JP2019514876A5 - - Google Patents
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- JP2019514876A5 JP2019514876A5 JP2018555152A JP2018555152A JP2019514876A5 JP 2019514876 A5 JP2019514876 A5 JP 2019514876A5 JP 2018555152 A JP2018555152 A JP 2018555152A JP 2018555152 A JP2018555152 A JP 2018555152A JP 2019514876 A5 JP2019514876 A5 JP 2019514876A5
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- 150000001875 compounds Chemical class 0.000 claims description 50
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- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 18
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 18
- 239000003446 ligand Substances 0.000 claims description 17
- 230000008685 targeting Effects 0.000 claims description 17
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 206010028980 Neoplasm Diseases 0.000 claims description 13
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 12
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 102000013742 Cyclin-Dependent Kinase 8 Human genes 0.000 claims description 9
- 108010025415 Cyclin-Dependent Kinase 8 Proteins 0.000 claims description 9
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
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- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
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- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
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- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 230000001105 regulatory effect Effects 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
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- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326584P | 2016-04-22 | 2016-04-22 | |
| US62/326,584 | 2016-04-22 | ||
| PCT/US2017/028948 WO2017185034A1 (en) | 2016-04-22 | 2017-04-21 | Degradation of cyclin-dependent kinase 8 (cdk8) by conjugation of cdk8 inhibitors with e3 ligase ligand and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019514876A JP2019514876A (ja) | 2019-06-06 |
| JP2019514876A5 true JP2019514876A5 (OSRAM) | 2020-05-28 |
| JP6921114B2 JP6921114B2 (ja) | 2021-08-18 |
Family
ID=60116433
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018555152A Active JP6921114B2 (ja) | 2016-04-22 | 2017-04-21 | サイクリン依存性キナーゼ８（ｃｄｋ８）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ｃｄｋ８の分解および使用法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10865205B2 (OSRAM) |
| EP (2) | EP3445764B1 (OSRAM) |
| JP (1) | JP6921114B2 (OSRAM) |
| CN (1) | CN109311869B (OSRAM) |
| AU (1) | AU2017254711B2 (OSRAM) |
| CA (1) | CA3020543A1 (OSRAM) |
| WO (1) | WO2017185034A1 (OSRAM) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109153675B (zh) * | 2016-04-22 | 2023-05-02 | 达纳－法伯癌症研究所公司 | 细胞周期蛋白依赖性激酶9通过cdk9抑制剂与e3连接酶配体的缀合的降解及使用方法 |
| JP6921115B2 (ja) * | 2016-04-22 | 2021-08-18 | 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４／６（ｃｄｋ４／６）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ｃｄｋ４／６の分解および使用法 |
| CA3038979A1 (en) | 2016-10-11 | 2018-04-19 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3535265A4 (en) * | 2016-11-01 | 2020-07-08 | Arvinas, Inc. | PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| CN108187035B (zh) * | 2018-01-05 | 2020-12-15 | 杭州师范大学 | E3连接酶fbw7在延缓衰老及相关疾病方面的医药用途 |
| EP3752517B1 (en) | 2018-02-13 | 2025-04-09 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| CN112074505B (zh) | 2018-03-08 | 2024-04-05 | 因赛特公司 | 作为PI3K-γ抑制剂的氨基吡嗪二醇化合物 |
| JP7252973B2 (ja) | 2018-03-26 | 2023-04-05 | ノバルティス アーゲー | Ｎ－（３－（７Ｈ－ピロロ［２，３－ｄ］ピリミジン－４－イル）フェニル）ベンズアミド誘導体 |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| CN111018857B (zh) * | 2018-10-09 | 2023-06-02 | 嘉兴优博生物技术有限公司 | 靶向蛋白酶降解平台(ted) |
| WO2020093370A1 (zh) * | 2018-11-09 | 2020-05-14 | 汪义朋 | 一种特异性降解tau蛋白的小分子化合物及其应用 |
| EP3880669A1 (en) | 2018-11-13 | 2021-09-22 | Biotheryx, Inc. | Substituted isoindolinones |
| US12233356B2 (en) | 2019-03-21 | 2025-02-25 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| MX2021011242A (es) | 2019-03-21 | 2022-01-19 | Codiak Biosciences Inc | Conjugados de vesícula extracelular y usos de estos. |
| CA3130706A1 (en) * | 2019-04-04 | 2020-10-08 | Dana-Farber Cancer Institute, Inc. | Cdk2/5 degraders and uses thereof |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| WO2021053495A1 (en) * | 2019-09-16 | 2021-03-25 | Novartis Ag | Bifunctional degraders and their methods of use |
| CA3154386A1 (en) | 2019-10-17 | 2021-04-22 | Michael Berlin | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| JP7629459B2 (ja) | 2019-11-19 | 2025-02-13 | ブリストル－マイヤーズ スクイブ カンパニー | Ｈｅｌｉｏｓタンパク質の阻害剤として有用な化合物 |
| CA3171580A1 (en) * | 2020-05-06 | 2021-11-11 | Hunter P. Shunatona | Bifunctional imidazol[4,5-c] pyridinyl derivatives and pharmaceutical compositions thereof useful as degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| CN115996918A (zh) | 2020-05-09 | 2023-04-21 | 阿尔维纳斯运营股份有限公司 | 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型 |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| IL307343A (en) | 2021-04-06 | 2023-11-01 | Bristol Myers Squibb Co | Pyridinyl substituted oxisoisoindoline compounds |
| AU2022259683A1 (en) | 2021-04-16 | 2023-10-19 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| AR125798A1 (es) | 2021-05-07 | 2023-08-16 | Kymera Therapeutics Inc | Degradadores cdk2 y usos de los mismos |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| WO2025122895A1 (en) | 2023-12-08 | 2025-06-12 | Arvinas Operations, Inc. | Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| MX387318B (es) * | 2014-04-14 | 2025-03-18 | Arvinas Operations Inc | Moduladores de la proteólisis basados en imida y métodos de uso asociados. |
| US10071164B2 (en) * | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
-
2017
- 2017-04-21 EP EP17786757.9A patent/EP3445764B1/en active Active
- 2017-04-21 CA CA3020543A patent/CA3020543A1/en active Pending
- 2017-04-21 US US16/094,105 patent/US10865205B2/en active Active
- 2017-04-21 EP EP21210171.1A patent/EP3985006A1/en active Pending
- 2017-04-21 JP JP2018555152A patent/JP6921114B2/ja active Active
- 2017-04-21 CN CN201780024815.5A patent/CN109311869B/zh active Active
- 2017-04-21 AU AU2017254711A patent/AU2017254711B2/en active Active
- 2017-04-21 WO PCT/US2017/028948 patent/WO2017185034A1/en not_active Ceased
-
2020
- 2020-10-29 US US17/083,940 patent/US11247991B2/en active Active
-
2021
- 2021-12-23 US US17/561,032 patent/US11827636B2/en active Active
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