JP6921115B2 - 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 - Google Patents
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 Download PDFInfo
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- JP6921115B2 JP6921115B2 JP2018555281A JP2018555281A JP6921115B2 JP 6921115 B2 JP6921115 B2 JP 6921115B2 JP 2018555281 A JP2018555281 A JP 2018555281A JP 2018555281 A JP2018555281 A JP 2018555281A JP 6921115 B2 JP6921115 B2 JP 6921115B2
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- 0 CC(C)*(C)*1[C@]([C@](C)N)C1C Chemical compound CC(C)*(C)*1[C@]([C@](C)N)C1C 0.000 description 6
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326571P | 2016-04-22 | 2016-04-22 | |
| US62/326,571 | 2016-04-22 | ||
| PCT/US2017/028941 WO2017185031A1 (en) | 2016-04-22 | 2017-04-21 | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019514883A JP2019514883A (ja) | 2019-06-06 |
| JP2019514883A5 JP2019514883A5 (enExample) | 2020-05-28 |
| JP6921115B2 true JP6921115B2 (ja) | 2021-08-18 |
Family
ID=60116458
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018555281A Active JP6921115B2 (ja) | 2016-04-22 | 2017-04-21 | 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 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10865204B2 (enExample) |
| EP (1) | EP3445765A4 (enExample) |
| JP (1) | JP6921115B2 (enExample) |
| CN (1) | CN109071552B (enExample) |
| AU (1) | AU2017254708B2 (enExample) |
| CA (1) | CA3018434A1 (enExample) |
| WO (1) | WO2017185031A1 (enExample) |
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| AU2017254702B2 (en) * | 2016-04-22 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 9 (CDK9) by conjugation of CDK9 inhibitors with E3 ligase ligand and methods of use |
| HUE061847T2 (hu) | 2016-10-11 | 2023-08-28 | Arvinas Operations Inc | Androgén receptor célzott degradálására alkalmas vegyületek és eljárások |
| MX2019004950A (es) | 2016-10-28 | 2019-09-26 | Icahn School Med Mount Sinai | Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2. |
| CA3045037A1 (en) * | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| CN109516989B (zh) * | 2017-09-17 | 2021-12-31 | 上海美志医药科技有限公司 | 一类抑制并降解cdk的化合物 |
| JP7569688B2 (ja) | 2017-12-22 | 2024-10-18 | ハイバーセル,インコーポレイテッド | ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体 |
| US12325725B2 (en) | 2018-02-13 | 2025-06-10 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| US11174252B2 (en) | 2018-02-15 | 2021-11-16 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| CA3091041A1 (en) * | 2018-02-22 | 2019-08-29 | Ichan School Of Medicine At Mount Sinai | Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use |
| JP2021515013A (ja) * | 2018-03-06 | 2021-06-17 | アイカーン スクール オブ メディスン アット マウント シナイ | セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法 |
| WO2019186343A1 (en) | 2018-03-26 | 2019-10-03 | Novartis Ag | N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives |
| AU2019251151B2 (en) | 2018-04-09 | 2022-07-07 | Shanghaitech University | Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates |
| WO2019246570A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| JP2021529807A (ja) * | 2018-07-05 | 2021-11-04 | アイカーン スクール オブ メディスン アット マウント シナイ | タンパク質チロシンキナーゼ6(ptk6)分解/破壊化合物および使用方法 |
| CA3106523A1 (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 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| CN113825752A (zh) * | 2018-11-02 | 2021-12-21 | 威斯特解剖及生物研究所 | 蛋白水解靶向嵌合体 |
| 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 |
| CN113747925B (zh) | 2019-03-21 | 2024-10-15 | 隆萨销售股份公司 | 胞外囊泡缀合物及其用途 |
| JP2022521825A (ja) * | 2019-03-28 | 2022-04-12 | エッサ ファーマ,インコーポレイテッド | アンドロゲン受容体モジュレーター及びタンパク質分解誘導キメラリガンドとして使用するための方法 |
| EP3947368B1 (en) | 2019-04-04 | 2025-09-03 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds comprising a cdk2/5 ligand, a linker and a e3 ubiquitin ligase binding degron for the treatment of cancer |
| WO2020210337A1 (en) * | 2019-04-09 | 2020-10-15 | Dana-Farber Cancer Institute, Inc. | Degradation of akt by conjugation of atp-competitive akt inhibitor gdc-0068 with e3 ligase ligands and methods of use |
| CA3132387A1 (en) * | 2019-04-23 | 2020-10-29 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof |
| CN118908962A (zh) | 2019-05-06 | 2024-11-08 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| EP3976621A4 (en) * | 2019-06-03 | 2023-11-15 | Regents of the University of Minnesota | KINASE DEGRADING COMPOUNDS AND THEIR USE |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| TWI769382B (zh) * | 2019-06-21 | 2022-07-01 | 長庚大學 | 利博西林用於製備治療罹患磷酸二酯酶4介導疾病的患者的醫藥組合物及用途 |
| CN110143948B (zh) * | 2019-06-21 | 2021-05-14 | 上海博悦生物科技有限公司 | Cdk4/6抑制剂、其药物组合物、制备方法及应用 |
| 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 |
| EP4045496A1 (en) | 2019-10-17 | 2022-08-24 | Arvinas Operations, Inc. | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| PE20230159A1 (es) | 2019-12-18 | 2023-02-01 | Novartis Ag | Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos |
| CN115380026B (zh) * | 2020-03-17 | 2023-11-07 | 南京明德新药研发有限公司 | 蛋白降解调节剂与其使用方法 |
| CN115605488B (zh) * | 2020-05-06 | 2024-08-09 | 新锐思生物制药股份有限公司 | 造血祖细胞激酶的双功能降解剂及其治疗用途 |
| AU2021273458A1 (en) | 2020-05-09 | 2022-12-01 | Arvinas Operations, Inc. | Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same |
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| CN111909155B (zh) * | 2020-08-21 | 2022-10-18 | 东莞理工学院 | 蛋白水解靶向嵌合体、提高其口服生物利用度的前药分子及应用 |
| 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 |
| CN114349738B (zh) * | 2020-10-14 | 2023-05-05 | 清华大学 | 一类靶向降解cdk2的小分子缀合物及其应用 |
| AU2021396308A1 (en) * | 2020-12-09 | 2023-06-22 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| AU2022259683A1 (en) | 2021-04-16 | 2023-10-19 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| AR126052A1 (es) | 2021-06-03 | 2023-09-06 | Novartis Ag | Derivados de 3-(5-oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos |
| EP4416145A1 (en) * | 2021-10-14 | 2024-08-21 | Cullgen (Shanghai), Inc. | Modified proteins and protein degraders |
| US20250186434A1 (en) * | 2022-03-16 | 2025-06-12 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| JP2025514839A (ja) * | 2022-04-25 | 2025-05-09 | オンクオリティ ファーマシューティカルズ チャイナ リミテッド | Cdk阻害剤、医薬組成物及びその治療応用 |
| CN115364100B (zh) * | 2022-08-25 | 2023-08-29 | 杭州天玑济世生物科技有限公司 | Ly2835219作为线粒体自噬诱导剂的用途 |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| CN119948027A (zh) * | 2022-10-21 | 2025-05-06 | 领泰生物医药(绍兴)有限公司 | Sos1蛋白降解剂及其应用 |
| WO2024183798A1 (en) * | 2023-03-07 | 2024-09-12 | Cullgen Inc. | Compounds and methods of treating cancers |
| 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 |
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| CN101001857B (zh) * | 2002-01-22 | 2011-06-22 | 沃尼尔·朗伯有限责任公司 | 2-(吡啶-2-基氨基)-吡啶并[2,3-d]嘧啶-7-酮 |
| US8685980B2 (en) * | 2008-08-22 | 2014-04-01 | Novartis Ag | Pyrrolopyrimidine compounds and their uses |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| KR20250127179A (ko) * | 2014-04-14 | 2025-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| CN105294683B (zh) | 2014-07-26 | 2018-01-23 | 广东东阳光药业有限公司 | Cdk类小分子抑制剂的化合物及其用途 |
| EP3191098A4 (en) | 2014-09-12 | 2018-04-25 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| 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 |
| AU2017254711B2 (en) * | 2016-04-22 | 2021-01-21 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 8 (CDK8) by conjugation of CDK8 inhibitors with E3 ligase ligand and methods of use |
| CA3106523A1 (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 |
-
2017
- 2017-04-21 US US16/094,098 patent/US10865204B2/en active Active
- 2017-04-21 AU AU2017254708A patent/AU2017254708B2/en active Active
- 2017-04-21 EP EP17786755.3A patent/EP3445765A4/en active Pending
- 2017-04-21 CN CN201780024853.0A patent/CN109071552B/zh active Active
- 2017-04-21 WO PCT/US2017/028941 patent/WO2017185031A1/en not_active Ceased
- 2017-04-21 JP JP2018555281A patent/JP6921115B2/ja active Active
- 2017-04-21 CA CA3018434A patent/CA3018434A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2017254708A1 (en) | 2018-10-11 |
| US10865204B2 (en) | 2020-12-15 |
| EP3445765A4 (en) | 2019-09-18 |
| CN109071552B (zh) | 2022-06-03 |
| CN109071552A (zh) | 2018-12-21 |
| AU2017254708B2 (en) | 2021-09-16 |
| EP3445765A1 (en) | 2019-02-27 |
| CA3018434A1 (en) | 2017-10-26 |
| US20190092768A1 (en) | 2019-03-28 |
| WO2017185031A1 (en) | 2017-10-26 |
| JP2019514883A (ja) | 2019-06-06 |
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