JPWO2020076996A5 - - Google Patents
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- Publication number
- JPWO2020076996A5 JPWO2020076996A5 JP2021519602A JP2021519602A JPWO2020076996A5 JP WO2020076996 A5 JPWO2020076996 A5 JP WO2020076996A5 JP 2021519602 A JP2021519602 A JP 2021519602A JP 2021519602 A JP2021519602 A JP 2021519602A JP WO2020076996 A5 JPWO2020076996 A5 JP WO2020076996A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- nhc
- och
- nhnh
- 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
- 125000003118 aryl group Chemical group 0.000 claims 28
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 28
- 229910052736 halogen Inorganic materials 0.000 claims 23
- 150000002367 halogens Chemical class 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 22
- 125000004404 heteroalkyl group Chemical group 0.000 claims 22
- -1 -CONH2 Chemical group 0.000 claims 16
- 229910006069 SO3H Inorganic materials 0.000 claims 16
- 239000011230 binding agent Substances 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 13
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 13
- 125000005647 linker group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 102000004169 proteins and genes Human genes 0.000 claims 8
- 108090000623 proteins and genes Proteins 0.000 claims 8
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims 7
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 7
- 125000000732 arylene group Chemical group 0.000 claims 7
- 125000004474 heteroalkylene group Chemical group 0.000 claims 7
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 7
- 125000005549 heteroarylene group Chemical group 0.000 claims 6
- 125000002993 cycloalkylene group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000004406 C3-C8 cycloalkylene group Chemical group 0.000 claims 3
- 230000001413 cellular effect Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006587 (C5-C10) heteroarylene group Chemical group 0.000 claims 1
- 108091005625 BRD4 Proteins 0.000 claims 1
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2025017433A JP2025072508A (ja) | 2018-10-09 | 2025-02-05 | Ｅ３リガーゼの共有結合による標的化 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862743337P | 2018-10-09 | 2018-10-09 | |
| US62/743,337 | 2018-10-09 | ||
| PCT/US2019/055461 WO2020076996A1 (en) | 2018-10-09 | 2019-10-09 | Covalent targeting of e3 ligases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025017433A Division JP2025072508A (ja) | 2018-10-09 | 2025-02-05 | Ｅ３リガーゼの共有結合による標的化 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022512643A JP2022512643A (ja) | 2022-02-07 |
| JPWO2020076996A5 true JPWO2020076996A5 (enExample) | 2022-10-18 |
| JP7631191B2 JP7631191B2 (ja) | 2025-02-18 |
Family
ID=70164411
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021519602A Active JP7631191B2 (ja) | 2018-10-09 | 2019-10-09 | Ｅ３リガーゼの共有結合による標的化 |
| JP2025017433A Pending JP2025072508A (ja) | 2018-10-09 | 2025-02-05 | Ｅ３リガーゼの共有結合による標的化 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025017433A Pending JP2025072508A (ja) | 2018-10-09 | 2025-02-05 | Ｅ３リガーゼの共有結合による標的化 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US12161648B2 (enExample) |
| EP (1) | EP3863642A4 (enExample) |
| JP (2) | JP7631191B2 (enExample) |
| CN (2) | CN113164495B (enExample) |
| WO (1) | WO2020076996A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11666661B2 (en) | 2018-03-23 | 2023-06-06 | The Regents Of The University Of California | Methods and compounds for targeted autophagy |
| GB202005876D0 (en) * | 2020-04-22 | 2020-06-03 | Univ Dundee | Protein degradation |
| EP4188907A1 (en) * | 2020-07-30 | 2023-06-07 | Sanofi | Acrylamide-substituted indane compounds and therapeutic use thereof |
| KR20230144008A (ko) * | 2021-01-08 | 2023-10-13 | 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 | 님볼리드 유사체 및 이의 사용 방법 |
| WO2022187650A1 (en) * | 2021-03-04 | 2022-09-09 | The Scripps Research Institute | Heterobifunctional compositions for targeted protein degradation and methods for their use |
| EP4313979A4 (en) * | 2021-03-25 | 2025-02-19 | Technion Research & Development Foundation Limited | RNF4-TARGETED COMPOUNDS AND USES THEREOF |
| CN113527270B (zh) * | 2021-07-16 | 2024-03-01 | 河南大学 | 一种靶向单酰基甘油脂肪酶的protac分子的医药中间体、制备方法及应用 |
| CN116676273A (zh) * | 2022-02-22 | 2023-09-01 | 中国科学院深圳先进技术研究院 | 一种蛋白水解靶向流感病毒及其制备方法和应用 |
| CN114560908B (zh) * | 2022-03-11 | 2024-10-25 | 国家纳米科学中心 | 一种多肽protac分子及其制备方法和应用 |
| CN115417913B (zh) * | 2022-08-26 | 2024-10-29 | 天津医科大学 | 靶向雌激素受体的谷胱甘肽响应protac降解剂的制备方法及应用 |
| TW202416958A (zh) * | 2022-10-13 | 2024-05-01 | 南韓商韓美藥品股份有限公司 | 用於抑制yap-tead交互作用的新穎雜雙環化合物及包含其之藥學組成物 |
| EP4605088A1 (en) * | 2022-10-21 | 2025-08-27 | Novartis AG | Molecular glue degrader compounds and uses thereof |
| WO2025226951A1 (en) * | 2024-04-24 | 2025-10-30 | Novartis Ag | Molecular glue degrader compounds and uses thereof |
| CN119331047B (zh) * | 2024-10-09 | 2025-09-30 | 重庆医科大学 | 一种蛋白水解靶向嵌合体及其制备方法 |
| CN119405823B (zh) * | 2024-11-15 | 2025-10-21 | 湖南大学 | 一种基于g四链体rna的蛋白降解靶向嵌合体及其制备方法与应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040171074A1 (en) * | 2002-10-17 | 2004-09-02 | Mount Sinai Hospital | Structures of substrate binding pockets of SCF complexes |
| HUE031073T2 (en) * | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| CN101928747B (zh) | 2010-08-31 | 2012-08-08 | 中国人民解放军第二军医大学 | E3泛素连接酶chip在脑胶质瘤疾病中的应用 |
| EP2846784A4 (en) | 2012-05-11 | 2016-03-09 | Univ Yale | COMPOUNDS FOR PROMOTING PROTEIN REMOVAL AND PROCESS THEREFOR |
| US20180228907A1 (en) * | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| CN104017879A (zh) * | 2014-06-16 | 2014-09-03 | 山东大学 | Fbxo31基因及其相关产物在制备胃癌诊断试剂中的应用 |
| JP7011467B2 (ja) * | 2015-05-29 | 2022-02-10 | ザ・トラステイーズ・オブ・ザ・ユニバーシテイ・オブ・ペンシルベニア | ミスフォールドタンパク質の分解のための組成物及び方法 |
| PE20181298A1 (es) | 2015-11-25 | 2018-08-07 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos |
| RU2752677C2 (ru) * | 2016-04-12 | 2021-07-29 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Деструкторы белка вет |
| JP6961684B2 (ja) * | 2016-09-13 | 2021-11-05 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔタンパク質分解物質としての縮合１，４−オキサゼピン |
| WO2020146779A1 (en) * | 2019-01-11 | 2020-07-16 | The Regents Of The University Of California | mTORC1 INHIBITORS FOR ACTIVATING AUTOPHAGY |
-
2019
- 2019-10-09 US US17/282,277 patent/US12161648B2/en active Active
- 2019-10-09 WO PCT/US2019/055461 patent/WO2020076996A1/en not_active Ceased
- 2019-10-09 CN CN201980079494.8A patent/CN113164495B/zh active Active
- 2019-10-09 CN CN202510552209.7A patent/CN120468320A/zh active Pending
- 2019-10-09 JP JP2021519602A patent/JP7631191B2/ja active Active
- 2019-10-09 EP EP19872219.1A patent/EP3863642A4/en active Pending
-
2024
- 2024-10-02 US US18/904,492 patent/US20250120982A1/en active Pending
-
2025
- 2025-02-05 JP JP2025017433A patent/JP2025072508A/ja active Pending
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