EP4747239A1 - Kleinmolekülige proteinabbauer einer kras-g12d-mutante - Google Patents
Kleinmolekülige proteinabbauer einer kras-g12d-mutanteInfo
- Publication number
- EP4747239A1 EP4747239A1 EP24844050.5A EP24844050A EP4747239A1 EP 4747239 A1 EP4747239 A1 EP 4747239A1 EP 24844050 A EP24844050 A EP 24844050A EP 4747239 A1 EP4747239 A1 EP 4747239A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- cancer
- group
- 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.)
- Pending
Links
Classifications
-
- 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
-
- 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
-
- 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
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06052—Val-amino acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202363527963P | 2023-07-20 | 2023-07-20 | |
| PCT/US2024/038859 WO2025019823A1 (en) | 2023-07-20 | 2024-07-19 | Small molecule protein degraders of kras g12d mutant |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EP4747239A1 true EP4747239A1 (de) | 2026-05-27 |
Family
ID=94282734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP24844050.5A Pending EP4747239A1 (de) | 2023-07-20 | 2024-07-19 | Kleinmolekülige proteinabbauer einer kras-g12d-mutante |
Country Status (2)
| Country | Link |
|---|---|
| EP (1) | EP4747239A1 (de) |
| WO (1) | WO2025019823A1 (de) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021085653A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| EP4067343A4 (de) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | Neuartige phenolverbindung oder salz davon |
| US12702658B2 (en) | 2020-04-24 | 2026-08-11 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| WO2022109487A1 (en) | 2020-11-23 | 2022-05-27 | Merck Sharp & Dohme Corp. | Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant |
| KR20260096846A (ko) | 2023-10-20 | 2026-06-24 | 머크 샤프 앤드 돔 엘엘씨 | Kras 단백질의 소분자 억제제 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110869358A (zh) * | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| CN116490508A (zh) * | 2020-11-20 | 2023-07-25 | 北京加科思新药研发有限公司 | Kras g12d抑制剂 |
| AU2022220678A1 (en) * | 2021-02-09 | 2023-09-21 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| MX2023008463A (es) * | 2021-02-16 | 2023-12-07 | Leidos Biomedical Res Inc | Composiciones y métodos para la inhibición del gen del virus de sarcoma de rata kirsten (kras). |
| US20240239788A1 (en) * | 2021-04-16 | 2024-07-18 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12d mutant |
| WO2023103523A1 (zh) * | 2021-12-09 | 2023-06-15 | 苏州浦合医药科技有限公司 | 取代的双环杂芳基化合物作为kras g12d抑制剂 |
-
2024
- 2024-07-19 WO PCT/US2024/038859 patent/WO2025019823A1/en not_active Ceased
- 2024-07-19 EP EP24844050.5A patent/EP4747239A1/de active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2025019823A1 (en) | 2025-01-23 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE |
|
| PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE |
|
| 17P | Request for examination filed |
Effective date: 20260220 |
|
| AK | Designated contracting states |
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| P01 | Opt-out of the competence of the unified patent court (upc) registered |
Free format text: CASE NUMBER: UPC_APP_0017619_4747239/2026 Effective date: 20260608 |