JP2024540410A - Ｋｒａｓ ｇ１２ｃ阻害剤 - Google Patents
Ｋｒａｓ ｇ１２ｃ阻害剤 Download PDFInfo
- Publication number
- JP2024540410A JP2024540410A JP2024527135A JP2024527135A JP2024540410A JP 2024540410 A JP2024540410 A JP 2024540410A JP 2024527135 A JP2024527135 A JP 2024527135A JP 2024527135 A JP2024527135 A JP 2024527135A JP 2024540410 A JP2024540410 A JP 2024540410A
- Authority
- JP
- Japan
- Prior art keywords
- group
- substituted
- compound
- alkyl
- halo
- 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
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
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)
- 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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163276478P | 2021-11-05 | 2021-11-05 | |
| US63/276,478 | 2021-11-05 | ||
| US202263356906P | 2022-06-29 | 2022-06-29 | |
| US63/356,906 | 2022-06-29 | ||
| US202263403565P | 2022-09-02 | 2022-09-02 | |
| US63/403,565 | 2022-09-02 | ||
| PCT/US2022/079324 WO2023081840A1 (en) | 2021-11-05 | 2022-11-04 | Kras g12c inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2024540410A true JP2024540410A (ja) | 2024-10-31 |
| JP2024540410A5 JP2024540410A5 (https=) | 2025-11-12 |
Family
ID=84537713
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024527135A Pending JP2024540410A (ja) | 2021-11-05 | 2022-11-04 | Ｋｒａｓ ｇ１２ｃ阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20250340548A1 (https=) |
| EP (1) | EP4426695A1 (https=) |
| JP (1) | JP2024540410A (https=) |
| KR (1) | KR20240114793A (https=) |
| AU (1) | AU2022380839A1 (https=) |
| CA (1) | CA3236238A1 (https=) |
| IL (1) | IL312381A (https=) |
| MX (1) | MX2024005228A (https=) |
| TW (1) | TW202334138A (https=) |
| WO (1) | WO2023081840A1 (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL312381A (en) | 2021-11-05 | 2024-06-01 | Frontier Medicines Corp | KRAS G12C inhibitors |
| CA3243798A1 (en) | 2022-02-09 | 2023-08-17 | Quanta Therapeutics, Inc. | Kras Modulators and Their Uses |
| JP2025510656A (ja) * | 2022-03-24 | 2025-04-15 | ベイジーン スウィッツァーランド ゲーエムベーハー | 複素環式化合物、その組成物、及びそれらを用いた治療方法 |
| WO2023230190A1 (en) | 2022-05-25 | 2023-11-30 | Quanta Therapeutics, Inc. | Pyrimidine based modulators and uses thereof |
| CN119630676A (zh) * | 2022-06-10 | 2025-03-14 | 百时美施贵宝公司 | 作为kras抑制剂的吡啶并[4,3-d]嘧啶衍生物 |
| CN119317629A (zh) * | 2022-06-10 | 2025-01-14 | 百时美施贵宝公司 | 作为kras抑制剂的四氢吡啶并3,4-d嘧啶衍生物 |
| WO2023246777A1 (en) * | 2022-06-20 | 2023-12-28 | Jacobio Pharmaceuticals Co., Ltd. | K-ras mutant protein inhibitors |
| EP4547666A1 (en) * | 2022-06-29 | 2025-05-07 | Frontier Medicines Corporation | Methods for treatment of cancer |
| KR20260041941A (ko) | 2023-03-15 | 2026-03-27 | 콴타 테라퓨틱스, 인크. | Kras 조절 인자 및 이의 용도 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| EP4705302A1 (en) * | 2023-05-04 | 2026-03-11 | Frontier Medicines Corporation | Pyrido[4,3-d]pyrimidine derivatives as mutant kras g12c inhibitors for the treatment of cancer |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025085580A1 (en) * | 2023-10-17 | 2025-04-24 | Windermere Therapeutics, Inc. | Kras(g12d) inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025179058A1 (en) | 2024-02-21 | 2025-08-28 | Frontier Medicines Corporation | Pyridopyrimidine derivative as kras g12c inhibitor for the treatment of brain metastasis |
| WO2025188668A1 (en) | 2024-03-04 | 2025-09-12 | Frontier Medicines Corporation | Combination of a kras g12c inhibitor with an immune checkpoint inhibitor for the treatment of cancer |
| WO2025194340A1 (en) | 2024-03-19 | 2025-09-25 | Frontier Medicines Corporation | Polymorphic forms of kras inhibitors and uses thereof |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (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 |
| WO2026015801A1 (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 |
| WO2026015790A1 (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 |
| 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 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102444509B1 (ko) * | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| EP3403569A1 (en) * | 2017-05-17 | 2018-11-21 | Koninklijke Philips N.V. | System for milk ejection reflex determination |
| LT3710439T (lt) | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| EA202190749A1 (ru) | 2018-09-10 | 2021-07-09 | Мирати Терапьютикс, Инк. | Способы комбинированной терапии |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| ES3017461T3 (en) | 2018-09-10 | 2025-05-13 | Mirati Therapeutics Inc | Combination of dasatinib and adagrasib for use in the treatment of non-small cell lung cancer |
| EP3849535A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| MX2021002804A (es) | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| CN112694475B (zh) | 2019-10-23 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 环烷基类和杂环烷基类抑制剂及其制备方法和应用 |
| CN113045565A (zh) * | 2019-12-27 | 2021-06-29 | 微境生物医药科技(上海)有限公司 | 新型K-Ras G12C抑制剂 |
| CN115135650A (zh) | 2020-02-20 | 2022-09-30 | 贝达医药公司 | 作为kras抑制剂的吡啶并嘧啶衍生物 |
| WO2021244603A1 (en) | 2020-06-04 | 2021-12-09 | Shanghai Antengene Corporation Limited | Inhibitors of kras g12c protein and uses thereof |
| EP4204412A4 (en) | 2020-08-26 | 2024-10-09 | InventisBio Co., Ltd. | HETEROARYL COMPOUNDS, PRODUCTION PROCESSES AND USES THEREOF |
| JP2023553492A (ja) | 2020-12-15 | 2023-12-21 | ミラティ セラピューティクス， インコーポレイテッド | アザキナゾリン汎ＫＲａｓ阻害剤 |
| WO2022187527A1 (en) | 2021-03-05 | 2022-09-09 | Nikang Therapeutics, Inc | Quinazoline nitrile derivatives as kras inhibitors |
| BR112023024906A2 (pt) | 2021-05-28 | 2024-02-15 | Redx Pharma Plc | Compostos |
| WO2022256459A1 (en) | 2021-06-01 | 2022-12-08 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| AR126166A1 (es) | 2021-06-18 | 2023-09-27 | Antengene Discovery Ltd | Combinación de un inhibidor de erk y un inhibidor de kras y usos de estos |
| WO2022271823A1 (en) | 2021-06-23 | 2022-12-29 | Newave Pharmaceutical Inc. | Mutant kras modulators and uses thereof |
| IL310291A (en) | 2021-07-23 | 2024-03-01 | Theras Inc | Compositions and methods for inhibition of ras |
| IL312381A (en) | 2021-11-05 | 2024-06-01 | Frontier Medicines Corp | KRAS G12C inhibitors |
| AR128212A1 (es) | 2022-01-06 | 2024-04-10 | Theras Inc | Composiciones y métodos para la inhibición de ras |
| WO2023137223A1 (en) | 2022-01-17 | 2023-07-20 | Newave Pharmaceutical Inc. | Pan-kras inhibitors and uses thereof |
| WO2023225252A1 (en) | 2022-05-20 | 2023-11-23 | Theras, Inc. | Compositions and methods for inhibition of ras |
| CN119630676A (zh) | 2022-06-10 | 2025-03-14 | 百时美施贵宝公司 | 作为kras抑制剂的吡啶并[4,3-d]嘧啶衍生物 |
| EP4547666A1 (en) | 2022-06-29 | 2025-05-07 | Frontier Medicines Corporation | Methods for treatment of cancer |
| JP2025526744A (ja) | 2022-08-11 | 2025-08-15 | ブリストル－マイヤーズ スクイブ カンパニー | Ｋｒａｓ阻害剤 |
| WO2024138206A1 (en) | 2022-12-23 | 2024-06-27 | Frontier Medicines Corporation | Fluoropyridopyrimidine and fluoroquinazoline derivaties and methods of use thereof |
| EP4655298A1 (en) | 2023-01-24 | 2025-12-03 | Theras Inc. | Compositions and methods for inhibition of ras |
-
2022
- 2022-11-04 IL IL312381A patent/IL312381A/en unknown
- 2022-11-04 KR KR1020247018884A patent/KR20240114793A/ko active Pending
- 2022-11-04 AU AU2022380839A patent/AU2022380839A1/en active Pending
- 2022-11-04 EP EP22826536.9A patent/EP4426695A1/en active Pending
- 2022-11-04 WO PCT/US2022/079324 patent/WO2023081840A1/en not_active Ceased
- 2022-11-04 MX MX2024005228A patent/MX2024005228A/es unknown
- 2022-11-04 JP JP2024527135A patent/JP2024540410A/ja active Pending
- 2022-11-04 US US18/707,499 patent/US20250340548A1/en active Pending
- 2022-11-04 CA CA3236238A patent/CA3236238A1/en active Pending
- 2022-11-04 TW TW111142228A patent/TW202334138A/zh unknown
-
2024
- 2024-07-24 US US18/783,394 patent/US12291539B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| MX2024005228A (es) | 2024-07-24 |
| WO2023081840A1 (en) | 2023-05-11 |
| EP4426695A1 (en) | 2024-09-11 |
| US12291539B2 (en) | 2025-05-06 |
| CA3236238A1 (en) | 2023-05-11 |
| KR20240114793A (ko) | 2024-07-24 |
| US20250340548A1 (en) | 2025-11-06 |
| TW202334138A (zh) | 2023-09-01 |
| IL312381A (en) | 2024-06-01 |
| AU2022380839A1 (en) | 2024-06-06 |
| US20250019387A1 (en) | 2025-01-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20240621 |
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| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20251104 |
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| A621 | Written request for application examination |
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