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PE20180799A1 - Reguladores de nrf2 - Google Patents

Reguladores de nrf2

Info

Publication number
PE20180799A1
PE20180799A1 PE2017002744A PE2017002744A PE20180799A1 PE 20180799 A1 PE20180799 A1 PE 20180799A1 PE 2017002744 A PE2017002744 A PE 2017002744A PE 2017002744 A PE2017002744 A PE 2017002744A PE 20180799 A1 PE20180799 A1 PE 20180799A1
Authority
PE
Peru
Prior art keywords
alkyl
nrf2
halo
phenyl
compound
Prior art date
Application number
PE2017002744A
Other languages
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
Jeffrey Charles Boehm
Paris L Hamilton
Original Assignee
Glaxosmithkline Ip Dev Ltd
Astex Therapeutics Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Ip Dev Ltd, Astex Therapeutics Ltd filed Critical Glaxosmithkline Ip Dev Ltd
Publication of PE20180799A1 publication Critical patent/PE20180799A1/es

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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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/56—Heterocyclic 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
    • C07D233/60—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/64—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/01—Heterocyclic 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
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D405/10—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 carbon chain containing aromatic rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Neurology (AREA)
  • Biomedical Technology (AREA)
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  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (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)
  • Paper (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Referido a un compuesto de Formula (I), en donde B es benzotriazolilo, fenilo, triazolopiridinilo, -(CH2)2-O-(CH2)2-OR4, entre otros; D es -C(O)OH, -C(O)NHSO2CH3, entre otros; R1 es independientemente H, alquilo C1-C3, F, entre otros; R2 es H, metilo, CF3, o halo; R4 es hidrogeno o -alquilo C1-C3; el conector es -CH2-, -CH2-N(-ciclopropil)-CH2-, entre otros; A es tetrahidrobenzoxazepinilo, piperidinilo, fenilo, entre otros; todos los cuales pueden estar no sustituidos o sustituidos con 1, 2, o 3 sustituyentes seleccionados independientemente entre -alquilo C1-C3, espirocicloalquilo C3-C6, halo, CN, entre otros. X es independientemente CH o N; o una de sus sales farmaceuticamente aceptables. Estos compuestos son analogos arilicos, reguladores del Factor 2 relacionado con NF-E2 (NRF2). Tambien se refiere a la preparacion de un compuesto, el que se utiliza para el tratamiento y/o la prevencion de afecciones asociadas con el desequilibrio de NRF2, como trastornos respiratorios y no respiratorios, que incluyen Enfermedad pulmonar obstructiva cronica (EPOC), asma, fibrosis, infeccion pulmonar, entre otros.
PE2017002744A 2015-06-15 2016-06-15 Reguladores de nrf2 PE20180799A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562175510P 2015-06-15 2015-06-15

Publications (1)

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PE20180799A1 true PE20180799A1 (es) 2018-05-09

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PE2017002744A PE20180799A1 (es) 2015-06-15 2016-06-15 Reguladores de nrf2

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US (3) US10604509B2 (es)
EP (2) EP3307739B1 (es)
JP (1) JP6789995B2 (es)
KR (1) KR102675041B1 (es)
CN (1) CN108112251B (es)
AU (1) AU2016279388B2 (es)
CA (1) CA2988338C (es)
CL (1) CL2017003226A1 (es)
CO (1) CO2017012995A2 (es)
CY (1) CY1123853T1 (es)
DK (2) DK3782996T3 (es)
DO (1) DOP2017000298A (es)
EA (1) EA035864B1 (es)
ES (2) ES2841574T3 (es)
FI (1) FI3782996T3 (es)
HR (2) HRP20240666T1 (es)
HU (2) HUE052919T2 (es)
IL (1) IL256297B (es)
LT (2) LT3782996T (es)
MA (1) MA52309B1 (es)
MX (1) MX375352B (es)
MY (1) MY207356A (es)
PE (1) PE20180799A1 (es)
PH (1) PH12017502255B1 (es)
PL (2) PL3307739T3 (es)
PT (2) PT3307739T (es)
RS (2) RS61302B1 (es)
SI (2) SI3307739T1 (es)
SM (1) SMT202400207T1 (es)
WO (1) WO2016202253A1 (es)
ZA (1) ZA201708145B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016280236B2 (en) 2015-06-15 2019-02-07 Astex Therapeutics Limited Nrf2 regulators
US10351530B2 (en) * 2015-10-06 2019-07-16 Glaxosmithkline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as NRF2 regulators
EP3359532A1 (en) 2015-10-06 2018-08-15 GlaxoSmithKline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
JP2020502123A (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ビスアリール複素環
JP2020502136A (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レギュレーターとしてのビスアリールアミド
US20220002272A1 (en) * 2016-12-14 2022-01-06 Glaxosmithkline Intellectual Property Development Limited Bisaryl lactams as nrf2 activators
US11059816B2 (en) 2016-12-15 2021-07-13 Glaxosmithkline Intellectual Property Development Limited Ether linked triazoles as NRF2 activators
KR20190091455A (ko) * 2016-12-15 2019-08-06 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 화합물
TWI794232B (zh) * 2017-05-17 2023-03-01 美商戴納立製藥公司 激酶抑制劑及其用途
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
WO2019195348A1 (en) * 2018-04-06 2019-10-10 The Board Of Trustees Of The University Of Illinois 1,4-substituted isoquinoline inhibitors of keap1/nrf2 protein-protein interaction
KR102590310B1 (ko) 2018-08-20 2023-10-17 얀센 파마슈티카 엔브이 KEAP1-Nrf2 단백질간 상호작용 억제제
MX2021006527A (es) 2018-12-05 2021-07-21 Scohia Pharma Inc Compuesto macrociclico y su uso.
BR112021016042A2 (pt) * 2019-02-15 2021-10-05 Glaxosmithkline Intellectual Property Development Limited Hidroxipiridoxazepinas como ativadores de nrf2
ES3047102T3 (en) * 2019-05-31 2025-12-03 Ube Corp 1h-benzo[d][1,2,3]triazole derivatives as keap1 inhibitors for the treatment of renal diseases
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
KR102590444B1 (ko) * 2020-10-16 2023-10-18 김홍렬 Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 치료용 조성물
KR102590438B1 (ko) * 2020-10-16 2023-10-18 김홍렬 Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 예방 또는 소독용 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
CA3206893A1 (en) 2020-12-28 2022-07-07 Senju Pharmaceutical Co., Ltd. Nrf2-activating compound
JPWO2023210740A1 (es) 2022-04-28 2023-11-02
AU2023259936A1 (en) 2022-04-28 2024-11-28 Daiichi Sankyo Company, Limited Benzotriazole compound

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CY1308A (en) 1979-12-06 1985-12-06 Glaxo Group Ltd Device for dispensing medicaments
EP0069715B1 (en) 1981-07-08 1986-11-05 Aktiebolaget Draco Powder inhalator
GB2169265B (en) 1982-10-08 1987-08-12 Glaxo Group Ltd Pack for medicament
IE56059B1 (en) 1982-10-08 1991-04-10 Glaxo Group Ltd Devices for administering medicaments to patients
US4778054A (en) 1982-10-08 1988-10-18 Glaxo Group Limited Pack for administering medicaments to patients
BE905189A (fr) 1985-07-30 1987-01-29 Glaxo Group Ltd Dispositif pour administrer des medicaments a des patients.
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
HU213221B (en) 1990-03-02 1997-03-28 Glaxo Group Ltd Inhalation device and medicine packet for device
US6536427B2 (en) 1990-03-02 2003-03-25 Glaxo Group Limited Inhalation device
IL99537A (en) 1990-09-27 1995-11-27 Merck & Co Inc Fibrinogen receptor antagonists and pharmaceutical compositions containing them
US5217994A (en) 1991-08-09 1993-06-08 Merck & Co., Inc. Method of inhibiting osteoclast-mediated bone resorption by administration of aminoalkyl-substituted phenyl derivatives
ES2107557T3 (es) 1991-12-10 1997-12-01 Shionogi & Co Derivado de acido hidroxamico a base de sulfonamida aromatica.
DE4220983A1 (de) * 1992-06-26 1994-01-05 Bayer Ag Imidazolyl-substituierte Phenylpropion- und -zimtsäurederivate
ES2186720T3 (es) 1994-05-27 2003-05-16 Merck & Co Inc Composiciones para inhibir la reabsorcion osea mediada por osteoclastos.
GB9700226D0 (en) 1997-01-08 1997-02-26 Glaxo Group Ltd Inhalation device
TWI262185B (en) 1999-10-01 2006-09-21 Eisai Co Ltd Carboxylic acid derivatives having anti-hyperglycemia and anti-hyperlipemia action, and pharmaceutical composition containing the derivatives
TWI284639B (en) 2000-01-24 2007-08-01 Shionogi & Co A compound having thrombopoietin receptor agonistic effect
CA2435829A1 (en) 2001-01-25 2002-08-01 Guilford Pharmaceuticals Inc. Trisubstituted carbocyclic cyclophilin binding compounds and their use
WO2002080899A1 (fr) 2001-03-30 2002-10-17 Eisai Co., Ltd. Agent de traitement de maladie digestive
TWI311133B (en) 2001-04-20 2009-06-21 Eisai R&D Man Co Ltd Carboxylic acid derivativeand the salt thereof
CN101357914A (zh) 2001-09-21 2009-02-04 百时美施贵宝公司 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂
TWI331526B (en) 2001-09-21 2010-10-11 Bristol Myers Squibb Pharma Co Lactam-containing compounds and derivatives thereof as factor xa inhibitors
GB0201677D0 (en) 2002-01-25 2002-03-13 Glaxo Group Ltd Medicament dispenser
US20040157919A1 (en) 2002-01-25 2004-08-12 Yong-Qian Wu Trisubstituted carbocyclic cyclophilin binding compounds and their use
WO2004007464A1 (ja) 2002-07-10 2004-01-22 Sumitomo Pharmaceuticals Co., Ltd. イミダゾール誘導体
EP1615895A4 (en) 2003-04-03 2007-11-07 Merck & Co Inc BIARYLSUBSTITUTED PYRAZOLE AS SODIUM CHANNEL BLOCKER
WO2006044133A1 (en) 2004-09-24 2006-04-27 Axys Pharmaceuticals, Inc. Active ketone inhibitors of tryptase
EP1876179B1 (en) 2005-04-28 2015-03-25 Takeda Pharmaceutical Company Limited Thienopyrimidone compounds
GB0515584D0 (en) 2005-07-28 2005-09-07 Glaxo Group Ltd Medicament dispenser
AR058289A1 (es) 2005-12-12 2008-01-30 Glaxo Group Ltd Colector para ser usado en dispensador de medicamento
US8933130B2 (en) 2006-06-23 2015-01-13 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
US8455638B2 (en) 2007-09-06 2013-06-04 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
CN102395270B (zh) 2008-07-07 2014-11-12 法斯根公司 化合物、含有其的药物组合物、其使用方法及其制备方法
CN102414194A (zh) 2009-02-26 2012-04-11 默沙东公司 可溶性鸟苷酸环化酶激活剂
WO2011094890A1 (en) 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
WO2012068589A2 (en) 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013067036A1 (en) * 2011-10-31 2013-05-10 Rutgers, The State University Of New Jersey Direct inhibitors of keap1-nrf2 interaction as antioxidant inflammation modulators
WO2013122028A1 (ja) 2012-02-13 2013-08-22 武田薬品工業株式会社 芳香環化合物
WO2013155528A2 (en) 2012-04-13 2013-10-17 Fasgen, Inc. Methods for reducing brain inflammation, increasing insulin sensitivity, and reducing ceramide levels
US20160046616A1 (en) * 2013-03-15 2016-02-18 The Johns Hopkins University Nrf2 small molecule inhibitors for cancer therapy
CA2934216C (en) * 2013-12-18 2021-03-16 Glaxosmithkline Intellectual Property Development Limited Substitued phenyl or benzyl propanote derivatives and pharmaceutical compositiions thereof useful as nrf2 regulators
AU2016280236B2 (en) 2015-06-15 2019-02-07 Astex Therapeutics Limited Nrf2 regulators
AU2016280235A1 (en) 2015-06-15 2017-12-14 Astex Therapeutics Limited Nrf2 regulators
EP3359532A1 (en) 2015-10-06 2018-08-15 GlaxoSmithKline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
US10351530B2 (en) 2015-10-06 2019-07-16 Glaxosmithkline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as NRF2 regulators

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