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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active 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
- 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)
- 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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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 (enExample) |
| EP (1) | EP3813829A4 (enExample) |
| JP (2) | JP7321194B2 (enExample) |
| KR (2) | KR20250020690A (enExample) |
| CN (1) | CN112638380B (enExample) |
| AU (1) | AU2019294835B2 (enExample) |
| CA (1) | CA3102214A1 (enExample) |
| WO (1) | WO2020006264A1 (enExample) |
Families Citing this family (25)
| 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 |
| JP2021519337A (ja) | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Ｉｋａｒｏｓの分解のためのセレブロン結合剤 |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| JP7293343B2 (ja) | 2018-05-09 | 2023-06-19 | アプリノイア セラピューティクス リミテッド | ヘテロアリール化合物及びその使用 |
| CA3102214A1 (en) * | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (crbn) |
| AU2020383593A1 (en) | 2019-11-13 | 2022-06-09 | Aprinoia Therapeutics Limited | Compounds for degrading Tau protein aggregates and uses thereof |
| JP2023507590A (ja) * | 2019-12-17 | 2023-02-24 | オリオニス バイオサイエンシズ，インコーポレイテッド | タンパク質の動員および／または分解を調節する化合物 |
| CN114828959B (zh) | 2019-12-18 | 2024-04-02 | 诺华股份有限公司 | 3-(5-甲氧基-1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途 |
| US20230203022A1 (en) * | 2020-04-30 | 2023-06-29 | Shanghaitech University | Heterocycle and glutarimide skeleton-based compound and applications thereof |
| CA3208313A1 (en) | 2021-01-13 | 2022-07-21 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| AR125798A1 (es) | 2021-05-07 | 2023-08-16 | Kymera Therapeutics Inc | Degradadores cdk2 y usos de los mismos |
| CA3215410A1 (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 |
| CN117715903A (zh) * | 2021-06-25 | 2024-03-15 | 新基公司 | Cereblon结合化合物、其组合物及其用于治疗的方法 |
| EP4426687A4 (en) * | 2021-11-04 | 2025-12-10 | Brigham & Womens Hospital Inc | DIRECTED DEGRON MOLECULES AND THEIR APPLICATIONS |
| AU2022419982A1 (en) * | 2021-12-22 | 2024-06-06 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| WO2023122615A1 (en) * | 2021-12-22 | 2023-06-29 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| KR102738668B1 (ko) | 2022-02-25 | 2024-12-06 | 계명대학교 산학협력단 | 항암 활성을 갖는 신규 화합물 및 이의 용도 |
| TW202346277A (zh) | 2022-03-17 | 2023-12-01 | 美商基利科學股份有限公司 | Ｉｋａｒｏｓ鋅指家族降解劑及其用途 |
| CN119325475A (zh) | 2022-06-06 | 2025-01-17 | C4医药公司 | 双环取代的戊二酰亚胺cereblon结合剂 |
| AR130961A1 (es) | 2022-11-04 | 2025-02-05 | Bristol Myers Squibb Co | Compuestos y su uso para el tratamiento de hemoglobinopatías |
| WO2024167423A1 (en) * | 2023-02-07 | 2024-08-15 | Captor Therapeutics S.A. | Gspt1 degrader compounds |
| WO2024238872A2 (en) * | 2023-05-18 | 2024-11-21 | 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 |
| MX2008002765A (es) * | 2005-08-31 | 2008-04-07 | Celgene Corp | Compuestos de isoindol-imida y composiciones que la comprenden y metodos para usar los mismos. |
| KR101149295B1 (ko) * | 2006-12-08 | 2012-07-05 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 |
| 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 |
| MX387318B (es) * | 2014-04-14 | 2025-03-18 | Arvinas Operations Inc | Moduladores de la proteólisis basados en imida y métodos de uso asociados. |
| JP6640126B2 (ja) * | 2014-06-27 | 2020-02-05 | セルジーン コーポレイション | セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法 |
| 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 |
| CN111278815B (zh) | 2017-09-04 | 2024-03-08 | C4医药公司 | 戊二酰亚胺 |
| EP3737675A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| WO2019241274A1 (en) | 2018-06-13 | 2019-12-19 | Biotheryx, Inc. | Aminoamide compounds |
| CA3102214A1 (en) * | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (crbn) |
-
2019
- 2019-06-27 CA CA3102214A patent/CA3102214A1/en active Pending
- 2019-06-27 AU AU2019294835A patent/AU2019294835B2/en active Active
- 2019-06-27 WO PCT/US2019/039555 patent/WO2020006264A1/en not_active Ceased
- 2019-06-27 CN CN201980057157.9A patent/CN112638380B/zh active Active
- 2019-06-27 US US17/255,734 patent/US11530219B2/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 KR KR1020217001892A patent/KR20210025061A/ko active Pending
- 2019-06-27 EP EP19827425.0A patent/EP3813829A4/en active Pending
-
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 |
|---|---|
| CA3102214A1 (en) | 2020-01-02 |
| US11530219B2 (en) | 2022-12-20 |
| AU2019294835B2 (en) | 2025-04-17 |
| WO2020006264A1 (en) | 2020-01-02 |
| KR20210025061A (ko) | 2021-03-08 |
| AU2019294835A1 (en) | 2020-12-17 |
| EP3813829A1 (en) | 2021-05-05 |
| CN112638380A (zh) | 2021-04-09 |
| JP2023139195A (ja) | 2023-10-03 |
| JP7631434B2 (ja) | 2025-02-18 |
| JP7321194B2 (ja) | 2023-08-04 |
| US20210292325A1 (en) | 2021-09-23 |
| US20230312575A1 (en) | 2023-10-05 |
| US12110292B2 (en) | 2024-10-08 |
| JP2021530451A (ja) | 2021-11-11 |
| EP3813829A4 (en) | 2021-12-08 |
| KR20250020690A (ko) | 2025-02-11 |
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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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| GR01 | Patent grant |