CN116003418A - Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 - Google Patents
Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 Download PDFInfo
- Publication number
- CN116003418A CN116003418A CN202211289138.9A CN202211289138A CN116003418A CN 116003418 A CN116003418 A CN 116003418A CN 202211289138 A CN202211289138 A CN 202211289138A CN 116003418 A CN116003418 A CN 116003418A
- Authority
- CN
- China
- Prior art keywords
- dione
- dioxopiperidin
- alkyl
- methyl
- diazabicyclo
- 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
Images
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- 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
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- 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
-
- 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
- C07D471/08—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
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-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
- C07D498/22—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 four or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2021112319639 | 2021-10-22 | ||
| CN202111231963 | 2021-10-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN116003418A true CN116003418A (zh) | 2023-04-25 |
Family
ID=86027290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202211289138.9A Pending CN116003418A (zh) | 2021-10-22 | 2022-10-20 | Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20250243210A1 (https=) |
| EP (1) | EP4421071A4 (https=) |
| JP (1) | JP2024539269A (https=) |
| KR (1) | KR20240110576A (https=) |
| CN (1) | CN116003418A (https=) |
| AU (1) | AU2022370021B2 (https=) |
| CA (1) | CA3235512A1 (https=) |
| WO (1) | WO2023066350A1 (https=) |
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117126133A (zh) * | 2023-08-14 | 2023-11-28 | 中国海洋大学 | 一种化合物及其用途 |
| WO2023241598A1 (zh) * | 2022-06-14 | 2023-12-21 | 海创药业股份有限公司 | 一种芳香类化合物及其制备方法及在制备雌激素受体降解剂中的用途 |
| CN117756818A (zh) * | 2023-12-12 | 2024-03-26 | 北京医院 | 一种戊二酰亚胺类化合物及其制备方法和应用 |
| WO2024083182A1 (zh) * | 2022-10-20 | 2024-04-25 | 西藏海思科制药有限公司 | 一种膦酰衍生物的制备方法 |
| WO2024083183A1 (zh) * | 2022-10-20 | 2024-04-25 | 西藏海思科制药有限公司 | 一种膦酰衍生物的盐及晶型和在医药上的用途 |
| US12097261B2 (en) | 2021-05-07 | 2024-09-24 | Kymera Therapeutics, Inc. | CDK2 degraders and uses thereof |
| CN118955474A (zh) * | 2024-07-29 | 2024-11-15 | 浙江爱索拓标记医药科技有限公司 | 一种放射性同位素碳-14标记的巴德卡鲁胺及其制备方法和应用 |
| WO2024245444A1 (zh) * | 2023-06-01 | 2024-12-05 | 标新生物医药科技(上海)有限公司 | 氧代异吲哚啉基取代的四氢嘧啶二酮衍生物及其应用 |
| CN120004863A (zh) * | 2025-02-27 | 2025-05-16 | 江苏天士力帝益药业有限公司 | 一种alk蛋白降解剂及其在抗肿瘤中的应用 |
| 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 |
| WO2025162221A1 (zh) * | 2024-02-04 | 2025-08-07 | 标新生物医药科技(上海)有限公司 | 基于取代的异吲哚啉酮新颖骨架化合物、含有其的双功能蛋白降解剂及它们的应用 |
| WO2025162225A1 (zh) * | 2024-02-04 | 2025-08-07 | 标新生物医药科技(上海)有限公司 | 具有取代的戊二酰亚胺基异吲哚啉酮新颖骨架的化合物及其应用 |
| WO2026061104A1 (zh) * | 2024-07-05 | 2026-03-26 | 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 |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4434978A4 (en) * | 2021-11-17 | 2025-03-26 | TYK Medicines Inc. | Compound for degrading EGFR protein and use thereof |
| JP7805983B2 (ja) | 2022-03-22 | 2026-01-26 | アッヴィ・インコーポレイテッド | ブルトン型チロシンキナーゼを分解するためのピリミジン |
| KR20250047743A (ko) * | 2022-07-12 | 2025-04-04 | 리젠츠 오브 더 유니버시티 오브 미시간 | 에스트로겐 수용체 분해제로서의 테트라하이드로나프탈렌 유도체 |
| WO2024032600A1 (zh) * | 2022-08-08 | 2024-02-15 | 西藏海思科制药有限公司 | 一种杂环衍生物及其组合物和药学上的应用 |
| WO2024173646A1 (en) * | 2023-02-16 | 2024-08-22 | Innovo Therapeutics, Inc. | Cyclin-dependent kinase degrading compounds |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
| WO2025036489A1 (zh) | 2023-08-17 | 2025-02-20 | 海思科医药集团股份有限公司 | 一种氰基芳香环衍生物及其在医药上的应用 |
| CN120548310A (zh) * | 2023-12-26 | 2025-08-26 | 标新生物医药科技(上海)有限公司 | 具有双氮杂环取代的异吲哚啉酮骨架的化合物及其应用 |
| WO2025212165A1 (en) * | 2024-04-05 | 2025-10-09 | Board Of Regents Of The University Of Nebraska | Targeted heterobifunctional small molecule proteolysis targeting chimeras |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN113292536A (zh) * | 2020-02-21 | 2021-08-24 | 四川海思科制药有限公司 | 一种具有降解Bcr-Abl或PARP的化合物及其制备方法和药学上的应用 |
| CN113387931A (zh) * | 2020-03-13 | 2021-09-14 | 四川海思科制药有限公司 | 一种具有抑制或降解蛋白激酶的化合物及其制备方法和药学上的应用 |
| WO2021194879A1 (en) * | 2020-03-21 | 2021-09-30 | Arvinas Operations, Inc. | Indazole based compounds and associated methods of use |
| CN116783179A (zh) * | 2020-10-21 | 2023-09-19 | 阿尔维纳斯运营股份有限公司 | 用于雄激素受体蛋白的靶向降解的化合物和方法 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018071306A1 (en) * | 2016-10-11 | 2018-04-19 | Northwestern University | Incremental rotary rolling mill and method |
| KR102674902B1 (ko) * | 2016-12-01 | 2024-06-14 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| CN117510491A (zh) * | 2016-12-23 | 2024-02-06 | 阿尔维纳斯运营股份有限公司 | 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法 |
| US11191741B2 (en) * | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| AU2018211975B2 (en) * | 2017-01-26 | 2022-05-26 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| BR112019015484A2 (pt) * | 2017-01-31 | 2020-04-28 | Arvinas Operations Inc | ligantes de cereblon e compostos bifuncionais compreendendo os mesmos |
| TWI793151B (zh) * | 2017-08-23 | 2023-02-21 | 瑞士商諾華公司 | 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途 |
| US11065231B2 (en) * | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| KR20210006356A (ko) * | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| CA3095912A1 (en) * | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| MX2021001957A (es) * | 2018-08-22 | 2021-07-15 | Cullgen Shanghai Inc | Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk). |
| KR102642203B1 (ko) * | 2018-09-07 | 2024-03-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행형 섬유육종 폴리펩티드의 표적화 분해를 위한 다중 고리 화합물 및 방법 |
| WO2020162725A1 (ko) * | 2019-02-07 | 2020-08-13 | 한국화학연구원 | 표적 단백질 eed 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 eed, ezh2, 또는 prc2 관련 질환의 예방 또는 치료용 약학적 조성물 |
| WO2020167518A1 (en) * | 2019-02-13 | 2020-08-20 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| CN113490528B (zh) * | 2019-02-15 | 2024-12-03 | 诺华股份有限公司 | 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途 |
| US11485735B2 (en) * | 2019-04-25 | 2022-11-01 | Wuxi Shuangliang Biotechnology Co., Ltd. | Selective CDK4/6 inhibitor and preparation thereof |
| CN119954801A (zh) * | 2019-07-17 | 2025-05-09 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| FI3835298T3 (fi) * | 2019-12-12 | 2024-07-29 | Accutar Biotechnology Inc | Uusia kromaanijohdannaisia, joilla on estrogeenireseptoria hajottava vaikutus, ja niiden käyttötapoja |
| CA3173262A1 (en) * | 2020-02-26 | 2021-09-02 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| EP4121167A1 (en) * | 2020-03-21 | 2023-01-25 | Arvinas Operations, Inc. | Selective modulators of mutant lrrk2 proteolysis and associated methods of use |
| US11739101B2 (en) * | 2020-05-06 | 2023-08-29 | Nurix Therapeutics, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| JP7834721B2 (ja) * | 2020-08-28 | 2026-03-24 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| EP4240733A1 (en) * | 2020-11-06 | 2023-09-13 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor and associated methods of use |
| WO2022099117A1 (en) * | 2020-11-06 | 2022-05-12 | Prelude Therapeutics Incorporated | Brm targeting compounds and associated methods of use |
| CA3196965A1 (en) * | 2020-11-20 | 2022-05-27 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2022133184A1 (en) * | 2020-12-20 | 2022-06-23 | Newave Pharmaceutical Inc. | Btk degrader |
| WO2022198112A1 (en) * | 2021-03-19 | 2022-09-22 | Arvinas Operations, Inc. | Indazole based compounds and associated methods of use |
| CN117279910A (zh) * | 2021-04-16 | 2023-12-22 | 阿尔维纳斯运营股份有限公司 | Bcl6蛋白水解的调节剂和其相关使用方法 |
| WO2023023941A1 (en) * | 2021-08-24 | 2023-03-02 | Biofront Ltd (Cayman) | Hpk1 degraders, compositions comprising the hpki degrader, and methods of using the same |
| WO2023249970A1 (en) * | 2022-06-21 | 2023-12-28 | Nikang Therapeutics, Inc. | Bifunctional compounds containing pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| CN119451967A (zh) * | 2022-06-22 | 2025-02-14 | 霖康疗法公司 | 用于经由泛素蛋白酶体途径降解细胞周期蛋白依赖性激酶2的含有吡啶并[2,3-d]嘧啶-7(8H)-酮衍生物的双功能化合物 |
| US20250367193A1 (en) * | 2022-06-22 | 2025-12-04 | Nikang Therapeutics, Inc. | Bifunctional compounds containing substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
-
2022
- 2022-10-20 AU AU2022370021A patent/AU2022370021B2/en active Active
- 2022-10-20 EP EP22882955.2A patent/EP4421071A4/en active Pending
- 2022-10-20 WO PCT/CN2022/126516 patent/WO2023066350A1/zh not_active Ceased
- 2022-10-20 CA CA3235512A patent/CA3235512A1/en active Pending
- 2022-10-20 KR KR1020247016562A patent/KR20240110576A/ko active Pending
- 2022-10-20 JP JP2024524582A patent/JP2024539269A/ja active Pending
- 2022-10-20 CN CN202211289138.9A patent/CN116003418A/zh active Pending
- 2022-10-20 US US18/703,316 patent/US20250243210A1/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN113292536A (zh) * | 2020-02-21 | 2021-08-24 | 四川海思科制药有限公司 | 一种具有降解Bcr-Abl或PARP的化合物及其制备方法和药学上的应用 |
| CN113387931A (zh) * | 2020-03-13 | 2021-09-14 | 四川海思科制药有限公司 | 一种具有抑制或降解蛋白激酶的化合物及其制备方法和药学上的应用 |
| WO2021194879A1 (en) * | 2020-03-21 | 2021-09-30 | Arvinas Operations, Inc. | Indazole based compounds and associated methods of use |
| CN116783179A (zh) * | 2020-10-21 | 2023-09-19 | 阿尔维纳斯运营股份有限公司 | 用于雄激素受体蛋白的靶向降解的化合物和方法 |
Non-Patent Citations (1)
| Title |
|---|
| ACS: "STN REGISTRY", 30 September 2021 (2021-09-30), pages 1 - 5 * |
Cited By (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12097261B2 (en) | 2021-05-07 | 2024-09-24 | Kymera Therapeutics, Inc. | CDK2 degraders and uses thereof |
| WO2023241598A1 (zh) * | 2022-06-14 | 2023-12-21 | 海创药业股份有限公司 | 一种芳香类化合物及其制备方法及在制备雌激素受体降解剂中的用途 |
| WO2024083182A1 (zh) * | 2022-10-20 | 2024-04-25 | 西藏海思科制药有限公司 | 一种膦酰衍生物的制备方法 |
| WO2024083183A1 (zh) * | 2022-10-20 | 2024-04-25 | 西藏海思科制药有限公司 | 一种膦酰衍生物的盐及晶型和在医药上的用途 |
| WO2024245444A1 (zh) * | 2023-06-01 | 2024-12-05 | 标新生物医药科技(上海)有限公司 | 氧代异吲哚啉基取代的四氢嘧啶二酮衍生物及其应用 |
| WO2025036132A1 (zh) * | 2023-08-14 | 2025-02-20 | 中国海洋大学 | 一种化合物及其用途 |
| CN117126133A (zh) * | 2023-08-14 | 2023-11-28 | 中国海洋大学 | 一种化合物及其用途 |
| 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 |
| CN117756818B (zh) * | 2023-12-12 | 2025-04-29 | 北京医院 | 一种戊二酰亚胺类化合物及其制备方法和应用 |
| CN117756818A (zh) * | 2023-12-12 | 2024-03-26 | 北京医院 | 一种戊二酰亚胺类化合物及其制备方法和应用 |
| WO2025162221A1 (zh) * | 2024-02-04 | 2025-08-07 | 标新生物医药科技(上海)有限公司 | 基于取代的异吲哚啉酮新颖骨架化合物、含有其的双功能蛋白降解剂及它们的应用 |
| WO2025162225A1 (zh) * | 2024-02-04 | 2025-08-07 | 标新生物医药科技(上海)有限公司 | 具有取代的戊二酰亚胺基异吲哚啉酮新颖骨架的化合物及其应用 |
| WO2026061104A1 (zh) * | 2024-07-05 | 2026-03-26 | 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 |
| CN118955474A (zh) * | 2024-07-29 | 2024-11-15 | 浙江爱索拓标记医药科技有限公司 | 一种放射性同位素碳-14标记的巴德卡鲁胺及其制备方法和应用 |
| CN120004863A (zh) * | 2025-02-27 | 2025-05-16 | 江苏天士力帝益药业有限公司 | 一种alk蛋白降解剂及其在抗肿瘤中的应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20240110576A (ko) | 2024-07-15 |
| JP2024539269A (ja) | 2024-10-28 |
| AU2022370021B2 (en) | 2026-04-16 |
| US20250243210A1 (en) | 2025-07-31 |
| EP4421071A4 (en) | 2026-03-11 |
| WO2023066350A1 (zh) | 2023-04-27 |
| EP4421071A1 (en) | 2024-08-28 |
| CA3235512A1 (en) | 2023-04-27 |
| AU2022370021A1 (en) | 2024-05-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN116003418A (zh) | Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 | |
| WO2024188209A1 (zh) | 新颖的e3泛素连接酶配体、蛋白降解剂及其应用 | |
| JP2025502928A (ja) | E3ユビキチンリガーゼリガンド化合物、当該リガンド化合物に基づいて開発したタンパク質分解剤及びそれらの応用 | |
| WO2024032689A1 (zh) | 基于异吲哚啉取代戊二酰亚胺骨架的化合物及其应用 | |
| CN115611902B (zh) | 基于布鲁顿酪氨酸激酶配体设计的蛋白降解化合物及其应用 | |
| CN118556047A (zh) | 氧代异吲哚啉基取代哌啶二酮衍生物及其应用 | |
| CN120202200A (zh) | 基于氧代异吲哚啉基取代的四氢嘧啶二酮的化合物及其应用 | |
| CN119630669A (zh) | 硫代的戊二酰亚胺基异吲哚啉酮衍生物、含有其的双功能蛋白降解剂及它们的应用 | |
| CN116589445B (zh) | 基于喹唑啉取代戊二酰亚胺骨架的化合物及其应用 | |
| CN119451952A (zh) | 氧代异吲哚啉基取代的四氢嘧啶二酮衍生物及其应用 | |
| CN112390785A (zh) | 一种bet家族溴域抑制剂环衍生物及其制备方法和药学上的应用 | |
| JP2026502207A (ja) | 硫黄/酸素置換グルタルイミジルイミドイソインドリノン骨格に基づいた化合物及びその応用 | |
| WO2024051766A1 (zh) | 基于cereblon蛋白设计的分子胶化合物及其应用 | |
| HK40085637A (en) | Crbn e3 ligase ligand compounds, protein degraders developed based on the ligand compounds, and their applications | |
| CN116396288A (zh) | 基于bcl-2家族蛋白配体化合物开发的蛋白降解剂及它们的应用 | |
| CN119768392A (zh) | 芳基或杂芳基取代的戊二酰亚胺衍生物及其应用 | |
| CN119654316A (zh) | 基于硫代的戊二酰亚胺基异吲哚啉酮骨架的化合物及其应用 | |
| CN121605108A (zh) | 含有硫/氧取代戊二酰亚胺基异吲哚啉酮骨架的双功能蛋白降解剂及它们的应用 | |
| WO2025140369A1 (zh) | 具有双氮杂环取代的异吲哚啉酮骨架的化合物及其应用 | |
| HK40087687A (zh) | E3泛素连接酶配体化合物、基於该配体化合物开发的蛋白降解剂及它们的应用 | |
| CN120787222A (zh) | 基于取代的异吲哚啉酮新颖骨架化合物、含有其的双功能蛋白降解剂及它们的应用 | |
| WO2025016359A1 (zh) | 戊二酰亚胺基异吲哚啉酮骨架的化合物 | |
| HK40089595A (zh) | 基於喹唑啉取代戊二酰亚胺骨架的化合物及其应用 | |
| CN121464138A (zh) | Mllt1和/或mllt3的protac降解剂 | |
| CN120787219A (zh) | 具有取代的戊二酰亚胺基异吲哚啉酮新颖骨架的化合物及其应用 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 40085637 Country of ref document: HK |