TWI843806B - 作為nrf2活化劑之羥基吡啶并氧氮呯 - Google Patents

作為nrf2活化劑之羥基吡啶并氧氮呯 Download PDF

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Publication number
TWI843806B
TWI843806B TW109104455A TW109104455A TWI843806B TW I843806 B TWI843806 B TW I843806B TW 109104455 A TW109104455 A TW 109104455A TW 109104455 A TW109104455 A TW 109104455A TW I843806 B TWI843806 B TW I843806B
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compound
disease
methyl
pharmaceutically acceptable
hydrate
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TW109104455A
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Chinese (zh)
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TW202045514A (zh
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馬克 艾朋
麥卡 葛羅古斯基
麥可 寇汀
布萊恩 羅弘
杰 馬修
潔科林 帕特森
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英商葛蘭素史克智慧財產發展有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic 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 oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW109104455A 2019-02-15 2020-02-13 作為nrf2活化劑之羥基吡啶并氧氮呯 TWI843806B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962806201P 2019-02-15 2019-02-15
US62/806,201 2019-02-15
US201962931877P 2019-11-07 2019-11-07
US62/931,877 2019-11-07

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TW202045514A TW202045514A (zh) 2020-12-16
TWI843806B true TWI843806B (zh) 2024-06-01

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TW113112455A TWI880702B (zh) 2019-02-15 2020-02-13 作為nrf2活化劑之羥基吡啶并氧氮呯

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US (3) US11945826B2 (enExample)
EP (1) EP3924356A1 (enExample)
JP (1) JP7602469B2 (enExample)
KR (1) KR20210126676A (enExample)
CN (2) CN118206566A (enExample)
AU (1) AU2020222080C1 (enExample)
BR (1) BR112021016042A2 (enExample)
CA (1) CA3129955A1 (enExample)
CL (1) CL2021002110A1 (enExample)
CO (1) CO2021010930A2 (enExample)
IL (2) IL285438B2 (enExample)
MA (1) MA54939A (enExample)
MX (1) MX2021009659A (enExample)
MY (1) MY209603A (enExample)
PH (1) PH12021551873A1 (enExample)
SG (1) SG11202108257TA (enExample)
TW (2) TWI843806B (enExample)
WO (1) WO2020165776A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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TWI880702B (zh) * 2019-02-15 2025-04-11 英商葛蘭素史克智慧財產發展有限公司 作為nrf2活化劑之羥基吡啶并氧氮呯

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ES2974026T3 (es) 2018-08-20 2024-06-25 Janssen Pharmaceutica Nv Inhibidores de la interacción proteína-proteína entre KEAP1-Nrf2
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
MX2021014680A (es) * 2019-05-31 2022-04-06 Ube Corp Derivado de benzotriazol.
PE20241779A1 (es) 2022-01-07 2024-09-03 Chugai Pharmaceutical Co Ltd Compuesto heterociclico que contiene nitrogeno que tiene un efecto de activacion del nrf2
EP4516792A1 (en) * 2022-04-28 2025-03-05 Kyoto Pharmaceutical Industries, Ltd. Benzothiophene compound
WO2023210741A1 (ja) 2022-04-28 2023-11-02 第一三共株式会社 ベンゾトリアゾール化合物
EP4580612A1 (en) * 2022-09-02 2025-07-09 Institut National de la Santé et de la Recherche Médicale Use of nrf2 activators for the treatment of cerebral small vessel disease
CN121152792A (zh) * 2023-06-19 2025-12-16 中外制药株式会社 具有Nrf2活化作用的含氮杂环化合物的晶体

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WO2016202253A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2018109646A1 (en) * 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 compounds

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AU2016280235A1 (en) * 2015-06-15 2017-12-14 Astex Therapeutics Limited Nrf2 regulators
KR20180018684A (ko) 2015-06-15 2018-02-21 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 조절제
CA2995325A1 (en) * 2015-08-12 2017-02-16 Mochida Pharmaceutical Co., Ltd. Isothiazole derivative
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EP3551621A1 (en) * 2016-12-12 2019-10-16 GlaxoSmithKline Intellectual Property Development Limited N-aryl pyrazoles as nrf2 regulators
US11078216B2 (en) * 2016-12-14 2021-08-03 Glaxosmithkline Intellectual Property Development Limited Bisaryl amides as NRF2 activators
MY209603A (en) * 2019-02-15 2025-07-24 Glaxosmithkline Ip Dev Ltd Hydroxypyridoxazepines as nrf2 activators

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WO2016202253A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2018109646A1 (en) * 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 compounds

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI880702B (zh) * 2019-02-15 2025-04-11 英商葛蘭素史克智慧財產發展有限公司 作為nrf2活化劑之羥基吡啶并氧氮呯

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US20250313573A1 (en) 2025-10-09
PH12021551873A1 (en) 2022-05-23
WO2020165776A1 (en) 2020-08-20
CL2021002110A1 (es) 2022-02-11
TWI880702B (zh) 2025-04-11
EP3924356A1 (en) 2021-12-22
MY209603A (en) 2025-07-24
JP7602469B2 (ja) 2024-12-18
IL313950A (en) 2024-08-01
US11945826B2 (en) 2024-04-02
CN118206566A (zh) 2024-06-18
CO2021010930A2 (es) 2021-09-09
TW202440593A (zh) 2024-10-16
US20220204526A1 (en) 2022-06-30
JP2022520442A (ja) 2022-03-30
CA3129955A1 (en) 2020-08-20
IL285438B2 (en) 2024-12-01
MX2021009659A (es) 2021-09-08
CN113474349B (zh) 2024-03-01
MA54939A (fr) 2021-12-22
US20240352034A1 (en) 2024-10-24
TW202045514A (zh) 2020-12-16
KR20210126676A (ko) 2021-10-20
AU2020222080B2 (en) 2022-05-19
AU2020222080A1 (en) 2021-09-02
BR112021016042A2 (pt) 2021-10-05
CN113474349A (zh) 2021-10-01
IL285438A (en) 2021-09-30
IL285438B1 (en) 2024-08-01
AU2020222080C1 (en) 2022-09-29
SG11202108257TA (en) 2021-08-30

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