TWI852436B - Kras抑制劑 - Google Patents
Kras抑制劑 Download PDFInfo
- Publication number
- TWI852436B TWI852436B TW112111395A TW112111395A TWI852436B TW I852436 B TWI852436 B TW I852436B TW 112111395 A TW112111395 A TW 112111395A TW 112111395 A TW112111395 A TW 112111395A TW I852436 B TWI852436 B TW I852436B
- Authority
- TW
- Taiwan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- compound
- acceptable salt
- alkyl
- Prior art date
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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263323607P | 2022-03-25 | 2022-03-25 | |
| US63/323,607 | 2022-03-25 | ||
| US202263406906P | 2022-09-15 | 2022-09-15 | |
| US63/406,906 | 2022-09-15 | ||
| US202263386404P | 2022-12-07 | 2022-12-07 | |
| US63/386,404 | 2022-12-07 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202404572A TW202404572A (zh) | 2024-02-01 |
| TWI852436B true TWI852436B (zh) | 2024-08-11 |
Family
ID=86331239
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW112111395A TWI852436B (zh) | 2022-03-25 | 2023-03-25 | Kras抑制劑 |
| TW113108193A TW202438502A (zh) | 2022-03-25 | 2023-03-25 | Kras抑制劑 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW113108193A TW202438502A (zh) | 2022-03-25 | 2023-03-25 | Kras抑制劑 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US12351591B2 (https=) |
| EP (1) | EP4499233A1 (https=) |
| JP (2) | JP7676677B2 (https=) |
| KR (2) | KR102847563B1 (https=) |
| CN (1) | CN119095853A (https=) |
| AU (1) | AU2023241055A1 (https=) |
| CA (1) | CA3246810A1 (https=) |
| CL (1) | CL2024002874A1 (https=) |
| CO (1) | CO2024012604A2 (https=) |
| DO (1) | DOP2024000186A (https=) |
| IL (1) | IL315782A (https=) |
| JO (1) | JOP20240210A1 (https=) |
| MX (1) | MX2024011631A (https=) |
| PE (1) | PE20251071A1 (https=) |
| TW (2) | TWI852436B (https=) |
| WO (1) | WO2023183585A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024112654A1 (en) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2024206747A1 (en) * | 2023-03-30 | 2024-10-03 | Eli Lilly And Company | Kras inhibitors |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| EP4688792A1 (en) * | 2023-03-31 | 2026-02-11 | Eli Lilly and Company | Kras inhibitors |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| AU2024323424A1 (en) | 2023-08-17 | 2026-03-05 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶ＫＲａｓ抑制劑 |
| 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 |
| TW202547457A (zh) * | 2024-04-08 | 2025-12-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 二氫呋喃并[3,4-f]喹唑啉類化合物、其製備方法及其在醫藥上的應用 |
| 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 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras 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 |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026059955A1 (en) * | 2024-09-11 | 2026-03-19 | Eli Lilly And Company | (3-((6-(2-amino-benzo[d]thiazol-4-yl)-3-(pyrrolidin-1-yl)-7,9-dihydrofuro[3,4-f]quinazolin-1-yl)amino)- piperidin-2-one derivatives as kras inhibitors for the treatment of cancer |
| 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 |
| WO2026075942A1 (en) * | 2024-10-01 | 2026-04-09 | Eli Lilly And Company | Kras inhibitors |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202033518A (zh) * | 2018-10-15 | 2020-09-16 | 美商美國禮來大藥廠 | Kras g12c 抑制劑 |
Family Cites Families (13)
| 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 |
| 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 |
| EP4161934A1 (en) * | 2020-06-04 | 2023-04-12 | Antengene Discovery Limited | Inhibitors of kras g12c protein and uses thereof |
| CN113880827B (zh) * | 2020-07-03 | 2024-10-01 | 苏州闻天医药科技有限公司 | 一种用于抑制krasg12c突变蛋白的化合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 |
| US20240166660A1 (en) | 2021-01-15 | 2024-05-23 | Beigene Switzerland Gmbh | Kras g12c inhibitors |
| WO2022184178A1 (en) | 2021-03-05 | 2022-09-09 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| CA3210383A1 (en) * | 2021-03-12 | 2022-09-15 | Bristol-Myers Squibb Company | Kras 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 |
| WO2023061294A1 (zh) | 2021-10-13 | 2023-04-20 | 再鼎医药(上海)有限公司 | 含氮杂环类衍生物调节剂、其制备方法及应用 |
-
2023
- 2023-03-24 JP JP2024556680A patent/JP7676677B2/ja active Active
- 2023-03-24 PE PE2024001867A patent/PE20251071A1/es unknown
- 2023-03-24 AU AU2023241055A patent/AU2023241055A1/en active Pending
- 2023-03-24 KR KR1020247035268A patent/KR102847563B1/ko active Active
- 2023-03-24 EP EP23723097.4A patent/EP4499233A1/en active Pending
- 2023-03-24 WO PCT/US2023/016257 patent/WO2023183585A1/en not_active Ceased
- 2023-03-24 US US18/189,713 patent/US12351591B2/en active Active
- 2023-03-24 KR KR1020257020079A patent/KR20250093430A/ko active Pending
- 2023-03-24 IL IL315782A patent/IL315782A/en unknown
- 2023-03-24 CA CA3246810A patent/CA3246810A1/en active Pending
- 2023-03-24 CN CN202380030401.9A patent/CN119095853A/zh active Pending
- 2023-03-24 MX MX2024011631A patent/MX2024011631A/es unknown
- 2023-03-25 TW TW112111395A patent/TWI852436B/zh active
- 2023-03-25 TW TW113108193A patent/TW202438502A/zh unknown
-
2024
- 2024-09-17 CO CONC2024/0012604A patent/CO2024012604A2/es unknown
- 2024-09-20 DO DO2024000186A patent/DOP2024000186A/es unknown
- 2024-09-25 CL CL2024002874A patent/CL2024002874A1/es unknown
- 2024-09-26 JO JOJO/P/2024/0210A patent/JOP20240210A1/ar unknown
-
2025
- 2025-04-30 JP JP2025075148A patent/JP2025118729A/ja active Pending
- 2025-05-29 US US19/222,746 patent/US20250289830A1/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202033518A (zh) * | 2018-10-15 | 2020-09-16 | 美商美國禮來大藥廠 | Kras g12c 抑制劑 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2023241055A1 (en) | 2024-10-10 |
| US20250289830A1 (en) | 2025-09-18 |
| WO2023183585A1 (en) | 2023-09-28 |
| EP4499233A1 (en) | 2025-02-05 |
| CN119095853A (zh) | 2024-12-06 |
| JP7676677B2 (ja) | 2025-05-14 |
| JP2025118729A (ja) | 2025-08-13 |
| KR102847563B1 (ko) | 2025-08-20 |
| PE20251071A1 (es) | 2025-04-10 |
| TW202438502A (zh) | 2024-10-01 |
| JP2025512811A (ja) | 2025-04-22 |
| US12351591B2 (en) | 2025-07-08 |
| US20240043451A1 (en) | 2024-02-08 |
| TW202404572A (zh) | 2024-02-01 |
| KR20240160650A (ko) | 2024-11-11 |
| MX2024011631A (es) | 2024-09-30 |
| IL315782A (en) | 2024-11-01 |
| CL2024002874A1 (es) | 2024-12-20 |
| KR20250093430A (ko) | 2025-06-24 |
| CO2024012604A2 (es) | 2024-12-09 |
| CA3246810A1 (en) | 2023-09-28 |
| JOP20240210A1 (ar) | 2024-09-26 |
| DOP2024000186A (es) | 2024-10-31 |
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