JPWO2020033359A5 - - Google Patents
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- Publication number
- JPWO2020033359A5 JPWO2020033359A5 JP2021506624A JP2021506624A JPWO2020033359A5 JP WO2020033359 A5 JPWO2020033359 A5 JP WO2020033359A5 JP 2021506624 A JP2021506624 A JP 2021506624A JP 2021506624 A JP2021506624 A JP 2021506624A JP WO2020033359 A5 JPWO2020033359 A5 JP WO2020033359A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- perfluoro
- hydrogen
- halo
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 208000028698 Cognitive impairment Diseases 0.000 claims description 3
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims description 3
- 230000032683 aging Effects 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 230000003959 neuroinflammation Effects 0.000 claims description 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 26
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000001475 halogen functional group Chemical group 0.000 claims 16
- -1 hydroxy, carboxy Chemical group 0.000 claims 15
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 14
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 10
- 229910052805 deuterium Inorganic materials 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000003282 alkyl amino group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 7
- 125000006657 (C1-C10) hydrocarbyl group Chemical group 0.000 claims 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 6
- 125000005518 carboxamido group Chemical group 0.000 claims 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000004442 acylamino group Chemical group 0.000 claims 3
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 3
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 125000003275 alpha amino acid group Chemical group 0.000 claims 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 3
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 3
- 150000002825 nitriles Chemical class 0.000 claims 3
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 208000016192 Demyelinating disease Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000026072 Motor neurone disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 238000000034 method Methods 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 239000002953 phosphate buffered saline Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 238000007792 addition Methods 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000013160 medical therapy Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024004449A JP2024056694A (ja) | 2018-08-06 | 2024-01-16 | 神経変性疾患を治療するためのＰｐａｒｇｃ１ａ活性化剤としての２‐アリールベンゾイミダゾール |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862714962P | 2018-08-06 | 2018-08-06 | |
| US62/714,962 | 2018-08-06 | ||
| PCT/US2019/045229 WO2020033359A1 (en) | 2018-08-06 | 2019-08-06 | 2-arylbenzimidazoles as ppargc1a activators for treating neurodegenerative diseases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024004449A Division JP2024056694A (ja) | 2018-08-06 | 2024-01-16 | 神経変性疾患を治療するためのＰｐａｒｇｃ１ａ活性化剤としての２‐アリールベンゾイミダゾール |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021534099A JP2021534099A (ja) | 2021-12-09 |
| JPWO2020033359A5 true JPWO2020033359A5 (https=) | 2022-08-12 |
| JP2021534099A5 JP2021534099A5 (https=) | 2022-08-12 |
| JP7422737B2 JP7422737B2 (ja) | 2024-01-26 |
Family
ID=69413327
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021506624A Active JP7422737B2 (ja) | 2018-08-06 | 2019-08-06 | 神経変性疾患を治療するためのＰｐａｒｇｃ１ａ活性化剤としての２‐アリールベンゾイミダゾール |
| JP2024004449A Pending JP2024056694A (ja) | 2018-08-06 | 2024-01-16 | 神経変性疾患を治療するためのＰｐａｒｇｃ１ａ活性化剤としての２‐アリールベンゾイミダゾール |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024004449A Pending JP2024056694A (ja) | 2018-08-06 | 2024-01-16 | 神経変性疾患を治療するためのＰｐａｒｇｃ１ａ活性化剤としての２‐アリールベンゾイミダゾール |
Country Status (13)
| Country | Link |
|---|---|
| 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)
| 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 |
Family Cites Families (42)
| 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 |
| US10022357B2 (en) | 2013-04-29 | 2018-07-17 | The General Hospital Corporation | Amyloid precursor protein MRNA blockers for treating Down syndrome and Alzheimer's disease |
| US10272070B2 (en) | 2014-10-14 | 2019-04-30 | The Board of Trustees of the Leland Stanford Junio r University | Method for treating neurodegenerative diseases |
| 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 |
| PT3390367T (pt) * | 2015-12-15 | 2020-09-23 | Univ Leland Stanford Junior | Método para prevenir e/ou tratar enfraquecimento cognitivo e neuroinflamação associados ao envelhecimento |
| 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 |
-
2019
- 2019-08-06 US US17/266,433 patent/US12195432B2/en active Active
- 2019-08-06 JP JP2021506624A patent/JP7422737B2/ja active Active
- 2019-08-06 MX MX2021001456A patent/MX2021001456A/es unknown
- 2019-08-06 WO PCT/US2019/045229 patent/WO2020033359A1/en not_active Ceased
- 2019-08-06 IL IL280664A patent/IL280664B2/en unknown
- 2019-08-06 CN CN201980065941.4A patent/CN112805000A/zh active Pending
- 2019-08-06 EP EP19845943.0A patent/EP3833344A4/en active Pending
- 2019-08-06 IL IL307972A patent/IL307972A/en unknown
- 2019-08-06 KR KR1020217006736A patent/KR20210068399A/ko not_active Ceased
- 2019-08-06 CN CN202411199938.0A patent/CN119033775A/zh active Pending
- 2019-08-06 SG SG11202101285YA patent/SG11202101285YA/en unknown
- 2019-08-06 BR BR112021002165-5A patent/BR112021002165A2/pt not_active Application Discontinuation
- 2019-08-06 TW TW108127925A patent/TWI904076B/zh active
- 2019-08-06 CA CA3108773A patent/CA3108773A1/en active Pending
- 2019-08-06 AU AU2019319745A patent/AU2019319745B2/en active Active
- 2019-08-06 IL IL298535A patent/IL298535B2/en unknown
-
2020
- 2020-05-29 US US16/888,040 patent/US10851066B2/en active Active
- 2020-10-13 US US17/068,985 patent/US11111217B2/en active Active
-
2021
- 2021-02-04 MX MX2023012694A patent/MX2023012694A/es unknown
-
2024
- 2024-01-16 JP JP2024004449A patent/JP2024056694A/ja active Pending
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