CN116783183B - 用于治疗贫血和癌症的vhl抑制剂 - Google Patents
用于治疗贫血和癌症的vhl抑制剂Info
- Publication number
- CN116783183B CN116783183B CN202080108318.5A CN202080108318A CN116783183B CN 116783183 B CN116783183 B CN 116783183B CN 202080108318 A CN202080108318 A CN 202080108318A CN 116783183 B CN116783183 B CN 116783183B
- Authority
- CN
- China
- Prior art keywords
- independently
- alkyl
- compound
- group
- foregoing
- 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.)
- Active
Links
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D409/14—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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063112609P | 2020-11-11 | 2020-11-11 | |
| US63/112,609 | 2020-11-11 | ||
| PCT/US2020/062627 WO2022103411A1 (en) | 2020-11-11 | 2020-11-30 | 1-(2-(4-cyclopropyl-1h-1,2,3-triazol-1-yl)acetyl)-4-hydroxy-n-(benzyl)pyrrolidin e-2-carboxamide derivatives as vhl inhibitors for the treatment of anemia and cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN116783183A CN116783183A (zh) | 2023-09-19 |
| CN116783183B true CN116783183B (zh) | 2026-03-20 |
Family
ID=73839136
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080108318.5A Active CN116783183B (zh) | 2020-11-11 | 2020-11-30 | 用于治疗贫血和癌症的vhl抑制剂 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230391766A1 (https=) |
| EP (1) | EP4244218A1 (https=) |
| JP (2) | JP7654075B2 (https=) |
| KR (1) | KR20230106637A (https=) |
| CN (1) | CN116783183B (https=) |
| AU (1) | AU2020476996A1 (https=) |
| CA (1) | CA3197092A1 (https=) |
| IL (1) | IL302678A (https=) |
| MX (1) | MX2023005305A (https=) |
| WO (1) | WO2022103411A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN119677735A (zh) * | 2022-05-11 | 2025-03-21 | 基因泰克公司 | 作为vhl配体的苯并噻唑化合物 |
| WO2025162250A1 (zh) * | 2024-02-04 | 2025-08-07 | 贝达药业股份有限公司 | 取代的三环化合物及其用途 |
| WO2025228305A1 (zh) * | 2024-04-28 | 2025-11-06 | 中国科学院上海药物研究所 | 一种蛋白降解剂缀合物及其偶联物 |
| WO2026012475A1 (en) * | 2024-07-12 | 2026-01-15 | Ascentage Pharma (Suzhou) Co., Ltd. | Vhl ligands and uses thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109952299A (zh) * | 2016-09-14 | 2019-06-28 | 邓迪大学 | 用于制备蛋白降解靶向嵌合体的氟代羟脯氨酸衍生物 |
| CN110573507A (zh) * | 2017-04-14 | 2019-12-13 | 邓迪大学 | 小分子 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| WO2013106646A2 (en) * | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| KR102668696B1 (ko) * | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| US11547759B2 (en) * | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
-
2020
- 2020-11-30 KR KR1020237018547A patent/KR20230106637A/ko active Pending
- 2020-11-30 CA CA3197092A patent/CA3197092A1/en active Pending
- 2020-11-30 EP EP20825085.2A patent/EP4244218A1/en active Pending
- 2020-11-30 JP JP2023528057A patent/JP7654075B2/ja active Active
- 2020-11-30 MX MX2023005305A patent/MX2023005305A/es unknown
- 2020-11-30 WO PCT/US2020/062627 patent/WO2022103411A1/en not_active Ceased
- 2020-11-30 CN CN202080108318.5A patent/CN116783183B/zh active Active
- 2020-11-30 IL IL302678A patent/IL302678A/en unknown
- 2020-11-30 AU AU2020476996A patent/AU2020476996A1/en active Pending
-
2023
- 2023-05-09 US US18/195,134 patent/US20230391766A1/en active Pending
-
2025
- 2025-01-23 JP JP2025009859A patent/JP2025063287A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109952299A (zh) * | 2016-09-14 | 2019-06-28 | 邓迪大学 | 用于制备蛋白降解靶向嵌合体的氟代羟脯氨酸衍生物 |
| CN110573507A (zh) * | 2017-04-14 | 2019-12-13 | 邓迪大学 | 小分子 |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2023005305A (es) | 2023-05-25 |
| WO2022103411A1 (en) | 2022-05-19 |
| US20230391766A1 (en) | 2023-12-07 |
| KR20230106637A (ko) | 2023-07-13 |
| AU2020476996A1 (en) | 2023-06-29 |
| CN116783183A (zh) | 2023-09-19 |
| CA3197092A1 (en) | 2022-05-19 |
| JP7654075B2 (ja) | 2025-03-31 |
| IL302678A (en) | 2023-07-01 |
| JP2023549187A (ja) | 2023-11-22 |
| EP4244218A1 (en) | 2023-09-20 |
| JP2025063287A (ja) | 2025-04-15 |
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