AU2020222080C1 - Hydroxypyridoxazepines as Nrf2 activators - Google Patents

Hydroxypyridoxazepines as Nrf2 activators Download PDF

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Publication number
AU2020222080C1
AU2020222080C1 AU2020222080A AU2020222080A AU2020222080C1 AU 2020222080 C1 AU2020222080 C1 AU 2020222080C1 AU 2020222080 A AU2020222080 A AU 2020222080A AU 2020222080 A AU2020222080 A AU 2020222080A AU 2020222080 C1 AU2020222080 C1 AU 2020222080C1
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compound
disease
tautomer
methyl
salt
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AU2020222080A
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AU2020222080B2 (en
AU2020222080A1 (en
Inventor
Mark ELBAN
Michal Pawel GLOGOWSKI
Michael Clinton KOETTING
Brian Griffin Lawhorn
Jay M. Matthews
Jaclyn Renee PATTERSON
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2020222080A 2019-02-15 2020-02-11 Hydroxypyridoxazepines as Nrf2 activators Active AU2020222080C1 (en)

Applications Claiming Priority (5)

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
PCT/IB2020/051100 WO2020165776A1 (en) 2019-02-15 2020-02-11 Hydroxypyridoxazepines as nrf2 activators

Publications (3)

Publication Number Publication Date
AU2020222080A1 AU2020222080A1 (en) 2021-09-02
AU2020222080B2 AU2020222080B2 (en) 2022-05-19
AU2020222080C1 true AU2020222080C1 (en) 2022-09-29

Family

ID=69726636

Family Applications (1)

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AU2020222080A Active AU2020222080C1 (en) 2019-02-15 2020-02-11 Hydroxypyridoxazepines as Nrf2 activators

Country Status (18)

Country Link
US (3) US11945826B2 (https=)
EP (1) EP3924356A1 (https=)
JP (1) JP7602469B2 (https=)
KR (1) KR102932313B1 (https=)
CN (2) CN113474349B (https=)
AU (1) AU2020222080C1 (https=)
BR (1) BR112021016042A2 (https=)
CA (1) CA3129955A1 (https=)
CL (1) CL2021002110A1 (https=)
CO (1) CO2021010930A2 (https=)
IL (2) IL313950A (https=)
MA (1) MA54939A (https=)
MX (1) MX2021009659A (https=)
MY (1) MY209603A (https=)
PH (1) PH12021551873A1 (https=)
SG (1) SG11202108257TA (https=)
TW (2) TWI843806B (https=)
WO (1) WO2020165776A1 (https=)

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EP3833662B1 (en) 2018-08-20 2024-01-17 Janssen Pharmaceutica NV Inhibitors of keap1-nrf2 protein-protein interaction
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
KR102932313B1 (ko) * 2019-02-15 2026-02-26 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 활성화제로서 히드록시피리드옥사제핀
AU2020283361B2 (en) * 2019-05-31 2025-11-27 Ube Corporation Benzotriazole derivative
CN118488944A (zh) 2022-01-07 2024-08-13 中外制药株式会社 具有Nrf2活化作用的含氮杂环化合物
US20250282724A1 (en) 2022-04-28 2025-09-11 Daiichi Sankyo Company, Limited Benzotriazole compound
JPWO2023210740A1 (https=) 2022-04-28 2023-11-02
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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WO2015092713A1 (en) * 2013-12-18 2015-06-25 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2016202253A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2016203400A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2016203401A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
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
WO2018109646A1 (en) * 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 compounds

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US9056850B2 (en) * 2008-10-17 2015-06-16 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of SGLT
CN104418834B (zh) * 2013-08-23 2017-09-15 重庆博腾制药科技股份有限公司 一种抗糖尿病药物中间体的合成方法
CN105272960A (zh) * 2014-07-18 2016-01-27 上海科胜药物研发有限公司 一种坎格列净中间体2-(2-甲基-5-溴苄基)-5-(4-氟苯)噻吩的制备方法
WO2016178148A1 (en) * 2015-05-05 2016-11-10 Glenmark Pharmaceuticals Limited Process for preparation of dapagliflozin
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
US10913762B2 (en) * 2016-01-27 2021-02-09 Msn Laboratories Private Limited Process for the preparation of D-glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl] oxy]phenyl] methyl] phenyl]-, (1S) and its crystalline forms thereof
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
ES2901617T3 (es) * 2016-12-14 2022-03-23 Glaxosmithkline Ip Dev Ltd Bisarilamidas como reguladores de NRF2
KR102932313B1 (ko) * 2019-02-15 2026-02-26 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 활성화제로서 히드록시피리드옥사제핀

Patent Citations (6)

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WO2015092713A1 (en) * 2013-12-18 2015-06-25 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2016202253A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2016203400A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2016203401A1 (en) * 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
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
WO2018109646A1 (en) * 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 compounds

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Publication number Publication date
KR102932313B1 (ko) 2026-02-26
CL2021002110A1 (es) 2022-02-11
MY209603A (en) 2025-07-24
MA54939A (fr) 2021-12-22
CA3129955A1 (en) 2020-08-20
TWI843806B (zh) 2024-06-01
CO2021010930A2 (es) 2021-09-09
TW202045514A (zh) 2020-12-16
US20250313573A1 (en) 2025-10-09
CN113474349A (zh) 2021-10-01
JP2022520442A (ja) 2022-03-30
WO2020165776A1 (en) 2020-08-20
MX2021009659A (es) 2021-09-08
CN118206566A (zh) 2024-06-18
TWI880702B (zh) 2025-04-11
CN113474349B (zh) 2024-03-01
US20240352034A1 (en) 2024-10-24
US11945826B2 (en) 2024-04-02
IL313950A (en) 2024-08-01
IL285438B2 (en) 2024-12-01
US20220204526A1 (en) 2022-06-30
AU2020222080B2 (en) 2022-05-19
TW202440593A (zh) 2024-10-16
IL285438B1 (en) 2024-08-01
PH12021551873A1 (en) 2022-05-23
BR112021016042A2 (pt) 2021-10-05
EP3924356A1 (en) 2021-12-22
JP7602469B2 (ja) 2024-12-18
KR20210126676A (ko) 2021-10-20
SG11202108257TA (en) 2021-08-30
IL285438A (en) 2021-09-30
AU2020222080A1 (en) 2021-09-02

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