[go: up one dir, main page]

PE20211205A1 - Inhibidores de la interaccion proteina-proteina keap1-nrf2 - Google Patents

Inhibidores de la interaccion proteina-proteina keap1-nrf2

Info

Publication number
PE20211205A1
PE20211205A1 PE2021000224A PE2021000224A PE20211205A1 PE 20211205 A1 PE20211205 A1 PE 20211205A1 PE 2021000224 A PE2021000224 A PE 2021000224A PE 2021000224 A PE2021000224 A PE 2021000224A PE 20211205 A1 PE20211205 A1 PE 20211205A1
Authority
PE
Peru
Prior art keywords
alkyl
protein
perhaloalkyl
halo
inhibitors
Prior art date
Application number
PE2021000224A
Other languages
English (en)
Inventor
J Kent Barbay
Wenying Chai
Gavin C Hirst
Kevin D Kreutter
David A Kummer
Kelly J Mcclure
Rachel Nishimura
Amy Y Shih
Jennifer D Venable
Hariharan Venkatesan
Jianmei Wei
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20211205A1 publication Critical patent/PE20211205A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—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
    • A61K31/554—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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D419/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur 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
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de la Formula (I) o una sal farmaceuticamente aceptable de este, en donde: X es CH o N; Q es CH o N; M es CH o N; R15 es CH3 o Cl; R13 es H, F o alquilo C1-C4; R14 es H, F o alquilo C1-C4; HetA se selecciona del grupo (a), (b) o (c); R1 es cicloalquilo C3-C4, alquilo C1- C4, entre otros; R2 es H, alquilo C1-C4 y perhaloalquilo C1-C4; R3 es H o alquilo C1-C4; R4 es alquilo C1-C4, perhaloalquilo C1-C4 y cicloalquilo C3-C4; R7 es H o alquilo C1-C4; R8 es alquilo C1-C4; R9 es alquilo C1-C4; R10 es H, -Ocicloalquilo C3-C4 y -Operhaloalquilo C1-C4; HetB es (e), (f), entre otros; Z es O, CH2, NH y N(CH3); T es CH o N; Y es CH o N; R16 es H o F; R17 es H o F; n es 0, 1 o 2; R18 es H, -CN, halo, C(O)NH2, alquilo C1-C4 y perhaloalquilo C1-C4; R19 es H, CN, halo, C(O)NH2, entre otros; R20 es H o alquilo C1-C4; R25 es H, CN, halo, C(O)NH2, entre otros; R26 es H, -CN, halo, alquilo C1-C4 y perhaloalquilo C1-C4; R27 es H o alquilo C1-C4. Dichos compuestos son inhibidores de la interaccion proteina-proteina KEAP1-Nrf2 y son {utiles en el tratamiento de enfermedades tales como la inflamacion intestinal, que incluye la enfermedad de Crohn y colitis ulcerante.
PE2021000224A 2018-08-20 2019-08-19 Inhibidores de la interaccion proteina-proteina keap1-nrf2 PE20211205A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201862719978P 2018-08-20 2018-08-20
US201962801433P 2019-02-05 2019-02-05
US201962823450P 2019-03-25 2019-03-25
US201962875737P 2019-07-18 2019-07-18
US201962881639P 2019-08-01 2019-08-01
PCT/US2019/047015 WO2020041169A2 (en) 2018-08-20 2019-08-19 Inhibitors of keap1-nrf2 protein-protein interaction

Publications (1)

Publication Number Publication Date
PE20211205A1 true PE20211205A1 (es) 2021-07-05

Family

ID=69523716

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2021000224A PE20211205A1 (es) 2018-08-20 2019-08-19 Inhibidores de la interaccion proteina-proteina keap1-nrf2

Country Status (30)

Country Link
US (3) US10947252B2 (es)
EP (2) EP4364804A3 (es)
JP (2) JP7212763B2 (es)
KR (2) KR102590310B1 (es)
CN (1) CN112930347B (es)
AU (3) AU2019326368B2 (es)
BR (1) BR112021002979A2 (es)
CA (1) CA3108534A1 (es)
CL (1) CL2021000426A1 (es)
CO (1) CO2021002670A2 (es)
CR (1) CR20210087A (es)
DK (1) DK3833662T3 (es)
EC (1) ECSP21016032A (es)
ES (1) ES2974026T3 (es)
FI (1) FI3833662T3 (es)
HU (1) HUE065501T2 (es)
IL (2) IL304110B2 (es)
JO (1) JOP20210030A1 (es)
MX (1) MX2021002060A (es)
MY (1) MY197921A (es)
NZ (1) NZ773129A (es)
PE (1) PE20211205A1 (es)
PH (1) PH12021500012A1 (es)
PL (1) PL3833662T3 (es)
PT (1) PT3833662T (es)
SG (1) SG11202101613XA (es)
TW (2) TWI781342B (es)
UA (1) UA126950C2 (es)
UY (1) UY38338A (es)
WO (1) WO2020041169A2 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102590310B1 (ko) 2018-08-20 2023-10-17 얀센 파마슈티카 엔브이 KEAP1-Nrf2 단백질간 상호작용 억제제
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
US20230107927A1 (en) 2020-02-28 2023-04-06 First Wave Bio, Inc. Methods of treating iatrogenic autoimmune colitis
CA3206893A1 (en) * 2020-12-28 2022-07-07 Senju Pharmaceutical Co., Ltd. Nrf2-activating compound
CN112661655B (zh) * 2020-12-29 2022-02-18 江苏云朴医药新材料科技有限公司 一种1-氨甲基-1-环丙醇类化合物及其合成方法
CN118891254A (zh) 2022-04-28 2024-11-01 日本农药株式会社 具有肟基的含氮杂环化合物、及含有该化合物的农业园艺用除草剂以及其使用方法
AU2023259936A1 (en) 2022-04-28 2024-11-28 Daiichi Sankyo Company, Limited Benzotriazole compound
CN115925606B (zh) * 2023-01-05 2023-10-13 宁夏医科大学 一种5-（3-（磺酰胺基）苯基）-1h-吡咯-2-羧酸衍生物及其制备方法和应用
CN116003397B (zh) * 2023-03-24 2023-06-16 凯思凯旭(上海)医药科技有限公司 一种苯并多元环噻唑啉酰胺类化合物及其应用
KR20260005897A (ko) * 2023-04-03 2026-01-12 에이스링크 테라퓨틱스, 인코포레이티드 신규 화합물 및 이의 용도
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

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1959969A2 (en) 2005-07-01 2008-08-27 The Johns Hopkins University Compositions and methods for the treatment or prevention of disorders relating to oxidative stress
WO2007008652A2 (en) 2005-07-08 2007-01-18 The University Of North Carolina At Chapel Hill Methods and compositions directed to dj-1 as regulator of the anti-oxidant transcription factor nrf2
EP2086318A4 (en) 2006-10-10 2009-12-23 Burnham Inst Medical Research NEUROPROTECTIVE COMPOSITIONS AND CORRESPONDING METHODS
US9139592B2 (en) 2010-06-14 2015-09-22 Trt Pharma Inc. Modulators of Nrf2 and uses thereof
JP5988101B2 (ja) 2011-01-21 2016-09-07 国立研究開発法人理化学研究所 酸化ストレスインジケーター発現用核酸構築物とその使用
US9075070B2 (en) 2011-02-09 2015-07-07 Rutgers, The State University Of New Jersey HTS fluorescence polarization assay for inhibitors of Keap1-Nrf2 interaction
EP2678305A4 (en) 2011-02-25 2015-11-04 Univ Johns Hopkins CHALCONE DERIVATIVES AS NRF2 ACTIVATORS
JP2013028575A (ja) 2011-07-29 2013-02-07 Toray Ind Inc Ｋｅａｐ１タンパク質結合化合物、該Ｋｅａｐ１タンパク質結合化合物とＫｅａｐ１タンパク質の複合体の結晶及びその製造方法
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
PT3444261T (pt) 2012-04-27 2021-03-12 Reata Pharmaceuticals Inc Derivados de 2,2-difluoropropionamida de metil bardoxolona, formas polimorfas e métodos de uso dos mesmos
WO2014058982A2 (en) 2012-10-10 2014-04-17 Temple University Of The Commonwealth System Of Higher Education Nuclear factor-erythroid 2 related factor 2 (nrf2) biosensors and modulators of nrf2
WO2014148455A1 (ja) 2013-03-19 2014-09-25 第一三共株式会社 テルペノイド誘導体
UY39092A (es) 2013-04-24 2021-03-26 Abbvie Inc Derivados de 2,2-difluoropropanamida y metil bardoxolona, formas polimórficas y métodos de uso
WO2014197818A2 (en) 2013-06-07 2014-12-11 The General Hospital Corporation Small molecule activators of nrf2 pathway
EP3062884B1 (en) 2013-10-29 2020-12-02 President and Fellows of Harvard College Compositions for use in the treatment of retinitis pigmentosa
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
US11053291B2 (en) 2014-02-19 2021-07-06 University Of Florida Research Foundation, Incorporated Delivery of Nrf2 as therapy for protection against reactive oxygen species
CN106661080A (zh) 2014-09-10 2017-05-10 第三共株式会社 用于治疗和预防眼科疾病的缓释药物组合物
ES2570452B1 (es) 2014-10-15 2017-04-19 Fundación Para La Investigación Biomédida Del Hospital Universitario De La Princesa Compuestos derivados de acrilato de 3-Alquilamino-1H-Indolilo y su uso en el tratamiento de enfermedades neurodegenerativas
US20160120158A1 (en) 2014-11-03 2016-05-05 The Johns Hopkins University Compositions and methods for the study and treatment of acute kidney injury
WO2016089648A1 (en) 2014-12-01 2016-06-09 Vtv Therapeutics Llc Bach 1 inhibitors in combination with nrf2 activators and pharmaceutical compositions thereof
CN104825443B (zh) 2015-04-27 2017-10-24 广东省中医院 青蒿烯的抗氧化应用
FI3782996T3 (fi) 2015-06-15 2024-06-26 Glaxosmithkline Ip Dev Ltd Nrf2-säätelijöitä
AU2016280235A1 (en) 2015-06-15 2017-12-14 Astex Therapeutics Limited Nrf2 regulators
US20180243190A1 (en) 2015-08-18 2018-08-30 The Arizona Board Of Regents On Behalf Of The University Of Arizona Activators of nrf2-dependent photoprotection and related uses thereof
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
CN105566241B (zh) 2016-01-18 2018-05-25 中国药科大学 1-磺酰胺基-4-芳氧基类化合物、制备方法及其医药用途
EP3429690A4 (en) 2016-03-16 2019-10-23 Ionis Pharmaceuticals, Inc. METHOD FOR MODULATING KEAP1
CN105753795B (zh) * 2016-04-29 2018-04-13 济南大学 一种具有1,2,3‑三氮唑结构片段的生物碱化合物及其用途
CN109803664A (zh) 2016-06-15 2019-05-24 尚特·德扎尔基西安 用于改善细胞、组织和器官的活力和功能的试剂、组合物和方法
WO2018089386A1 (en) 2016-11-11 2018-05-17 The Broad Institute, Inc. Modulation of intestinal epithelial cell differentiation, maintenance and/or function through t cell action
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
WO2018109641A1 (en) 2016-12-12 2018-06-21 Glaxosmithkline Intellectual Property Development Limited 3-carboxylic acid pyrroles as nrf2 regulators
EP3551621A1 (en) 2016-12-12 2019-10-16 GlaxoSmithKline Intellectual Property Development Limited N-aryl pyrazoles as nrf2 regulators
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
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
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
EP3573968A1 (en) 2017-01-30 2019-12-04 Biogen MA Inc. Nrf2 activator
WO2018145109A1 (en) * 2017-02-06 2018-08-09 Massachusetts Institute Of Technology Methods and products related to glutaminase inhibitors
JP2020097526A (ja) 2017-03-28 2020-06-25 武田薬品工業株式会社 複素環化合物
CN107033100B (zh) 2017-05-24 2019-03-01 济南大学 一种苯并噻唑衍生物、制备方法及其医药用途
CN107236813A (zh) 2017-07-02 2017-10-10 东北林业大学 一种指示Nrf2‑Keap1相互作用的BiFC细胞内检测方法及系统
CN107881195B (zh) 2017-10-26 2021-08-27 深圳市第三人民医院 一种双基因共表达质粒pIRES2-Nrf2-DKK1及其制备方法和应用
AU2018386464B2 (en) 2017-12-22 2021-08-05 Medimmune Limited Small molecule modulators of the BTB domain of Keap1
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
WO2019224667A1 (en) 2018-05-23 2019-11-28 Glaxosmithkline Intellectual Property Development Limited Indanes as nrf2 activators
CN110724669A (zh) 2018-06-29 2020-01-24 李陶 一种Nrf2基因修饰的脐带间充质干细胞及其制备方法与应用
CN108752245A (zh) 2018-07-16 2018-11-06 宁夏医科大学 萘磺酰胺乙酰胺类化合物及其应用和药物组合物
KR102590310B1 (ko) * 2018-08-20 2023-10-17 얀센 파마슈티카 엔브이 KEAP1-Nrf2 단백질간 상호작용 억제제
CA3117109A1 (en) 2018-10-19 2020-04-23 Aclipse One Inc. Treatment of neurological diseases
BR112021007513A2 (pt) 2018-10-22 2021-07-27 C4X Discovery Limited composto, composição farmacêutica, e, método
MX2021006527A (es) 2018-12-05 2021-07-21 Scohia Pharma Inc Compuesto macrociclico y su uso.
WO2020132040A1 (en) 2018-12-20 2020-06-25 President And Fellows Of Harvard College Compositions and methods for the treatment of degenerative ocular diseases
US12122742B2 (en) 2019-01-18 2024-10-22 Rutgers, The State University Of New Jersey Small molecule direct inhibitors of KEAP1-NRF2 protein-protein interaction
BR112021016042A2 (pt) 2019-02-15 2021-10-05 Glaxosmithkline Intellectual Property Development Limited Hidroxipiridoxazepinas como ativadores de nrf2
MX2021013299A (es) 2019-04-30 2022-01-31 Sitryx Therapeutics Ltd Derivados de acido itaconico y usos de estos en el tratamiento de una enfermedad inflamatoria asociada con una respuesta inmunitaria indeseable.
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
CN110256305B (zh) 2019-07-24 2020-05-26 中国药科大学 一种萘磺酰胺类化合物、制备方法和应用
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
CN111362857B (zh) 2020-04-23 2023-02-28 中国药科大学 一类具有吲哚啉骨架的化合物、制备方法及其医药用途
CN112321620B (zh) 2020-11-10 2022-03-29 中国药科大学 一种Keap1-Nrf2 PPI抑制剂前药、制备方法和用途

Also Published As

Publication number Publication date
CR20210087A (es) 2021-05-25
BR112021002979A2 (pt) 2021-06-08
TWI781342B (zh) 2022-10-21
DK3833662T3 (da) 2024-02-26
IL304110B1 (en) 2024-08-01
AU2019326368B2 (en) 2021-11-11
EP4364804A3 (en) 2024-09-04
JP2023038270A (ja) 2023-03-16
CN112930347A (zh) 2021-06-08
US20200055874A1 (en) 2020-02-20
WO2020041169A2 (en) 2020-02-27
PT3833662T (pt) 2024-03-18
SG11202101613XA (en) 2021-03-30
JP2021535118A (ja) 2021-12-16
UY38338A (es) 2020-02-28
KR20210047895A (ko) 2021-04-30
CL2021000426A1 (es) 2021-08-20
TW202309020A (zh) 2023-03-01
ECSP21016032A (es) 2021-04-29
UA126950C2 (uk) 2023-02-22
CN112930347B (zh) 2024-07-23
PH12021500012A1 (en) 2021-09-13
EP4364804A2 (en) 2024-05-08
EP3833662B1 (en) 2024-01-17
AU2022200478B2 (en) 2023-07-06
AU2022200478A1 (en) 2022-04-21
WO2020041169A3 (en) 2020-04-02
CO2021002670A2 (es) 2021-03-08
US20220315604A1 (en) 2022-10-06
US11897900B2 (en) 2024-02-13
IL304110B2 (en) 2024-12-01
HUE065501T2 (hu) 2024-05-28
KR20230146136A (ko) 2023-10-18
KR102753167B1 (ko) 2025-01-09
JOP20210030A1 (ar) 2021-02-16
IL304110A (en) 2023-09-01
PL3833662T3 (pl) 2024-05-13
AU2019326368A1 (en) 2021-04-15
ES2974026T3 (es) 2024-06-25
IL280950B2 (en) 2023-12-01
CA3108534A1 (en) 2020-02-27
IL280950A (en) 2021-04-29
US11427601B1 (en) 2022-08-30
NZ773129A (en) 2024-11-29
IL280950B1 (en) 2023-08-01
KR102590310B1 (ko) 2023-10-17
TW202021594A (zh) 2020-06-16
MY197921A (en) 2023-07-25
MX2021002060A (es) 2021-07-21
US10947252B2 (en) 2021-03-16
JP7212763B2 (ja) 2023-01-25
EP3833662A2 (en) 2021-06-16
AU2023237198A1 (en) 2023-10-19
FI3833662T3 (fi) 2024-03-01

Similar Documents

Publication Publication Date Title
PE20211205A1 (es) Inhibidores de la interaccion proteina-proteina keap1-nrf2
CO2021015698A2 (es) Moduladores de thr-β y métodos de uso de estos
UY40470A (es) Compuestos tricíclicos y sus usos
CO5590957A2 (es) Amino-1,3,5-triazinas sustituidas en n con radicales biciclicos quirales, procedimiento para su preparacion, composiciones de las mismas y su uso como herbicidas y reguladores del crecimiento de las plantas
PE20191532A1 (es) Compuestos heterociclicos como inmunomoduladores
PE20250021A1 (es) Cicloalquil 3-oxopiperazin carboxamidas y cicloheteroalquil 3-oxopiperazin carboxamidas como inhibidores de nav1.8
UY39261A (es) Compuestos para el tratamiento de enfermedades y trastornos asociados a braf
PE20240879A1 (es) Inhibidor sos1 y uso del mismo
AR113895A1 (es) Compuestos de heteroarilo sustituidos con alquilamida de piridinsulfona
AR114290A1 (es) Péptidos macrocíclicos contra actinetobacter baumannii
AR106314A1 (es) COMPUESTOS DE ESPIRO[3H-INDOL-3,2’-PIRROLIDIN]-2(1H)-ONA Y DERIVADOS COMO INHIBIDORES DE MDM2 - p53
AR082201A1 (es) Bencenosulfonamidas utiles como inhibidores del canal de sodio
AR053120A1 (es) Aminopiridinas como inhibidores de beta secretasa
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
AR116115A1 (es) Dimetil amino azetidina amidas como inhibidores de jak
PE20210478A1 (es) Compuestos heteroaromaticos como inhibidores de vanina
PE20141352A1 (es) Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento
AR043700A1 (es) Derivados de 3-substituida-4-pirimidona
AR083953A1 (es) Compuestos para tratar enfermedades neurodegenerativas
AR065785A1 (es) Compuestos biarilo y biheteroarilo de utilidad en el tratamiento de trastornos de hierro
PE20200340A1 (es) Compuestos heteroaromaticos como inhibidores de vanina
CO2019004978A2 (es) Compuestos terapéuticos y métodos para utilizarlos
PE20200333A1 (es) Compuestos y metodos para tratar infecciones bacterianas
PE20181017A1 (es) Compuestos heteroarilo y su uso como farmacos terapeuticos
CO2025005880A2 (es) Inhibidores del miembro 19 de la familia de portadores de solutos 6a (slc6a19) y métodos de uso de los mismos