JP7675020B2 - Ｂａｘ阻害剤およびその使用 - Google Patents

Ｂａｘ阻害剤およびその使用 Download PDF

Info

Publication number
JP7675020B2
JP7675020B2 JP2021570180A JP2021570180A JP7675020B2 JP 7675020 B2 JP7675020 B2 JP 7675020B2 JP 2021570180 A JP2021570180 A JP 2021570180A JP 2021570180 A JP2021570180 A JP 2021570180A JP 7675020 B2 JP7675020 B2 JP 7675020B2
Authority
JP
Japan
Prior art keywords
alkyl
equiv
umol
mmol
ethyl
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
JP2021570180A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022534902A (ja
JP2022534902A5 (https=
Inventor
茂実 松山
グリーンリー，ウィリアム
Original Assignee
ケース ウエスタン リザーブ ユニバーシティ
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 ケース ウエスタン リザーブ ユニバーシティ filed Critical ケース ウエスタン リザーブ ユニバーシティ
Publication of JP2022534902A publication Critical patent/JP2022534902A/ja
Publication of JP2022534902A5 publication Critical patent/JP2022534902A5/ja
Priority to JP2025010128A priority Critical patent/JP2025066800A/ja
Application granted granted Critical
Publication of JP7675020B2 publication Critical patent/JP7675020B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61P39/00—General protective or antinoxious agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C13/00—Cyclic hydrocarbons containing rings other than, or in addition to, six-membered aromatic rings
    • C07C13/28—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2021570180A 2019-05-31 2020-06-01 Ｂａｘ阻害剤およびその使用 Active JP7675020B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025010128A JP2025066800A (ja) 2019-05-31 2025-01-23 Ｂａｘ阻害剤およびその使用

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962855185P 2019-05-31 2019-05-31
US62/855,185 2019-05-31
PCT/US2020/035564 WO2021002986A2 (en) 2019-05-31 2020-06-01 Bax inhibitors and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025010128A Division JP2025066800A (ja) 2019-05-31 2025-01-23 Ｂａｘ阻害剤およびその使用

Publications (3)

Publication Number Publication Date
JP2022534902A JP2022534902A (ja) 2022-08-04
JP2022534902A5 JP2022534902A5 (https=) 2023-06-08
JP7675020B2 true JP7675020B2 (ja) 2025-05-12

Family

ID=74100581

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2021570180A Active JP7675020B2 (ja) 2019-05-31 2020-06-01 Ｂａｘ阻害剤およびその使用
JP2025010128A Pending JP2025066800A (ja) 2019-05-31 2025-01-23 Ｂａｘ阻害剤およびその使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025010128A Pending JP2025066800A (ja) 2019-05-31 2025-01-23 Ｂａｘ阻害剤およびその使用

Country Status (6)

Country Link
US (1) US12479857B2 (https=)
EP (1) EP3976009A4 (https=)
JP (2) JP7675020B2 (https=)
AU (1) AU2020299526B2 (https=)
CA (1) CA3142424A1 (https=)
WO (1) WO2021002986A2 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020299526B2 (en) 2019-05-31 2026-01-29 Case Western Reserve University Bax inhibitors and uses thereof
EP4479383A4 (en) * 2022-02-17 2026-01-07 Sunnybrook Res Inst ISOQUINOLINE DERIVATIVES USED AS BAX AND/OR BAK INHIBITORS, COMPOSITIONS AND ASSOCIATED USES
KR102896033B1 (ko) * 2022-12-22 2025-12-04 연세대학교 산학협력단 N-벤질퀴나졸린-4-아민 화합물을 포함하는, 비만 및 지질 관련 대사성 질환의 예방 또는 치료용 조성물
WO2024208292A1 (zh) * 2023-04-04 2024-10-10 江苏亚虹医药科技股份有限公司 泛素特异性蛋白酶1抑制剂、其制备方法及其医药用途
CN120882721A (zh) * 2023-07-28 2025-10-31 双翼原创（上海）医药有限公司 Arf1抑制剂及其应用
CN120554372A (zh) * 2024-02-27 2025-08-29 浙江养生堂天然药物研究所有限公司 嘧啶并杂芳类化合物及其应用

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6046206A (en) 1995-06-07 2000-04-04 Cell Pathways, Inc. Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
US20020091263A1 (en) 1999-03-17 2002-07-11 Trova Michael Peter Biaryl substituted purine derivatives as potent antiproliferative agents
JP2003523332A (ja) 2000-02-15 2003-08-05 アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ アポトーシスの治療のためのアミン誘導体
JP2006500385A (ja) 2002-08-30 2006-01-05 ノバルティス アクチエンゲゼルシャフト ヘテロアリールニトリル誘導体
WO2012079079A1 (en) 2010-12-10 2012-06-14 President And Fellows Of Harvard College Production of induced pluripotent stem cells
US20150190366A1 (en) 2012-07-06 2015-07-09 Newsouth Innovations Pty Limited Methods for inhibiting neuron apoptosis and necrosis
WO2016011394A1 (en) 2014-07-18 2016-01-21 The General Hospital Corporation Imaging agents for neural flux
JP2016504365A (ja) 2012-12-28 2016-02-12 アメリカ合衆国 Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用
WO2018019284A1 (en) 2016-07-28 2018-02-01 Realinn Life Science Limited Compounds for enhancing bax/bcl-2 expression and activity and therapeutic use thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4798824A (en) 1985-10-03 1989-01-17 Wisconsin Alumni Research Foundation Perfusate for the preservation of organs
US4879283A (en) 1985-10-03 1989-11-07 Wisconsin Alumni Research Foundation Solution for the preservation of organs
RU2025973C1 (ru) 1992-02-10 1995-01-09 Научно-производственное предприятие "Биофарм" Раствор для консервации живых органов
US5552267A (en) 1992-04-03 1996-09-03 The Trustees Of Columbia University In The City Of New York Solution for prolonged organ preservation
US5370989A (en) 1992-04-03 1994-12-06 The Trustees Of Columbia University In The City Of New York Solution for prolonged organ preservation
AU664074B2 (en) 1992-06-26 1995-11-02 Torii Pharmaceutical Co., Ltd. Organ preserving fluid
US5405742A (en) 1993-07-16 1995-04-11 Cyromedical Sciences, Inc. Solutions for tissue preservation and bloodless surgery and methods using same
AU2020299526B2 (en) 2019-05-31 2026-01-29 Case Western Reserve University Bax inhibitors and uses thereof
JP7674020B1 (ja) * 2024-07-19 2025-05-09 株式会社大都技研 遊技台

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6046206A (en) 1995-06-07 2000-04-04 Cell Pathways, Inc. Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
US20020091263A1 (en) 1999-03-17 2002-07-11 Trova Michael Peter Biaryl substituted purine derivatives as potent antiproliferative agents
JP2003523332A (ja) 2000-02-15 2003-08-05 アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ アポトーシスの治療のためのアミン誘導体
JP2006500385A (ja) 2002-08-30 2006-01-05 ノバルティス アクチエンゲゼルシャフト ヘテロアリールニトリル誘導体
WO2012079079A1 (en) 2010-12-10 2012-06-14 President And Fellows Of Harvard College Production of induced pluripotent stem cells
US20150190366A1 (en) 2012-07-06 2015-07-09 Newsouth Innovations Pty Limited Methods for inhibiting neuron apoptosis and necrosis
JP2016504365A (ja) 2012-12-28 2016-02-12 アメリカ合衆国 Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用
WO2016011394A1 (en) 2014-07-18 2016-01-21 The General Hospital Corporation Imaging agents for neural flux
WO2018019284A1 (en) 2016-07-28 2018-02-01 Realinn Life Science Limited Compounds for enhancing bax/bcl-2 expression and activity and therapeutic use thereof

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DATABASE PUBCHEM COMPOUND，26 March 2005 (2005-03-26), "Benzyl phenyl ether | C13H12O", XP055826796, Database accession no. CID 70352
Klittich, Carla J. R.; Ray, Scott L.，Effects of physical properties on the translaminar activity of fungicides，Pesticide Biochemistry and Physiology，2013年，107(3)，351-359.
Read, Matthew L. et al.，Synthesis and biological evaluation of pyrimidine analogs of antimycobacterial purines，Bioorganic & Medicinal Chemistry ，2010年，18(11)，3885-3897.
REGISTRY（STN）[online]，2008.3.31[検索日 2024.5.20] CAS登録番号 1011107-28-0

Also Published As

Publication number Publication date
AU2020299526A1 (en) 2022-01-20
WO2021002986A2 (en) 2021-01-07
JP2022534902A (ja) 2022-08-04
WO2021002986A3 (en) 2021-05-27
CA3142424A1 (en) 2021-01-07
US20220389028A1 (en) 2022-12-08
EP3976009A4 (en) 2023-07-05
AU2020299526B2 (en) 2026-01-29
US12479857B2 (en) 2025-11-25
JP2025066800A (ja) 2025-04-23
EP3976009A2 (en) 2022-04-06

Similar Documents

Publication Publication Date Title
JP7675020B2 (ja) Ｂａｘ阻害剤およびその使用
JP7652697B2 (ja) ピリダジン系誘導体阻害剤、その製造方法及び使用
AU2019416589B2 (en) Heterocyclic compound intermediate, preparation method therefor and application thereof
DE602004010151T2 (de) Zusammensetzungen, die sich als inhibitoren von proteinkinasen eignen
US11312705B2 (en) Heteroaryl[4,3-C]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
AU2020348675B2 (en) Azole-fused pyridazin-3(2H)-one derivatives
JP5501369B2 (ja) 可溶性グアニレートシクラーゼ活性化剤
TWI617559B (zh) ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
JP2024543497A (ja) ユビキチン特異的プロテアーゼ１（ｕｓｐ１）の小分子阻害剤及びその使用
JP2008531537A (ja) 化合物
AU2013351642A1 (en) Inhibitors of bruton's tyrosine kinase
TR201808380T4 (tr) Napdh Oksidaz enzimleri olarak Pirazolo Piridin Türevleri.
JP2009544625A (ja) Ｒｈｏキナーゼのベンゾチオフェン阻害剤
WO2018090869A1 (zh) 酰胺衍生物及其在药物中的应用
CN106715440A (zh) 咪唑并异吲哚类衍生物、其制备方法及其在医药上的应用
JP2018135335A (ja) Ｓｈｉｐ１モジュレーターおよびそれに関連する方法
JP2024537110A (ja) Ｅｎｔ１阻害活性を有する大環状化合物
JP2025537876A (ja) Ｇｐｒ１７モジュレーター及びその使用
EA030962B1 (ru) Замещенные пиримидиновые соединения и их применение в качестве syk ингибиторов
JP2022549601A (ja) ヘテロアリール血漿カリクレインインヒビター
IL325314A (en) Tyk2 inhibitors, compositions and methods thereof
JP2021535924A (ja) 新規なチアゾール誘導体及びその薬学的に許容される塩
JP2025541286A (ja) タンパク質ミスフォールディングに関連する障害を処置する化合物、組成物、及び方法
HK40029610B (zh) 一种哒嗪类衍生物抑制剂、其制备方法和应用
HK40119624A (en) Tyk2 inhibitors and uses thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220722

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230531

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20230531

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20240530

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240611

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240906

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20240924

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250123

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20250401

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250425

R150 Certificate of patent or registration of utility model

Ref document number: 7675020

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150