AU2017254708B2 - Degradation of cyclin-dependent kinase 4/6 (CDK4/6) by conjugation of CDK4/6 inhibitors with E3 ligase ligand and methods of use - Google Patents
Degradation of cyclin-dependent kinase 4/6 (CDK4/6) by conjugation of CDK4/6 inhibitors with E3 ligase ligand and methods of use Download PDFInfo
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- AU2017254708B2 AU2017254708B2 AU2017254708A AU2017254708A AU2017254708B2 AU 2017254708 B2 AU2017254708 B2 AU 2017254708B2 AU 2017254708 A AU2017254708 A AU 2017254708A AU 2017254708 A AU2017254708 A AU 2017254708A AU 2017254708 B2 AU2017254708 B2 AU 2017254708B2
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- Prior art keywords
- cancer
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- cdk4
- bifunctional compound
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Classifications
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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 (2)
| Publication Number | Publication Date |
|---|---|
| AU2017254708A1 AU2017254708A1 (en) | 2018-10-11 |
| AU2017254708B2 true AU2017254708B2 (en) | 2021-09-16 |
Family
ID=60116458
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017254708A Active AU2017254708B2 (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 |
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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| WO2017185023A1 (en) * | 2016-04-22 | 2017-10-26 | 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 |
| HUE070289T2 (hu) | 2016-10-11 | 2025-05-28 | Arvinas Operations Inc | Vegyületek és módszerek az androgénreceptor célzott lebontására |
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| WO2018106870A1 (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 |
| US11667651B2 (en) | 2017-12-22 | 2023-06-06 | Hibercell, Inc. | Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| EP3752517B1 (en) | 2018-02-13 | 2025-04-09 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| KR20200131246A (ko) | 2018-02-15 | 2020-11-23 | 누베이션 바이오 인크. | 키나제 억제제로서의 헤테로시클릭 화합물 |
| 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 |
| US11472799B2 (en) | 2018-03-06 | 2022-10-18 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (AKT) degradation / disruption compounds and methods of use |
| 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 |
| US12226424B2 (en) | 2018-04-09 | 2025-02-18 | Shanghaitech University | Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates |
| EP3810145A4 (en) * | 2018-06-21 | 2022-06-01 | Icahn School of Medicine at Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| WO2020010204A1 (en) * | 2018-07-05 | 2020-01-09 | Icahn School Of Medicine At Mount Sinai | Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use |
| US20210340140A1 (en) * | 2018-07-23 | 2021-11-04 | 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 |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| EP3873906A4 (en) * | 2018-11-02 | 2022-07-27 | The Wistar Institute of Anatomy and Biology | PROTEOLYSIS-TARGETED CHIMERAS |
| CN113423701A (zh) | 2018-11-13 | 2021-09-21 | 拜欧斯瑞克斯公司 | 取代的异吲哚啉酮 |
| WO2020191369A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| WO2020191377A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Extracellular vesicle conjugates and uses thereof |
| WO2020198711A1 (en) * | 2019-03-28 | 2020-10-01 | Essa Pharma, Inc. | Androgen receptor modulators and methods for use as proteolysis targeting chimera ligands |
| CA3130706A1 (en) * | 2019-04-04 | 2020-10-08 | Dana-Farber Cancer Institute, Inc. | Cdk2/5 degraders and uses thereof |
| CA3134491A1 (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 |
| AU2020263390B2 (en) * | 2019-04-23 | 2026-01-08 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof |
| EP3965824B1 (en) | 2019-05-06 | 2025-01-08 | Icahn School of Medicine at Mount Sinai | Heterobifunctional compounds as degraders of hpk1 |
| WO2020247537A1 (en) * | 2019-06-03 | 2020-12-10 | Regents Of The University Of Minnesota | Compounds that degrade kinases and uses thereof |
| 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 |
| 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 |
| 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 |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 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 |
| JP7785663B2 (ja) * | 2019-09-16 | 2025-12-15 | ノバルティス アーゲー | 二機能性分解誘導薬及びそれらの使用方法 |
| 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 |
| AR120773A1 (es) | 2019-12-18 | 2022-03-16 | Novartis Ag | Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona como reductor de la actividad de la proteína wiz |
| EP4122925A4 (en) * | 2020-03-17 | 2024-04-17 | Medshine Discovery Inc. | PROTEOLYSIS REGULATOR AND METHOD OF USE |
| TW202208381A (zh) * | 2020-05-06 | 2022-03-01 | 美商紐力克斯醫療股份有限公司 | 造血前驅細胞激酶之雙官能降解劑及其治療用途 |
| 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 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| 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 |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | 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 |
| EP4259128A4 (en) * | 2020-12-09 | 2025-04-30 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CR20230516A (es) | 2021-04-16 | 2024-01-23 | Arvinas Operations Inc | Moduladores de la proteólisis bcl6 y métodos de uso asociados |
| CN117062811A (zh) | 2021-06-03 | 2023-11-14 | 诺华股份有限公司 | 3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其医疗用途 |
| CN118451078A (zh) * | 2021-10-14 | 2024-08-06 | 上海睿跃生物科技有限公司 | 经修饰的蛋白质和蛋白质降解剂 |
| US20250186434A1 (en) * | 2022-03-16 | 2025-06-12 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| EP4514796A1 (en) * | 2022-04-25 | 2025-03-05 | OnQuality Pharmaceuticals China Ltd. | Cdk inhibitors, pharmaceutical compositions, and therapeutic applications |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015160845A2 (en) * | 2014-04-14 | 2015-10-22 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GEP20063909B (en) * | 2002-01-22 | 2006-08-25 | Warner Lambert Co | 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES |
| SI2331547T1 (sl) | 2008-08-22 | 2014-11-28 | Novartis Ag | Pirolopirimidinske spojine kot CDK inhibitorji |
| PA8852901A1 (es) * | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| WO2016015605A1 (en) * | 2014-07-26 | 2016-02-04 | Sunshine Lake Pharma Co., Ltd. | Compounds as cdk small-molecule inhibitors and uses thereof |
| 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 |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| 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 |
| CA3020543A1 (en) * | 2016-04-22 | 2017-10-26 | 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 |
| US20210340140A1 (en) * | 2018-07-23 | 2021-11-04 | 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 JP JP2018555281A patent/JP6921115B2/ja active Active
- 2017-04-21 EP EP17786755.3A patent/EP3445765A4/en active Pending
- 2017-04-21 AU AU2017254708A patent/AU2017254708B2/en active Active
- 2017-04-21 CA CA3018434A patent/CA3018434A1/en active Pending
- 2017-04-21 US US16/094,098 patent/US10865204B2/en active Active
- 2017-04-21 CN CN201780024853.0A patent/CN109071552B/zh active Active
- 2017-04-21 WO PCT/US2017/028941 patent/WO2017185031A1/en not_active Ceased
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015160845A2 (en) * | 2014-04-14 | 2015-10-22 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| CN109071552A (zh) | 2018-12-21 |
| EP3445765A1 (en) | 2019-02-27 |
| US20190092768A1 (en) | 2019-03-28 |
| WO2017185031A1 (en) | 2017-10-26 |
| US10865204B2 (en) | 2020-12-15 |
| JP2019514883A (ja) | 2019-06-06 |
| CN109071552B (zh) | 2022-06-03 |
| JP6921115B2 (ja) | 2021-08-18 |
| EP3445765A4 (en) | 2019-09-18 |
| AU2017254708A1 (en) | 2018-10-11 |
| CA3018434A1 (en) | 2017-10-26 |
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Legal Events
| Date | Code | Title | Description |
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| DA3 | Amendments made section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ GRAY, NATHANAEL; ZHANG, TINGHU; OLSON, CALLA M.; LIANG, YANKE; KWIATKOWSKI, NICHOLAS; WANG, ERIC AND JIANG, BAISHAN |
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| FGA | Letters patent sealed or granted (standard patent) |