CN113677668B - 用于雄激素受体靶向泛素化的双官能化合物和方法 - Google Patents
用于雄激素受体靶向泛素化的双官能化合物和方法 Download PDFInfo
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- CN113677668B CN113677668B CN202080026615.5A CN202080026615A CN113677668B CN 113677668 B CN113677668 B CN 113677668B CN 202080026615 A CN202080026615 A CN 202080026615A CN 113677668 B CN113677668 B CN 113677668B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962798554P | 2019-01-30 | 2019-01-30 | |
| US62/798,554 | 2019-01-30 | ||
| PCT/US2020/015922 WO2020160295A1 (en) | 2019-01-30 | 2020-01-30 | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN113677668A CN113677668A (zh) | 2021-11-19 |
| CN113677668B true CN113677668B (zh) | 2024-09-27 |
Family
ID=71733785
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080026615.5A Expired - Fee Related CN113677668B (zh) | 2019-01-30 | 2020-01-30 | 用于雄激素受体靶向泛素化的双官能化合物和方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US11098025B2 (https=) |
| EP (1) | EP3917916A4 (https=) |
| JP (1) | JP7555938B2 (https=) |
| CN (1) | CN113677668B (https=) |
| WO (1) | WO2020160295A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7555938B2 (ja) | 2019-01-30 | 2024-09-25 | モンテリノ・セラピューティクス・インコーポレイテッド | アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法 |
| CA3165168A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| 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 |
| WO2021236695A1 (en) * | 2020-05-18 | 2021-11-25 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| CN114262319B (zh) * | 2020-12-01 | 2023-05-05 | 南昌奥瑞药业有限公司 | 一类双功能分子、其制备方法及其应用 |
| JP2024508841A (ja) * | 2021-02-25 | 2024-02-28 | メイヨ・ファウンデーション・フォー・メディカル・エデュケーション・アンド・リサーチ | プログラム可能なタンパク質分解のための化合物及び疾患処置のための使用方法 |
| WO2023039601A1 (en) * | 2021-09-13 | 2023-03-16 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| US11981672B2 (en) | 2021-09-13 | 2024-05-14 | Montelino Therapeutics Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| US20240376118A1 (en) * | 2021-09-13 | 2024-11-14 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| WO2023039603A2 (en) * | 2021-09-13 | 2023-03-16 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| US20240382603A1 (en) * | 2021-09-13 | 2024-11-21 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| EP4426286A4 (en) * | 2021-11-03 | 2025-12-24 | Relay Therapeutics Inc | Bifunctional PI3K-Alpha Inhibitors and Their Uses |
| AU2022424178A1 (en) | 2021-12-30 | 2024-07-11 | Beone Medicines I Gmbh | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| CN119301111A (zh) | 2022-03-24 | 2025-01-10 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物 |
| CN114890989B (zh) * | 2022-05-25 | 2024-03-22 | 广东晨康生物科技有限公司 | 一种含氮衍生物为Linker的HDAC8降解剂其制备方法和应用 |
| US20240207415A1 (en) * | 2022-11-08 | 2024-06-27 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| KR20250047848A (ko) * | 2023-09-27 | 2025-04-07 | 강원대학교산학협력단 | Kras의 g12v 돌연변이체 단백질의 특이적 분해 방법 및 그 조성물 |
| US12496301B2 (en) | 2023-12-08 | 2025-12-16 | Arvinas Operations, Inc. | Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106164071A (zh) * | 2014-02-14 | 2016-11-23 | 不列颠哥伦比亚大学 | 作为治疗剂的人雄激素受体dna‑结合结构域(dbd)化合物及其使用方法 |
| CN107428734A (zh) * | 2015-01-20 | 2017-12-01 | 阿尔维纳斯股份有限公司 | 用于雄激素受体的靶向降解的化合物和方法 |
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| GB9817224D0 (en) | 1998-08-08 | 1998-10-07 | Univ Nottingham | Ocular surface infection |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| EP1087334B1 (fr) | 1999-09-15 | 2007-12-19 | European Community | Scellé multi-usage électronique à transpondeur passif |
| CN102186836A (zh) | 2008-10-17 | 2011-09-14 | 雅培制药有限公司 | Trpv1拮抗剂 |
| EP2519664A4 (en) | 2009-12-30 | 2014-03-12 | Avila Therapeutics Inc | LIGAND-RELATED COVALENTS MODIFYING A PROTEIN |
| WO2011098904A1 (en) | 2010-02-12 | 2011-08-18 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
| JP5934986B2 (ja) * | 2011-09-07 | 2016-06-15 | 公益財団法人ヒューマンサイエンス振興財団 | アポトーシス阻害タンパク質リガンド−エストロゲン受容体リガンドハイブリッド化合物並びにそれを利用したエストロゲン受容体分解誘導剤及び乳癌、子宮頚癌又は卵巣癌の予防及び治療剤 |
| CA2861066C (en) | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| US20150284422A1 (en) | 2012-08-10 | 2015-10-08 | Epizyme, Inc. | Inhibitors of protein methyltransferase dot1l and methods of use thereof |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| AU2015247817C1 (en) * | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| 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 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2017011371A1 (en) * | 2015-07-10 | 2017-01-19 | Arvinas, Inc | Mdm2-based modulators of proteolysis and associated methods of use |
| CA2988436A1 (en) * | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| AU2017246452C1 (en) | 2016-04-06 | 2021-06-03 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| WO2018071606A1 (en) | 2016-10-11 | 2018-04-19 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3555091A1 (en) * | 2016-12-19 | 2019-10-23 | H. Hoffnabb-La Roche Ag | Ar-v7 inhibitors |
| BR112019015484A2 (pt) * | 2017-01-31 | 2020-04-28 | Arvinas Operations Inc | ligantes de cereblon e compostos bifuncionais compreendendo os mesmos |
| US20200172927A1 (en) | 2017-05-15 | 2020-06-04 | The Trustees Of Columbia University In The City Of New York | Reprogramming metabolism by inhibiting vhl for treatment of neurodegeneration |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| US20220356185A1 (en) * | 2018-07-06 | 2022-11-10 | Kymera Therapeutics, Inc. | Mertk degraders and uses thereof |
| KR102596354B1 (ko) | 2018-11-05 | 2023-10-31 | 삼성디스플레이 주식회사 | 액정 표시 장치 및 그 제조 방법 |
| WO2020102575A1 (en) | 2018-11-16 | 2020-05-22 | Inception Ibd, Inc. | Heterocyclic aminothiazoles and uses thereof |
| US11547759B2 (en) | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| JP7555938B2 (ja) | 2019-01-30 | 2024-09-25 | モンテリノ・セラピューティクス・インコーポレイテッド | アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法 |
| JP2022549222A (ja) | 2019-09-23 | 2022-11-24 | アキュター バイオテクノロジー インコーポレイテッド | アンドロゲン受容体分解活性を有する新規尿素およびその使用 |
| US11820781B2 (en) | 2019-12-04 | 2023-11-21 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway |
| WO2021236695A1 (en) | 2020-05-18 | 2021-11-25 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
-
2020
- 2020-01-30 JP JP2021544763A patent/JP7555938B2/ja active Active
- 2020-01-30 EP EP20748314.0A patent/EP3917916A4/en not_active Withdrawn
- 2020-01-30 CN CN202080026615.5A patent/CN113677668B/zh not_active Expired - Fee Related
- 2020-01-30 WO PCT/US2020/015922 patent/WO2020160295A1/en not_active Ceased
- 2020-01-30 US US16/777,294 patent/US11098025B2/en active Active
-
2021
- 2021-05-27 US US17/331,940 patent/US11787778B2/en active Active
-
2023
- 2023-09-01 US US18/459,944 patent/US20240002360A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106164071A (zh) * | 2014-02-14 | 2016-11-23 | 不列颠哥伦比亚大学 | 作为治疗剂的人雄激素受体dna‑结合结构域(dbd)化合物及其使用方法 |
| CN107428734A (zh) * | 2015-01-20 | 2017-12-01 | 阿尔维纳斯股份有限公司 | 用于雄激素受体的靶向降解的化合物和方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020160295A1 (en) | 2020-08-06 |
| EP3917916A1 (en) | 2021-12-08 |
| CN113677668A (zh) | 2021-11-19 |
| US11098025B2 (en) | 2021-08-24 |
| JP2022523916A (ja) | 2022-04-27 |
| US11787778B2 (en) | 2023-10-17 |
| US20210292298A1 (en) | 2021-09-23 |
| US20200239430A1 (en) | 2020-07-30 |
| EP3917916A4 (en) | 2022-12-14 |
| US20240002360A1 (en) | 2024-01-04 |
| JP7555938B2 (ja) | 2024-09-25 |
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