihydroquinoline derivative having (substituted phenyl or substituted heterocyclic) carbonyloxy lower alkyl group and ester-introduced phenyl group as substituents
US8580784B2 (en) 2006-11-14 2013-11-12 Santen Pharmaceutical Co., Ltd. Method for treating a disease related to the glucocorticoid receptor
US8563551B2 (en) 2006-11-14 2013-10-22 Santen Pharmaceutical Co., Ltd. Method for preventing or treating a disease related to the glucocorticoid receptor
US8193187B2 (en) 2007-05-29 2012-06-05 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline compound with a phenyl group substituent having a sulfonic acid ester structure or a sulfonic acid amide structure introduced therein and having glucocorticoid receptor-binding activity
US8569493B2 (en) 2007-05-29 2013-10-29 Santen Pharmaceutical Co., Ltd. Method for treating a homeostasis-related disease or glaucoma by administering a 1,2,3,4-tetrahyroquinoxaline compound
EA019091B1 (ru) * 2008-05-12 2014-01-30 Сантен Фармасьютикал Ко., Лтд. Агонист глюкокортикоидного рецептора, включающий 2,2,4-триметил-6-фенил-1,2-дигидрохинолиновые производные, содержащие замещенную оксигруппу
WO2009139361A1 (ja) * 2008-05-12 2009-11-19 参天製薬株式会社 置換オキシ基を有する２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト
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JP2013166752A (ja) * 2012-01-20 2013-08-29 Santen Pharmaceut Co Ltd １，２−ジヒドロキノリン誘導体またはその塩の工業的製造方法およびその製造中間体
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WO2018230713A1 (ja) 2017-06-16 2018-12-20 学校法人同志社 カスパーゼ阻害活性を有する化合物、これらの化合物を含む、角膜内皮の症状、障害または疾患を治療または予防するための医薬およびその応用
US11433090B2 (en) 2017-06-16 2022-09-06 The Doshisha mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof
US12343356B2 (en) 2017-06-16 2025-07-01 The Doshisha mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof

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