TWI904076B - 作為用於治療神經退化性疾病的ppargc1a活化劑的2-芳基苯并咪唑 - Google Patents

作為用於治療神經退化性疾病的ppargc1a活化劑的2-芳基苯并咪唑

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Publication number
TWI904076B
TWI904076B TW108127925A TW108127925A TWI904076B TW I904076 B TWI904076 B TW I904076B TW 108127925 A TW108127925 A TW 108127925A TW 108127925 A TW108127925 A TW 108127925A TW I904076 B TWI904076 B TW I904076B
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esi
alkyl
benzo
lcms
nmr
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TW108127925A
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TW202019410A (zh
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塞繆爾 D 班尼斯特
埃德加 恩格爾曼
科阿 D 尼古恩
馬克 史密斯
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小利蘭史丹佛大學董事會
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57Aryl or substituted aryl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/64Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C07D277/66Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
TW108127925A 2018-08-06 2019-08-06 作為用於治療神經退化性疾病的ppargc1a活化劑的2-芳基苯并咪唑 TWI904076B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862714962P 2018-08-06 2018-08-06
US62/714,962 2018-08-06

Publications (2)

Publication Number Publication Date
TW202019410A TW202019410A (zh) 2020-06-01
TWI904076B true TWI904076B (zh) 2025-11-11

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US (3) US12195432B2 (https=)
EP (1) EP3833344A4 (https=)
JP (2) JP7422737B2 (https=)
KR (1) KR20210068399A (https=)
CN (2) CN112805000A (https=)
AU (1) AU2019319745B2 (https=)
BR (1) BR112021002165A2 (https=)
CA (1) CA3108773A1 (https=)
IL (3) IL280664B2 (https=)
MX (2) MX2021001456A (https=)
SG (1) SG11202101285YA (https=)
TW (1) TWI904076B (https=)
WO (1) WO2020033359A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12195432B2 (en) 2018-08-06 2025-01-14 The Board Of Trustees Of The Leland Stanford Junior University 2-arylbenzimidazoles as Ppargc1a activators for treating neurodegenerative diseases
KR20220154772A (ko) * 2020-03-13 2022-11-22 주식회사 바이오오케스트라 Pgc-1a 발현을 사용하는 진단 방법
CN112933232A (zh) * 2021-02-02 2021-06-11 袁玉佳 PGC-1α激活TFEB介导的自噬在制备治疗急性肾损伤的药物中的应用
EP4426295A1 (en) * 2021-11-02 2024-09-11 Tranquis Therapeutics, Inc. Selection and treatment of subjects having a circulating myeloid cell inflammatory phenotype
US20250262189A1 (en) * 2022-04-22 2025-08-21 Rdiscovery, LLC Treatment of diseases associated with reductive stress
EP4618982A1 (en) * 2022-11-18 2025-09-24 GOJO, Satoshi Uses of zln-005 and related compounds
WO2024118936A1 (en) * 2022-12-02 2024-06-06 Tranquis Therapeutics, Inc. 2-arylbenzimidazole compounds for the treatment of hemoglobinopathies

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014179303A1 (en) * 2013-04-29 2014-11-06 The General Hospital Corporation Amyloid precursor protein mrna blockers for treating down syndrome and alzheimer's disease
WO2016061190A1 (en) * 2014-10-14 2016-04-21 The Board Of Trustees Of The Leland Stanford Junior University Method for treating neurodegenerative diseases
WO2017106050A1 (en) * 2015-12-15 2017-06-22 The Board Of Trustees Of The Leland Stanford Junior University Method for preventing and/or treating aging-associated cognitive impairment and neuroinflammation

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE614236A (https=) 1961-03-01
FR1569337A (https=) * 1968-06-18 1969-05-30
US4038396A (en) * 1975-02-24 1977-07-26 Merck & Co., Inc. Anti-inflammatory oxazole[4,5-b]pyridines
GB1584296A (en) 1976-12-07 1981-02-11 Kanebo Ltd 2-substituted benzimidazole compounds
NZ234564A (en) 1986-11-21 1991-04-26 Haessle Ab 1-substituted benzimidazoles and pharmaceutical compositions
DE3830060A1 (de) 1988-09-03 1990-03-15 Boehringer Mannheim Gmbh 2-phenylbenzimidazole - verfahren zu ihrer herstellung sowie diese verbindungen enthaltende arzneimittel
US5552426A (en) 1994-04-29 1996-09-03 Eli Lilly And Company Methods for treating a physiological disorder associated with β-amyloid peptide
JPH09169729A (ja) * 1995-12-19 1997-06-30 Green Cross Corp:The 非ペプチド型インターロイキン8拮抗剤
CA2258728C (en) * 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
JP2000143635A (ja) * 1998-06-10 2000-05-26 Takeda Chem Ind Ltd 血管新生阻害剤
JP2000095767A (ja) * 1998-09-28 2000-04-04 Takeda Chem Ind Ltd 性腺刺激ホルモン放出ホルモン拮抗剤
DE59911249D1 (de) 1998-11-03 2005-01-13 Abbott Gmbh & Co Kg Substituierte 2-phenylbenzimidazole, deren herstellung und anwendung
US20070004713A1 (en) * 2000-12-07 2007-01-04 Bernard Barlaam Therapeutic benimidazole compounds
DE10134775A1 (de) * 2001-07-06 2003-01-30 Schering Ag 1-Alkyl-2.aryl-benzimidazolderivate, deren Verwendung zur Herstellung von Arzneimitteln sowie diese Derivate enthaltende pharmazeutische Präparate
SE0301371D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab New Compounds
KR20070032700A (ko) 2004-05-20 2007-03-22 폴드알엑스 파마슈티칼스, 인크. 트랜스티레틴을 안정화하고 트랜스티레틴 미스폴딩을억제하기 위한, 2-((헤테로)아릴)-벤즈옥사졸 화합물 및유도체, 그리고 조성물 및 방법
RU2007101509A (ru) 2004-06-17 2008-07-27 Уайт (Us) Способ получения антагонистов рецепторов гормона, высвобождающего гонадотропин
WO2006122546A1 (de) * 2005-05-18 2006-11-23 Forschungsverbund Berlin E.V. Nicht-peptidische inhibitoren der akap-pka-wechselwirkung
CA2616512A1 (en) 2005-07-28 2007-02-08 Intervet International B.V. Novel benzimidazole (thio) carbamates with antiparasitic activity and the synthesis thereof
EP1910385B1 (en) 2005-08-04 2013-07-24 Sirtris Pharmaceuticals, Inc. Benzothiazoles and thiazolopyridines as sirtuin modulators
US7915299B2 (en) 2006-11-15 2011-03-29 High Point Pharmaceuticals, Llc 2-(2-hydroxyphenyl)benzimidazoles useful for treating obesity and diabetes
GB0807103D0 (en) 2008-04-18 2008-05-21 Univ Bradford The Compounds
JP2012529449A (ja) * 2009-06-11 2012-11-22 シエナ ビオテク ソシエタ ペル アチオニ ヘッジホッグ経路アンタゴニストおよびそれらの治療的応用
WO2011047129A1 (en) * 2009-10-15 2011-04-21 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
BR112012010738A2 (pt) * 2009-11-06 2019-09-24 Univ Vanderbilt ''aril e heteroaril sulfonas como potenciadores alostéricos de mglur4,composições e métodos de tratamento de disfunção neurológica''
GB201009656D0 (en) 2010-06-09 2010-07-21 Univ St Andrews Carboxylation catalysts
JP5083393B2 (ja) 2010-09-16 2012-11-28 カシオ計算機株式会社 画像表示装置及びプログラム
EP2651405A2 (en) * 2010-12-14 2013-10-23 Electrophoretics Limited Casein kinase 1 (ck1 ) inhibitors
US8865754B2 (en) * 2011-03-03 2014-10-21 Proteotech Inc. Compounds for the treatment of neurodegenerative diseases
AU2013250726B2 (en) 2012-04-20 2017-01-05 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
EA201590482A1 (ru) * 2012-09-05 2015-07-30 Байер Кропсайенс Аг Применение замещенных 2-амидобензимидазолов, 2-амидобензоксазолов и 2-амидобензотиазолов или их солей в качестве биологически активных веществ против абиотического стресса растений
KR101435496B1 (ko) 2012-10-22 2014-08-28 한국과학기술연구원 미토콘드리아 기능 조절제로서의 벤즈이미다졸 유도체
GB201302927D0 (en) * 2013-02-20 2013-04-03 Cancer Therapeutics Crc Pty Ltd Compounds
CN103113307B (zh) * 2013-02-27 2015-08-05 南京大学 苯并咪唑类化合物及其应用
CN104873500A (zh) 2015-04-29 2015-09-02 中国人民解放军第四军医大学 化合物zln005的用途
CA2984971A1 (en) * 2015-05-11 2016-11-17 Kancera Ab Benzimidazole derivates useful as inhibitors of mammalian histone deacetylase activity
RU2747431C2 (ru) * 2015-12-22 2021-05-05 Кансера Аб Бициклические гидроксамовые кислоты, полезные в качестве ингибиторов активности деацетилазы гистонов млекопитающих
JP2018083799A (ja) 2016-11-15 2018-05-31 バイオエレクトロン テクノロジー コーポレイション 2−置換アミノ−ナフト[1,2−d]イミダゾール−5−オン化合物またはその製薬学上許容される塩
US12195432B2 (en) 2018-08-06 2025-01-14 The Board Of Trustees Of The Leland Stanford Junior University 2-arylbenzimidazoles as Ppargc1a activators for treating neurodegenerative diseases

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014179303A1 (en) * 2013-04-29 2014-11-06 The General Hospital Corporation Amyloid precursor protein mrna blockers for treating down syndrome and alzheimer's disease
WO2016061190A1 (en) * 2014-10-14 2016-04-21 The Board Of Trustees Of The Leland Stanford Junior University Method for treating neurodegenerative diseases
WO2017106050A1 (en) * 2015-12-15 2017-06-22 The Board Of Trustees Of The Leland Stanford Junior University Method for preventing and/or treating aging-associated cognitive impairment and neuroinflammation

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BR112021002165A2 (pt) 2021-05-04
AU2019319745A1 (en) 2021-03-25
TW202019410A (zh) 2020-06-01
US12195432B2 (en) 2025-01-14
IL280664A (en) 2021-03-25
US20200299244A1 (en) 2020-09-24
AU2019319745B2 (en) 2025-06-26
MX2021001456A (es) 2021-05-27
IL280664B (en) 2022-12-01
US20210061769A1 (en) 2021-03-04
IL307972A (en) 2023-12-01
IL298535A (en) 2023-01-01
WO2020033359A1 (en) 2020-02-13
CN112805000A (zh) 2021-05-14
SG11202101285YA (en) 2021-03-30
US11111217B2 (en) 2021-09-07
US20210300877A1 (en) 2021-09-30
CN119033775A (zh) 2024-11-29
EP3833344A4 (en) 2022-07-06
IL280664B2 (en) 2023-04-01
US10851066B2 (en) 2020-12-01
MX2023012694A (es) 2023-11-21
JP2021534099A (ja) 2021-12-09
CA3108773A1 (en) 2020-02-13
JP7422737B2 (ja) 2024-01-26
EP3833344A1 (en) 2021-06-16
IL298535B2 (en) 2024-03-01
JP2024056694A (ja) 2024-04-23
KR20210068399A (ko) 2021-06-09
IL298535B1 (en) 2023-11-01

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