DK3782996T3 - NRF2-regulatorer - Google Patents

NRF2-regulatorer Download PDF

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Publication number
DK3782996T3
DK3782996T3 DK20200207.7T DK20200207T DK3782996T3 DK 3782996 T3 DK3782996 T3 DK 3782996T3 DK 20200207 T DK20200207 T DK 20200207T DK 3782996 T3 DK3782996 T3 DK 3782996T3
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Prior art keywords
nrf2 regulators
nrf2
regulators
Prior art date
Application number
DK20200207.7T
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English (en)
Inventor
Jeffrey K Kerns
James Francis Callahan
Hongxing Yan
Thomas Daniel Heightman
Charlotte Mary Griffiths-Jones
Alison Jo-Anne Woolford
Tindy Li
Shah Ami Lakdawala
Roderick S Davis
David Norton
Nicole Cathleen Goodwin
Yun Jin
Paris L Hamilton
Jeffrey Charles Boehm
Original Assignee
Glaxosmithkline Ip Dev Ltd
Astex Therapeutics Ltd
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Application filed by Glaxosmithkline Ip Dev Ltd, Astex Therapeutics Ltd filed Critical Glaxosmithkline Ip Dev Ltd
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Publication of DK3782996T3 publication Critical patent/DK3782996T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18Benzotriazoles
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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 carbon chain containing aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D255/00Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/04Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/01Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having one nitrogen atom
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    • C07ORGANIC CHEMISTRY
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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
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    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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 carbon chain containing aromatic rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
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    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • C07D471/02Heterocyclic 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
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    • C07D498/04Ortho-condensed systems

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  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Detergent Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
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DK20200207.7T 2015-06-15 2016-06-15 NRF2-regulatorer DK3782996T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562175510P 2015-06-15 2015-06-15
EP16810994.0A EP3307739B1 (en) 2015-06-15 2016-06-15 Nrf2 regulators

Publications (1)

Publication Number Publication Date
DK3782996T3 true DK3782996T3 (da) 2024-04-22

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Family Applications (2)

Application Number Title Priority Date Filing Date
DK16810994.0T DK3307739T3 (da) 2015-06-15 2016-06-15 NRF2-regulatorer
DK20200207.7T DK3782996T3 (da) 2015-06-15 2016-06-15 NRF2-regulatorer

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US (3) US10604509B2 (da)
EP (2) EP3307739B1 (da)
JP (1) JP6789995B2 (da)
KR (1) KR102675041B1 (da)
CN (1) CN108112251B (da)
AU (1) AU2016279388B2 (da)
CA (1) CA2988338C (da)
CL (1) CL2017003226A1 (da)
CO (1) CO2017012995A2 (da)
CY (1) CY1123853T1 (da)
DK (2) DK3307739T3 (da)
DO (1) DOP2017000298A (da)
EA (1) EA035864B1 (da)
ES (2) ES2980945T3 (da)
FI (1) FI3782996T3 (da)
HR (2) HRP20240666T1 (da)
HU (2) HUE066668T2 (da)
IL (1) IL256297B (da)
LT (2) LT3782996T (da)
MA (1) MA52309B1 (da)
MX (1) MX375352B (da)
MY (1) MY207356A (da)
PE (1) PE20180799A1 (da)
PH (1) PH12017502255B1 (da)
PL (2) PL3782996T3 (da)
PT (2) PT3307739T (da)
RS (2) RS61302B1 (da)
SI (2) SI3307739T1 (da)
SM (1) SMT202400207T1 (da)
WO (1) WO2016202253A1 (da)
ZA (1) ZA201708145B (da)

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KR20180018684A (ko) 2015-06-15 2018-02-21 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 조절제
JP2018529744A (ja) * 2015-10-06 2018-10-11 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アリールシクロヘキシルピラゾール
EP3359532A1 (en) 2015-10-06 2018-08-15 GlaxoSmithKline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
WO2018109647A1 (en) 2016-12-14 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Bisaryl amides as nrf2 regulators
US20220002272A1 (en) * 2016-12-14 2022-01-06 Glaxosmithkline Intellectual Property Development Limited Bisaryl lactams as nrf2 activators
EP3555078B1 (en) 2016-12-14 2024-03-27 GlaxoSmithKline Intellectual Property Development Limited Bisaryl heterocycles as nrf2 activators
ES2908941T3 (es) 2016-12-15 2022-05-04 Glaxosmithkline Ip Dev Ltd Triazoles unidos a éter como reguladores de NRF2
US11028099B2 (en) * 2016-12-15 2021-06-08 Glaxosmithkline Intellectual Property Development Limited NRF2 activators
CN119264073A (zh) * 2017-05-17 2025-01-07 戴纳立制药公司 激酶抑制剂及其用途
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
JP7378156B2 (ja) * 2018-04-06 2023-11-13 ザ ボード オブ トラスティーズ オブ ザ ユニバーシティ オブ イリノイ Keap1/nrf2タンパク質間相互作用の1,4-置換イソキノリン阻害剤
AU2019326368B2 (en) 2018-08-20 2021-11-11 Janssen Pharmaceutica Nv Inhibitors of KEAP1-Nrf2 protein-protein interaction
MX2021006527A (es) 2018-12-05 2021-07-21 Scohia Pharma Inc Compuesto macrociclico y su uso.
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
JP7583718B2 (ja) 2019-07-03 2024-11-14 千寿製薬株式会社 Nrf2活性化化合物
CN110845435B (zh) * 2019-11-28 2021-06-08 中国药科大学 一种过氧化氢响应型Keap1-Nrf2 PPI抑制剂前药、制备方法及其医药用途
KR102590438B1 (ko) * 2020-10-16 2023-10-18 김홍렬 Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 예방 또는 소독용 조성물
KR102590444B1 (ko) * 2020-10-16 2023-10-18 김홍렬 Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 치료용 조성물
CN114539085B (zh) * 2020-11-26 2023-10-20 山东诚创蓝海医药科技有限公司 一种脲基衍生物的制备
US20240132519A1 (en) 2020-12-28 2024-04-25 Senju Pharmaceutical Co., Ltd. Nrf2-activating compound
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
EP4516792A4 (en) * 2022-04-28 2026-04-01 Kyoto Pharma Ind BENZOTHIOPHENE COMPOUND

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