JPWO2020257278A5 - - Google Patents
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- Publication number
- JPWO2020257278A5 JPWO2020257278A5 JP2021573829A JP2021573829A JPWO2020257278A5 JP WO2020257278 A5 JPWO2020257278 A5 JP WO2020257278A5 JP 2021573829 A JP2021573829 A JP 2021573829A JP 2021573829 A JP2021573829 A JP 2021573829A JP WO2020257278 A5 JPWO2020257278 A5 JP WO2020257278A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- pharmaceutically acceptable
- bispecific compound
- stereoisomer
- alkyl
- 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 63
- 150000003839 salts Chemical class 0.000 claims description 46
- 238000000034 method Methods 0.000 claims description 31
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 28
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 24
- 125000002837 carbocyclic group Chemical group 0.000 claims description 18
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 208000035475 disorder Diseases 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 13
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 10
- 239000003937 drug carrier Substances 0.000 claims description 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 102100038885 Histone acetyltransferase p300 Human genes 0.000 claims description 7
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 6
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 6
- 206010029260 Neuroblastoma Diseases 0.000 claims description 6
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 6
- 230000001594 aberrant effect Effects 0.000 claims description 5
- 239000002775 capsule Substances 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 5
- 239000003446 ligand Substances 0.000 claims description 5
- 230000008685 targeting Effects 0.000 claims description 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 3
- 208000034578 Multiple myelomas Diseases 0.000 claims description 3
- 102100038895 Myc proto-oncogene protein Human genes 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 3
- 208000029742 colonic neoplasm Diseases 0.000 claims description 3
- 230000001419 dependent effect Effects 0.000 claims description 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 3
- 206010017758 gastric cancer Diseases 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 206010038038 rectal cancer Diseases 0.000 claims description 3
- 201000001275 rectum cancer Diseases 0.000 claims description 3
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 101710155878 Histone acetyltransferase p300 Proteins 0.000 claims description 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 2
- 108091012301 cAMP response element binding protein binding proteins Proteins 0.000 claims description 2
- 102000022531 cAMP response element binding protein binding proteins Human genes 0.000 claims description 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 2
- -1 dimethylaminyl Chemical group 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 4
- 125000005647 linker group Chemical group 0.000 claims 4
- 229920001223 polyethylene glycol Polymers 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 101000941994 Homo sapiens Protein cereblon Proteins 0.000 description 1
- 102100032783 Protein cereblon Human genes 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962862879P | 2019-06-18 | 2019-06-18 | |
| US62/862,879 | 2019-06-18 | ||
| PCT/US2020/038130 WO2020257278A2 (en) | 2019-06-18 | 2020-06-17 | Small molecule target bromo/acetyl proteins and uses thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022537521A JP2022537521A (ja) | 2022-08-26 |
| JP2022537521A5 JP2022537521A5 (https=) | 2023-06-26 |
| JPWO2020257278A5 true JPWO2020257278A5 (https=) | 2023-06-26 |
| JP7626721B2 JP7626721B2 (ja) | 2025-02-04 |
Family
ID=74037322
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021573829A Active JP7626721B2 (ja) | 2019-06-18 | 2020-06-17 | 小分子標的ブロモ／アセチルタンパク質およびその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US12496348B2 (https=) |
| EP (1) | EP3986470A4 (https=) |
| JP (1) | JP7626721B2 (https=) |
| CN (1) | CN114007652A (https=) |
| AU (1) | AU2020295399B2 (https=) |
| CA (1) | CA3143507A1 (https=) |
| WO (1) | WO2020257278A2 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7712867B2 (ja) * | 2018-11-02 | 2025-07-24 | 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 | アセチル化ライター阻害剤の開発およびその使用 |
| JP2024504932A (ja) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス， インコーポレイテッド | イソインドリノン化合物 |
| CN114989158A (zh) * | 2021-03-02 | 2022-09-02 | 复旦大学 | 组蛋白乙酰转移酶p300溴结构域抑制剂及其药用组合物及其应用 |
| CN117321053A (zh) * | 2021-06-07 | 2023-12-29 | 贝达药业股份有限公司 | P300抑制剂及其在医药上的应用 |
| CN118359600A (zh) * | 2023-01-17 | 2024-07-19 | 中国科学院广州生物医药与健康研究院 | 一种芳基咪唑基异恶唑类化合物及其制备方法和应用 |
| CN121005703A (zh) * | 2024-05-24 | 2025-11-25 | 中国科学院广州生物医药与健康研究院 | 一种酰胺吲嗪类化合物及其制备方法和应用 |
| CN119707936B (zh) * | 2025-02-25 | 2025-07-25 | 中南大学 | 一种2,4-二取代-5-氟嘧啶衍生物的盐的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2016004570A (es) | 2013-10-11 | 2016-09-08 | Genentech Inc | Uso de inhibidores del bromodominio de cbp/ep300 para la inmunoterapia del cáncer. |
| WO2016055028A1 (en) | 2014-10-10 | 2016-04-14 | Genentech, Inc. | Therapeutic compounds and uses thereof |
| 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 |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| CN109641874A (zh) * | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| EP4717317A2 (en) * | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| MX2020003190A (es) | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| JP7712867B2 (ja) * | 2018-11-02 | 2025-07-24 | 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 | アセチル化ライター阻害剤の開発およびその使用 |
-
2020
- 2020-06-17 AU AU2020295399A patent/AU2020295399B2/en active Active
- 2020-06-17 CN CN202080044388.9A patent/CN114007652A/zh active Pending
- 2020-06-17 EP EP20825420.1A patent/EP3986470A4/en active Pending
- 2020-06-17 US US17/617,226 patent/US12496348B2/en active Active
- 2020-06-17 CA CA3143507A patent/CA3143507A1/en active Pending
- 2020-06-17 WO PCT/US2020/038130 patent/WO2020257278A2/en not_active Ceased
- 2020-06-17 JP JP2021573829A patent/JP7626721B2/ja active Active
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