WO2009035067A1 - １，３，３－トリメチル－７－フェニル－３，４－ジヒドロ－１ｈ－キノキサリン－２－オ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

１，３，３－トリメチル－７－フェニル－３，４－ジヒドロ－１ｈ－キノキサリン－２－オ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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WO2009035067A1
WO2009035067A1 PCT/JP2008/066512 JP2008066512W WO2009035067A1 WO 2009035067 A1 WO2009035067 A1 WO 2009035067A1 JP 2008066512 W JP2008066512 W JP 2008066512W WO 2009035067 A1 WO2009035067 A1 WO 2009035067A1
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Prior art keywords
quinoxalin
dihydro
phenyl
glucocorticoid receptor
tri
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PCT/JP2008/066512
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English (en)
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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Publication of WO2009035067A1 publication Critical patent/WO2009035067A1/ja

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    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

　本発明は式（１）で表されるからなる１，３，３－トリメチル－７－フェニル－３，４－ジヒドロ－１Ｈ－キノキサリン－２－オン誘導体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およびそのアゴニストの新たな薬理作用を提供する。式中、Ｒ1は下記一般式（２ａ）、（３ａ）、（４ａ）又は（５ａ）を示し；Ｒ2および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、ヒドロキシ基、ヒドロキシ基のエステル等、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、ヒドロキシ基、低級アルコキシ基等、ｍ、ｎ、ｐ又はｑは、０、１又は２を示す。 　【化１】
PCT/JP2008/066512 2007-09-13 2008-09-12 １，３，３－トリメチル－７－フェニル－３，４－ジヒドロ－１ｈ－キノキサリン－２－オ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 WO2009035067A1 (ja)

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JP2007237877 2007-09-13
JP2007-237877 2007-09-13

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Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US8551991B2 (en) 2006-03-14 2013-10-08 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity
CN107922356A (zh) * 2015-08-25 2018-04-17 参天制药株式会社 [4‑(1,3,3‑三甲基‑2‑氧代‑3,4‑二氢‑1h‑喹喔啉‑7‑基)苯氧基]乙基氧基化合物或其盐
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
WO2019121611A1 (en) 2017-12-18 2019-06-27 Grünenthal GmbH Substituted pyrrolidine amides ii
WO2019121606A1 (en) 2017-12-18 2019-06-27 Grünenthal GmbH Substituted pyrrolidine amides i
WO2020016452A1 (en) 2018-07-20 2020-01-23 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
WO2020016453A1 (en) 2018-07-20 2020-01-23 Grünenthal GmbH Substituted triazolo quinoxaline derivatives
WO2020144375A1 (en) 2019-01-11 2020-07-16 Grünenthal GmbH Substituted pyrrolidine amides iii
WO2020254552A2 (en) 2019-06-19 2020-12-24 Grünenthal GmbH Substituted pyrrolidine amides v
WO2020254551A1 (en) 2019-06-19 2020-12-24 Grünenthal GmbH Substituted pyrrolidine amides iv
WO2021144440A1 (en) 2020-01-17 2021-07-22 Grünenthal GmbH Quinoxaline derivatives as modulators of the glucocorticoid receptor
WO2021144439A1 (en) 2020-01-17 2021-07-22 Grünenthal GmbH Quinoxaline derivatives
WO2022008705A1 (en) 2020-07-09 2022-01-13 Grünenthal GmbH Substituted pyrrolidine amines and amides as mediator of the glucocortoid receptor
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 (3)

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WO2006015259A2 (en) * 2004-07-28 2006-02-09 Irm Llc Compounds and compositions as modulators of steroid hormone nuclear receptors
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
WO2007105766A1 (ja) * 2006-03-14 2007-09-20 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１，２，３，４－テトラヒドロキノキサリン誘導体

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006015259A2 (en) * 2004-07-28 2006-02-09 Irm Llc Compounds and compositions as modulators of steroid hormone nuclear receptors
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
WO2007105766A1 (ja) * 2006-03-14 2007-09-20 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１，２，３，４－テトラヒドロキノキサリン誘導体

Cited By (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
EA018420B1 (ru) * 2008-09-12 2013-07-30 Сантен Фармасьютикал Ко., Лтд. Агонист глюкокортикоидного рецептора, содержащий новые производные 1,2,3,4-тетрагидрохиноксалина с фенильной группой, имеющей структуру эфира сульфоновой кислоты, введенной в нее в качестве заместителя
US8664221B2 (en) 2008-09-12 2014-03-04 Santen Pharmaceutical Co., Ltd. Method for treating an inflammatory disease by administering a 1,2,3,4- tetrahydroquinoxaline compound containing a phenyl group having a sulfonic acid ester structure introduced therein as a substituent
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
CN107922356A (zh) * 2015-08-25 2018-04-17 参天制药株式会社 [4‑(1,3,3‑三甲基‑2‑氧代‑3,4‑二氢‑1h‑喹喔啉‑7‑基)苯氧基]乙基氧基化合物或其盐
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
US10626106B2 (en) 2017-12-18 2020-04-21 Gruenenthal Gmbh Substituted pyrrolidine amides I
WO2019121611A1 (en) 2017-12-18 2019-06-27 Grünenthal GmbH Substituted pyrrolidine amides ii
WO2019121606A1 (en) 2017-12-18 2019-06-27 Grünenthal GmbH Substituted pyrrolidine amides i
WO2020016453A1 (en) 2018-07-20 2020-01-23 Grünenthal GmbH Substituted triazolo quinoxaline derivatives
CN112673009A (zh) * 2018-07-20 2021-04-16 格吕伦塔尔有限公司 被取代的三唑并喹喔啉衍生物
US10981918B2 (en) 2018-07-20 2021-04-20 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
WO2020016452A1 (en) 2018-07-20 2020-01-23 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
CN112673009B (zh) * 2018-07-20 2023-09-19 格吕伦塔尔有限公司 被取代的三唑并喹喔啉衍生物
US11981677B2 (en) 2018-07-20 2024-05-14 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
US12110293B2 (en) 2018-07-20 2024-10-08 Grünenthal GmbH Substituted triazolo quinoxaline derivatives
WO2020144375A1 (en) 2019-01-11 2020-07-16 Grünenthal GmbH Substituted pyrrolidine amides iii
WO2020254552A2 (en) 2019-06-19 2020-12-24 Grünenthal GmbH Substituted pyrrolidine amides v
WO2020254551A1 (en) 2019-06-19 2020-12-24 Grünenthal GmbH Substituted pyrrolidine amides iv
WO2021144440A1 (en) 2020-01-17 2021-07-22 Grünenthal GmbH Quinoxaline derivatives as modulators of the glucocorticoid receptor
WO2021144439A1 (en) 2020-01-17 2021-07-22 Grünenthal GmbH Quinoxaline derivatives
WO2022008705A1 (en) 2020-07-09 2022-01-13 Grünenthal GmbH Substituted pyrrolidine amines and amides as mediator of the glucocortoid receptor

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