WO2009035067A1 - Glucocorticoid receptor agonists consisting of 1,3,3-tri- methyl-7-phenyl-3,4-dihydro-1h-quinoxalin-2-one derivatives - Google Patents
Glucocorticoid receptor agonists consisting of 1,3,3-tri- methyl-7-phenyl-3,4-dihydro-1h-quinoxalin-2-one derivatives Download PDFInfo
- Publication number
- 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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- WIPO (PCT)
- Prior art keywords
- quinoxalin
- dihydro
- phenyl
- glucocorticoid receptor
- tri
- Prior art date
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- Ceased
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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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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- 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
- A61P19/00—Drugs for skeletal disorders
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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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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- 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
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- 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
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Orthopedic Medicine & Surgery (AREA)
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- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
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- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Transplantation (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
The invention provides a glucocorticoid receptor agonist consisting of a 1,3,3-trimethyl-7-phenyl-3,4-dihydro-1H -quinoxalin-2-one derivative represented by the general formula (1) or a salt thereof and novel pharmacological effects of the agonist: [Chemical formula 1] (1) (2a) (4a) (3a) (5a) wherein R1 is a group represented by the general formula (2a), (3a), (4a) or (5a); R2 and R3 may be the same or different from each other and are each hydrogen, halogeno, lower alkyl, hydroxy, esterified hydroxy, or the like; R4 is lower alkyl; R5, R6, R7 and R8 are each halogeno, lower alkyl, hydroxy, lower alkoxy, or the like; and m, n, p and q are each 0, 1 or 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2007-237877 | 2007-09-13 | ||
| JP2007237877 | 2007-09-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2009035067A1 true WO2009035067A1 (en) | 2009-03-19 |
Family
ID=40452073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/JP2008/066512 Ceased WO2009035067A1 (en) | 2007-09-13 | 2008-09-12 | Glucocorticoid receptor agonists consisting of 1,3,3-tri- methyl-7-phenyl-3,4-dihydro-1h-quinoxalin-2-one derivatives |
Country Status (2)
| Country | Link |
|---|---|
| JP (1) | JP2009084273A (en) |
| WO (1) | WO2009035067A1 (en) |
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010029986A1 (en) * | 2008-09-12 | 2010-03-18 | 参天製薬株式会社 | Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group having sulfonic acid ester structure introduced therein as substituent |
| 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 (en) * | 2015-08-25 | 2018-04-17 | 参天制药株式会社 | [4 (1,3,3 trimethyl, 2 oxo, 3,4 dihydro 1H quinoxalines, 7 base) phenoxy group] ethyl oxo-compound or its salt |
| WO2018230713A1 (en) | 2017-06-16 | 2018-12-20 | 学校法人同志社 | Compounds having caspase inhibitory activity, pharmaceutical agent containing said compounds and for treating or preventing corneal endothelial symptoms, disorders, or diseases, and application of said pharmaceutical agent |
| 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 |
| WO2020016452A1 (en) | 2018-07-20 | 2020-01-23 | Grünenthal GmbH | Further 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)
| 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 (en) * | 2005-09-14 | 2007-03-22 | Santen Pharmaceutical Co., Ltd. | Novel 1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity |
| WO2007105766A1 (en) * | 2006-03-14 | 2007-09-20 | Santen Pharmaceutical Co., Ltd. | Novel 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity |
-
2008
- 2008-09-12 JP JP2008234098A patent/JP2009084273A/en not_active Withdrawn
- 2008-09-12 WO PCT/JP2008/066512 patent/WO2009035067A1/en not_active Ceased
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 (en) * | 2005-09-14 | 2007-03-22 | Santen Pharmaceutical Co., Ltd. | Novel 1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity |
| WO2007105766A1 (en) * | 2006-03-14 | 2007-09-20 | Santen Pharmaceutical Co., Ltd. | Novel 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity |
Cited By (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| WO2010029986A1 (en) * | 2008-09-12 | 2010-03-18 | 参天製薬株式会社 | Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group having sulfonic acid ester structure introduced therein as substituent |
| EA018420B1 (en) * | 2008-09-12 | 2013-07-30 | Сантен Фармасьютикал Ко., Лтд. | Glucocorticoid receptor agonist comprising novel 1,2,3,4-tetrahydroquinoxaline derivatives containing phenyl group having sulfonic acid ester structure introduced therein as substituent |
| 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 |
| CN107922356A (en) * | 2015-08-25 | 2018-04-17 | 参天制药株式会社 | [4 (1,3,3 trimethyl, 2 oxo, 3,4 dihydro 1H quinoxalines, 7 base) phenoxy group] ethyl oxo-compound or its salt |
| 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 |
| WO2018230713A1 (en) | 2017-06-16 | 2018-12-20 | 学校法人同志社 | Compounds having caspase inhibitory activity, pharmaceutical agent containing said compounds and for treating or preventing corneal endothelial symptoms, disorders, or diseases, and application of said pharmaceutical agent |
| 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 |
| 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 |
| US10626106B2 (en) | 2017-12-18 | 2020-04-21 | Gruenenthal Gmbh | Substituted pyrrolidine amides I |
| WO2020016453A1 (en) | 2018-07-20 | 2020-01-23 | Grünenthal GmbH | Substituted triazolo quinoxaline derivatives |
| WO2020016452A1 (en) | 2018-07-20 | 2020-01-23 | Grünenthal GmbH | Further substituted triazolo quinoxaline derivatives |
| US12110293B2 (en) | 2018-07-20 | 2024-10-08 | Grünenthal GmbH | Substituted triazolo quinoxaline derivatives |
| CN112673009A (en) * | 2018-07-20 | 2021-04-16 | 格吕伦塔尔有限公司 | Substituted triazoloquinoxaline derivatives |
| US10981918B2 (en) | 2018-07-20 | 2021-04-20 | Grünenthal GmbH | Further substituted triazolo quinoxaline derivatives |
| US11981677B2 (en) | 2018-07-20 | 2024-05-14 | Grünenthal GmbH | Further substituted triazolo quinoxaline derivatives |
| CN112673009B (en) * | 2018-07-20 | 2023-09-19 | 格吕伦塔尔有限公司 | Substituted triazoloquinoxaline derivatives |
| WO2020144375A1 (en) | 2019-01-11 | 2020-07-16 | Grünenthal GmbH | Substituted pyrrolidine amides iii |
| US12358907B2 (en) | 2019-01-11 | 2025-07-15 | Grünenthal GmbH | Substituted pyrrolidine amides III |
| WO2020254551A1 (en) | 2019-06-19 | 2020-12-24 | Grünenthal GmbH | Substituted pyrrolidine amides iv |
| US12331034B2 (en) | 2019-06-19 | 2025-06-17 | Gruenenthal Gmbh | Substituted pyrrolidine amides V |
| WO2020254552A2 (en) | 2019-06-19 | 2020-12-24 | Grünenthal GmbH | Substituted pyrrolidine amides v |
| WO2021144439A1 (en) | 2020-01-17 | 2021-07-22 | Grünenthal GmbH | Quinoxaline derivatives |
| WO2021144440A1 (en) | 2020-01-17 | 2021-07-22 | Grünenthal GmbH | Quinoxaline derivatives as modulators of the glucocorticoid receptor |
| WO2022008705A1 (en) | 2020-07-09 | 2022-01-13 | Grünenthal GmbH | Substituted pyrrolidine amines and amides as mediator of the glucocortoid receptor |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2009084273A (en) | 2009-04-23 |
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