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
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- tautomer
- salt
- mmol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
-
- 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
-
- 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)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB2204142.0 | 2022-03-24 | ||
| GBGB2204142.0A GB202204142D0 (en) | 2022-03-24 | 2022-03-24 | Novel compounds |
| GBGB2213816.8A GB202213816D0 (en) | 2022-09-22 | 2022-09-22 | Novel compounds |
| GB2213816.8 | 2022-09-22 | ||
| GB2301448.3 | 2023-02-01 | ||
| GBGB2301448.3A GB202301448D0 (en) | 2023-02-01 | 2023-02-01 | Novel compounds |
| GB2301757.7 | 2023-02-08 | ||
| GB202301757 | 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 (enExample) | 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 (enExample) |
| EP (1) | EP4499628A1 (enExample) |
| JP (1) | JP2025510074A (enExample) |
| CN (1) | CN119301111A (enExample) |
| CA (1) | CA3246569A1 (enExample) |
| WO (1) | WO2023180388A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024146617A1 (zh) * | 2023-01-04 | 2024-07-11 | 甘李药业股份有限公司 | 用于雄激素受体靶向降解的化合物和方法 |
| 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 |
| IL326555A (en) * | 2023-09-22 | 2026-04-01 | Glaxosmithkline Ip Dev Ltd | Androgen receptor protax |
| CN120025326A (zh) * | 2023-11-22 | 2025-05-23 | 广东东阳光药业股份有限公司 | 一种靶向降解雄激素受体的双功能嵌合体的杂环化合物及其用途 |
| US20250197411A1 (en) | 2023-12-14 | 2025-06-19 | Astrazeneca Ab | Irak4 protacs |
| US12558428B2 (en) | 2024-03-08 | 2026-02-24 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and their use in treating disease |
| 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 |
| CN119591582A (zh) | 2014-04-14 | 2025-03-11 | 阿尔维纳斯运营股份有限公司 | 基于酰亚胺的蛋白水解调节剂和相关使用方法 |
| 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 |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| LT3660004T (lt) | 2016-10-11 | 2023-06-12 | Arvinas Operations, Inc. | Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai |
| EP3577109A4 (en) * | 2017-01-31 | 2020-11-18 | Arvinas Operations, Inc. | CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| US20230045737A1 (en) * | 2018-12-05 | 2023-02-09 | Vividion Therapeutics, Inc. | Substituted isoindolinones as modulators of cereblon-mediated neo-substrate recruitment |
| WO2020160295A1 (en) | 2019-01-30 | 2020-08-06 | Montelino Therapeutics, Llc | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| KR20220004978A (ko) | 2019-03-28 | 2022-01-12 | 에싸 파마 아이엔씨. | 단백질 분해 표적 키메라 리간드로서 사용하기 위한 안드로겐 수용체 조절제 및 방법 |
| US12331061B2 (en) | 2019-04-18 | 2025-06-17 | Accutar Biotechnology Inc. | Compounds having BET, estrogen receptor, and androgen receptor degradation activity and uses thereof |
| KR20220004100A (ko) | 2019-04-18 | 2022-01-11 | 하이노바 파마슈티컬스 인코포레이티드 | 안드로겐 수용체를 표적 분해하는 이중 기능성의 키메라 헤테로 고리 화합물 및 이의 용도 |
| US12310975B2 (en) | 2019-10-17 | 2025-05-27 | Arvinas Operations, Inc. | Modulators of BCL6 proteolysis and associated methods of use |
| EP4221756A1 (en) | 2020-09-30 | 2023-08-09 | Astrazeneca AB | Compounds and their use in treating cancer |
-
2023
- 2023-03-22 CN CN202380029742.4A patent/CN119301111A/zh active Pending
- 2023-03-22 US US18/849,815 patent/US20250205344A1/en active Pending
- 2023-03-22 EP EP23715429.9A patent/EP4499628A1/en 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 CA CA3246569A patent/CA3246569A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20250205344A1 (en) | 2025-06-26 |
| CN119301111A (zh) | 2025-01-10 |
| WO2023180388A1 (en) | 2023-09-28 |
| EP4499628A1 (en) | 2025-02-05 |
| CA3246569A1 (en) | 2023-09-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA3246569A1 (en) | 2,4-DIOXOTETRAHYDROPYRIMIDINYL DERIVATIVES USED AS DEGRONS IN PROTACS | |
| JP6746679B2 (ja) | 化合物 | |
| AU2018200277B2 (en) | Compounds | |
| CN1264843C (zh) | 具有pde7抑制作用的吡唑并嘧啶酮衍生物 | |
| CN1407985A (zh) | 用作钾通道抑制剂的杂环二氢嘧啶 | |
| CN1278819A (zh) | 作为促肾上腺皮质素释放激素拮抗剂、可用于治疗cns障碍和紧张相关性疾病的杂环基取代的环稠合吡啶和嘧啶 | |
| CN1382144A (zh) | 作为p38蛋白激酶的抑制剂的杂烷基氨基－取代的双环氮杂环类化合物 | |
| WO2010128425A1 (en) | Gpr 119 modulators | |
| CN1535968A (zh) | 四氢吡啶基或哌啶基杂环衍生物 | |
| JP2009530233A (ja) | Ｐｉ−３キナーゼインヒビターおよびそれらの使用方法 | |
| EP2427448A1 (en) | Gpr 119 modulators | |
| CN1809576A (zh) | 抗寄生物萜类生物碱 | |
| CN1684964A (zh) | 一些新的咪唑并吡啶及其用途 | |
| HK1049834A1 (zh) | 用作磷酸二酯酶抑制剂的5-(2-取代的-5-杂环基磺酰基吡啶-3-基)-二氢吡唑并[4，3-d]嘧啶-7-酮类化合物 | |
| CN1351497A (zh) | 用作山梨醇脱氢酶抑制剂的氨基嘧啶类化合物 | |
| CN1476442A (zh) | 具有IKB-激酶(IKK-β)抑制活性的吡啶衍生物 | |
| US10858367B2 (en) | Compounds | |
| CN1816541A (zh) | Vr－1拮抗剂取代－1－酞嗪胺 | |
| CN1918159A (zh) | 调节香草素－1受体(vr1)功能的取代氨基杂双环类前药 | |
| CN101052629A (zh) | 芳基－氨基取代的吡咯并嘧啶多激酶抑制化合物 | |
| CN1104432C (zh) | 吡咯并三嗪和嘧啶化合物 | |
| CN101035791A (zh) | 作为c－JUN N末端激酶（JNK）和P－38激酶的抑制剂的吡咯并[1,2－D][1,2,4]三嗪 | |
| CN1870896A (zh) | 用作hiv整合酶抑制剂的羟基吡啶并吡咯并吡嗪二酮化合物 | |
| CN101056632A (zh) | 用作蛋白激酶抑制剂的化合物和组合物 | |
| CN1968949A (zh) | 脯氨酸衍生物和其作为二肽基肽酶iv抑制剂的用途 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20241121 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20260319 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20260319 |