JP7852923B2 - セレブロンに結合するピペリジン-2,6-ジオン誘導体、及びその使用方法 - Google Patents
セレブロンに結合するピペリジン-2,6-ジオン誘導体、及びその使用方法Info
- Publication number
- JP7852923B2 JP7852923B2 JP2022532037A JP2022532037A JP7852923B2 JP 7852923 B2 JP7852923 B2 JP 7852923B2 JP 2022532037 A JP2022532037 A JP 2022532037A JP 2022532037 A JP2022532037 A JP 2022532037A JP 7852923 B2 JP7852923 B2 JP 7852923B2
- Authority
- JP
- Japan
- Prior art keywords
- nhr
- hydrogen
- compound
- aryl
- nhc
- 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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—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 two hetero rings
- C07D495/04—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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL2019000109 | 2019-11-27 | ||
| PLPCT/PL2019/000109 | 2019-11-27 | ||
| PCT/EP2020/083596 WO2021105334A1 (en) | 2019-11-27 | 2020-11-27 | Piperidine-2, 6-dione derivatives which bind to cereblon, and methods of use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023504445A JP2023504445A (ja) | 2023-02-03 |
| JP2023504445A5 JP2023504445A5 (https=) | 2023-12-05 |
| JP7852923B2 true JP7852923B2 (ja) | 2026-04-28 |
Family
ID=69024572
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022532037A Active JP7852923B2 (ja) | 2019-11-27 | 2020-11-27 | セレブロンに結合するピペリジン-2,6-ジオン誘導体、及びその使用方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20240343706A1 (https=) |
| EP (1) | EP4065571A1 (https=) |
| JP (1) | JP7852923B2 (https=) |
| KR (1) | KR20220106801A (https=) |
| CN (1) | CN115023419A (https=) |
| AU (1) | AU2020392427B2 (https=) |
| WO (1) | WO2021105334A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022255888A1 (en) * | 2021-06-01 | 2022-12-08 | Captor Therapeutics S.A. | Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein |
| WO2024015340A1 (en) * | 2022-07-12 | 2024-01-18 | Regents Of The University Of Michigan | Cereblon ligands and uses thereof |
| EP4584259A1 (en) | 2022-09-09 | 2025-07-16 | Innovo Therapeutics, Inc. | Ck1alpha and dual ck1alpha / gspt1 degrading compounds |
| WO2024123195A1 (en) * | 2022-12-06 | 2024-06-13 | Captor Therapeutics S.A. | Targeted protein degradation using prodrugs of bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein |
| KR20250130610A (ko) * | 2022-12-06 | 2025-09-02 | 캡터 테라퓨틱스 에스.에이. | 유비퀴틴 리가제 및 표적 mcl-1 단백질에 결합하는 이작용성 화합물을 사용하는 표적화된 단백질 분해 |
| CN120530094A (zh) * | 2023-01-12 | 2025-08-22 | 田边三菱制药株式会社 | Cereblon E3连接酶结合化合物、包含其的药物组合物及其制造方法 |
| CN121843932A (zh) | 2023-08-31 | 2026-04-10 | 先正达农作物保护股份公司 | 杀有害生物活性吲唑化合物 |
| CN117224547B (zh) * | 2023-09-12 | 2025-05-27 | 中国医科大学附属第一医院 | 一种小分子化合物dBET1在银屑病治疗中的应用 |
| WO2025063888A1 (en) | 2023-09-19 | 2025-03-27 | Kancure Pte. Ltd. | Survivin-targeted compounds |
| WO2025179161A1 (en) | 2024-02-21 | 2025-08-28 | Innovo Therapeutics, Inc. | Protein degrading compounds |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010149309A2 (de) | 2009-06-24 | 2010-12-29 | Bayer Cropscience Ag | Cycloalkylamidbenzoxa(thia)zole |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| JP2019512497A (ja) | 2016-03-16 | 2019-05-16 | エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド | エフェクターt細胞機能を増進するための、セレブロンを標的とする小分子 |
| WO2020006233A1 (en) | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Immunomodulatory compounds |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5635517B1 (en) | 1996-07-24 | 1999-06-29 | Celgene Corp | Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines |
| US7323479B2 (en) | 2002-05-17 | 2008-01-29 | Celgene Corporation | Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline |
| WO2008007979A1 (en) * | 2006-07-12 | 2008-01-17 | Auckland Uniservices Limited | (2,6-dioxo-3-piperinyl)amidobenzoic immunomodulatory and anti-cancer derivatives |
| CL2007002513A1 (es) | 2006-08-30 | 2008-04-04 | Celgene Corp Soc Organizada Ba | Compuestos derivados de isoindolina sustituidos, compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento y prevencion de enfermedades tales como cancer, dolor, degeneracion macular, entre otras. |
| ME02420B (me) | 2006-09-26 | 2016-09-20 | Celgene Corp | 5-supstituirani derivati kinazolinona kao sredstva protiv raka |
| PL3202460T3 (pl) | 2010-02-11 | 2019-12-31 | Celgene Corporation | Pochodne arylometoksyizoindoliny i zawierające je kompozycje oraz sposoby ich zastosowania |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| EP4467143B1 (en) | 2017-07-10 | 2026-03-11 | Celgene Corporation | Method for preparing 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-l-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-l-yl)-3-fluorobenzonitrile |
| IL302595A (en) | 2018-04-13 | 2023-07-01 | Arvinas Operations Inc | Servalon ligands and bifunctional compounds containing them |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CA3154386A1 (en) * | 2019-10-17 | 2021-04-22 | Michael Berlin | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
-
2020
- 2020-11-27 JP JP2022532037A patent/JP7852923B2/ja active Active
- 2020-11-27 AU AU2020392427A patent/AU2020392427B2/en active Active
- 2020-11-27 WO PCT/EP2020/083596 patent/WO2021105334A1/en not_active Ceased
- 2020-11-27 EP EP20811632.7A patent/EP4065571A1/en active Pending
- 2020-11-27 CN CN202080094725.5A patent/CN115023419A/zh active Pending
- 2020-11-27 KR KR1020227021713A patent/KR20220106801A/ko active Pending
- 2020-11-27 US US17/780,891 patent/US20240343706A1/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010149309A2 (de) | 2009-06-24 | 2010-12-29 | Bayer Cropscience Ag | Cycloalkylamidbenzoxa(thia)zole |
| JP2019512497A (ja) | 2016-03-16 | 2019-05-16 | エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド | エフェクターt細胞機能を増進するための、セレブロンを標的とする小分子 |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| WO2020006233A1 (en) | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Immunomodulatory compounds |
Non-Patent Citations (1)
| Title |
|---|
| REGISTRY(STN), [online],2019年05月28日,[2024年10月19日検索], CAS登録番号2319329-84-3、2126512-61-4、1955105-26-6、1609734-02-2、1496481-02-7、1372083-28-7、1290770-85-2 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20240343706A1 (en) | 2024-10-17 |
| EP4065571A1 (en) | 2022-10-05 |
| AU2020392427A1 (en) | 2022-06-16 |
| CN115023419A (zh) | 2022-09-06 |
| AU2020392427B2 (en) | 2024-03-07 |
| JP2023504445A (ja) | 2023-02-03 |
| WO2021105334A1 (en) | 2021-06-03 |
| KR20220106801A (ko) | 2022-07-29 |
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