CN112638380B - 小脑蛋白(crbn)配体 - Google Patents
小脑蛋白(crbn)配体 Download PDFInfo
- Publication number
- CN112638380B CN112638380B CN201980057157.9A CN201980057157A CN112638380B CN 112638380 B CN112638380 B CN 112638380B CN 201980057157 A CN201980057157 A CN 201980057157A CN 112638380 B CN112638380 B CN 112638380B
- Authority
- CN
- China
- Prior art keywords
- mmol
- amino
- mixture
- cancer
- oxoisoindolin
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
-
- 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
-
- 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
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
- A61K31/52—Purines, e.g. adenine
-
- 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
- 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
- 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
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Immunology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862692167P | 2018-06-29 | 2018-06-29 | |
| US62/692,167 | 2018-06-29 | ||
| PCT/US2019/039555 WO2020006264A1 (en) | 2018-06-29 | 2019-06-27 | Ligands to cereblon (crbn) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN112638380A CN112638380A (zh) | 2021-04-09 |
| CN112638380B true CN112638380B (zh) | 2024-05-24 |
Family
ID=68987146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980057157.9A Active CN112638380B (zh) | 2018-06-29 | 2019-06-27 | 小脑蛋白(crbn)配体 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US11530219B2 (https=) |
| EP (1) | EP3813829A4 (https=) |
| JP (2) | JP7321194B2 (https=) |
| KR (2) | KR20250020690A (https=) |
| CN (1) | CN112638380B (https=) |
| AU (1) | AU2019294835B2 (https=) |
| CA (1) | CA3102214A1 (https=) |
| WO (1) | WO2020006264A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2767532T3 (en) | 2012-12-21 | 2016-09-12 | Nat Inst For Quantum And Radiological Science And Tech | New connection for reproduction of tau protein heavy in the brain. |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| EP3773576A4 (en) | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| TW201946624A (zh) | 2018-05-09 | 2019-12-16 | 新旭生技股份有限公司 | 雜芳基化合物及其用途 |
| AU2019294835B2 (en) * | 2018-06-29 | 2025-04-17 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (CRBN) |
| CN111606883B (zh) | 2019-02-25 | 2023-05-09 | 上海科技大学 | 基于戊二酰亚胺骨架的含硫化合物及其应用 |
| WO2021023233A1 (zh) | 2019-08-05 | 2021-02-11 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| CN114728071B (zh) | 2019-11-13 | 2024-12-06 | 新旭生技股份有限公司 | 用于降解tau蛋白聚集体的化合物及其用途 |
| WO2021126973A1 (en) * | 2019-12-17 | 2021-06-24 | Orionis Biosciences, Inc. | Compounds modulating protein recruitment and/or degradation |
| PH12022551482A1 (en) | 2019-12-18 | 2023-11-29 | Novartis Ag | 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| CN113582980B (zh) * | 2020-04-30 | 2023-11-24 | 上海科技大学 | 基于杂环和戊二酰亚胺骨架的化合物及其应用 |
| AU2022207648A1 (en) | 2021-01-13 | 2023-07-27 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| WO2022254362A1 (en) | 2021-06-03 | 2022-12-08 | Novartis Ag | 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof |
| CN115504963A (zh) * | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | 一种c-Myc蛋白降解剂 |
| WO2022272061A1 (en) * | 2021-06-25 | 2022-12-29 | Celgene Corporation | Cereblon binding compounds, compositions thereof, and methods of treatment therewith |
| US20250066325A1 (en) * | 2021-11-04 | 2025-02-27 | The Brigham And Women's Hospital, Inc. | Directed degron molecules and applications thereof |
| US12122764B2 (en) | 2021-12-22 | 2024-10-22 | Gilead Sciences, Inc. | IKAROS zinc finger family degraders and uses thereof |
| KR20240123836A (ko) * | 2021-12-22 | 2024-08-14 | 길리애드 사이언시즈, 인코포레이티드 | 이카로스 아연 핑거 패밀리 분해제 및 이의 용도 |
| KR102738668B1 (ko) | 2022-02-25 | 2024-12-06 | 계명대학교 산학협력단 | 항암 활성을 갖는 신규 화합물 및 이의 용도 |
| WO2023178181A1 (en) | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| CA3249074A1 (en) | 2022-06-06 | 2023-12-14 | C4 Therapeutics, Inc. | BICYCLIC SUBSTITUTION GLUTARIMIDE CEREBLON BINDERS |
| US20260028326A1 (en) * | 2022-08-10 | 2026-01-29 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | Compound based on isoindoline-substituted glutarimide backbone and use thereof |
| EP4612128A4 (en) | 2022-11-04 | 2025-09-10 | Bristol Myers Squibb Co | COMPOUNDS AND THEIR USE FOR THE TREATMENT OF HEMOGLOBINOPATHIES |
| WO2024167423A1 (en) * | 2023-02-07 | 2024-08-15 | Captor Therapeutics S.A. | Gspt1 degrader compounds |
| EP4713023A2 (en) * | 2023-05-18 | 2026-03-25 | Firefly Bio, Inc. | Isoindolinone-glutarimide antibody conjugates, and uses thereof |
| WO2025101912A1 (en) * | 2023-11-09 | 2025-05-15 | The Board Of Trustees Of The Leland Stanford Junior University | Hells helicase degraders and uses thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1968695A (zh) * | 2004-04-14 | 2007-05-23 | 细胞基因公司 | 含有用于治疗和控制骨髓发育不良综合征的免疫调节化合物的组合物和使用方法 |
| CN101966183A (zh) * | 2003-12-02 | 2011-02-09 | 细胞基因公司 | 用于治疗和控制血红蛋白病和贫血病的方法和组合物 |
| CN102264720A (zh) * | 2008-10-29 | 2011-11-30 | 细胞基因公司 | 用于治疗癌症的异吲哚啉化合物 |
| CN106660991A (zh) * | 2014-07-11 | 2017-05-10 | 细胞基因公司 | 抗增殖化合物及其使用方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030045552A1 (en) * | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| UA91560C2 (ru) * | 2005-08-31 | 2010-08-10 | Селджин Корпорэйшн | Соединения ряда изоиндолимидов, их композиция и применение |
| EA017405B9 (ru) * | 2006-12-08 | 2014-05-30 | АйАрЭм ЭлЭлСи | Соединения и композиции в качестве ингибиторов протеинкиназы |
| CN101580501B (zh) * | 2009-06-01 | 2011-03-09 | 南京卡文迪许生物工程技术有限公司 | 3-(取代二氢异吲哚酮-2-基)-2,6-哌啶二酮的合成方法及其中间体 |
| RU2738833C9 (ru) * | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| EP3827836A1 (en) * | 2014-06-27 | 2021-06-02 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| CA3101338A1 (en) | 2018-06-13 | 2019-12-19 | Biotheryx, Inc. | Aminoamide compounds |
| AU2019294835B2 (en) * | 2018-06-29 | 2025-04-17 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (CRBN) |
-
2019
- 2019-06-27 AU AU2019294835A patent/AU2019294835B2/en active Active
- 2019-06-27 JP JP2020571833A patent/JP7321194B2/ja active Active
- 2019-06-27 KR KR1020257001993A patent/KR20250020690A/ko active Pending
- 2019-06-27 EP EP19827425.0A patent/EP3813829A4/en active Pending
- 2019-06-27 KR KR1020217001892A patent/KR20210025061A/ko active Pending
- 2019-06-27 CA CA3102214A patent/CA3102214A1/en active Pending
- 2019-06-27 CN CN201980057157.9A patent/CN112638380B/zh active Active
- 2019-06-27 WO PCT/US2019/039555 patent/WO2020006264A1/en not_active Ceased
- 2019-06-27 US US17/255,734 patent/US11530219B2/en active Active
-
2022
- 2022-11-11 US US17/985,415 patent/US12110292B2/en active Active
-
2023
- 2023-07-25 JP JP2023120536A patent/JP7631434B2/ja active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101966183A (zh) * | 2003-12-02 | 2011-02-09 | 细胞基因公司 | 用于治疗和控制血红蛋白病和贫血病的方法和组合物 |
| CN1968695A (zh) * | 2004-04-14 | 2007-05-23 | 细胞基因公司 | 含有用于治疗和控制骨髓发育不良综合征的免疫调节化合物的组合物和使用方法 |
| CN102264720A (zh) * | 2008-10-29 | 2011-11-30 | 细胞基因公司 | 用于治疗癌症的异吲哚啉化合物 |
| CN106660991A (zh) * | 2014-07-11 | 2017-05-10 | 细胞基因公司 | 抗增殖化合物及其使用方法 |
Non-Patent Citations (1)
| Title |
|---|
| 巴德年主编.《基础医学卷 分子药理学》.黑龙江科学技术出版社,1999,(第1版),第299-302页，尤其是第300页第2段，第301页第2段、倒数第2段. * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20230312575A1 (en) | 2023-10-05 |
| AU2019294835B2 (en) | 2025-04-17 |
| US11530219B2 (en) | 2022-12-20 |
| EP3813829A4 (en) | 2021-12-08 |
| JP7321194B2 (ja) | 2023-08-04 |
| AU2019294835A1 (en) | 2020-12-17 |
| US20210292325A1 (en) | 2021-09-23 |
| JP2021530451A (ja) | 2021-11-11 |
| JP2023139195A (ja) | 2023-10-03 |
| WO2020006264A1 (en) | 2020-01-02 |
| KR20250020690A (ko) | 2025-02-11 |
| JP7631434B2 (ja) | 2025-02-18 |
| US12110292B2 (en) | 2024-10-08 |
| KR20210025061A (ko) | 2021-03-08 |
| CN112638380A (zh) | 2021-04-09 |
| EP3813829A1 (en) | 2021-05-05 |
| CA3102214A1 (en) | 2020-01-02 |
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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 | ||
| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: N. Grey Inventor after: T.Zhang Inventor after: E. Fisher Inventor after: Z.He Inventor after: G.Du Inventor after: K.DONOVAN Inventor after: R. Novak Inventor after: J.T.C.Yuan Inventor before: N. Grey Inventor before: T.Zhang Inventor before: E. Fisher Inventor before: A. Villeno Inventor before: Z.He Inventor before: G.Du Inventor before: K.DONOVAN Inventor before: R. Novak Inventor before: J.T.C.Yuan |
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