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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- Prior art keywords
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- pharmaceutically acceptable
- acceptable salt
- solvate
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- 150000001875 compounds Chemical class 0.000 claims description 91
- 150000003839 salts Chemical class 0.000 claims description 86
- 239000012453 solvate Substances 0.000 claims description 86
- 206010028980 Neoplasm Diseases 0.000 claims description 38
- 201000011510 cancer Diseases 0.000 claims description 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 11
- 125000003107 substituted aryl group Chemical group 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 208000023275 Autoimmune disease Diseases 0.000 claims description 7
- 206010040047 Sepsis Diseases 0.000 claims description 7
- 208000036142 Viral infection Diseases 0.000 claims description 7
- 230000001684 chronic effect Effects 0.000 claims description 7
- 230000004968 inflammatory condition Effects 0.000 claims description 7
- 230000002062 proliferating effect Effects 0.000 claims description 7
- 230000009385 viral infection Effects 0.000 claims description 7
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 125000005466 alkylenyl group Chemical group 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 10
- 208000000587 small cell lung carcinoma Diseases 0.000 description 10
- 238000000034 method Methods 0.000 description 7
- 0 **1C(*)=*C=C1* Chemical compound **1C(*)=*C=C1* 0.000 description 6
- 206010000871 Acute monocytic leukaemia Diseases 0.000 description 5
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 5
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 description 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 5
- 206010006187 Breast cancer Diseases 0.000 description 5
- 208000026310 Breast neoplasm Diseases 0.000 description 5
- 208000011691 Burkitt lymphomas Diseases 0.000 description 5
- 206010008342 Cervix carcinoma Diseases 0.000 description 5
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 5
- 206010009944 Colon cancer Diseases 0.000 description 5
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 5
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 5
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 description 5
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 description 5
- 208000034578 Multiple myelomas Diseases 0.000 description 5
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 5
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 5
- 206010029260 Neuroblastoma Diseases 0.000 description 5
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 5
- 206010033128 Ovarian cancer Diseases 0.000 description 5
- 206010061535 Ovarian neoplasm Diseases 0.000 description 5
- 206010035226 Plasma cell myeloma Diseases 0.000 description 5
- 206010060862 Prostate cancer Diseases 0.000 description 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 5
- 201000010881 cervical cancer Diseases 0.000 description 5
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 description 5
- 201000004101 esophageal cancer Diseases 0.000 description 5
- 208000032839 leukemia Diseases 0.000 description 5
- 208000035475 disorder Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 239000000090 biomarker Substances 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 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
- 101100218425 Gallus gallus BCL2L1 gene Proteins 0.000 description 1
- 101001056180 Homo sapiens Induced myeloid leukemia cell differentiation protein Mcl-1 Proteins 0.000 description 1
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 239000000126 substance Substances 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 Active 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 (45)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2017185036A1 (en) | 2016-04-22 | 2017-10-26 | Dana Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| EP4483875A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| US11285218B2 (en) * | 2016-06-23 | 2022-03-29 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use |
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| CN109422751B (zh) * | 2017-09-03 | 2022-04-22 | 上海美志医药科技有限公司 | 一类具有降解酪氨酸蛋白激酶jak3活性的化合物 |
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| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| CA3082077A1 (en) * | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l degraders and methods of treatment therewith |
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| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
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| WO2020064002A1 (zh) * | 2018-09-30 | 2020-04-02 | 中国科学院上海药物研究所 | 异吲哚啉类化合物、其制备方法、药物组合物及用途 |
| WO2020076996A1 (en) * | 2018-10-09 | 2020-04-16 | The Regents Of The University Of California | Covalent targeting of e3 ligases |
| WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| WO2020146250A1 (en) * | 2019-01-07 | 2020-07-16 | Dana-Farber Cancer Institute, Inc. | SMALL MOLECULE DEGRADERS OF FKBP12 VIA RECRUITMENT OF VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) E3 UBIQUITIN LIGASE, AND USES IN dTAG SYSTEMS |
| BR112021014220A2 (pt) * | 2019-01-22 | 2022-01-18 | Merck Patent Gmbh | Derivados heterocíclicos |
| KR102758231B1 (ko) * | 2019-06-12 | 2025-01-23 | 상하이테크 유니버시티 | Alk 단백질 조절제 및 이의 항종양 용도 |
| AU2020360170A1 (en) * | 2019-09-30 | 2022-05-19 | Kyowa Kirin Co., Ltd. | Bet degrader |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US12410171B2 (en) | 2020-02-26 | 2025-09-09 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | 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 |
| CA3188313A1 (en) | 2020-08-05 | 2022-02-10 | 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 |
| EP4333899A1 (en) | 2021-05-05 | 2024-03-13 | Biogen MA Inc. | Compounds for targeting degradation of bruton's tyrosine kinase |
| 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 |
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| 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 |
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| WO2025096855A1 (en) | 2023-11-02 | 2025-05-08 | Kumquat Biosciences Inc. | Degraders and uses thereof |
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2017
- 2017-04-06 AU AU2017250076A patent/AU2017250076B2/en not_active Ceased
- 2017-04-06 SG SG11201808729WA patent/SG11201808729WA/en unknown
- 2017-04-06 MX MX2018012379A patent/MX384905B/es unknown
- 2017-04-06 UA UAA201811059A patent/UA123168C2/uk unknown
- 2017-04-06 RU RU2018139537A patent/RU2752677C2/ru active
- 2017-04-06 KR KR1020187032621A patent/KR20180132861A/ko not_active Abandoned
- 2017-04-06 EP EP17717993.4A patent/EP3442976B1/en active Active
- 2017-04-06 CA CA3020541A patent/CA3020541A1/en active Pending
- 2017-04-06 CN CN201780036434.9A patent/CN109311890B/zh not_active Expired - Fee Related
- 2017-04-06 US US16/093,160 patent/US10633386B2/en active Active
- 2017-04-06 WO PCT/US2017/026278 patent/WO2017180417A1/en not_active Ceased
- 2017-04-06 BR BR112018070859A patent/BR112018070859A2/pt not_active IP Right Cessation
- 2017-04-06 JP JP2018553365A patent/JP7072519B2/ja active Active
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2018
- 2018-10-04 IL IL262139A patent/IL262139B/en active IP Right Grant
- 2018-10-18 ZA ZA2018/06969A patent/ZA201806969B/en unknown
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