JP2020527559A5 - - Google Patents
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- Publication number
- JP2020527559A5 JP2020527559A5 JP2020501505A JP2020501505A JP2020527559A5 JP 2020527559 A5 JP2020527559 A5 JP 2020527559A5 JP 2020501505 A JP2020501505 A JP 2020501505A JP 2020501505 A JP2020501505 A JP 2020501505A JP 2020527559 A5 JP2020527559 A5 JP 2020527559A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- pharmaceutically acceptable
- acceptable salt
- 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 23
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 229910005965 SO 2 Inorganic materials 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000005549 heteroarylene group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 102000013498 tau Proteins Human genes 0.000 claims 3
- 108010026424 tau Proteins Proteins 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000000732 arylene group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004474 heteroalkylene group Chemical group 0.000 claims 2
- -1 nitro, cyano, amino Chemical group 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- 102100032783 Protein cereblon Human genes 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000005001 aminoaryl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 238000006731 degradation reaction Methods 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023062212A JP2023106366A (ja) | 2017-07-12 | 2023-04-06 | タウタンパク質分解の化合物 |
| JP2024209477A JP2025060612A (ja) | 2017-07-12 | 2024-12-02 | タウタンパク質分解の化合物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762531773P | 2017-07-12 | 2017-07-12 | |
| US62/531,773 | 2017-07-12 | ||
| PCT/US2018/041787 WO2019014429A1 (en) | 2017-07-12 | 2018-07-12 | COMPOUNDS FOR THE DEGRADATION OF TAU PROTEIN |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023062212A Division JP2023106366A (ja) | 2017-07-12 | 2023-04-06 | タウタンパク質分解の化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020527559A JP2020527559A (ja) | 2020-09-10 |
| JP2020527559A5 true JP2020527559A5 (enExample) | 2021-08-19 |
| JP7260521B2 JP7260521B2 (ja) | 2023-04-18 |
Family
ID=65001509
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020501505A Active JP7260521B2 (ja) | 2017-07-12 | 2018-07-12 | タウタンパク質分解の化合物 |
| JP2023062212A Withdrawn JP2023106366A (ja) | 2017-07-12 | 2023-04-06 | タウタンパク質分解の化合物 |
| JP2024209477A Pending JP2025060612A (ja) | 2017-07-12 | 2024-12-02 | タウタンパク質分解の化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023062212A Withdrawn JP2023106366A (ja) | 2017-07-12 | 2023-04-06 | タウタンパク質分解の化合物 |
| JP2024209477A Pending JP2025060612A (ja) | 2017-07-12 | 2024-12-02 | タウタンパク質分解の化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20210154184A1 (enExample) |
| EP (2) | EP4310496A3 (enExample) |
| JP (3) | JP7260521B2 (enExample) |
| AU (1) | AU2018300982B2 (enExample) |
| CA (1) | CA3069181A1 (enExample) |
| ES (1) | ES2965049T3 (enExample) |
| WO (1) | WO2019014429A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2894994C (en) | 2012-12-21 | 2019-11-12 | National Institute Of Radiological Sciences | Compounds for imaging tau proteins that accumulate in brain |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| KR20230127371A (ko) * | 2016-11-01 | 2023-08-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법 |
| KR20190134997A (ko) | 2017-02-17 | 2019-12-05 | 데날리 테라퓨틱스 인크. | 항-tau 항체 및 이의 사용 방법 |
| CA3069181A1 (en) * | 2017-07-12 | 2019-01-17 | Dana-Farber Cancer Institute, Inc. | Compounds for tau protein degradation |
| HRP20230183T1 (hr) | 2017-12-21 | 2023-05-12 | Ribon Therapeutics Inc. | Kinazolinoni kao inhibitori parp14 |
| EP3774804A1 (en) | 2018-03-26 | 2021-02-17 | Novartis AG | N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives |
| EP3774772A1 (en) * | 2018-04-13 | 2021-02-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP4272737A3 (en) | 2018-04-23 | 2024-01-17 | Celgene Corporation | Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma |
| JP7293343B2 (ja) | 2018-05-09 | 2023-06-19 | アプリノイア セラピューティクス リミテッド | ヘテロアリール化合物及びその使用 |
| EP3831811A4 (en) | 2018-07-31 | 2022-04-20 | Fimecs, Inc. | HETEROCYCLIC COMPOUND |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| US11389438B2 (en) * | 2019-02-25 | 2022-07-19 | Chdi Foundation, Inc. | Compounds for targeting mutant huntingtin protein and uses thereof |
| KR20210152515A (ko) | 2019-04-12 | 2021-12-15 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스 및 아이올로스의 트리시클릭 분해제 |
| MA56513A (fr) * | 2019-06-19 | 2022-04-27 | Ribon Therapeutics Inc | Dégradation de protéine ciblée de parp14 pour une utilisation en thérapie |
| US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
| EP4031247A1 (en) * | 2019-09-16 | 2022-07-27 | Novartis AG | Bifunctional degraders and their methods of use |
| KR20220100921A (ko) * | 2019-11-13 | 2022-07-18 | 아프리노이아 테라퓨틱스 리미티드 | 타우 단백질 응집체를 분해하기 위한 화합물 및 이의 용도 |
| CN110878095B (zh) * | 2019-12-02 | 2023-01-24 | 中山大学 | 一种姜黄素双功能分子及其制备方法和应用 |
| CA3171337A1 (en) * | 2020-03-18 | 2021-09-23 | Dana-Farber Cancer Institute, Inc. | Targeted degraders of aberrant tau based on the pet tracer pbb3 |
| US20230312639A1 (en) * | 2020-04-23 | 2023-10-05 | University Of Iowa Research Foundation | Gper proteolytic targeting chimeras |
| EP4149505A1 (en) * | 2020-05-15 | 2023-03-22 | Vib Vzw | Means and methods for the treatment of pathological aggregation |
| WO2021242982A1 (en) * | 2020-05-28 | 2021-12-02 | Bristol-Myers Squibb Company | Galectin-3 inhibitors |
| CA3181979A1 (en) * | 2020-06-17 | 2021-12-23 | Fleur M. FERGUSON | Targeted aberrant alpha-synuclein species and induced ubiquitination and proteosomal clearance via co-recruitment of an e3-ligase system |
| WO2022201063A1 (en) * | 2021-03-23 | 2022-09-29 | Covabind Joint Research Private Limited | Nanoparticle composition for targeted protein degradation |
| EP4337259A1 (en) | 2021-05-14 | 2024-03-20 | Aprinoia Therapeutics Limited | Compounds for degrading alpha-synuclein aggregates and uses thereof |
| AU2022288713A1 (en) | 2021-06-07 | 2023-12-21 | Dana-Farber Cancer Institute, Inc. | Inhibitors of ttbk1 |
| CN115504963A (zh) * | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | 一种c-Myc蛋白降解剂 |
| WO2023036936A1 (en) * | 2021-09-09 | 2023-03-16 | Booster Therapeutics Gmbh | Bifunctional molecules as proteasome stimulators for improved targeted protein degradation, and their uses as targeted boosting degraders (tarbods) |
| EP4147723A1 (en) | 2021-09-09 | 2023-03-15 | Booster Therapeutics GmbH | Bifunctional molecules as proteasome stimulators for improved targeted protein degradation, and their uses as targeted boosting degraders (tarbods) |
| WO2024081690A2 (en) * | 2022-10-11 | 2024-04-18 | The General Hospital Corporation | Engineered bifunctional receptors and uses thereof |
| WO2024182633A2 (en) * | 2023-03-01 | 2024-09-06 | The Regents Of The University Of California | Targeted dephosphorylation of tau |
| CN116344058B (zh) * | 2023-05-29 | 2023-08-18 | 之江实验室 | 一种基于图信号的阿尔兹海默风险标注方法及装置 |
| WO2025117551A1 (en) * | 2023-11-27 | 2025-06-05 | Amydis, Inc. | Amino acid derivatives for detecting neurological disorders |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8932557B2 (en) * | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
| US9378662B2 (en) | 2011-08-04 | 2016-06-28 | Ats Holdings Llc | Simplified spine testing device |
| EP3049411B1 (en) * | 2013-09-26 | 2017-04-26 | F. Hoffmann-La Roche AG | Imidazo[1,2-a]pyridin-7-amines as imaging tools |
| TW201605852A (zh) * | 2013-09-26 | 2016-02-16 | 美國禮來大藥廠 | 新穎化合物及其製備ｔａｕ造影劑及ｔａｕ造影調配物之用途 |
| EP3061748A4 (en) * | 2013-10-22 | 2017-04-05 | Clino Ltd. | Tau imaging probe |
| KR20250127179A (ko) * | 2014-04-14 | 2025-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| WO2016197032A1 (en) * | 2015-06-04 | 2016-12-08 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| RU2018105094A (ru) * | 2015-07-13 | 2019-08-14 | Арвинас, Инк. | Модуляторы протеолиза на основе аланина и связанные с ними способы применения |
| EP3331905B1 (en) * | 2015-08-06 | 2022-10-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| US10772962B2 (en) * | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| KR20230127371A (ko) * | 2016-11-01 | 2023-08-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법 |
| CN106543185B (zh) * | 2016-11-10 | 2017-12-15 | 吉林大学 | 一种靶向泛素化降解plk1和brd4蛋白的化合物及其应用 |
| CA3069181A1 (en) * | 2017-07-12 | 2019-01-17 | Dana-Farber Cancer Institute, Inc. | Compounds for tau protein degradation |
-
2018
- 2018-07-12 CA CA3069181A patent/CA3069181A1/en active Pending
- 2018-07-12 EP EP23195169.0A patent/EP4310496A3/en active Pending
- 2018-07-12 JP JP2020501505A patent/JP7260521B2/ja active Active
- 2018-07-12 AU AU2018300982A patent/AU2018300982B2/en active Active
- 2018-07-12 EP EP18831849.7A patent/EP3652329B1/en active Active
- 2018-07-12 WO PCT/US2018/041787 patent/WO2019014429A1/en not_active Ceased
- 2018-07-12 ES ES18831849T patent/ES2965049T3/es active Active
- 2018-07-12 US US16/630,294 patent/US20210154184A1/en not_active Abandoned
-
2023
- 2023-04-06 JP JP2023062212A patent/JP2023106366A/ja not_active Withdrawn
- 2023-05-23 US US18/200,950 patent/US20240091213A1/en active Pending
-
2024
- 2024-12-02 JP JP2024209477A patent/JP2025060612A/ja active Pending
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