CA3246569A1 - 2,4-DIOXOTETRAHYDROPYRIMIDINYL DERIVATIVES USED AS DEGRONS IN PROTACS - Google Patents
2,4-DIOXOTETRAHYDROPYRIMIDINYL DERIVATIVES USED AS DEGRONS IN PROTACSInfo
- Publication number
- CA3246569A1 CA3246569A1 CA3246569A CA3246569A CA3246569A1 CA 3246569 A1 CA3246569 A1 CA 3246569A1 CA 3246569 A CA3246569 A CA 3246569A CA 3246569 A CA3246569 A CA 3246569A CA 3246569 A1 CA3246569 A1 CA 3246569A1
- Authority
- CA
- Canada
- 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)
- 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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3246569A1 true CA3246569A1 (en) | 2023-09-28 |
Family
ID=85937360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3246569A Pending CA3246569A1 (en) | 2022-03-24 | 2023-03-22 | 2,4-DIOXOTETRAHYDROPYRIMIDINYL DERIVATIVES USED AS DEGRONS IN PROTACS |
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 (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20260234157A1 (en) * | 2023-01-04 | 2026-08-13 | Gan & Lee Pharmaceuticals Co., Ltd. | Compound and method for targeted degradation of androgen receptor |
| US20240374588A1 (en) | 2023-04-07 | 2024-11-14 | Astrazeneca Ab | Irak4 protacs |
| CN122161821A (zh) * | 2023-07-12 | 2026-06-05 | 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 protacs |
| WO2025085738A1 (en) | 2023-10-18 | 2025-04-24 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| WO2025108404A1 (zh) * | 2023-11-22 | 2025-05-30 | 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 |
| WO2025162210A1 (zh) | 2024-02-04 | 2025-08-07 | 上海超阳药业有限公司 | 一种具备降解酪氨酸蛋白激酶btk活性的化合物及其制备方法和用途 |
| WO2025189056A1 (en) | 2024-03-08 | 2025-09-12 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and their use in treating disease |
| TW202617722A (zh) * | 2024-06-19 | 2026-05-01 | 大陸商上海翰森生物醫藥科技有限公司 | 含氮雜環類衍生物抑制劑、其製備方法和應用 |
| WO2026120044A1 (en) * | 2024-12-04 | 2026-06-11 | Astrazeneca Ab | Smarca2 degraders and uses thereof |
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 |
| EP4649963A3 (en) | 2014-04-14 | 2026-05-13 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| 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 |
| SI3526202T1 (sl) | 2016-10-11 | 2025-04-30 | Arvinas Operations, Inc. | Spojine in postopki za ciljno razgradnjo androgenskih receptorjev |
| IL319363A (en) * | 2017-01-31 | 2025-05-01 | Arvinas Operations Inc | Cervalon ligands and bifunctional compounds containing them |
| 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 |
| WO2020160295A1 (en) | 2019-01-30 | 2020-08-06 | Montelino Therapeutics, Llc | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| 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 |
| US12331061B2 (en) | 2019-04-18 | 2025-06-17 | Accutar Biotechnology Inc. | Compounds having BET, estrogen receptor, and androgen receptor degradation activity and uses thereof |
| BR112021020775A2 (pt) | 2019-04-18 | 2021-12-14 | Hinova Pharmaceuticals Inc | Classe de compostos heterocíclicos quiméricos bifuncionais para a degradação direcionada de receptores de andrógeno e uso dos mesmos |
| MX2022004526A (es) | 2019-10-17 | 2022-07-21 | Arvinas Operations Inc | Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6. |
| PE20230782A1 (es) | 2020-09-30 | 2023-05-09 | Astrazeneca Ab | Compuestos y su uso en el tratamiento del cancer |
-
2023
- 2023-03-22 CN CN202380029742.4A patent/CN119301111A/zh active Pending
- 2023-03-22 CA CA3246569A patent/CA3246569A1/en active Pending
- 2023-03-22 WO PCT/EP2023/057338 patent/WO2023180388A1/en not_active Ceased
- 2023-03-22 JP JP2024556319A patent/JP2025510074A/ja 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
Also Published As
| Publication number | Publication date |
|---|---|
| EP4499628A1 (en) | 2025-02-05 |
| CN119301111A (zh) | 2025-01-10 |
| WO2023180388A1 (en) | 2023-09-28 |
| US20250205344A1 (en) | 2025-06-26 |
| JP2025510074A (ja) | 2025-04-14 |
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