KR20250163395A - KRas 억제제 - Google Patents
KRas 억제제Info
- Publication number
- KR20250163395A KR20250163395A KR1020257035985A KR20257035985A KR20250163395A KR 20250163395 A KR20250163395 A KR 20250163395A KR 1020257035985 A KR1020257035985 A KR 1020257035985A KR 20257035985 A KR20257035985 A KR 20257035985A KR 20250163395 A KR20250163395 A KR 20250163395A
- Authority
- KR
- South Korea
- Prior art keywords
- cancer
- pharmaceutically acceptable
- acceptable salt
- optionally substituted
- compound
- 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
- 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
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- 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
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP23382315.2 | 2023-03-31 | ||
| EP23382315 | 2023-03-31 | ||
| EP23382531.4 | 2023-06-02 | ||
| EP23382531 | 2023-06-02 | ||
| EP23382857.3 | 2023-08-18 | ||
| EP23382857 | 2023-08-18 | ||
| EP23382985 | 2023-09-27 | ||
| EP23382985.2 | 2023-09-27 | ||
| EP24382267 | 2024-03-12 | ||
| EP24382267.3 | 2024-03-12 | ||
| PCT/US2024/022154 WO2024206766A1 (en) | 2023-03-31 | 2024-03-29 | Kras inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20250163395A true KR20250163395A (ko) | 2025-11-20 |
Family
ID=90826251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020257035985A Pending KR20250163395A (ko) | 2023-03-31 | 2024-03-29 | KRas 억제제 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20240368193A1 (https=) |
| EP (1) | EP4688792A1 (https=) |
| JP (2) | JP7669556B2 (https=) |
| KR (1) | KR20250163395A (https=) |
| CN (1) | CN121002032A (https=) |
| AR (1) | AR132295A1 (https=) |
| AU (1) | AU2024241889A1 (https=) |
| CL (1) | CL2025002769A1 (https=) |
| CO (1) | CO2025013134A2 (https=) |
| DO (1) | DOP2025000245A (https=) |
| IL (1) | IL323362A (https=) |
| JO (1) | JOP20250246A1 (https=) |
| MX (1) | MX2025011449A (https=) |
| PE (1) | PE20252444A1 (https=) |
| TW (1) | TWI901059B (https=) |
| WO (1) | WO2024206766A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025092798A1 (zh) * | 2023-10-30 | 2025-05-08 | 江苏恒瑞医药股份有限公司 | 稠合杂芳基类化合物、其制备方法及其在医药上的应用 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025214344A1 (zh) * | 2024-04-09 | 2025-10-16 | 上海和誉生物医药科技有限公司 | 一种kras抑制剂及其在药学上的应用 |
| 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 |
| WO2026015801A1 (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 |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| US12600733B2 (en) | 2024-10-01 | 2026-04-14 | Eli Lilly And Company | KRAS inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10844051B2 (en) | 2015-07-22 | 2020-11-24 | The Royal Institution For The Advancement Of Learning/Mcgill University | Substituted oxazoles for the treatment of cancer |
| HRP20230377T1 (hr) | 2017-11-15 | 2023-06-23 | Mirati Therapeutics, Inc. | Inhibitori mutacije kras g12c |
| TW202033518A (zh) | 2018-10-15 | 2020-09-16 | 美商美國禮來大藥廠 | Kras g12c 抑制劑 |
| WO2020146613A1 (en) | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| WO2021041671A1 (en) | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| ES2929700T3 (es) | 2019-12-11 | 2022-12-01 | Lilly Co Eli | Inhibidores de KRas g12c |
| WO2022037631A1 (zh) | 2020-08-21 | 2022-02-24 | 浙江海正药业股份有限公司 | 杂环类衍生物及其制备方法和用途 |
| CN116368130A (zh) * | 2020-08-28 | 2023-06-30 | 金橘生物科技公司 | 杂环化合物及其用途 |
| TWI880049B (zh) | 2020-12-04 | 2025-04-11 | 美商美國禮來大藥廠 | Kras g12c抑制劑 |
| US20240166660A1 (en) * | 2021-01-15 | 2024-05-23 | Beigene Switzerland Gmbh | Kras g12c inhibitors |
| CN117500799A (zh) * | 2021-06-09 | 2024-02-02 | 伊莱利利公司 | 作为kras g12d抑制剂的取代的稠合吖嗪 |
| CN115611923A (zh) | 2021-07-12 | 2023-01-17 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| CN117222654A (zh) | 2021-09-06 | 2023-12-12 | 苏州赞荣医药科技有限公司 | Kras g12c抑制剂和其用途 |
| CN115785199A (zh) | 2021-09-10 | 2023-03-14 | 润佳（苏州）医药科技有限公司 | 一种双官能化合物及其用途 |
| JP7676677B2 (ja) | 2022-03-25 | 2025-05-14 | イーライ リリー アンド カンパニー | Ｋｒａｓ阻害剤 |
-
2024
- 2024-03-29 EP EP24721007.3A patent/EP4688792A1/en active Pending
- 2024-03-29 AU AU2024241889A patent/AU2024241889A1/en active Pending
- 2024-03-29 TW TW113112022A patent/TWI901059B/zh active
- 2024-03-29 JP JP2024055240A patent/JP7669556B2/ja active Active
- 2024-03-29 CN CN202480023688.7A patent/CN121002032A/zh active Pending
- 2024-03-29 KR KR1020257035985A patent/KR20250163395A/ko active Pending
- 2024-03-29 WO PCT/US2024/022154 patent/WO2024206766A1/en not_active Ceased
- 2024-03-29 US US18/621,388 patent/US20240368193A1/en active Pending
- 2024-03-29 PE PE2025001908A patent/PE20252444A1/es unknown
- 2024-04-03 AR ARP240100807A patent/AR132295A1/es unknown
-
2025
- 2025-04-16 JP JP2025067243A patent/JP2025111535A/ja active Pending
- 2025-09-11 CL CL2025002769A patent/CL2025002769A1/es unknown
- 2025-09-14 IL IL323362A patent/IL323362A/en unknown
- 2025-09-25 CO CONC2025/0013134A patent/CO2025013134A2/es unknown
- 2025-09-26 MX MX2025011449A patent/MX2025011449A/es unknown
- 2025-09-28 JO JOJO/P/2025/0246A patent/JOP20250246A1/ar unknown
- 2025-09-29 DO DO2025000245A patent/DOP2025000245A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP7669556B2 (ja) | 2025-04-28 |
| AU2024241889A1 (en) | 2025-09-25 |
| PE20252444A1 (es) | 2025-10-20 |
| IL323362A (en) | 2025-11-01 |
| WO2024206766A1 (en) | 2024-10-03 |
| CL2025002769A1 (es) | 2025-11-07 |
| CO2025013134A2 (es) | 2025-10-09 |
| JOP20250246A1 (ar) | 2025-09-28 |
| US20240368193A1 (en) | 2024-11-07 |
| JP2024146897A (ja) | 2024-10-15 |
| DOP2025000245A (es) | 2025-11-16 |
| EP4688792A1 (en) | 2026-02-11 |
| MX2025011449A (es) | 2025-11-03 |
| TWI901059B (zh) | 2025-10-11 |
| TW202506688A (zh) | 2025-02-16 |
| JP2025111535A (ja) | 2025-07-30 |
| CN121002032A (zh) | 2025-11-21 |
| AR132295A1 (es) | 2025-06-11 |
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