WO2008146871A1 - グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド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 - Google Patents

グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド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 Download PDF

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WO2008146871A1
WO2008146871A1 PCT/JP2008/059866 JP2008059866W WO2008146871A1 WO 2008146871 A1 WO2008146871 A1 WO 2008146871A1 JP 2008059866 W JP2008059866 W JP 2008059866W WO 2008146871 A1 WO2008146871 A1 WO 2008146871A1
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sulfonic acid
alkyl group
lower alkyl
hydrogen atom
glucocorticoid receptor
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PCT/JP2008/059866
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English (en)
French (fr)
Inventor
Mamoru Matsuda
Toshiyuki Mori
Masaaki Nagatsuka
Sachiko Kobayashi
Masatomo Kato
Miwa Takai
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Santen Pharmaceutical Co Ltd
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Santen Pharmaceutical Co Ltd
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Priority to ES08764835T priority Critical patent/ES2419239T3/es
Priority to PL08764835T priority patent/PL2151436T3/pl
Priority to EP08764835.8A priority patent/EP2151436B1/en
Priority to CN2008800179279A priority patent/CN101679317B/zh
Priority to MX2009012885A priority patent/MX2009012885A/es
Priority to NZ581666A priority patent/NZ581666A/en
Priority to BRPI0811262-2A2A priority patent/BRPI0811262A2/pt
Priority to CA002687948A priority patent/CA2687948A1/en
Application filed by Santen Pharmaceutical Co Ltd filed Critical Santen Pharmaceutical Co Ltd
Priority to AU2008255733A priority patent/AU2008255733B8/en
Priority to RU2009149185/04A priority patent/RU2498980C2/ru
Priority to US12/451,653 priority patent/US8193187B2/en
Publication of WO2008146871A1 publication Critical patent/WO2008146871A1/ja
Anticipated expiration legal-status Critical
Priority to US13/364,680 priority patent/US8569493B2/en
Ceased legal-status Critical Current

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    • C07D241/40—Benzopyrazines
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Abstract

　一般式（１）で表される化合物又はその塩はグルココルチコイド受容体のモジュレーターとして有用である。式中、Ｒ1は低級アルキル基、低級シクロアルキル基、アリール基等を示し；Ｒ2は水素原子、低級アルキル基等を示し；Ｒ3は水素原子、低級アルキル基等を示し；Ｒ4及びＲ5は水素原子、低級アルキル基等を示し；Ｒ6は水素原子、低級アルキル基等を示し；Ｒ7は水素原子、低級アルキル基、低級アルケニル基等を示し；Ｗは酸素原子、硫黄原子、ＮＲ8等を示し；Ｒ8は水素原子、低級アルキル基等を示し；Ｘは酸素原子、硫黄原子を示し；Ｙは低級アルキレン基等を示し；Ｚは酸素原子、硫黄原子、ＮＲ9、ＯＣＯ、ＯＳＯ2を示し；Ｒ9は水素原子、低級アルキル基等をそれぞれ示す。
PCT/JP2008/059866 2007-05-29 2008-05-29 グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド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 Ceased WO2008146871A1 (ja)

Priority Applications (12)

Application Number Priority Date Filing Date Title
BRPI0811262-2A2A BRPI0811262A2 (pt) 2007-05-29 2008-05-29 Composto, composto ou sal do mesmo, composição farmacêutica, modulador de receptor de glicocorticóide, método para prevenção e/ou tratamento de bistúrbios metabólicos, doenças inflamatórias, doenças auto-imunes, doenças alérgicas, doenças do sistema nervoso central, doenças cardiovasculares, doenças relacionadas com homeostase ou glaucoma, e uso de pelo menos um composto ou um sal do mesmo
EP08764835.8A EP2151436B1 (en) 2007-05-29 2008-05-29 Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity
CN2008800179279A CN101679317B (zh) 2007-05-29 2008-05-29 具有糖皮质激素受体结合活性且具有导入了磺酸酯或磺酰胺结构的苯基作为取代基的1，2，3，4-四氢喹喔啉衍生物
MX2009012885A MX2009012885A (es) 2007-05-29 2008-05-29 Nuevo derivado de 1,2,3,4-tetrahidroquinoxalina que tiene, como sustituyente, grupo fenilo que tiene estructura de ester de acido sulfonico o estructura de amida de acido sulfonico introducida en este, y tiene actividad de enlace al receptor de gluco
NZ581666A NZ581666A (en) 2007-05-29 2008-05-29 Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity
CA002687948A CA2687948A1 (en) 2007-05-29 2008-05-29 Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein andhas glucocorticoid receptor-binding activity
AU2008255733A AU2008255733B8 (en) 2007-05-29 2008-05-29 Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity
ES08764835T ES2419239T3 (es) 2007-05-29 2008-05-29 Nuevo derivado de 1,2,3,4-tetrahidroquinoxalina que tiene como sustituyente un grupo fenilo con una estructura de éster de ácido sulfónico o una estructura de amida de ácido sulfónico introducida en el mismo y que tienen una actividad de unión al receptor de glucocorticoides
PL08764835T PL2151436T3 (pl) 2007-05-29 2008-05-29 Nowe pochodne 1,2,3,4-tetrahydrochinoksaliny, które jako podstawnik zawierają grupę fenylową z wprowadzoną strukturą estru kwasu sulfonowego lub amidu kwasu sulfonowego i które mają aktywność wiążącą wobec receptora glukokortykoidowego
RU2009149185/04A RU2498980C2 (ru) 2007-05-29 2008-05-29 Новое производное 1,2,3,4-тетрагидрохиноксалина, содержащее в качестве заместителя фенильную группу, имеющую структуру эфира сульфокислоты или амида сульфокислоты, и обладающее связывающей активностью в отношении рецептора глюкокортикоидов
US12/451,653 US8193187B2 (en) 2007-05-29 2008-05-29 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
US13/364,680 US8569493B2 (en) 2007-05-29 2012-02-02 Method for treating a homeostasis-related disease or glaucoma by administering a 1,2,3,4-tetrahyroquinoxaline compound

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-141568 2007-05-29
JP2007141568 2007-05-29

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/451,653 A-371-Of-International US8193187B2 (en) 2007-05-29 2008-05-29 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
US13/364,680 Division US8569493B2 (en) 2007-05-29 2012-02-02 Method for treating a homeostasis-related disease or glaucoma by administering a 1,2,3,4-tetrahyroquinoxaline compound

Publications (1)

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WO2008146871A1 true WO2008146871A1 (ja) 2008-12-04

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PCT/JP2008/059866 Ceased WO2008146871A1 (ja) 2007-05-29 2008-05-29 グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド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

Country Status (14)

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US (2) US8193187B2 (ja)
EP (1) EP2151436B1 (ja)
JP (1) JP5183302B2 (ja)
KR (1) KR20100022456A (ja)
CN (1) CN101679317B (ja)
AU (1) AU2008255733B8 (ja)
BR (1) BRPI0811262A2 (ja)
CA (1) CA2687948A1 (ja)
ES (1) ES2419239T3 (ja)
MX (1) MX2009012885A (ja)
NZ (1) NZ581666A (ja)
PL (1) PL2151436T3 (ja)
RU (1) RU2498980C2 (ja)
WO (1) WO2008146871A1 (ja)

Cited By (14)

* 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
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2011161030A1 (de) 2010-06-21 2011-12-29 Sanofi Heterocyclisch substituierte methoxyphenylderivate mit oxogruppe, verfahren zu ihrer herstellung und ihre verwendung als gpr40 rezeptor modulatoren
WO2012004269A1 (de) 2010-07-05 2012-01-12 Sanofi ( 2 -aryloxy -acetylamino) - phenyl - propionsäurederivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2012004270A1 (de) 2010-07-05 2012-01-12 Sanofi Spirocyclisch substituierte 1,3-propandioxidderivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2012010413A1 (de) 2010-07-05 2012-01-26 Sanofi Aryloxy-alkylen-substituierte hydroxy-phenyl-hexinsäuren, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
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
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
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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
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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
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
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
CN112771046A (zh) * 2018-07-20 2021-05-07 格吕伦塔尔有限公司 其他被取代的三唑并喹喔啉衍生物
CN112771046B (zh) * 2018-07-20 2023-09-19 格吕伦塔尔有限公司 其他被取代的三唑并喹喔啉衍生物
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
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
WO2025111184A1 (en) 2023-11-21 2025-05-30 Fmc Corporation Substituted tetrahydroquinoline and tetrahydroquinoxaline herbicides

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US20120129866A1 (en) 2012-05-24
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