TWI880702B - 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
TWI880702B
TWI880702B TW113112455A TW113112455A TWI880702B TW I880702 B TWI880702 B TW I880702B TW 113112455 A TW113112455 A TW 113112455A TW 113112455 A TW113112455 A TW 113112455A TW I880702 B TWI880702 B TW I880702B
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Taiwan
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methyl
compound
dimethyl
benzo
triazol
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TW113112455A
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Chinese (zh)
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TW202440593A (zh
Inventor
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61K31/553—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 oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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]
    • 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
    • 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
    • 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
    • A61P9/10—Drugs 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
TW113112455A 2019-02-15 2020-02-13 作為nrf2活化劑之羥基吡啶并氧氮呯 TWI880702B (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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TW202440593A TW202440593A (zh) 2024-10-16
TWI880702B true TWI880702B (zh) 2025-04-11

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TW109104455A TWI843806B (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)
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Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
PT3833662T (pt) 2018-08-20 2024-03-18 Janssen Pharmaceutica Nv Inibidores da interação proteína-proteína keap1-nrf2
PH12021551873A1 (en) * 2019-02-15 2022-05-23 Glaxosmithkline Ip Dev Ltd Hydroxypyridoxazepines as nrf2 activators
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
JP7524899B2 (ja) * 2019-05-31 2024-07-30 Ｕｂｅ株式会社 ベンゾトリアゾール誘導体
KR20240133727A (ko) 2022-01-07 2024-09-04 추가이 세이야쿠 가부시키가이샤 Nrf2 활성화 작용을 갖는 함질소 헤테로환 화합물
TW202404984A (zh) * 2022-04-28 2024-02-01 日商第一三共股份有限公司 苯并三唑化合物
TW202345792A (zh) 2022-04-28 2023-12-01 日商第一三共股份有限公司 苯并噻吩化合物
WO2024047248A1 (en) * 2022-09-02 2024-03-07 Institut National de la Santé et de la Recherche Médicale Use of nrf2 activators for the treatment of cerebral small vessel disease
AU2024314540A1 (en) 2023-06-19 2025-11-27 Chugai Seiyaku Kabushiki Kaisha Crystal of nitrogen-containing heterocyclic compound having nrf2 activation effect

Citations (3)

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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
TWI843806B (zh) * 2019-02-15 2024-06-01 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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EP2094651A1 (en) * 2006-11-17 2009-09-02 Trustees Of Dartmouth College Synthesis and biological activities of new tricyclic-bis-enones (tbes)
AU2014369153B2 (en) * 2013-12-18 2017-09-21 Astex Therapeutics Limited Nrf2 regulators
EP3307729B1 (en) 2015-06-15 2020-09-02 GlaxoSmithKline Intellectual Property Development Limited Nrf2 regulators
RU2018101077A (ru) 2015-06-15 2019-07-15 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Регуляторы nrf2
US10201531B2 (en) * 2015-08-12 2019-02-12 Mochida Pharmaceutical Co., Ltd. Indazolyl-oxo-isothiazole compounds
US10364256B2 (en) * 2015-10-06 2019-07-30 Glaxosmithkline Intellectual Property Development Limited Biaryl pyrazoles as NRF2 regulators
KR20190088404A (ko) * 2016-12-06 2019-07-26 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 3-(2,3-디히드로-1h-인덴-5-일)프로판산 유도체 및 nrf2 조절제로서의 그의 용도
JP2020500918A (ja) * 2016-12-12 2020-01-16 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レギュレーターとしてのｎ−アリールピラゾール
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WO2018109646A1 (en) * 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 compounds
TWI843806B (zh) * 2019-02-15 2024-06-01 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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IL285438B1 (en) 2024-08-01
AU2020222080B2 (en) 2022-05-19
SG11202108257TA (en) 2021-08-30
TWI843806B (zh) 2024-06-01
CN113474349A (zh) 2021-10-01
MY209603A (en) 2025-07-24
JP7602469B2 (ja) 2024-12-18
CO2021010930A2 (es) 2021-09-09
CN113474349B (zh) 2024-03-01
IL285438A (en) 2021-09-30
IL285438B2 (en) 2024-12-01
JP2022520442A (ja) 2022-03-30
TW202440593A (zh) 2024-10-16
PH12021551873A1 (en) 2022-05-23
AU2020222080C1 (en) 2022-09-29
US20220204526A1 (en) 2022-06-30
CN118206566A (zh) 2024-06-18
CL2021002110A1 (es) 2022-02-11
WO2020165776A1 (en) 2020-08-20
US20250313573A1 (en) 2025-10-09
TW202045514A (zh) 2020-12-16
US11945826B2 (en) 2024-04-02
MX2021009659A (es) 2021-09-08
KR20210126676A (ko) 2021-10-20
MA54939A (fr) 2021-12-22
US20240352034A1 (en) 2024-10-24
IL313950A (en) 2024-08-01
BR112021016042A2 (pt) 2021-10-05
AU2020222080A1 (en) 2021-09-02
CA3129955A1 (en) 2020-08-20
EP3924356A1 (en) 2021-12-22

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