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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (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 (4)
| Publication Number | Publication Date |
|---|---|
| JP2023512113A JP2023512113A (ja) | 2023-03-23 |
| JPWO2021107160A5 JPWO2021107160A5 (https=) | 2023-12-01 |
| JP2023512113A5 JP2023512113A5 (https=) | 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 (https=) |
| EP (1) | EP4065583A1 (https=) |
| JP (1) | JP7707189B2 (https=) |
| CN (1) | CN115003677B (https=) |
| TW (1) | TW202134243A (https=) |
| WO (2) | WO2021106231A1 (https=) |
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 |
|---|---|---|---|---|
| KR20210006356A (ko) | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| SMT202500028T1 (it) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Terapie combinate |
| WO2020055761A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| 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 |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | 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 |
| CN113164418A (zh) | 2018-12-05 | 2021-07-23 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| 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 |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| CN114867726B (zh) | 2019-10-28 | 2023-11-28 | 默沙东有限责任公司 | Kras g12c突变体的小分子抑制剂 |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| BR112022010254A2 (pt) * | 2019-12-02 | 2022-09-06 | Shanghai Yingli Pharm Co Ltd | Composto heterocíclico contendo oxigênio representado pela fórmula i, método para preparar o composto heterocíclico contendo oxigênio, composto, composição farmacêutica e uso composto heterocíclico contendo oxigênio |
| 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 |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| WO2022056307A1 (en) | 2020-09-11 | 2022-03-17 | Mirati Therapeutics, Inc. | Crystalline forms of a kras g12c inhibitor |
| EP4216951B1 (en) | 2020-09-22 | 2026-04-01 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| US20230365563A1 (en) * | 2020-09-30 | 2023-11-16 | Shanghai Pharmaceuticals Holding Co., Ltd. | Quinazoline compound and application thereof |
| WO2022098625A1 (en) | 2020-11-03 | 2022-05-12 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| US20240059710A1 (en) * | 2020-11-20 | 2024-02-22 | Jacobio Pharmaceuticals Co., Ltd. | KRAS G12D Inhibitors |
| WO2022105855A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| UY39526A (es) * | 2020-11-20 | 2022-06-30 | Jacobio Pharmaceuticals Co Ltd | Inhibidores de kras g12d |
| WO2022132200A1 (en) | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| US20240140957A1 (en) * | 2021-01-08 | 2024-05-02 | Beigene Switzerland Gmbh | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| WO2022148421A1 (en) * | 2021-01-08 | 2022-07-14 | Beigene, Ltd. | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| US20250066387A9 (en) * | 2021-02-01 | 2025-02-27 | D3 Bio (Wuxi) Co., Ltd. | Pyrimidopyran compound |
| BR112023015976A2 (pt) * | 2021-02-09 | 2023-12-12 | Medshine Discovery Inc | Compostos de anel aromático de pirimidina |
| 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 |
| 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 |
| AU2022219651A1 (en) * | 2021-02-15 | 2023-09-07 | Astellas Pharma Inc. | 4-aminoquinazoline compound |
| KR20230145361A (ko) | 2021-02-15 | 2023-10-17 | 아스텔라스세이야쿠 가부시키가이샤 | G12d 변이 kras 단백의 분해를 유도하기 위한 퀴나졸린화합물 |
| IL305568A (en) * | 2021-03-12 | 2023-10-01 | Bristol Myers Squibb Co | KRAS G12D inhibitors |
| 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 |
| 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 |
| 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 |
| WO2022206724A1 (zh) * | 2021-03-30 | 2022-10-06 | 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 |
| JP2024517695A (ja) * | 2021-04-29 | 2024-04-23 | アムジエン・インコーポレーテツド | 複素環式化合物及び使用方法 |
| 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 |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| 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 |
| 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 |
| JP2024520791A (ja) * | 2021-06-10 | 2024-05-24 | レデックス・ファーマ・パブリック・リミテッド・カンパニー | 化合物 |
| US20240293558A1 (en) | 2021-06-16 | 2024-09-05 | Erasca, Inc. | Kras inhibitor conjugates |
| WO2022262838A1 (en) * | 2021-06-18 | 2022-12-22 | Silexon Ai Technology Co., Ltd. | Deuterated compounds useful as kras g12d inhibitors |
| CN117255793A (zh) * | 2021-06-21 | 2023-12-19 | 江苏恒瑞医药股份有限公司 | 稠合四环类化合物、其制备方法及其在医药上的应用 |
| WO2023278600A1 (en) * | 2021-06-30 | 2023-01-05 | Dana-Farber Cancer Institute, Inc. | Small molecule inhibitors of 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 |
| WO2023280280A1 (zh) * | 2021-07-07 | 2023-01-12 | 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 |
| WO2023284730A1 (en) * | 2021-07-14 | 2023-01-19 | Nikang Therapeutics, Inc. | Alkylidene derivatives as kras inhibitors |
| CN117157292A (zh) * | 2021-07-16 | 2023-12-01 | 苏州赞荣医药科技有限公司 | Kras g12d抑制剂和其用途 |
| 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 |
| CN117677398A (zh) | 2021-07-27 | 2024-03-08 | 东丽株式会社 | 用于癌的治疗和/或预防的药品 |
| EP4382133A4 (en) * | 2021-08-06 | 2025-06-18 | Interoligo Corporation | Pharmaceutical composition for the treatment of triple-negative breast cancer with non-natural nucleic acid ligand as active ingredient |
| WO2023018699A1 (en) * | 2021-08-10 | 2023-02-16 | Erasca, Inc. | Selective kras inhibitors |
| US20240327929A1 (en) * | 2021-08-12 | 2024-10-03 | Merck Sharp & Dohme Llc | Dosage regimen for administration of belzutifan |
| 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 |
| TW202328124A (zh) * | 2021-08-18 | 2023-07-16 | 大陸商北京加科思新藥研發有限公司 | 1,4-氧雜氮雜環庚烷衍生物及其用途 |
| CN117222646A (zh) * | 2021-09-16 | 2023-12-12 | 苏州赞荣医药科技有限公司 | Kras g12c抑制剂和其用途 |
| CN118043330A (zh) * | 2021-09-29 | 2024-05-14 | 海南先声再明医药股份有限公司 | Kras g12d抑制剂化合物及其制备方法和应用 |
| CA3233571A1 (en) | 2021-10-05 | 2023-04-13 | Jill HALLIN | Combinations of kras g12d inhibitors with irinotecan and related methods of treatment |
| KR20240073114A (ko) | 2021-10-05 | 2024-05-24 | 미라티 테라퓨틱스, 인크. | Shp-2 억제제와 kras g12d 억제제의 병용 요법 |
| CA3233567A1 (en) | 2021-10-05 | 2023-04-13 | Jill HALLIN | Combination therapies of kras g12d inhibitors with pan erbb family inhibitors |
| AU2022359282A1 (en) | 2021-10-05 | 2024-04-11 | Mirati Therapeutics, Inc. | Combinations of kras g12d inhibitors with pi3ka inhibitors and related methods of treatment |
| 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 |
| WO2023103523A1 (zh) * | 2021-12-09 | 2023-06-15 | 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 |
| US20250109146A1 (en) * | 2022-01-21 | 2025-04-03 | D3 Bio (Wuxi) Co., Ltd. | Bridged ring-substituted heteroaryl-pyran derivative, and use thereof |
| MX2024008849A (es) * | 2022-01-21 | 2024-07-25 | Usynova Pharmaceuticals Ltd | Compuestos de benzopirimidina y uso de estos. |
| 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 |
| AU2023218370B2 (en) | 2022-02-09 | 2024-11-28 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| WO2023152255A1 (en) * | 2022-02-10 | 2023-08-17 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
| AU2023231912A1 (en) | 2022-03-11 | 2024-08-15 | Astellas Pharma Inc. | Heterocyclic compound for inducing degradation of g12d mutant kras protein |
| CN119317628A (zh) * | 2022-03-22 | 2025-01-14 | 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 |
| IL317601A (en) | 2022-05-25 | 2025-02-01 | Quanta Therapeutics Inc | Pyrimidine-based modulators and their uses |
| 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 |
| 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 |
| KR20250034963A (ko) | 2022-06-24 | 2025-03-11 | 메드샤인 디스커버리 아이엔씨. | 헤테로사이클릭 치환 피리미도피란 화합물 및 이의 용도 |
| TW202409002A (zh) | 2022-07-21 | 2024-03-01 | 日商安斯泰來製藥股份有限公司 | 作用於g12d突變kras蛋白之雜環化合物 |
| TW202408536A (zh) * | 2022-07-29 | 2024-03-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種包含kras g12d抑制劑的醫藥組成物 |
| CN119630656A (zh) | 2022-08-05 | 2025-03-14 | 安斯泰来制药株式会社 | 用于诱导突变kras蛋白分解的杂环化合物 |
| JP7733274B1 (ja) | 2022-08-12 | 2025-09-02 | アステラス製薬株式会社 | G12d変異kras阻害活性を有する二官能性化合物を含む抗がん剤の組合せ |
| 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 |
| WO2024044667A2 (en) * | 2022-08-26 | 2024-02-29 | 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 |
| EP4631942A1 (en) | 2022-10-21 | 2025-10-15 | Leadingtac Pharmaceutical (Shaoxing) Co., Ltd. | Pan-kras degrading agent, and preparation method therefor and use thereof |
| 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 |
| 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 |
| 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 |
| WO2024192424A1 (en) | 2023-03-15 | 2024-09-19 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| EP4671252A1 (en) * | 2023-03-23 | 2025-12-31 | D3 Bio(Wuxi) Co., Ltd. | HETEROCYCLIC SUBSTITUTION PYRIMIDOPYRANE COMPOUND AND ITS USE |
| AU2024245313A1 (en) * | 2023-03-27 | 2025-10-16 | Foshan Ionova Biotherapeutics Co., Inc. | Compounds for degradation and inhibition of kras (g12d) protein |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| AR133028A1 (es) | 2023-06-22 | 2025-08-20 | Astellas Pharma Inc | Composición farmacéutica que comprende un degradador de todas las kras |
| AR133027A1 (es) | 2023-06-22 | 2025-08-20 | Astellas Pharma Inc | Composición farmacéutica que comprende un compuesto de quinazolina |
| 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 |
| 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 |
| 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 |
| US20250114339A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor |
| AU2024357850A1 (en) | 2023-10-09 | 2026-04-23 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025085748A1 (en) | 2023-10-20 | 2025-04-24 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| JP3560609B2 (ja) | 1992-11-13 | 2004-09-02 | イミュネックス・コーポレーション | Elkリガンドと呼ばれる新規なサイトカイン |
| 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 |
| WO1995014023A1 (en) | 1993-11-19 | 1995-05-26 | Abbott Laboratories | Semisynthetic analogs of rapamycin (macrolides) being immunomodulators |
| US5912253A (en) | 1993-12-17 | 1999-06-15 | Novartis Ag | Rapamycin derivatives |
| 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 |
| DK0821671T3 (da) | 1995-04-20 | 2001-04-23 | Pfizer | Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer |
| EP0833828B1 (en) | 1995-06-09 | 2002-11-20 | Novartis AG | Rapamycin derivatives |
| DE69624081T2 (de) | 1995-12-20 | 2003-06-12 | Agouron Pharmaceuticals, Inc. | Matrix-metalloprotease Inhibitoren |
| US6258823B1 (en) | 1996-07-12 | 2001-07-10 | Ariad Pharmaceuticals, Inc. | Materials and method for treating or preventing pathogenic fungal infection |
| EP0923585B1 (en) | 1996-07-18 | 2002-05-08 | Pfizer Inc. | Phosphinate based inhibitors of matrix metalloproteases |
| WO1998007697A1 (en) | 1996-08-23 | 1998-02-26 | Pfizer Inc. | Arylsulfonylamino hydroxamic acid derivatives |
| WO1998030566A1 (en) | 1997-01-06 | 1998-07-16 | Pfizer Inc. | Cyclic sulfone derivatives |
| EP0977733B1 (en) | 1997-02-03 | 2003-09-03 | Pfizer Products Inc. | Arylsulfonylamino hydroxamic acid derivatives |
| 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 |
| EA002546B1 (ru) | 1997-02-11 | 2002-06-27 | Пфайзер Инк. | Производные арилсульфонилгидроксамовой кислоты |
| US6150395A (en) | 1997-05-30 | 2000-11-21 | The Regents Of The University Of California | Indole-3-carbinol (I3C) derivatives and methods |
| AU730248B2 (en) | 1997-08-08 | 2001-03-01 | 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 |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| DK1004578T3 (da) | 1998-11-05 | 2004-06-28 | Pfizer Prod Inc | 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| US6521424B2 (en) | 1999-06-07 | 2003-02-18 | Immunex Corporation | Recombinant expression of Tek antagonists |
| ES2262518T5 (es) | 1999-06-07 | 2009-05-08 | Immunex Corporation | Antagonistas de tek. |
| AU783158B2 (en) | 1999-08-24 | 2005-09-29 | Ariad Pharmaceuticals, Inc. | 28-epirapalogs |
| US6727225B2 (en) | 1999-12-20 | 2004-04-27 | Immunex Corporation | TWEAK receptor |
| CA2400040A1 (en) | 2000-02-25 | 2001-08-30 | Immunex Corporation | Integrin antagonists |
| AU2004255340B2 (en) | 2003-07-08 | 2008-05-01 | Novartis Ag | Use of rapamycin and rapamycin derivatives for the treatment of bone loss |
| EP1648900A4 (en) | 2003-07-11 | 2010-02-10 | Ariad Pharma Inc | PHOSPHORUS 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 |
| BR122020017756B1 (pt) | 2004-08-26 | 2022-02-15 | Pfizer Inc | Uso de compostos de aminoeteroarila enantiomericamente puros na preparação de um medicamento para o tratamento de crescimento celular anormal em um mamífero |
| PE20060608A1 (es) | 2004-10-13 | 2006-08-22 | Wyeth Corp | Analogos de 17-hidroxiwortmanina como inhibidores de pi3k |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CN101267824A (zh) | 2005-09-20 | 2008-09-17 | 辉瑞产品公司 | 使用酪氨酸激酶抑制剂的治疗剂型和方法 |
| AU2008298948B2 (en) | 2007-09-12 | 2014-09-04 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| US8354528B2 (en) | 2007-10-25 | 2013-01-15 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| KR101658274B1 (ko) | 2011-04-06 | 2016-09-22 | 다이호야쿠힌고교 가부시키가이샤 | 신규 이미다조 옥사진 화합물 또는 그의 염 |
| WO2015035223A1 (en) | 2013-09-09 | 2015-03-12 | Peloton Therapeutics, Inc. | Aryl ethers and uses thereof |
| AU2014331794C1 (en) * | 2013-10-10 | 2019-09-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C |
| JP2018513853A (ja) * | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| EP3365334B1 (en) | 2015-10-21 | 2024-07-17 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| 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 |
| EA201992781A1 (ru) * | 2017-05-22 | 2020-04-01 | Эмджен Инк. | Ингибиторы g12c kras и способы их применения |
| AU2018271990A1 (en) * | 2017-05-25 | 2019-12-12 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| HRP20230377T1 (hr) * | 2017-11-15 | 2023-06-23 | Mirati Therapeutics, Inc. | Inhibitori mutacije kras g12c |
| NZ766835A (en) | 2018-03-02 | 2023-09-29 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| JP7174143B2 (ja) | 2018-07-24 | 2022-11-17 | 大鵬薬品工業株式会社 | Shp2活性を阻害するヘテロ二環性化合物 |
| WO2020146613A1 (en) * | 2019-01-10 | 2020-07-16 | 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 |
| US20220363681A1 (en) * | 2019-08-16 | 2022-11-17 | Genfleet Therapeutics (Shanghai) Inc. | Oxo six-membered cyclopyrimidine compound, preparation method and medical use thereof |
-
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 EP EP20833977.0A patent/EP4065583A1/en active Pending
- 2020-11-27 JP JP2022558819A patent/JP7707189B2/ja active Active
- 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 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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| TW202134243A (zh) | 2021-09-16 |
| US20230348495A1 (en) | 2023-11-02 |
| JP2023512113A (ja) | 2023-03-23 |
| CN115003677B (zh) | 2024-08-27 |
| CN115003677A (zh) | 2022-09-02 |
| EP4065583A1 (en) | 2022-10-05 |
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| WO2021106231A1 (en) | 2021-06-03 |
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