KR102932313B1 - Nrf2 활성화제로서 히드록시피리드옥사제핀 - Google Patents

Nrf2 활성화제로서 히드록시피리드옥사제핀

Info

Publication number
KR102932313B1
KR102932313B1 KR1020217029193A KR20217029193A KR102932313B1 KR 102932313 B1 KR102932313 B1 KR 102932313B1 KR 1020217029193 A KR1020217029193 A KR 1020217029193A KR 20217029193 A KR20217029193 A KR 20217029193A KR 102932313 B1 KR102932313 B1 KR 102932313B1
Authority
KR
South Korea
Prior art keywords
methyl
compound
dimethyl
dihydropyrido
benzo
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
KR1020217029193A
Other languages
English (en)
Korean (ko)
Other versions
KR20210126676A (ko
Inventor
마크 엘반
미첼 파월 글로고프스키
마이클 클린턴 쾨팅
브라이언 그리핀 로혼
제이 엠. 매튜스
재클린 레니 패터슨
Original Assignee
글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드
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 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 filed Critical 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드
Publication of KR20210126676A publication Critical patent/KR20210126676A/ko
Application granted granted Critical
Publication of KR102932313B1 publication Critical patent/KR102932313B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
KR1020217029193A 2019-02-15 2020-02-11 Nrf2 활성화제로서 히드록시피리드옥사제핀 Active KR102932313B1 (ko)

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 (2)

Publication Number Publication Date
KR20210126676A KR20210126676A (ko) 2021-10-20
KR102932313B1 true KR102932313B1 (ko) 2026-02-26

Family

ID=69726636

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217029193A Active KR102932313B1 (ko) 2019-02-15 2020-02-11 Nrf2 활성화제로서 히드록시피리드옥사제핀

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=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016202253A1 (en) 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
JP2017503786A (ja) 2013-12-18 2017-02-02 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
WO2018109646A1 (en) 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 compounds

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7714012B2 (en) * 2006-11-17 2010-05-11 Trustees Of Dartmouth University Synthesis and biological activities of new tricyclic-bis-enones (TBEs)
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
CA2988373A1 (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
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
CN108779108A (zh) * 2016-12-06 2018-11-09 葛兰素史密斯克莱知识产权发展有限公司 3-(2,3-二氢-1h-茚-5-基)丙酸衍生物和它们作为nrf2调节剂的用途
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017503786A (ja) 2013-12-18 2017-02-02 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
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

Also Published As

Publication number Publication date
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
AU2020222080C1 (en) 2022-09-29
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

Similar Documents

Publication Publication Date Title
KR102932313B1 (ko) Nrf2 활성화제로서 히드록시피리드옥사제핀
JP6637136B2 (ja) バルドキソロンメチルの２，２−ジフルオロプロピオンアミド誘導体、その多形体および使用方法
EP4050008A1 (en) Pyridazinone or pyridazine compound and derivative and pharmaceutical composition thereof
JP7110197B2 (ja) Ｎｒｆ２アクチベーター
WO2020051058A1 (en) 2,6-diamino pyridine compounds
JP2021532107A (ja) ジカチオン化合物及びその製造方法と使用
EP3796906A1 (en) Indanes as nrf2 activators
EP3555068A1 (en) 3-oxo-1,4-diazepinyle compounds as nrf2 activators
RU2812931C2 (ru) Гидроксипиридоксазепины в качестве активаторов nrf2
HK40106672A (zh) 作为nrf2活化剂的羟基吡啶并氧氮杂环庚三烯
JP7262843B2 (ja) ジアリールピラゾール化合物、該化合物を含む組成物およびその使用
JP2021527116A (ja) 選択的ａ２ａ受容体アンタゴニスト
JP6809781B2 (ja) プテリン誘導体又はその塩
JP2016216446A (ja) ピロリジン−２，５−ジオン誘導体の多形形態、医薬組成物、およびｉｄｏ１阻害薬としての使用方法
BR112019012300B1 (pt) Composto ativador de nrf2, composição farmacêutica que compreende o mesmo e uso do dito composto para o tratamento de distúrbios respiratórios e não-respiratórios

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

E13 Pre-grant limitation requested

Free format text: ST27 STATUS EVENT CODE: A-2-3-E10-E13-LIM-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

D22 Grant of ip right intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D22-EXM-PE0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

F11 Ip right granted following substantive examination

Free format text: ST27 STATUS EVENT CODE: A-2-4-F10-F11-EXM-PR0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

U12 Designation fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U12-OTH-PR1002 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

Q13 Ip right document published

Free format text: ST27 STATUS EVENT CODE: A-4-4-Q10-Q13-NAP-PG1601 (AS PROVIDED BY THE NATIONAL OFFICE)