JP7707189B2 - Kras g12d変異に対して阻害活性を有する化合物 - Google Patents
Kras g12d変異に対して阻害活性を有する化合物 Download PDFInfo
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- JP7707189B2 JP7707189B2 JP2022558819A JP2022558819A JP7707189B2 JP 7707189 B2 JP7707189 B2 JP 7707189B2 JP 2022558819 A JP2022558819 A JP 2022558819A JP 2022558819 A JP2022558819 A JP 2022558819A JP 7707189 B2 JP7707189 B2 JP 7707189B2
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- C07D487/08—Bridged systems
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2019216165 | 2019-11-29 | ||
| JP2019216165 | 2019-11-29 | ||
| JPPCT/JP2019/049074 | 2019-12-06 | ||
| PCT/JP2019/049074 WO2021106231A1 (en) | 2019-11-29 | 2019-12-06 | A compound having inhibitory activity against kras g12d mutation |
| PCT/JP2020/045146 WO2021107160A1 (en) | 2019-11-29 | 2020-11-27 | A compound having inhibitory activity against kras g12d mutation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023512113A JP2023512113A (ja) | 2023-03-23 |
| JP2023512113A5 JP2023512113A5 (enExample) | 2023-12-01 |
| JP7707189B2 true JP7707189B2 (ja) | 2025-07-14 |
Family
ID=76128832
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022558819A Active JP7707189B2 (ja) | 2019-11-29 | 2020-11-27 | Kras g12d変異に対して阻害活性を有する化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20230348495A1 (enExample) |
| EP (1) | EP4065583A1 (enExample) |
| JP (1) | JP7707189B2 (enExample) |
| CN (1) | CN115003677B (enExample) |
| TW (1) | TW202134243A (enExample) |
| WO (2) | WO2021106231A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024521979A (ja) * | 2021-05-28 | 2024-06-04 | 大鵬薬品工業株式会社 | Kras変異タンパク質の小分子阻害剤関連出願の相互参照 |
Families Citing this family (133)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| 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 |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| EA202190749A1 (ru) | 2018-09-10 | 2021-07-09 | Мирати Терапьютикс, Инк. | Способы комбинированной терапии |
| EP3849535A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| 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 |
| MX2022002465A (es) | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| WO2021061749A1 (en) | 2019-09-24 | 2021-04-01 | Mirati Therapeutics, Inc. | Combination therapies |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| WO2021109737A1 (zh) * | 2019-12-02 | 2021-06-10 | 上海璎黎药业有限公司 | 一种含氧杂环化合物、其制备方法及应用 |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| WO2022002102A1 (en) * | 2020-06-30 | 2022-01-06 | InventisBio Co., Ltd. | Quinazoline compounds, preparation methods and uses thereof |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| EP4210833A4 (en) | 2020-09-11 | 2024-09-11 | Mirati Therapeutics, Inc. | CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR |
| US20230357277A1 (en) | 2020-09-22 | 2023-11-09 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022068921A1 (zh) * | 2020-09-30 | 2022-04-07 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| WO2022098625A1 (en) | 2020-11-03 | 2022-05-12 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022105859A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| WO2022105855A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| 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 |
| 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 |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| US20240092803A1 (en) * | 2021-01-08 | 2024-03-21 | Beigene Switzerland Gmbh | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| WO2022148422A1 (en) * | 2021-01-08 | 2022-07-14 | Beigene, Ltd. | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| MX2023009037A (es) * | 2021-02-01 | 2023-08-10 | Medshine Discovery Inc | Compuesto de pirimidopirano. |
| WO2022170999A1 (zh) * | 2021-02-09 | 2022-08-18 | 南京明德新药研发有限公司 | 吡啶[4,3-d]嘧啶类化合物 |
| KR20230136636A (ko) * | 2021-02-09 | 2023-09-26 | 메드샤인 디스커버리 아이엔씨. | 피리미딘 방향족 환 화합물 |
| WO2022171143A1 (zh) * | 2021-02-09 | 2022-08-18 | 南京明德新药研发有限公司 | 5,6,7,8-四氢吡啶[3,4-d]嘧啶化合物 |
| EP4293025B1 (en) * | 2021-02-15 | 2025-10-29 | Astellas Pharma Inc. | 4-aminoquinazoline compound |
| WO2022173032A1 (ja) | 2021-02-15 | 2022-08-18 | アステラス製薬株式会社 | G12d変異krasタンパクの分解を誘導するためのキナゾリン化合物 |
| MX2023010430A (es) * | 2021-03-12 | 2023-09-12 | Bristol Myers Squibb Co | Inhibidores del homologo del oncogen viral del sarcoma de rata kirsten con mutacion g12d (kras g12d). |
| TWI810803B (zh) * | 2021-03-15 | 2023-08-01 | 大陸商藥雅科技(上海)有限公司 | 突變蛋白抑制劑的製備及其應用 |
| CN116964058A (zh) * | 2021-03-15 | 2023-10-27 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| WO2022194192A1 (zh) * | 2021-03-18 | 2022-09-22 | 四川科伦博泰生物医药股份有限公司 | 一类杂芳环化合物、其制备方法及用途 |
| CN116157400B (zh) * | 2021-03-30 | 2024-10-22 | 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 |
| WO2022217042A1 (en) * | 2021-04-09 | 2022-10-13 | Ikena Oncology, Inc. | Naphthyl-substituted quinoline-4(1h)-ones and related compounds and their use in treating medical conditions |
| CN117203208A (zh) * | 2021-04-23 | 2023-12-08 | 清华大学 | 靶向活化与失活态kras g12d的抑制剂 |
| US20250059205A1 (en) * | 2021-04-29 | 2025-02-20 | Amgen Inc. | Heterocyclic Compounds and Methods of Use |
| CN117222650A (zh) * | 2021-04-30 | 2023-12-12 | 劲方医药科技(上海)有限公司 | 吡啶或嘧啶并环类化合物,其制法与医药上的用途 |
| JP2024516450A (ja) | 2021-05-05 | 2024-04-15 | レボリューション メディシンズ インコーポレイテッド | 共有結合性ras阻害剤及びその使用 |
| CN115385937A (zh) * | 2021-05-25 | 2022-11-25 | 江苏恒瑞医药股份有限公司 | 嘧啶并环烷基类化合物、其制备方法及其在医药上的应用 |
| WO2022261154A1 (en) * | 2021-06-09 | 2022-12-15 | Eli Lilly And Company | Substituted fused azines as kras g12d inhibitors |
| BR112023025869A2 (pt) * | 2021-06-10 | 2024-02-27 | Redx Pharma Plc | Derivados de quinazolina úteis como inibidores de ras |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| TW202317580A (zh) * | 2021-06-18 | 2023-05-01 | 大陸商南京燧坤智能科技有限公司 | 用作kras g12d抑制劑的氘代化合物 |
| EP4361157A4 (en) * | 2021-06-21 | 2024-10-16 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | FUSED TETRACYCLIC COMPOUND, ITS PREPARATION METHOD AND ITS USE IN MEDICINE |
| EP4363412A4 (en) * | 2021-06-30 | 2025-05-14 | Dana-Farber Cancer Institute, Inc. | Small-molecule inhibitors of the KRAS G12D mutant |
| CN117460737A (zh) * | 2021-07-05 | 2024-01-26 | 四川科伦博泰生物医药股份有限公司 | 杂芳环化合物、其制备方法及用途 |
| CN117751116A (zh) * | 2021-07-07 | 2024-03-22 | 微境生物医药科技(上海)有限公司 | 作为KRas G12D抑制剂的稠环化合物 |
| TW202317589A (zh) * | 2021-07-14 | 2023-05-01 | 美商尼坎醫療公司 | 作為kras抑制劑的伸烷基衍生物 |
| WO2023284537A1 (en) * | 2021-07-16 | 2023-01-19 | Shanghai Zion Pharma Co. Limited | Kras g12d inhibitors and uses thereof |
| WO2023284881A1 (en) * | 2021-07-16 | 2023-01-19 | Silexon Ai Technology Co., Ltd. | Heterocyclic compounds useful as kras g12d inhibitors |
| WO2023283933A1 (en) * | 2021-07-16 | 2023-01-19 | Silexon Biotech Co., Ltd. | Compounds useful as kras g12d inhibitors |
| KR20240041917A (ko) | 2021-07-27 | 2024-04-01 | 도레이 카부시키가이샤 | 암의 치료 및/또는 예방을 위한 의약품 |
| KR20230022816A (ko) * | 2021-08-06 | 2023-02-16 | 인터올리고 주식회사 | 올리고뉴클레오티드를 유효성분으로 포함하는 삼중음성 유방암을 예방 또는 치료하기 위한 약학적 조성물 |
| TW202321261A (zh) * | 2021-08-10 | 2023-06-01 | 美商伊瑞斯卡公司 | 選擇性kras抑制劑 |
| KR20240046745A (ko) * | 2021-08-12 | 2024-04-09 | 머크 샤프 앤드 돔 엘엘씨 | 벨주티판의 투여를 위한 투여량 레지멘 |
| CN116669740A (zh) * | 2021-08-16 | 2023-08-29 | 华润医药研究院(深圳)有限公司 | 嘧啶并吡啶类化合物及其制备方法和医药用途 |
| CN117858878A (zh) * | 2021-08-18 | 2024-04-09 | 北京加科思新药研发有限公司 | N-环丙基吡啶并[4,3-d]嘧啶-4-胺衍生物及其用途 |
| UY39906A (es) * | 2021-08-18 | 2023-03-31 | Jacobio Pharmaceuticals Co Ltd | Derivados de 1,4-oxazepano y usos de los mismos |
| WO2023040989A1 (en) * | 2021-09-16 | 2023-03-23 | Suzhou Zanrong Pharma Limited | Kras g12c inhibitors and uses thereof |
| WO2023051586A1 (zh) * | 2021-09-29 | 2023-04-06 | 先声再明医药有限公司 | Kras g12d抑制剂化合物及其制备方法和应用 |
| CN118401254A (zh) * | 2021-10-05 | 2024-07-26 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂与shp-2抑制剂的组合疗法 |
| MX2024004216A (es) | 2021-10-05 | 2024-06-20 | Mirati Therapeutics Inc | Terapias combinadas de inhibidores de kras g12d con inhibidores de la familia pan erbb. |
| AU2022361219A1 (en) * | 2021-10-05 | 2024-04-11 | Mirati Therapeutics, Inc. | Combinations of kras g12d inhibitors with irinotecan and related methods of treatment |
| IL311834A (en) | 2021-10-05 | 2024-05-01 | Mirati Therapeutics Inc | Combinations of KRAS G12D inhibitors with PI3KA inhibitors and therapeutic methods |
| EP4419686A4 (en) * | 2021-10-21 | 2025-10-15 | Nanothera Biosciences Inc | COMPOSITIONS AND METHODS OF EXTINGUISHING KRAS |
| CN114057776A (zh) * | 2021-10-31 | 2022-02-18 | 南京碳硅人工智能生物医药技术研究院有限公司 | 一种具有抗癌活性的嘧啶并哌啶衍生物的新合成方法 |
| CN116253748A (zh) * | 2021-12-09 | 2023-06-13 | 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 |
| WO2023119677A1 (en) * | 2021-12-24 | 2023-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising a quinazoline compound |
| WO2023125989A1 (zh) * | 2021-12-31 | 2023-07-06 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| CA3249537A1 (en) * | 2022-01-21 | 2025-06-17 | D3 Bio (Wuxi) Co., Ltd. | HETEROARYL-PYRANE DERIVATIVE SUBSTITUTED BY A BRIDGED CYCLE AND ITS USE |
| EP4371991A4 (en) * | 2022-01-21 | 2025-02-26 | Usynova Pharmaceuticals Ltd. | Benzopyrimidine compounds and use thereof |
| WO2023138524A1 (zh) * | 2022-01-24 | 2023-07-27 | 贝达药业股份有限公司 | Kras g12d降解剂及其在医药上的应用 |
| CA3243798A1 (en) | 2022-02-09 | 2023-08-17 | Quanta Therapeutics, Inc. | Kras Modulators and Their Uses |
| WO2023152255A1 (en) * | 2022-02-10 | 2023-08-17 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
| TW202346270A (zh) | 2022-03-11 | 2023-12-01 | 日商安斯泰來製藥股份有限公司 | 用於誘發g12d突變kras蛋白分解之雜環化合物 |
| WO2023179629A1 (zh) * | 2022-03-22 | 2023-09-28 | 苏州泽璟生物制药股份有限公司 | 取代桥环类抑制剂及其制备方法和应用 |
| CN116891488B (zh) | 2022-04-11 | 2025-12-12 | 成都海博为药业有限公司 | 稠环化合物、包含其的药物组合物及应用 |
| CN114989195B (zh) * | 2022-05-25 | 2024-10-29 | 广东晨康生物科技有限公司 | 一种噻吩并嘧啶类化合物或其药学上可接受的盐及其制备方法和应用 |
| WO2023230190A1 (en) | 2022-05-25 | 2023-11-30 | Quanta Therapeutics, Inc. | Pyrimidine based modulators and uses thereof |
| CN117164580A (zh) * | 2022-05-27 | 2023-12-05 | 苏州泽璟生物制药股份有限公司 | 一种kras g12c抑制剂的制备方法及其中间体 |
| AU2023289822A1 (en) * | 2022-06-24 | 2025-01-30 | Medshine Discovery Inc. | Heterocyclic substituted pyrimidopyran compound and use thereof |
| US20250145631A1 (en) | 2022-07-21 | 2025-05-08 | Astellas Pharma Inc. | Heterocyclic compound acting on g12d mutant kras protein |
| AU2023314335A1 (en) * | 2022-07-29 | 2025-02-27 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Pharmaceutical composition comprising kras g12d inhibitor |
| TW202412789A (zh) | 2022-08-05 | 2024-04-01 | 日商安斯泰來製藥股份有限公司 | 用於誘導突變kras蛋白分解之雜環化合物 |
| AR130191A1 (es) | 2022-08-12 | 2024-11-13 | Astellas Pharma Inc | Combinaciones antineoplásicas que comprenden tratamiento dirigido |
| AR130192A1 (es) * | 2022-08-12 | 2024-11-13 | Astellas Pharma Inc | Combinaciones antineoplásicas que comprenden quimioterapia |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| US20260083750A1 (en) * | 2022-08-26 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| WO2024064335A1 (en) * | 2022-09-23 | 2024-03-28 | Ikena Oncology, Inc. | Naphthyl-substituted pyranopyrimidinones and related compounds and their use in treating medical conditions |
| CN117800976A (zh) * | 2022-09-30 | 2024-04-02 | 上海凌达生物医药有限公司 | 一类含氮杂环类化合物、制备方法和用途 |
| JP2025536369A (ja) | 2022-10-21 | 2025-11-05 | リーディングタック ファーマシューティカル(シャオシン)カンパニー,リミテッド | Kras g12d分解剤及びその製造方法並びに応用 |
| EP4631942A1 (en) | 2022-10-21 | 2025-10-15 | Leadingtac Pharmaceutical (Shaoxing) Co., Ltd. | Pan-kras degrading agent, and preparation method therefor and use thereof |
| CN116554208A (zh) * | 2022-12-02 | 2023-08-08 | 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 |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
| KR20260041941A (ko) | 2023-03-15 | 2026-03-27 | 콴타 테라퓨틱스, 인크. | Kras 조절 인자 및 이의 용도 |
| JP2026511123A (ja) * | 2023-03-23 | 2026-04-10 | 徳昇済医薬(無錫)有限公司 | 複素環置換ピリミドピラン化合物及びその使用 |
| KR20260016466A (ko) * | 2023-03-27 | 2026-02-03 | 셴젠 이오노바 라이프 사이언스 시오., 엘티디. | Kras(g12d) 단백질의 분해 및 억제를 위한 화합물 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| 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 |
| PE20252789A1 (es) | 2023-05-24 | 2025-12-22 | Kumquat Biosciences Inc | Compuestos heterociclicos y usos de estos |
| AR133027A1 (es) | 2023-06-22 | 2025-08-20 | Astellas Pharma Inc | Composición farmacéutica que comprende un compuesto de quinazolina |
| AR133028A1 (es) | 2023-06-22 | 2025-08-20 | Astellas Pharma Inc | Composición farmacéutica que comprende un degradador de todas las kras |
| WO2025019823A1 (en) * | 2023-07-20 | 2025-01-23 | Merck Sharp & Dohme Llc | Small molecule protein degraders of kras g12d mutant |
| WO2025026903A1 (en) * | 2023-07-31 | 2025-02-06 | Bayer Aktiengesellschaft | Imidazo pyrimidine compounds for the treatment of cancer |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
| 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 |
| US20250114339A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024361909A1 (en) | 2023-10-20 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| WO2025108479A1 (en) * | 2023-11-24 | 2025-05-30 | Shenzhen Ionova Life Science Co., Ltd. | Compounds for degradation or inhibition of kras mutant proteins and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025218811A1 (zh) * | 2024-04-19 | 2025-10-23 | 领泰生物医药(绍兴)有限公司 | pan-KRAS靶向蛋白降解剂及其制备方法和应用 |
| WO2025230961A1 (en) * | 2024-04-29 | 2025-11-06 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| WO2025240740A1 (en) * | 2024-05-15 | 2025-11-20 | Merck Sharp & Dohme Llc | Small molecule protein degraders of kras g12d mutant |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ras抑制劑 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| 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 |
| 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 |
| 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 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014533259A (ja) | 2011-11-15 | 2014-12-11 | ゼンション・リミテッドXention Limited | カリウムチャネル阻害剤として有用なチエノおよびフロピリミジンならびにピリジン |
| JP2016512514A (ja) | 2013-03-13 | 2016-04-28 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | チエノピリミジン及びチエノピリジン化合物を含有する組成物並びにそれらの使用方法 |
| JP2019516718A (ja) | 2016-05-18 | 2019-06-20 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12c阻害剤 |
| JP2019529484A (ja) | 2016-09-29 | 2019-10-17 | アラクセス ファーマ エルエルシー | Kras g12c変異体タンパク質の阻害剤 |
| JP2022546043A (ja) | 2019-08-29 | 2022-11-02 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12d阻害剤 |
Family Cites Families (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| PT98990A (pt) | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
| US5120842A (en) | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5100883A (en) | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
| US5118678A (en) | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5118677A (en) | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
| US5151413A (en) | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| GB9125660D0 (en) | 1991-12-03 | 1992-01-29 | Smithkline Beecham Plc | Novel compound |
| ZA935111B (en) | 1992-07-17 | 1994-02-04 | Smithkline Beecham Corp | Rapamycin derivatives |
| ZA935112B (en) | 1992-07-17 | 1994-02-08 | Smithkline Beecham Corp | Rapamycin derivatives |
| US5256790A (en) | 1992-08-13 | 1993-10-26 | American Home Products Corporation | 27-hydroxyrapamycin and derivatives thereof |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5258389A (en) | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| WO1994011384A1 (en) | 1992-11-13 | 1994-05-26 | Immunex Corporation | Novel cytokine designated elk ligand |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5516658A (en) | 1993-08-20 | 1996-05-14 | Immunex Corporation | DNA encoding cytokines that bind the cell surface receptor hek |
| CA2175215C (en) | 1993-11-19 | 2008-06-03 | Yat Sun Or | Semisynthetic analogs of rapamycin (macrolides) being immunomodulators |
| SK78196A3 (en) | 1993-12-17 | 1997-02-05 | Sandoz Ag | Rapamycin demethoxy-derivatives, preparation method thereof and pharmaceutical agent containing them |
| EP0756627A1 (en) | 1994-04-15 | 1997-02-05 | Amgen Inc. | Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases |
| US6303769B1 (en) | 1994-07-08 | 2001-10-16 | Immunex Corporation | Lerk-5 dna |
| US5919905A (en) | 1994-10-05 | 1999-07-06 | Immunex Corporation | Cytokine designated LERK-6 |
| US6057124A (en) | 1995-01-27 | 2000-05-02 | Amgen Inc. | Nucleic acids encoding ligands for HEK4 receptors |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| ES2153031T4 (es) | 1995-04-20 | 2001-05-16 | Pfizer | Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf. |
| US5985890A (en) | 1995-06-09 | 1999-11-16 | Novartis Ag | Rapamycin derivatives |
| ATE225343T1 (de) | 1995-12-20 | 2002-10-15 | Hoffmann La Roche | Matrix-metalloprotease inhibitoren |
| AU735648B2 (en) | 1996-07-12 | 2001-07-12 | Ariad Pharmaceuticals, Inc. | Materials and method for treating or preventing pathogenic fungal infection |
| KR20000067904A (ko) | 1996-07-18 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 매트릭스 메탈로프로테아제의 포스피네이트계 억제제 |
| KR20000068248A (ko) | 1996-08-23 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 아릴설포닐아미노 하이드록삼산 유도체 |
| JP3338064B2 (ja) | 1997-01-06 | 2002-10-28 | ファイザー・インク | 環状スルホン誘導体 |
| NZ336840A (en) | 1997-02-03 | 2001-01-26 | Pfizer Prod Inc | Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases |
| JP2000507975A (ja) | 1997-02-07 | 2000-06-27 | ファイザー・インク | N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用 |
| EP0960098A1 (en) | 1997-02-11 | 1999-12-01 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| US6150395A (en) | 1997-05-30 | 2000-11-21 | The Regents Of The University Of California | Indole-3-carbinol (I3C) derivatives and methods |
| CA2299355C (en) | 1997-08-08 | 2005-09-27 | Pfizer Products Inc. | Aryloxyarylsulfonylamino hydroxamic acid derivatives |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| EP1004578B1 (en) | 1998-11-05 | 2004-02-25 | Pfizer Products Inc. | 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| ATE324444T1 (de) | 1999-06-07 | 2006-05-15 | Immunex Corp | Tek-antagonisten |
| US6521424B2 (en) | 1999-06-07 | 2003-02-18 | Immunex Corporation | Recombinant expression of Tek antagonists |
| ATE264863T1 (de) | 1999-08-24 | 2004-05-15 | Ariad Gene Therapeutics Inc | 28-epirapaloge |
| US6727225B2 (en) | 1999-12-20 | 2004-04-27 | Immunex Corporation | TWEAK receptor |
| NZ521437A (en) | 2000-02-25 | 2004-04-30 | Immunex Corp | Integrin antagonists suitable as inhibitors of angiogenesis |
| US20060173033A1 (en) | 2003-07-08 | 2006-08-03 | Michaela Kneissel | Use of rapamycin and rapamycin derivatives for the treatment of bone loss |
| WO2005016252A2 (en) | 2003-07-11 | 2005-02-24 | Ariad Gene Therapeutics, Inc. | Phosphorus-containing macrocycles |
| AR045134A1 (es) | 2003-07-29 | 2005-10-19 | Smithkline Beecham Plc | Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic |
| DE602005020465D1 (de) | 2004-08-26 | 2010-05-20 | Pfizer | Enantiomerenreine aminoheteroaryl-verbindungen als proteinkinasehemmer |
| EP1799699A1 (en) | 2004-10-13 | 2007-06-27 | Wyeth | Analogs of 17-hydroxywortmannin as pi3k inhibitors |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| KR20080040007A (ko) | 2005-09-20 | 2008-05-07 | 화이자 프로덕츠 인크. | 티로신 키나제 억제제를 이용한 치료의 투여형 및 방법 |
| EP2205242B1 (en) | 2007-09-12 | 2015-04-15 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| JP5348725B2 (ja) | 2007-10-25 | 2013-11-20 | ジェネンテック, インコーポレイテッド | チエノピリミジン化合物の製造方法 |
| SG193327A1 (en) | 2011-04-06 | 2013-10-30 | Taiho Pharmaceutical Co Ltd | Novel imidazo-oxazine compound or salt thereof |
| PL3417851T3 (pl) | 2013-09-09 | 2020-12-14 | Peloton Therapeutics, Inc. | Etery arylowe i ich zastosowanie |
| EP3055290B1 (en) * | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
| ES2898765T3 (es) * | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| HUE068392T2 (hu) | 2015-10-21 | 2024-12-28 | Otsuka Pharma Co Ltd | Benzolaktám vegyületek mint fehérje kináz gátlók |
| KR20180081596A (ko) * | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| EP3523289A1 (en) * | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| JOP20190186A1 (ar) * | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| AU2018273356B2 (en) * | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| US10745385B2 (en) * | 2017-05-25 | 2020-08-18 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| LT3710439T (lt) * | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| IL276232B2 (en) | 2018-03-02 | 2024-04-01 | Otsuka Pharma Co Ltd | Pyrazine derivatives, pharmaceutical compositions comprising them and their use for treating diseases |
| MX2021000795A (es) | 2018-07-24 | 2021-04-12 | Taiho Pharmaceutical Co Ltd | Compuestos heterociclicos para inhibir la actividad de shp2. |
| EP3908283A4 (en) * | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| CN112390797A (zh) * | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | 新型螺环类K-Ras G12C抑制剂 |
| WO2021031952A1 (zh) * | 2019-08-16 | 2021-02-25 | 劲方医药科技(上海)有限公司 | 氧代六元环并嘧啶类化合物,其制法与医药上的用途 |
-
2019
- 2019-12-06 WO PCT/JP2019/049074 patent/WO2021106231A1/en not_active Ceased
-
2020
- 2020-11-27 TW TW109141900A patent/TW202134243A/zh unknown
- 2020-11-27 CN CN202080094483.XA patent/CN115003677B/zh active Active
- 2020-11-27 WO PCT/JP2020/045146 patent/WO2021107160A1/en not_active Ceased
- 2020-11-27 JP JP2022558819A patent/JP7707189B2/ja active Active
- 2020-11-27 EP EP20833977.0A patent/EP4065583A1/en active Pending
- 2020-11-27 US US17/780,597 patent/US20230348495A1/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014533259A (ja) | 2011-11-15 | 2014-12-11 | ゼンション・リミテッドXention Limited | カリウムチャネル阻害剤として有用なチエノおよびフロピリミジンならびにピリジン |
| JP2016512514A (ja) | 2013-03-13 | 2016-04-28 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | チエノピリミジン及びチエノピリジン化合物を含有する組成物並びにそれらの使用方法 |
| JP2019516718A (ja) | 2016-05-18 | 2019-06-20 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12c阻害剤 |
| JP2019529484A (ja) | 2016-09-29 | 2019-10-17 | アラクセス ファーマ エルエルシー | Kras g12c変異体タンパク質の阻害剤 |
| JP2022546043A (ja) | 2019-08-29 | 2022-11-02 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12d阻害剤 |
Non-Patent Citations (1)
| Title |
|---|
| Gyula PALFY et al.,1H, 15N backbone assignment and comparative analysis of the wildtype and G12C, G12D, G12V mutants of K-Ras bound to GDP at physiological pH,Biomolecular NMR Assignments,2019年08月29日,Vol. 14,No. 1,p.1-7 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024521979A (ja) * | 2021-05-28 | 2024-06-04 | 大鵬薬品工業株式会社 | Kras変異タンパク質の小分子阻害剤関連出願の相互参照 |
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| US20230348495A1 (en) | 2023-11-02 |
| CN115003677A (zh) | 2022-09-02 |
| CN115003677B (zh) | 2024-08-27 |
| TW202134243A (zh) | 2021-09-16 |
| WO2021107160A1 (en) | 2021-06-03 |
| JP2023512113A (ja) | 2023-03-23 |
| EP4065583A1 (en) | 2022-10-05 |
| WO2021106231A1 (en) | 2021-06-03 |
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