EA030431B1 - РЕГУЛЯТОРЫ Nrf2 - Google Patents
РЕГУЛЯТОРЫ Nrf2 Download PDFInfo
- Publication number
- EA030431B1 EA030431B1 EA201691259A EA201691259A EA030431B1 EA 030431 B1 EA030431 B1 EA 030431B1 EA 201691259 A EA201691259 A EA 201691259A EA 201691259 A EA201691259 A EA 201691259A EA 030431 B1 EA030431 B1 EA 030431B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- methyl
- benzo
- dioxido
- phenyl
- dihydro
- Prior art date
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Classifications
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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
- C07D417/02—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
- C07D417/10—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 carbon chain containing aromatic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
- C07D249/18—Benzotriazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D281/02—Seven-membered rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
- C07D291/08—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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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
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D419/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D515/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361917466P | 2013-12-18 | 2013-12-18 | |
| US201461980091P | 2014-04-16 | 2014-04-16 | |
| PCT/IB2014/067027 WO2015092713A1 (en) | 2013-12-18 | 2014-12-17 | Nrf2 regulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201691259A1 EA201691259A1 (ru) | 2016-11-30 |
| EA030431B1 true EA030431B1 (ru) | 2018-08-31 |
Family
ID=52355021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201691259A EA030431B1 (ru) | 2013-12-18 | 2014-12-17 | РЕГУЛЯТОРЫ Nrf2 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US10144731B2 (enExample) |
| EP (1) | EP3083614B1 (enExample) |
| JP (1) | JP6630671B2 (enExample) |
| KR (1) | KR102301867B1 (enExample) |
| CN (1) | CN105829305B (enExample) |
| AU (2) | AU2014369153B2 (enExample) |
| BR (1) | BR112016014180A2 (enExample) |
| CA (1) | CA2934216C (enExample) |
| CL (1) | CL2016001516A1 (enExample) |
| CR (1) | CR20160272A (enExample) |
| DO (1) | DOP2016000145A (enExample) |
| EA (1) | EA030431B1 (enExample) |
| ES (1) | ES2784244T3 (enExample) |
| IL (1) | IL245727B (enExample) |
| MX (1) | MX370410B (enExample) |
| PE (1) | PE20160901A1 (enExample) |
| PH (1) | PH12016501151A1 (enExample) |
| SG (1) | SG11201604611SA (enExample) |
| WO (1) | WO2015092713A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12559504B2 (en) | 2019-05-31 | 2026-02-24 | Ube Corporation | Benzotriazole derivative |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108137557B (zh) | 2015-06-15 | 2021-09-07 | 葛兰素史密斯克莱知识产权发展有限公司 | Nrf2调节剂 |
| CA2988338C (en) | 2015-06-15 | 2024-05-14 | Glaxosmithkline Intellectual Property Development Limited | Nrf2 regulators |
| JP2018517732A (ja) * | 2015-06-15 | 2018-07-05 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | Nrf2レギュレーター |
| WO2017060854A1 (en) | 2015-10-06 | 2017-04-13 | Glaxosmithkline Intellectual Property Development Limited | Biaryl pyrazoles as nrf2 regulators |
| WO2017060855A1 (en) * | 2015-10-06 | 2017-04-13 | Glaxosmithkline Intellectual Property Development Limited | Arylcyclohexyl pyrazoles as nrf2 regulators |
| CN105566241B (zh) * | 2016-01-18 | 2018-05-25 | 中国药科大学 | 1-磺酰胺基-4-芳氧基类化合物、制备方法及其医药用途 |
| HUE052269T2 (hu) | 2016-02-03 | 2021-04-28 | Rigel Pharmaceuticals Inc | NRF2-t aktiváló vegyületek és alkalmazásuk |
| WO2018104766A1 (en) * | 2016-12-06 | 2018-06-14 | Glaxosmithkline Intellectual Property Development Limited | 3-(2,3-dihydro-1h-inden-5-yl)propanoic acid derivatives and their use as nrf2 regulators |
| WO2018109641A1 (en) * | 2016-12-12 | 2018-06-21 | Glaxosmithkline Intellectual Property Development Limited | 3-carboxylic acid pyrroles as nrf2 regulators |
| WO2018109642A1 (en) * | 2016-12-12 | 2018-06-21 | Glaxosmithkline Intellectual Property Development Limited | N-aryl pyrazoles as nrf2 regulators |
| ES2901617T3 (es) | 2016-12-14 | 2022-03-23 | Glaxosmithkline Ip Dev Ltd | Bisarilamidas como reguladores de NRF2 |
| US11117905B2 (en) * | 2016-12-14 | 2021-09-14 | Glaxosmithkline Intellectual Property Development Limited | Bisaryl heterocycles as NRF2 activators |
| JP2020502129A (ja) * | 2016-12-14 | 2020-01-23 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | Nrf2アクチベーターとしての3−オキソ−1,4−ジアゼピニル化合物 |
| US11059816B2 (en) | 2016-12-15 | 2021-07-13 | Glaxosmithkline Intellectual Property Development Limited | Ether linked triazoles as NRF2 activators |
| AU2017376900A1 (en) * | 2016-12-15 | 2019-05-23 | Glaxosmithkline Intellectual Property Development Limited | NRF2 compounds |
| WO2018145109A1 (en) | 2017-02-06 | 2018-08-09 | Massachusetts Institute Of Technology | Methods and products related to glutaminase inhibitors |
| JP2020097526A (ja) * | 2017-03-28 | 2020-06-25 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2019116231A1 (en) | 2017-12-11 | 2019-06-20 | Glaxosmithkline Intellectual Property Development Limited | Nrf2 activator for the treatment of acute lung injury, acute respiratory distress syndrome and multiple organ dysfunction syndrome |
| US20210177861A1 (en) * | 2017-12-11 | 2021-06-17 | Glaxosmithkline Intellectual Property Development Limited | Nrf2 activator for the treatment of acute lung injury, acute respiratory distress syndrome and multiple organ dysfunction syndrome |
| US11643407B2 (en) | 2018-05-23 | 2023-05-09 | Glaxosmithkline Intellectual Property Development Limited | Indanes as NRF2 activators |
| AU2019307631A1 (en) | 2018-07-20 | 2020-12-17 | Dana-Farber Cancer Institute, Inc. | Degraders that target proteins via KEAP1 |
| MX2021002060A (es) * | 2018-08-20 | 2021-07-21 | Janssen Pharmaceutica Nv | Inhibidores de la interacción proteína-proteína keap1-nrf2. |
| CA3121952C (en) * | 2018-12-05 | 2025-05-13 | Scohia Pharma, Inc. | MACROCYCLICAL COMPOUND AND ITS USES |
| CN113474349B (zh) | 2019-02-15 | 2024-03-01 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为nrf2活化剂的羟基吡啶并氧氮杂环庚三烯 |
| EP3953337A4 (en) * | 2019-04-08 | 2023-08-09 | Dana-Farber Cancer Institute, Inc. | Degraders of kelch-like ech-associated protein 1 (keap1) |
| EP3998262A4 (en) * | 2019-07-03 | 2023-07-26 | Senju Pharmaceutical Co., Ltd. | NRF2 ACTIVATING COMPOUND |
| EP4110776A1 (en) * | 2020-02-28 | 2023-01-04 | Les Laboratoires Servier | New macrocyclic compounds, a process for their preparation and pharmaceutical compositions containing them |
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