JP7321194B2 - セレブロン(crbn)に対するリガンド - Google Patents
セレブロン(crbn)に対するリガンド Download PDFInfo
- Publication number
- JP7321194B2 JP7321194B2 JP2020571833A JP2020571833A JP7321194B2 JP 7321194 B2 JP7321194 B2 JP 7321194B2 JP 2020571833 A JP2020571833 A JP 2020571833A JP 2020571833 A JP2020571833 A JP 2020571833A JP 7321194 B2 JP7321194 B2 JP 7321194B2
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- JP
- Japan
- Prior art keywords
- mmol
- amino
- mixture
- cancer
- tfa
- 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)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Immunology (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023120536A JP7631434B2 (ja) | 2018-06-29 | 2023-07-25 | セレブロン(crbn)に対するリガンド |
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) |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023120536A Division JP7631434B2 (ja) | 2018-06-29 | 2023-07-25 | セレブロン(crbn)に対するリガンド |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021530451A JP2021530451A (ja) | 2021-11-11 |
| JPWO2020006264A5 JPWO2020006264A5 (https=) | 2022-06-29 |
| JP2021530451A5 JP2021530451A5 (https=) | 2022-06-29 |
| JP7321194B2 true JP7321194B2 (ja) | 2023-08-04 |
Family
ID=68987146
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020571833A Active JP7321194B2 (ja) | 2018-06-29 | 2019-06-27 | セレブロン(crbn)に対するリガンド |
| JP2023120536A Active JP7631434B2 (ja) | 2018-06-29 | 2023-07-25 | セレブロン(crbn)に対するリガンド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023120536A Active JP7631434B2 (ja) | 2018-06-29 | 2023-07-25 | セレブロン(crbn)に対するリガンド |
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=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023139195A (ja) * | 2018-06-29 | 2023-10-03 | 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 | セレブロン(crbn)に対するリガンド |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2767532B1 (en) | 2012-12-21 | 2016-07-13 | National Institutes for Quantum and Radiological Science and Technology | Novel compound for imaging tau protein accumulated in the brain |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| 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 |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| 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 |
| EP3932922A4 (en) | 2019-02-25 | 2022-05-11 | ShanghaiTech University | SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE |
| 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 |
| CA3161455A1 (en) | 2019-11-13 | 2021-05-20 | 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 |
| JP7682181B2 (ja) | 2019-12-18 | 2025-05-23 | ノバルティス アーゲー | 3-(5-メトキシ-1-オキソイソインドリン-2-イル)ピペリジン-2,6-ジオン誘導体及びその使用 |
| EP4144728A4 (en) * | 2020-04-30 | 2023-08-23 | Shanghaitech University | HETEROCYCLIC COMPOUND BASED ON A GLUTARIMIDE SKELETON AND USES THEREOF |
| JP2024504932A (ja) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス, インコーポレイテッド | イソインドリノン化合物 |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| PY2243958A (es) | 2021-06-03 | 2023-01-20 | Novartis Ag | Derivados de 3–(5–oxi)–1–oxoisoindolin–2–il)piperidina–2,6–diona y sus usos |
| 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 |
| EP4359404A4 (en) * | 2021-06-25 | 2025-06-04 | 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 |
| CN118488946A (zh) * | 2021-12-22 | 2024-08-13 | 吉利德科学公司 | Ikaros锌指家族降解剂及其用途 |
| EP4452415B1 (en) | 2021-12-22 | 2026-02-25 | 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 |
| CA3253296A1 (en) | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Zinc Finger Degradation Agents of the Ikaros Family and Their Uses |
| JP2025523393A (ja) | 2022-06-06 | 2025-07-23 | シーフォー セラピューティクス, インコーポレイテッド | 二環式置換グルタルイミドセレブロンバインダー |
| EP4570792A1 (en) * | 2022-08-10 | 2025-06-18 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | Compound based on isoindoline-substituted glutarimide backbone and use thereof |
| CN120129677A (zh) | 2022-11-04 | 2025-06-10 | 百时美施贵宝公司 | 化合物及其用于治疗血红素病变的用途 |
| WO2024167423A1 (en) * | 2023-02-07 | 2024-08-15 | Captor Therapeutics S.A. | Gspt1 degrader compounds |
| TW202500195A (zh) * | 2023-05-18 | 2025-01-01 | 美商飛爾富來生物公司 | 異吲哚啉酮-戊二醯亞胺抗體結合物及其用途 |
| 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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004525889A (ja) | 2000-12-27 | 2004-08-26 | セルジーン・コーポレーション | イソインドール−イミド化合物、組成物、およびそれらの使用 |
| JP2007513164A (ja) | 2003-12-02 | 2007-05-24 | セルジーン・コーポレーション | 異常ヘモグロビン症及び貧血症の治療及び管理のための方法及び組成物 |
| JP2007532641A (ja) | 2004-04-14 | 2007-11-15 | セルジーン・コーポレーション | 脊髄形成異常症候群の治療及び管理のための免疫調節化合物の使用法、及びそれを含む組成物 |
| JP2009506117A (ja) | 2005-08-31 | 2009-02-12 | セルジーン・コーポレーション | イソインドール−イミド化合物及びそれを含有する組成物及びそれの使用法 |
| JP2010512329A (ja) | 2006-12-08 | 2010-04-22 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| JP2012528802A (ja) | 2009-06-01 | 2012-11-15 | ナンジン キャベンディッシュ バイオ−エンジニアリング テクノロジー カンパニー,リミテッド | 3−(置換二水素イソインドールケトン−2−イル)−2,6−ピペリジンジオンの合成方法及びその中間体 |
| JP2017525757A (ja) | 2014-07-11 | 2017-09-07 | セルジーン コーポレイション | 抗増殖性化合物及びその使用方法 |
| JP2017528690A (ja) | 2014-06-27 | 2017-09-28 | 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 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20110547A1 (es) | 2008-10-29 | 2011-08-04 | Celgene Corp | Compuestos de isoindolina con actividad anticancerigena |
| AU2015247817C1 (en) * | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| 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 |
| AU2019284608A1 (en) | 2018-06-13 | 2020-12-17 | Biotheryx, Inc. | Aminoamide compounds |
| KR20250020690A (ko) | 2018-06-29 | 2025-02-11 | 다나-파버 캔서 인스티튜트 인크. | 세레블론(crbn)에 대한 리간드 |
-
2019
- 2019-06-27 KR KR1020257001993A patent/KR20250020690A/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 EP EP19827425.0A patent/EP3813829A4/en active Pending
- 2019-06-27 AU AU2019294835A patent/AU2019294835B2/en active Active
- 2019-06-27 JP JP2020571833A patent/JP7321194B2/ja active Active
- 2019-06-27 US US17/255,734 patent/US11530219B2/en active Active
- 2019-06-27 KR KR1020217001892A patent/KR20210025061A/ko active Pending
- 2019-06-27 WO PCT/US2019/039555 patent/WO2020006264A1/en not_active Ceased
-
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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004525889A (ja) | 2000-12-27 | 2004-08-26 | セルジーン・コーポレーション | イソインドール−イミド化合物、組成物、およびそれらの使用 |
| JP2007513164A (ja) | 2003-12-02 | 2007-05-24 | セルジーン・コーポレーション | 異常ヘモグロビン症及び貧血症の治療及び管理のための方法及び組成物 |
| JP2007532641A (ja) | 2004-04-14 | 2007-11-15 | セルジーン・コーポレーション | 脊髄形成異常症候群の治療及び管理のための免疫調節化合物の使用法、及びそれを含む組成物 |
| JP2009506117A (ja) | 2005-08-31 | 2009-02-12 | セルジーン・コーポレーション | イソインドール−イミド化合物及びそれを含有する組成物及びそれの使用法 |
| JP2010512329A (ja) | 2006-12-08 | 2010-04-22 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| JP2012528802A (ja) | 2009-06-01 | 2012-11-15 | ナンジン キャベンディッシュ バイオ−エンジニアリング テクノロジー カンパニー,リミテッド | 3−(置換二水素イソインドールケトン−2−イル)−2,6−ピペリジンジオンの合成方法及びその中間体 |
| JP2017528690A (ja) | 2014-06-27 | 2017-09-28 | 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 |
| JP2017525757A (ja) | 2014-07-11 | 2017-09-07 | セルジーン コーポレイション | 抗増殖性化合物及びその使用方法 |
Non-Patent Citations (1)
| Title |
|---|
| Medicinal Chemistry Communications,2011年,2,1073 |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023139195A (ja) * | 2018-06-29 | 2023-10-03 | 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 | セレブロン(crbn)に対するリガンド |
| JP7631434B2 (ja) | 2018-06-29 | 2025-02-18 | 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 | セレブロン(crbn)に対するリガンド |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20210025061A (ko) | 2021-03-08 |
| US12110292B2 (en) | 2024-10-08 |
| KR20250020690A (ko) | 2025-02-11 |
| WO2020006264A1 (en) | 2020-01-02 |
| EP3813829A1 (en) | 2021-05-05 |
| JP2023139195A (ja) | 2023-10-03 |
| JP2021530451A (ja) | 2021-11-11 |
| JP7631434B2 (ja) | 2025-02-18 |
| CA3102214A1 (en) | 2020-01-02 |
| CN112638380B (zh) | 2024-05-24 |
| US20210292325A1 (en) | 2021-09-23 |
| CN112638380A (zh) | 2021-04-09 |
| US11530219B2 (en) | 2022-12-20 |
| US20230312575A1 (en) | 2023-10-05 |
| AU2019294835A1 (en) | 2020-12-17 |
| AU2019294835B2 (en) | 2025-04-17 |
| EP3813829A4 (en) | 2021-12-08 |
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