WO2009035068A1 - 新規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 - Google Patents
新規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 Download PDFInfo
- Publication number
- WO2009035068A1 WO2009035068A1 PCT/JP2008/066513 JP2008066513W WO2009035068A1 WO 2009035068 A1 WO2009035068 A1 WO 2009035068A1 JP 2008066513 W JP2008066513 W JP 2008066513W WO 2009035068 A1 WO2009035068 A1 WO 2009035068A1
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- lower alkyl
- diseases
- derivatives
- quinoxalin
- dihydro
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- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/12—Radicals substituted by halogen atoms or nitro or nitroso radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
本発明は、一般式(1)で表される新規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、およびその薬理作用を提供する。該化合物又はその塩は、グルココルチコイド受容体モジュレーターとして有用である。特にステロイド類等のグルココルチコイド受容体アゴニストが有効とされる疾患、例えば、炎症性の骨・関節疾患、眼炎症性疾患(前眼部又は後眼部炎症性疾患)の治療剤として有用である。式中、R1は下記一般式(2a)、(3a)、(4a)又は(5a)を示し;R2は低級アルキル基等を、R3は水素原子、低級アルキル基、シクロアルキル基、アリール基、複素環基、アラルキル基等を、R4又はR5は、水素原子、低級アルキル基等を、Aは低級アルキレン基を、R6、R7、R8又はR9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を、m、n、p又はqは、0、1又は2を示す。 【化1】
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2007-237896 | 2007-09-13 | ||
JP2007237896 | 2007-09-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2009035068A1 true WO2009035068A1 (ja) | 2009-03-19 |
Family
ID=40452074
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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PCT/JP2008/066513 WO2009035068A1 (ja) | 2007-09-13 | 2008-09-12 | 新規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 |
Country Status (2)
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JP (1) | JP2009084274A (ja) |
WO (1) | WO2009035068A1 (ja) |
Cited By (8)
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 |
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 |
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 |
US11981677B2 (en) | 2018-07-20 | 2024-05-14 | Grünenthal GmbH | Further substituted triazolo quinoxaline derivatives |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2861261A1 (en) | 2012-01-31 | 2013-08-08 | Santen Pharmaceutical Co., Ltd. | Non-aqueous liquid composition |
TW201609145A (zh) | 2013-12-25 | 2016-03-16 | 參天製藥股份有限公司 | 注射劑及形成緩釋(depot)之方法 |
Citations (3)
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 |
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2008
- 2008-09-12 WO PCT/JP2008/066513 patent/WO2009035068A1/ja active Application Filing
- 2008-09-12 JP JP2008234101A patent/JP2009084274A/ja not_active Withdrawn
Patent Citations (3)
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 (13)
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 |
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 |
US11981677B2 (en) | 2018-07-20 | 2024-05-14 | Grünenthal GmbH | Further substituted triazolo quinoxaline derivatives |
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JP2009084274A (ja) | 2009-04-23 |
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