JP2019511528A5 - - Google Patents
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- JP2019511528A5 JP2019511528A5 JP2018553365A JP2018553365A JP2019511528A5 JP 2019511528 A5 JP2019511528 A5 JP 2019511528A5 JP 2018553365 A JP2018553365 A JP 2018553365A JP 2018553365 A JP2018553365 A JP 2018553365A JP 2019511528 A5 JP2019511528 A5 JP 2019511528A5
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- JP
- Japan
- Prior art keywords
- group
- pharmaceutically acceptable
- acceptable salt
- solvate
- formula
- 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
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- 0 **1C(*)=*C=C1* Chemical compound **1C(*)=*C=C1* 0.000 description 6
- LCNLCZYJDNFGLE-UHFFFAOYSA-N CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(C(NCCOCCOCCOCCOCCOCCOCCOCCNc(cccc2C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)=O)n1 Chemical compound CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(C(NCCOCCOCCOCCOCCOCCOCCOCCNc(cccc2C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)=O)n1 LCNLCZYJDNFGLE-UHFFFAOYSA-N 0.000 description 1
- KELXSFPNQGNTTJ-UHFFFAOYSA-N CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(CNCCCCNc2cccc(C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)n1 Chemical compound CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(CNCCCCNc2cccc(C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)n1 KELXSFPNQGNTTJ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662321499P | 2016-04-12 | 2016-04-12 | |
| US62/321,499 | 2016-04-12 | ||
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| US62/393,888 | 2016-09-13 | ||
| PCT/US2017/026278 WO2017180417A1 (en) | 2016-04-12 | 2017-04-06 | Bet protein degraders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019511528A JP2019511528A (ja) | 2019-04-25 |
| JP2019511528A5 true JP2019511528A5 (enExample) | 2020-05-14 |
| JP7072519B2 JP7072519B2 (ja) | 2022-05-20 |
Family
ID=58548921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018553365A Expired - Fee Related JP7072519B2 (ja) | 2016-04-12 | 2017-04-06 | Betタンパク質分解剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10633386B2 (enExample) |
| EP (1) | EP3442976B1 (enExample) |
| JP (1) | JP7072519B2 (enExample) |
| KR (1) | KR20180132861A (enExample) |
| CN (1) | CN109311890B (enExample) |
| AU (1) | AU2017250076B2 (enExample) |
| BR (1) | BR112018070859A2 (enExample) |
| CA (1) | CA3020541A1 (enExample) |
| IL (1) | IL262139B (enExample) |
| MX (1) | MX384905B (enExample) |
| RU (1) | RU2752677C2 (enExample) |
| SG (1) | SG11201808729WA (enExample) |
| UA (1) | UA123168C2 (enExample) |
| WO (1) | WO2017180417A1 (enExample) |
| ZA (1) | ZA201806969B (enExample) |
Families Citing this family (46)
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| AU2019323446B2 (en) | 2018-08-22 | 2025-01-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
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| EP3846800A4 (en) | 2018-09-04 | 2022-08-24 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| US12459921B2 (en) * | 2018-09-30 | 2025-11-04 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Isoindoline compound, preparation method, pharmaceutical composition and use thereof |
| EP3863642A4 (en) * | 2018-10-09 | 2022-06-29 | The Regents of the University of California | Covalent targeting of e3 ligases |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| EP3908291A4 (en) * | 2019-01-07 | 2023-01-11 | Dana-Farber Cancer Institute, Inc. | SMALL MOLECULAR DEGRADERS OF FKBP12 VIA RECRUITMENT OF THE VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) AND USE IN DTAG SYSTEMS |
| BR112021014220A2 (pt) * | 2019-01-22 | 2022-01-18 | Merck Patent Gmbh | Derivados heterocíclicos |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | C4 Therapeutics Inc | Heterocyclic compounds for medical treatment |
| WO2020249048A1 (zh) * | 2019-06-12 | 2020-12-17 | 上海科技大学 | Alk蛋白调节剂及其抗肿瘤应用 |
| TW202126638A (zh) * | 2019-09-30 | 2021-07-16 | 日商協和麒麟股份有限公司 | Bet分解劑 |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| JP7692924B2 (ja) | 2020-02-26 | 2025-06-16 | クルゲン(シャンハイ),インク. | トロポミオシン受容体キナーゼ(trk)分解化合物とその使用方法 |
| IL295709A (en) | 2020-03-05 | 2022-10-01 | C4 Therapeutics Inc | Compounds for targeted degradation of brd9 |
| CN113387932B (zh) * | 2020-03-14 | 2023-05-09 | 成都先导药物开发股份有限公司 | 一种诱导brd4蛋白降解的双功能化合物 |
| CN112920176B (zh) * | 2020-05-25 | 2022-11-04 | 四川大学华西医院 | 可诱导prc2蛋白复合物核心亚基降解的双功能化合物和药物组合物及应用 |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| WO2022051616A1 (en) * | 2020-09-03 | 2022-03-10 | Board Of Regents Of The University Of Nebraska | Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras |
| BR112023023065A2 (pt) | 2021-05-05 | 2024-01-30 | Biogen Ma Inc | Compostos para direcionar a degradação da tirosina quinase de bruton |
| CN113336801B (zh) * | 2021-06-08 | 2023-08-22 | 中国人民解放军空军军医大学 | 含有bet抑制剂的四价铂配合物与应用 |
| KR20240035526A (ko) | 2021-07-07 | 2024-03-15 | 바이오젠 엠에이 인코포레이티드 | Irak4 단백질의 분해를 표적하는 화합물 |
| JP2024525580A (ja) | 2021-07-07 | 2024-07-12 | バイオジェン・エムエイ・インコーポレイテッド | Irak4タンパク質の分解をターゲティングするための化合物 |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| AU2023298115A1 (en) | 2022-06-27 | 2025-01-16 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and use thereof |
| WO2024050016A1 (en) | 2022-08-31 | 2024-03-07 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| CN116585322B (zh) * | 2023-01-16 | 2023-10-13 | 中山大学中山眼科中心 | Bet蛋白降解剂在预防和治疗视网膜退行性改变相关疾病中的应用 |
| EP4720059A1 (en) | 2023-05-24 | 2026-04-08 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| WO2025049555A1 (en) | 2023-08-31 | 2025-03-06 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| TW202523291A (zh) | 2023-11-02 | 2025-06-16 | 美商金橘生物科技公司 | 降解劑及其用途 |
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-
2017
- 2017-04-06 AU AU2017250076A patent/AU2017250076B2/en not_active Ceased
- 2017-04-06 UA UAA201811059A patent/UA123168C2/uk unknown
- 2017-04-06 CA CA3020541A patent/CA3020541A1/en active Pending
- 2017-04-06 RU RU2018139537A patent/RU2752677C2/ru active
- 2017-04-06 BR BR112018070859A patent/BR112018070859A2/pt not_active IP Right Cessation
- 2017-04-06 CN CN201780036434.9A patent/CN109311890B/zh not_active Expired - Fee Related
- 2017-04-06 EP EP17717993.4A patent/EP3442976B1/en active Active
- 2017-04-06 KR KR1020187032621A patent/KR20180132861A/ko not_active Abandoned
- 2017-04-06 US US16/093,160 patent/US10633386B2/en active Active
- 2017-04-06 JP JP2018553365A patent/JP7072519B2/ja not_active Expired - Fee Related
- 2017-04-06 MX MX2018012379A patent/MX384905B/es unknown
- 2017-04-06 SG SG11201808729WA patent/SG11201808729WA/en unknown
- 2017-04-06 WO PCT/US2017/026278 patent/WO2017180417A1/en not_active Ceased
-
2018
- 2018-10-04 IL IL262139A patent/IL262139B/en active IP Right Grant
- 2018-10-18 ZA ZA2018/06969A patent/ZA201806969B/en unknown