JPWO2020219650A5 - - Google Patents
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- Publication number
- JPWO2020219650A5 JPWO2020219650A5 JP2021562085A JP2021562085A JPWO2020219650A5 JP WO2020219650 A5 JPWO2020219650 A5 JP WO2020219650A5 JP 2021562085 A JP2021562085 A JP 2021562085A JP 2021562085 A JP2021562085 A JP 2021562085A JP WO2020219650 A5 JPWO2020219650 A5 JP WO2020219650A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- formula
- optionally
- pharmaceutically acceptable
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 22
- 239000013078 crystal Substances 0.000 claims 16
- 239000000651 prodrug Substances 0.000 claims 16
- 229940002612 prodrug Drugs 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 239000012453 solvate Substances 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000000547 substituted alkyl group Chemical group 0.000 claims 11
- 125000002252 acyl group Chemical group 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000004452 carbocyclyl group Chemical group 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 5
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 102100038111 Cyclin-dependent kinase 12 Human genes 0.000 claims 1
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims 1
- 101000884345 Homo sapiens Cyclin-dependent kinase 12 Proteins 0.000 claims 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 238000006731 degradation reaction Methods 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962837331P | 2019-04-23 | 2019-04-23 | |
| US62/837,331 | 2019-04-23 | ||
| PCT/US2020/029483 WO2020219650A1 (en) | 2019-04-23 | 2020-04-23 | Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022529700A JP2022529700A (ja) | 2022-06-23 |
| JPWO2020219650A5 true JPWO2020219650A5 (enExample) | 2023-05-01 |
Family
ID=72941778
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021562085A Pending JP2022529700A (ja) | 2019-04-23 | 2020-04-23 | サイクリン依存性キナーゼ１２（ｃｄｋ１２）の分解剤およびその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20220227734A1 (enExample) |
| EP (1) | EP3958861A4 (enExample) |
| JP (1) | JP2022529700A (enExample) |
| CN (1) | CN113993519B (enExample) |
| AU (1) | AU2020263390B2 (enExample) |
| CA (1) | CA3132387A1 (enExample) |
| WO (1) | WO2020219650A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| BR112021024108A2 (pt) | 2019-05-31 | 2022-03-22 | Ikena Oncology Inc | Inibidores de tead e usos dos mesmos |
| TW202108559A (zh) | 2019-05-31 | 2021-03-01 | 美商醫肯納腫瘤學公司 | Tead抑制劑及其用途 |
| US20220233702A1 (en) * | 2019-06-03 | 2022-07-28 | Regents Of The University Of Minnesota | Compounds that degrade kinases and uses thereof |
| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
| WO2022120355A1 (en) * | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| JP2024537394A (ja) * | 2021-10-14 | 2024-10-10 | クルゲン（シャンハイ），インク． | 修飾タンパク質およびタンパク質分解剤 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| WO2023143482A1 (zh) * | 2022-01-29 | 2023-08-03 | 上海辉启生物医药科技有限公司 | 2-氨基嘧啶类化合物或其盐及其制备方法和用途 |
| CN121358732A (zh) * | 2023-03-07 | 2026-01-16 | 睿跃生物科技有限公司 | 治疗癌症的化合物和方法 |
| CN119950745B (zh) * | 2025-01-14 | 2025-10-17 | 浙江大学 | 一种药物组合物及其在制备抗肿瘤药物中的应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2666530C2 (ru) * | 2012-01-12 | 2018-09-11 | Йейл Юниверсити | Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы |
| EP3057954A2 (en) * | 2013-10-18 | 2016-08-24 | Syros Pharmaceuticals, Inc. | Heteromaromatic compounds useful for the treatment of proliferative diseases |
| AU2014337122B2 (en) * | 2013-10-18 | 2019-01-03 | Dana-Farber Cancer Institute, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
| LT3126352T (lt) * | 2014-04-04 | 2019-01-10 | Syros Pharmaceuticals, Inc. | Nuo ciklino priklausomos kinazės 7 (cdk7) inhibitoriai |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| JP6927999B2 (ja) * | 2016-04-22 | 2021-09-01 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ９（ｃｄｋ９）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ９の分解および使用法 |
| CA3018434A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| KR102587758B1 (ko) * | 2016-07-13 | 2023-10-12 | 사이로스 파마수티컬스, 인크. | 시클린-의존성 키나제 7 (cdk7)의 억제제 |
| CA3041563C (en) * | 2016-11-22 | 2023-10-31 | Dana-Farber Cancer Institute, Inc. | Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12) |
| WO2020023480A1 (en) * | 2018-07-23 | 2020-01-30 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
-
2020
- 2020-04-23 JP JP2021562085A patent/JP2022529700A/ja active Pending
- 2020-04-23 EP EP20795755.6A patent/EP3958861A4/en active Pending
- 2020-04-23 AU AU2020263390A patent/AU2020263390B2/en active Active
- 2020-04-23 US US17/604,852 patent/US20220227734A1/en active Pending
- 2020-04-23 WO PCT/US2020/029483 patent/WO2020219650A1/en not_active Ceased
- 2020-04-23 CA CA3132387A patent/CA3132387A1/en active Pending
- 2020-04-23 CN CN202080044331.9A patent/CN113993519B/zh active Active
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