JP2025510074A - Ｐｒｏｔａｃにおけるデグロンとしての２，４－ジオキソテトラヒドロピリミジニル誘導体 - Google Patents
Ｐｒｏｔａｃにおけるデグロンとしての２，４－ジオキソテトラヒドロピリミジニル誘導体 Download PDFInfo
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- JP2025510074A JP2025510074A JP2024556319A JP2024556319A JP2025510074A JP 2025510074 A JP2025510074 A JP 2025510074A JP 2024556319 A JP2024556319 A JP 2024556319A JP 2024556319 A JP2024556319 A JP 2024556319A JP 2025510074 A JP2025510074 A JP 2025510074A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- 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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- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB2204142.0A GB202204142D0 (en) | 2022-03-24 | 2022-03-24 | Novel compounds |
| GB2204142.0 | 2022-03-24 | ||
| GBGB2213816.8A GB202213816D0 (en) | 2022-09-22 | 2022-09-22 | Novel compounds |
| GB2213816.8 | 2022-09-22 | ||
| GBGB2301448.3A GB202301448D0 (en) | 2023-02-01 | 2023-02-01 | Novel compounds |
| GB2301448.3 | 2023-02-01 | ||
| GB202301757 | 2023-02-08 | ||
| GB2301757.7 | 2023-02-08 | ||
| PCT/EP2023/057338 WO2023180388A1 (en) | 2022-03-24 | 2023-03-22 | 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2025510074A true JP2025510074A (ja) | 2025-04-14 |
| JP2025510074A5 JP2025510074A5 (https=) | 2026-03-30 |
Family
ID=85937360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024556319A Pending JP2025510074A (ja) | 2022-03-24 | 2023-03-22 | Ｐｒｏｔａｃにおけるデグロンとしての２，４－ジオキソテトラヒドロピリミジニル誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20250205344A1 (https=) |
| EP (1) | EP4499628A1 (https=) |
| JP (1) | JP2025510074A (https=) |
| CN (1) | CN119301111A (https=) |
| CA (1) | CA3246569A1 (https=) |
| WO (1) | WO2023180388A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4647431A1 (en) * | 2023-01-04 | 2025-11-12 | Gan & lee Pharm Co., Ltd. | Compound and method for targeted degradation of androgen receptor |
| TW202508568A (zh) | 2023-04-07 | 2025-03-01 | 瑞典商阿斯特捷利康公司 | Ｉｒａｋ４蛋白水解靶向嵌合體 |
| WO2025011623A1 (zh) * | 2023-07-12 | 2025-01-16 | 上海壹迪生物技术有限公司 | 氰基喹啉类靶向蛋白降解分子、其制备方法和应用 |
| TW202530192A (zh) | 2023-09-22 | 2025-08-01 | 英商葛蘭素史密斯克藍智慧財產發展有限公司 | 新穎化合物 |
| TW202532055A (zh) * | 2023-11-22 | 2025-08-16 | 大陸商廣東東陽光藥業股份有限公司 | 靶向降解雄激素受體的雙功能嵌合體的雜環化合物及其用途 |
| WO2025125575A1 (en) | 2023-12-14 | 2025-06-19 | Astrazeneca Ab | Irak4 protacs |
| TW202543650A (zh) | 2024-03-08 | 2025-11-16 | 美商海爾達醫療運營公司 | 異雙官能化合物及其在治療疾病中之用途 |
| WO2025261436A1 (zh) * | 2024-06-19 | 2025-12-26 | 上海翰森生物医药科技有限公司 | 含氮杂环类衍生物抑制剂、其制备方法和应用 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7737149B2 (en) | 2006-12-21 | 2010-06-15 | Astrazeneca Ab | N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof |
| RU2738833C9 (ru) | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| 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 |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN110506039A (zh) | 2016-10-11 | 2019-11-26 | 阿尔维纳斯股份有限公司 | 用于雄激素受体靶向降解的化合物和方法 |
| IL312367A (en) * | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2020118098A1 (en) * | 2018-12-05 | 2020-06-11 | Vividion Therapeutics, Inc. | Substituted isoindolinones as modulators of cereblon-mediated neo-substrate recruitment |
| EP3917916A4 (en) | 2019-01-30 | 2022-12-14 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| CN114269331A (zh) | 2019-03-28 | 2022-04-01 | 埃萨制药股份有限公司 | 雄激素受体调节剂和用作蛋白水解靶向嵌合体配体的方法 |
| WO2020211822A1 (zh) | 2019-04-18 | 2020-10-22 | 成都海创药业有限公司 | 一类靶向降解雄激素受体的双功能嵌合体杂环化合物及其用途 |
| US12331061B2 (en) | 2019-04-18 | 2025-06-17 | Accutar Biotechnology Inc. | Compounds having BET, estrogen receptor, and androgen receptor degradation activity and uses thereof |
| 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 |
| CA3195695A1 (en) | 2020-09-30 | 2022-04-07 | Astrazeneca Ab | Compounds and their use in treating cancer |
-
2023
- 2023-03-22 US US18/849,815 patent/US20250205344A1/en active Pending
- 2023-03-22 CN CN202380029742.4A patent/CN119301111A/zh active Pending
- 2023-03-22 JP JP2024556319A patent/JP2025510074A/ja active Pending
- 2023-03-22 WO PCT/EP2023/057338 patent/WO2023180388A1/en not_active Ceased
- 2023-03-22 EP EP23715429.9A patent/EP4499628A1/en active Pending
- 2023-03-22 CA CA3246569A patent/CA3246569A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP4499628A1 (en) | 2025-02-05 |
| CA3246569A1 (en) | 2023-09-28 |
| US20250205344A1 (en) | 2025-06-26 |
| WO2023180388A1 (en) | 2023-09-28 |
| CN119301111A (zh) | 2025-01-10 |
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