WO2008111632A1 - Agoniste de récepteur de glucocorticoïde constitué d'un dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine - Google Patents

Agoniste de récepteur de glucocorticoïde constitué d'un dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine Download PDF

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Publication number
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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PCT/JP2008/054568
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English (en)
Japanese (ja)
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 WO2008111632A1 publication Critical patent/WO2008111632A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • 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

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Abstract

L'invention concerne un agoniste de récepteur de glucocorticoïde constitué d'un dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine. Une nouvelle activité pharmacologique de l'agoniste est également décrite. Un agoniste de récepteur de glucocorticoïde constitué d'un composé représenté par la formule (1) ci-dessous ou d'un sel de celui-ci, est décrit spécifiquement. [dans la formule ci-dessous, R1 représente un groupe représenté par la formule générale (2a), (3a), (4a) ou (5a); R2 et R3 peuvent être identiques ou différents, et peuvent représenter un atome d'hydrogène, un atome d'halogène, un groupe alkyle inférieur ou similaire; R4 représente un groupe alkyle inférieur; R5, R6, R7 et R8 représentent un atome d'halogène, un groupe alkyle inférieur, un groupe alcényle inférieur, un groupe alcoxy inférieur ou similaire, et m, n, p et q représentent 0, 1 ou 2.]
PCT/JP2008/054568 2007-03-13 2008-03-13 Agoniste de récepteur de glucocorticoïde constitué d'un dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine WO2008111632A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-063010 2007-03-13
JP2007063010 2007-03-13

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WO2008111632A1 true WO2008111632A1 (fr) 2008-09-18

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JP (1) JP2008255112A (fr)
WO (1) WO2008111632A1 (fr)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2085388A1 (fr) * 2006-11-14 2009-08-05 Santen Pharmaceutical Co., Ltd Nouveau dérivé 1,2-dihydroquinoline comprenant un groupe alkyle inférieur à substitution phénylamino et un groupe phényle dans lequel est introduit un ester en tant que substituants
WO2009139361A1 (fr) * 2008-05-12 2009-11-19 参天製薬株式会社 Agoniste des récepteurs de glucocorticoïdes composé de dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine ayant un groupe oxy substitué
WO2010029986A1 (fr) * 2008-09-12 2010-03-18 参天製薬株式会社 Agoniste de récepteur de glucocorticoïde comprenant un nouveau dérivé de 1,2,3,4-tétrahydroquinoxaline contenant un groupe phényle ayant une structure d’ester d’acide sulfonique introduite dans celui-ci en tant que substituant
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 (fr) * 2012-01-20 2013-07-25 参天製薬株式会社 Procédé industriel de préparation d'un dérivé de 1,2-dihydroquinoline ou d'un sel de celui-ci, et intermédiaire servant à sa préparation
US8551991B2 (en) 2006-03-14 2013-10-08 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity
WO2018230713A1 (fr) 2017-06-16 2018-12-20 学校法人同志社 Composés ayant une activité inhibitrice de caspase, agent pharmaceutique les contenant pour le traitement ou la prévention des symptômes, troubles ou maladies de l'endothélium cornéen, et application dudit agent pharmaceutique
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 (fr) * 2004-07-14 2006-02-23 Ligand Pharmaceuticals, Inc. Composés modulateurs de récepteurs intracellulaires et procédés de production et d'utilisation de ceux-ci
WO2007032556A1 (fr) * 2005-09-14 2007-03-22 Santen Pharmaceutical Co., Ltd. Nouveau dérivé de 1-2-dihydroquinoline présentant une activité de liaison aux récepteurs glucocorticoïdes

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 (fr) * 2004-07-14 2006-02-23 Ligand Pharmaceuticals, Inc. Composés modulateurs de récepteurs intracellulaires et procédés de production et d'utilisation de ceux-ci
WO2007032556A1 (fr) * 2005-09-14 2007-03-22 Santen Pharmaceutical Co., Ltd. Nouveau dérivé de 1-2-dihydroquinoline présentant une activité de liaison aux récepteurs glucocorticoïdes

Cited By (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8420635B2 (en) 2005-09-14 2013-04-16 Santen Pharmaceutical Co., Ltd. Method for preventing or treating a glucocorticoid receptor-related disease
US8017775B2 (en) 2005-09-14 2011-09-13 Santen Pharmaceutical Co., Ltd. 1-2-dihydroquinoline derivative 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
US8975256B2 (en) 2006-03-14 2015-03-10 Santen Pharmaceutical Co., Ltd. 1,2,3,4-tetrahydroquinoxaline compounds having glucocorticoid receptor binding activity
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
EP2085387A4 (fr) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd Nouveau dérivé 1,2-dihydroquinoline comprenant un groupe alkyle inférieur phénylchalcogéno substitué et un groupe phényle introduit par un ester en tant que substituants
EP2085388A4 (fr) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd Nouveau dérivé 1,2-dihydroquinoline comprenant un groupe alkyle inférieur à substitution phénylamino et un groupe phényle dans lequel est introduit un ester en tant que substituants
EP2085389A4 (fr) * 2006-11-14 2010-12-15 Santen Pharmaceutical Co Ltd Nouveau dérivé de 1,2-dihydroquinoline comprenant en tant que substituants un groupe alkyle inférieur-carbonyloxy (à substitution phényle ou substitution hétérocyclique) et un groupe phényle lié par un ester
US8580784B2 (en) 2006-11-14 2013-11-12 Santen Pharmaceutical Co., Ltd. Method for treating a disease related to the glucocorticoid receptor
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
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
EP2085389A1 (fr) * 2006-11-14 2009-08-05 Santen Pharmaceutical Co., Ltd Nouveau dérivé de 1,2-dihydroquinoline comprenant en tant que substituants un groupe alkyle inférieur-carbonyloxy (à substitution phényle ou substitution hétérocyclique) et un groupe phényle lié par un ester
EP2085388A1 (fr) * 2006-11-14 2009-08-05 Santen Pharmaceutical Co., Ltd Nouveau dérivé 1,2-dihydroquinoline comprenant un groupe alkyle inférieur à substitution phénylamino et un groupe phényle dans lequel est introduit un ester en tant que substituants
EP2085387A1 (fr) * 2006-11-14 2009-08-05 Santen Pharmaceutical Co., Ltd Nouveau dérivé 1,2-dihydroquinoline comprenant un groupe alkyle inférieur phénylchalcogéno substitué et un groupe phényle introduit par un ester en tant que substituants
US8563551B2 (en) 2006-11-14 2013-10-22 Santen Pharmaceutical Co., Ltd. Method for preventing or treating a disease related to the glucocorticoid receptor
US8440660B2 (en) 2006-11-14 2013-05-14 Santen Pharmaceutical Co., Ltd. Method for treating a disease related to the glucocorticoid receptor
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
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
US8426406B2 (en) 2008-05-12 2013-04-23 Santen Pharmaceutical Co., Ltd. Glucocorticoid receptor agonist comprising 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivatives having substituted oxy group
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 (fr) * 2008-05-12 2009-11-19 参天製薬株式会社 Agoniste des récepteurs de glucocorticoïdes composé de dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine ayant un groupe oxy substitué
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WO2010029986A1 (fr) * 2008-09-12 2010-03-18 参天製薬株式会社 Agoniste de récepteur de glucocorticoïde comprenant un nouveau dérivé de 1,2,3,4-tétrahydroquinoxaline contenant un groupe phényle ayant une structure d’ester d’acide sulfonique introduite dans celui-ci en tant que substituant
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WO2013108921A1 (fr) * 2012-01-20 2013-07-25 参天製薬株式会社 Procédé industriel de préparation d'un dérivé de 1,2-dihydroquinoline ou d'un sel de celui-ci, et intermédiaire servant à sa préparation
CN104136432A (zh) * 2012-01-20 2014-11-05 参天制药株式会社 1,2-二氢喹啉衍生物或其盐的工业制备方法及其制备中间体
WO2018230713A1 (fr) 2017-06-16 2018-12-20 学校法人同志社 Composés ayant une activité inhibitrice de caspase, agent pharmaceutique les contenant pour le traitement ou la prévention des symptômes, troubles ou maladies de l'endothélium cornéen, et application dudit agent pharmaceutique
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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