CN114401960A - 胶降解剂及其使用方法 - Google Patents
胶降解剂及其使用方法 Download PDFInfo
- Publication number
- CN114401960A CN114401960A CN202080063698.5A CN202080063698A CN114401960A CN 114401960 A CN114401960 A CN 114401960A CN 202080063698 A CN202080063698 A CN 202080063698A CN 114401960 A CN114401960 A CN 114401960A
- Authority
- CN
- China
- Prior art keywords
- heteroatoms selected
- aryl
- carbocyclyl
- alkyl
- membered heteroaryl
- Prior art date
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Classifications
-
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- 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
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/14—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 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (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)
- Neurosurgery (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962901229P | 2019-09-16 | 2019-09-16 | |
| US62/901,229 | 2019-09-16 | ||
| PCT/IB2020/058641 WO2021053555A1 (en) | 2019-09-16 | 2020-09-16 | Glue degraders and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN114401960A true CN114401960A (zh) | 2022-04-26 |
Family
ID=72717893
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080063698.5A Pending CN114401960A (zh) | 2019-09-16 | 2020-09-16 | 胶降解剂及其使用方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20220363671A1 (https=) |
| EP (1) | EP4031243A1 (https=) |
| JP (1) | JP2022548095A (https=) |
| CN (1) | CN114401960A (https=) |
| WO (1) | WO2021053555A1 (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116804005A (zh) * | 2022-05-13 | 2023-09-26 | 上海湃隆生物科技有限公司 | 驱动蛋白kif18a抑制剂及其应用 |
| WO2024074127A1 (en) * | 2022-10-04 | 2024-04-11 | Biofront Ltd | Gspt1 degraders, compositions comprising the degrader, and methods of using the same |
| WO2025256460A1 (en) * | 2023-06-15 | 2025-12-18 | Linkcure Therapeutics | Dihydropyrimidine-2,4(1h,3h)-dione-containing polycyclic derivatives and pharmaceutical composition thereof, preparation method thereof and use thereof |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CA3119773A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| PH12022500002A1 (en) | 2019-06-28 | 2023-04-03 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2021011868A1 (en) | 2019-07-17 | 2021-01-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2021119159A1 (en) | 2019-12-10 | 2021-06-17 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| EP4076524A4 (en) | 2019-12-17 | 2023-11-29 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
| KR20220145325A (ko) | 2019-12-17 | 2022-10-28 | 카이메라 쎄라퓨틱스 인코포레이티드 | Irak 분해제 및 이의 용도 |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| IL303458A (en) * | 2020-12-09 | 2023-08-01 | Kymera Therapeutics Inc | IRAK joints and their uses |
| CN116867758A (zh) | 2020-12-30 | 2023-10-10 | 凯麦拉医疗公司 | Irak降解剂和其用途 |
| AU2022207648A1 (en) | 2021-01-13 | 2023-07-27 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| US20240085421A1 (en) | 2021-01-13 | 2024-03-14 | Monte Rosa Therapeutics, Inc. | Methods for the identification of degrons |
| US12171768B2 (en) | 2021-02-15 | 2024-12-24 | Kymera Therapeutics, Inc. | IRAK4 degraders and uses thereof |
| WO2022254362A1 (en) | 2021-06-03 | 2022-12-08 | Novartis Ag | 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof |
| WO2022256623A1 (en) | 2021-06-04 | 2022-12-08 | Monte Rosa Therapeutics, Inc. | E3 ligase fusion proteins for proximity detection |
| CA3236265A1 (en) | 2021-10-29 | 2023-05-04 | William Leong | Irak4 degraders and synthesis thereof |
| WO2023091567A1 (en) | 2021-11-17 | 2023-05-25 | Monte Rosa Therapeutics, Inc. | Degron and neosubstrate identification |
| CN114487379A (zh) * | 2022-01-17 | 2022-05-13 | 东南大学 | 一种用于联合检测ca125与he4的试纸条 |
| CA3243560A1 (en) | 2022-01-31 | 2023-08-03 | Kymera Therapeutics, Inc. | Iraqi Degradation Agents and Their Uses |
| CN114410607A (zh) * | 2022-03-22 | 2022-04-29 | 上海威高医疗技术发展有限公司 | 嗜热羧酸酯酶突变体及其应用 |
| CN121311479A (zh) | 2023-01-09 | 2026-01-09 | 蒙特罗萨治疗股份公司 | Vav1的靶向降解 |
| PE20260307A1 (es) | 2023-06-14 | 2026-02-11 | Astrazeneca Ab | Degradadores de smarca2 y usos de estos |
| PE20260301A1 (es) | 2023-06-14 | 2026-02-10 | Astrazeneca Ab | Derivados de 3-[3-amino-6-(2-hidroxifenil)piridazin-4-il]-3,8-diazabiciclo[3.2.1]octano como protacs degradantes de smarca2 para el tratamiento del cancer |
| AU2024298923A1 (en) | 2023-07-25 | 2026-01-22 | Monte Rosa Therapeutics Ag | Substituted piperidinediones for targeted protein degradation |
| WO2025232887A1 (en) * | 2024-05-10 | 2025-11-13 | Shanghai Degron Biomedical Technology Co., Ltd. | Wee1 degraders and uses thereof |
| WO2026013577A1 (en) * | 2024-07-10 | 2026-01-15 | Monte Rosa Therapeutics Ag | Piperidine-2, 6-dione derivatives useful for the targeted degradation of vav1 |
| WO2026013576A1 (en) * | 2024-07-10 | 2026-01-15 | Monte Rosa Therapeutics Ag | Dihydrouracil derivatives useful for the targeted degradation of vav1 |
| WO2026013578A1 (en) * | 2024-07-10 | 2026-01-15 | Monte Rosa Therapeutics Ag | Combinations comprising vav1-targeting degraders |
| WO2026067646A1 (zh) * | 2024-09-27 | 2026-04-02 | 上海美悦生物科技发展有限公司 | 联苯类化合物、及其药物组合物和用途 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102803216A (zh) * | 2009-06-09 | 2012-11-28 | 弗·哈夫曼-拉罗切有限公司 | 杂环抗病毒化合物 |
| WO2018144649A1 (en) * | 2017-01-31 | 2018-08-09 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5114946A (en) | 1987-06-12 | 1992-05-19 | American Cyanamid Company | Transdermal delivery of pharmaceuticals |
| US4818541A (en) | 1987-08-19 | 1989-04-04 | Schering Corporation | Transdermal delivery of enantiomers of phenylpropanolamine |
| BR112018068906A2 (pt) * | 2016-03-16 | 2019-01-22 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | composição, método, método de redução de risco, prevenção ou tratamento de um indivíduo que tem uma doença ou distúrbio autoimune, método de indução de degradação de uma proteína-alvo numa célula, método para reduzir o risco, prevenir ou tratar um estado da doença ou afecção num paciente em que a atividade proteica desregulada é responsável pelo referido estado da doença ou afecção, método para reduzir o risco, prevenir ou tratar câncer num indivíduo e método de tratamento de uma doença ou distúrbio genético num indivíduo |
| WO2019140387A1 (en) * | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| CN120698983A (zh) * | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
-
2020
- 2020-09-16 WO PCT/IB2020/058641 patent/WO2021053555A1/en not_active Ceased
- 2020-09-16 EP EP20785841.6A patent/EP4031243A1/en active Pending
- 2020-09-16 CN CN202080063698.5A patent/CN114401960A/zh active Pending
- 2020-09-16 US US17/642,292 patent/US20220363671A1/en active Pending
- 2020-09-16 JP JP2022516379A patent/JP2022548095A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102803216A (zh) * | 2009-06-09 | 2012-11-28 | 弗·哈夫曼-拉罗切有限公司 | 杂环抗病毒化合物 |
| WO2018144649A1 (en) * | 2017-01-31 | 2018-08-09 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
Non-Patent Citations (3)
| Title |
|---|
| "RN 1500994-95-5", STN REGISTRY, 22 December 2013 (2013-12-22), pages 1 * |
| "RN 1711790-34-9", STN REGISTRY, 25 May 2015 (2015-05-25), pages 1 * |
| FRANCISCO X. TALAMAS ET AL: "Discovery of N-[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 5, 6 November 2013 (2013-11-06), pages 1914 - 1931, XP055343623, DOI: 10.1021/jm401329s * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116804005A (zh) * | 2022-05-13 | 2023-09-26 | 上海湃隆生物科技有限公司 | 驱动蛋白kif18a抑制剂及其应用 |
| CN116804005B (zh) * | 2022-05-13 | 2024-07-19 | 上海湃隆生物科技有限公司 | 驱动蛋白kif18a抑制剂及其应用 |
| WO2024074127A1 (en) * | 2022-10-04 | 2024-04-11 | Biofront Ltd | Gspt1 degraders, compositions comprising the degrader, and methods of using the same |
| WO2025256460A1 (en) * | 2023-06-15 | 2025-12-18 | Linkcure Therapeutics | Dihydropyrimidine-2,4(1h,3h)-dione-containing polycyclic derivatives and pharmaceutical composition thereof, preparation method thereof and use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| US20220363671A1 (en) | 2022-11-17 |
| EP4031243A1 (en) | 2022-07-27 |
| WO2021053555A1 (en) | 2021-03-25 |
| JP2022548095A (ja) | 2022-11-16 |
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