JP2025510656A - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP2025510656A JP2025510656A JP2024555128A JP2024555128A JP2025510656A JP 2025510656 A JP2025510656 A JP 2025510656A JP 2024555128 A JP2024555128 A JP 2024555128A JP 2024555128 A JP2024555128 A JP 2024555128A JP 2025510656 A JP2025510656 A JP 2025510656A
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- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- fluoro
- pyrrolidin
- 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
-
- 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
- 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
- A61K31/537—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 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
- A61K31/535—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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2022/082722 | 2022-03-24 | ||
| CN2022082722 | 2022-03-24 | ||
| PCT/CN2023/083294 WO2023179703A1 (en) | 2022-03-24 | 2023-03-23 | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2025510656A true JP2025510656A (ja) | 2025-04-15 |
| JP2025510656A5 JP2025510656A5 (cg-RX-API-DMAC10.html) | 2026-04-08 |
Family
ID=88100085
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024555128A Pending JP2025510656A (ja) | 2022-03-24 | 2023-03-23 | 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 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20250101028A1 (cg-RX-API-DMAC10.html) |
| EP (1) | EP4499639A4 (cg-RX-API-DMAC10.html) |
| JP (1) | JP2025510656A (cg-RX-API-DMAC10.html) |
| CN (1) | CN118900838A (cg-RX-API-DMAC10.html) |
| WO (1) | WO2023179703A1 (cg-RX-API-DMAC10.html) |
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| WO2021085653A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| 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 |
| 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 |
| CA3227138A1 (en) | 2021-07-23 | 2023-01-26 | Theras, Inc. | Compositions and methods for inhibition of ras |
| US20260200925A1 (en) * | 2021-11-24 | 2026-07-16 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras mutated proteins |
| CN120019052A (zh) * | 2022-08-05 | 2025-05-16 | 瑟拉斯有限公司 | 用于抑制kras的组合物和方法 |
| KR20250109197A (ko) | 2022-11-21 | 2025-07-16 | 트리라인 바이오사이언시스, 인크. | 스피로환식 디하이드로피라노피리미딘 KRas 억제제 |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| WO2025006967A1 (en) | 2023-06-30 | 2025-01-02 | Bristol-Myers Squibb Company | Kras inhibitors |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| KR20260054710A (ko) | 2023-08-17 | 2026-04-22 | 트리라인 바이오사이언시스, 인크. | 스피로시클릭 디히드로피라노피리미딘 KRas 저해제 |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2025064848A1 (en) | 2023-09-21 | 2025-03-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyridine kras inhibitors |
| US20250114346A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| KR20260110993A (ko) | 2023-10-09 | 2026-07-14 | 인사이트 코포레이션 | Kras g12d 억제제 및 egfr 억제제를 포함하는 암 치료용 조합 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| KR20260102810A (ko) * | 2023-10-25 | 2026-07-01 | 컴쿼트 바이오사이언시즈 인크. | 세포 증식을 조절하는 방법 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| TW202615038A (zh) | 2024-08-07 | 2026-04-16 | 美商太斯萊特醫藥美國有限責任公司 | 包含拓樸異構酶有效載荷之靶向ｋｒａｓ之共價誘導之藥物結合物 |
| 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 |
| 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 |
| US20260137674A1 (en) | 2024-10-23 | 2026-05-21 | Incyte Corporation | Combination therapy using a kras g12d inhibitor, and a nucleoside analog, and/or a microtubule inhibitor |
| WO2026090333A1 (en) | 2024-10-23 | 2026-04-30 | Incyte Corporation | Combination using a kras g12d inhibitor and chemotherapy combinations as well as their use in the treatment of cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | 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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2022002102A1 (en) * | 2020-06-30 | 2022-01-06 | InventisBio Co., Ltd. | Quinazoline compounds, preparation methods and uses thereof |
| US12655160B2 (en) * | 2020-08-04 | 2026-06-16 | Mirati Therapeutics, Inc. | KRAS G12D inhibitors |
| EP4204412A4 (en) * | 2020-08-26 | 2024-10-09 | InventisBio Co., Ltd. | HETEROARYL COMPOUNDS, PRODUCTION PROCESSES AND USES THEREOF |
| CA3191279A1 (en) * | 2020-08-28 | 2022-03-03 | Yi Liu | Heterocyclic compounds and uses thereof |
| EP4262807A4 (en) * | 2020-12-15 | 2025-04-23 | Mirati Therapeutics, Inc. | Azachinazoline pan-KRAS inhibitors |
| AU2022220678A1 (en) * | 2021-02-09 | 2023-09-21 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| JP2024505594A (ja) * | 2021-02-09 | 2024-02-06 | メッドシャイン ディスカバリー インコーポレイテッド | ピリミジン芳香環化合物 |
| 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). |
| CN117715915A (zh) * | 2021-04-09 | 2024-03-15 | 杭州英创医药科技有限公司 | 作为kras g12d抑制剂的杂环化合物 |
| US20240239788A1 (en) * | 2021-04-16 | 2024-07-18 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12d mutant |
| EP4329888A1 (en) * | 2021-04-29 | 2024-03-06 | Amgen Inc. | 2-aminobenzothiazole compounds and methods of use thereof |
| CN115304623A (zh) * | 2021-04-30 | 2022-11-08 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| US20240300980A1 (en) * | 2021-05-22 | 2024-09-12 | Shanghai Kechow Pharma, Inc. | Heterocyclic compounds as kras inhibitor, and preparation therefor and use thereof in treatment |
| BR112023024906A2 (pt) * | 2021-05-28 | 2024-02-15 | Redx Pharma Plc | Compostos |
| 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 |
| CA3227138A1 (en) * | 2021-07-23 | 2023-01-26 | Theras, Inc. | Compositions and methods for inhibition of ras |
| EP4384522A1 (en) * | 2021-08-10 | 2024-06-19 | Erasca, Inc. | Selective kras inhibitors |
| WO2023020521A1 (en) * | 2021-08-18 | 2023-02-23 | Jacobio Pharmaceuticals Co., Ltd. | Pyridine fused pyrimidine derivatives and use thereof |
| WO2023020519A1 (en) * | 2021-08-18 | 2023-02-23 | Jacobio Pharmaceuticals Co., Ltd. | 1, 4-oxazepane derivatives and uses thereof |
| WO2023020518A1 (en) * | 2021-08-18 | 2023-02-23 | Jacobio Pharmaceuticals Co., Ltd. | N-cyclopropylpyrido [4, 3-d] pyrimidin-4-amine derivatives and uses thereof |
| EP4389751A1 (en) * | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2023056951A1 (zh) * | 2021-10-08 | 2023-04-13 | 杭州德睿智药科技有限公司 | 芳基取代并杂环化合物 |
| 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 |
| WO2023072188A1 (zh) * | 2021-10-29 | 2023-05-04 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| KR20240114793A (ko) * | 2021-11-05 | 2024-07-24 | 프론티어 메디슨즈 코포레이션 | Kras g12c 억제제 |
| US20260200925A1 (en) * | 2021-11-24 | 2026-07-16 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras mutated proteins |
| JP7629580B1 (ja) * | 2022-01-21 | 2025-02-13 | ユーシノヴァ・ファーマシューティカルズ・リミテッド | ベンゾピリミジン化合物及びその使用 |
| IL314486A (en) * | 2022-02-03 | 2024-09-01 | Mirati Therapeutics Inc | Quinazoline compounds inhibit PAN-KRAS |
| JP2025508702A (ja) * | 2022-02-16 | 2025-04-10 | アムジエン・インコーポレーテツド | キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 |
-
2023
- 2023-03-23 JP JP2024555128A patent/JP2025510656A/ja active Pending
- 2023-03-23 CN CN202380028687.7A patent/CN118900838A/zh active Pending
- 2023-03-23 EP EP23773949.5A patent/EP4499639A4/en active Pending
- 2023-03-23 WO PCT/CN2023/083294 patent/WO2023179703A1/en not_active Ceased
-
2024
- 2024-09-19 US US18/889,657 patent/US20250101028A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2023179703A1 (en) | 2023-09-28 |
| CN118900838A (zh) | 2024-11-05 |
| EP4499639A1 (en) | 2025-02-05 |
| US20250101028A1 (en) | 2025-03-27 |
| EP4499639A4 (en) | 2026-06-17 |
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