JP2023511472A - がんの治療のための二官能性化合物 - Google Patents
がんの治療のための二官能性化合物 Download PDFInfo
- Publication number
- JP2023511472A JP2023511472A JP2022525186A JP2022525186A JP2023511472A JP 2023511472 A JP2023511472 A JP 2023511472A JP 2022525186 A JP2022525186 A JP 2022525186A JP 2022525186 A JP2022525186 A JP 2022525186A JP 2023511472 A JP2023511472 A JP 2023511472A
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- Japan
- Prior art keywords
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- alkyl
- formula
- cancer
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- 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.)
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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
-
- 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
-
- 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
-
- 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
- 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
- C07D487/08—Bridged 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962927340P | 2019-10-29 | 2019-10-29 | |
| US62/927,340 | 2019-10-29 | ||
| EP19209344.1 | 2019-11-15 | ||
| EP19209344 | 2019-11-15 | ||
| PCT/EP2020/080265 WO2021083949A1 (en) | 2019-10-29 | 2020-10-28 | Bifunctional compounds for the treatment of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023511472A true JP2023511472A (ja) | 2023-03-20 |
| JP2023511472A5 JP2023511472A5 (https=) | 2023-11-01 |
Family
ID=73020226
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022525186A Pending JP2023511472A (ja) | 2019-10-29 | 2020-10-28 | がんの治療のための二官能性化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230024096A1 (https=) |
| EP (1) | EP4051674A1 (https=) |
| JP (1) | JP2023511472A (https=) |
| CN (1) | CN114728936A (https=) |
| WO (1) | WO2021083949A1 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| WO2021126973A1 (en) * | 2019-12-17 | 2021-06-24 | Orionis Biosciences, Inc. | Compounds modulating protein recruitment and/or degradation |
| WO2021133917A1 (en) | 2019-12-23 | 2021-07-01 | Kymera Therapeutics, Inc. | Smarca inhibitors and uses thereof |
| EP4081308A4 (en) | 2019-12-23 | 2024-01-24 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| KR20230005160A (ko) | 2020-03-19 | 2023-01-09 | 카이메라 쎄라퓨틱스 인코포레이티드 | Mdm2 분해제 및 이의 용도 |
| WO2021207291A1 (en) * | 2020-04-06 | 2021-10-14 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| IL300397A (en) | 2020-08-05 | 2023-04-01 | C4 Therapeutics Inc | Compounds for targeted knockdown of RET |
| EP4259144A4 (en) * | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| KR20240004983A (ko) * | 2021-05-10 | 2024-01-11 | 포그혼 쎄라퓨틱스 인크. | 화합물 및 이의 용도 |
| CA3219183A1 (en) | 2021-05-17 | 2022-11-24 | Amedeo Caflisch | N6-adenosine-methyltransferase inhibitors in cancer treatment |
| US20240358842A1 (en) * | 2021-06-25 | 2024-10-31 | Stablix, Inc. | Protein stabilizing compounds containing usp7 ligands |
| US20250018046A1 (en) * | 2021-07-07 | 2025-01-16 | Biogen Ma Inc | Compounds for targeting degradation of irak4 proteins |
| KR20240046498A (ko) | 2021-08-09 | 2024-04-09 | 제넨테크, 인크. | Brm의 조절에 사용하기 위한 페놀 유도체 |
| WO2023039573A1 (en) * | 2021-09-10 | 2023-03-16 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Compounds for targeted degradation of taf1 |
| CN117384161A (zh) * | 2022-07-04 | 2024-01-12 | 华东理工大学 | 靶向降解cdk蛋白的化合物及其应用 |
| WO2024026083A1 (en) * | 2022-07-29 | 2024-02-01 | Ribon Therapeutics, Inc. | Targeted protein degradation of parp14 for use in therapy |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| CN116120311B (zh) * | 2022-11-28 | 2025-10-24 | 中国药科大学 | 一种靶向降解atr蛋白的双功能化合物及其制法与用途 |
| CN116284202B (zh) * | 2023-03-28 | 2024-07-02 | 华侨大学 | 白桦脂酸的PROTACs化合物及其制备方法和应用 |
| WO2024213125A1 (zh) * | 2023-04-14 | 2024-10-17 | 南京再明医药有限公司 | Brm选择性降解剂及其应用 |
| TW202502750A (zh) | 2023-06-08 | 2025-01-16 | 美商新銳思生物製藥股份有限公司 | Smarca2之雙官能選擇性降解劑及其治療用途 |
| PE20260301A1 (es) * | 2023-06-14 | 2026-02-10 | Astrazeneca Ab | Derivados de 3-[3-amino-6-(2-hidroxifenil)piridazin-4-il]-3,8-diazabiciclo[3.2.1]octano como protacs degradantes de smarca2 para el tratamiento del cancer |
| WO2025006902A2 (en) * | 2023-06-29 | 2025-01-02 | Dana-Farber Cancer Institute, Inc. | Synthesis and in vitro characterization of proteolysis targeting chimeras (protacs) for degradation of dna methyltransferase 1 (dnmt1) |
| WO2025061035A1 (zh) * | 2023-09-19 | 2025-03-27 | 南京再明医药有限公司 | Brm选择性降解剂化合物及其应用 |
| WO2025094065A1 (en) | 2023-11-01 | 2025-05-08 | Aurigene Oncology Limited | Amino-substituted pyridazine compounds as smarca2 and/or smarca4 degraders |
| WO2026061475A1 (zh) * | 2024-09-19 | 2026-03-26 | 标新生物医药科技(上海)有限公司 | 含有芳基取代杂芳基的双功能蛋白降解剂及其应用 |
| CN119798218A (zh) * | 2024-12-31 | 2025-04-11 | 南京优氟医药科技有限公司 | 一种e3酶配体-连接链复合物及其制备方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2018502097A (ja) * | 2014-12-23 | 2018-01-25 | 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 |
| WO2019195201A1 (en) * | 2018-04-01 | 2019-10-10 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
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| WO2020010227A1 (en) * | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| US20230072658A1 (en) * | 2019-06-10 | 2023-03-09 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
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-
2020
- 2020-10-28 JP JP2022525186A patent/JP2023511472A/ja active Pending
- 2020-10-28 WO PCT/EP2020/080265 patent/WO2021083949A1/en not_active Ceased
- 2020-10-28 US US17/771,204 patent/US20230024096A1/en active Pending
- 2020-10-28 EP EP20797473.4A patent/EP4051674A1/en not_active Withdrawn
- 2020-10-28 CN CN202080076232.9A patent/CN114728936A/zh active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018502097A (ja) * | 2014-12-23 | 2018-01-25 | 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 |
| WO2019195201A1 (en) * | 2018-04-01 | 2019-10-10 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
Non-Patent Citations (1)
| Title |
|---|
| BIOCHEMICAL JOURNAL, vol. 474, JPN6024049883, 2017, pages 1127 - 1147, ISSN: 0005619039 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20230024096A1 (en) | 2023-01-26 |
| WO2021083949A1 (en) | 2021-05-06 |
| EP4051674A1 (en) | 2022-09-07 |
| CN114728936A (zh) | 2022-07-08 |
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