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 PDF

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
diazabicyclo
methoxy
octan
compound
cyclopropyl
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.)
Active
Application number
JP2022558819A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023512113A (ja
JP2023512113A5 (enExample
Inventor
祐一 河合
和朗 柴田
大樹 朝倉
貴夫 宇野
武 相良
昌幸 中村
優 小早川
ホルベイ,ライアン・サラ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Astex Therapeutics Ltd
Original Assignee
Astex Therapeutics Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of JP2023512113A publication Critical patent/JP2023512113A/ja
Publication of JP2023512113A5 publication Critical patent/JP2023512113A5/ja
Application granted granted Critical
Publication of JP7707189B2 publication Critical patent/JP7707189B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • 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)
JP2022558819A 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 Active JP7707189B2 (ja)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
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

Similar Documents

Publication Publication Date Title
JP7707189B2 (ja) Kras g12d変異に対して阻害活性を有する化合物
JP7611978B2 (ja) がんを処置するためのkras g12c阻害剤
JP7361720B2 (ja) がんの治療のためのkras g12c阻害剤
JP7373014B2 (ja) 肺がん、膵臓がん、または大腸がんを治療するためのKRAS G12C阻害剤としての、ベンズイソチアゾール、イソチアゾロ[3,4-b]ピリジン、キナゾリン、フタラジン、ピリド[2,3-d]ピリダジンおよびピリド[2,3-d]ピリミジン誘導体
JP7360396B2 (ja) Kras g12c阻害剤及び同一物の使用方法
JP7771047B2 (ja) Kif18a阻害剤
JP7361722B2 (ja) Kras g12c阻害剤及び同一物の使用方法
JP7640521B2 (ja) Kif18a阻害剤として有用なヘテロアリールアミド
US12473281B2 (en) Synthesis of KRAS G12C inhibitor compound
US12466825B2 (en) Synthesis of KRAS G12C inhibitor compound
JP2023515235A (ja) 4-アミノブタ-2-エンアミド誘導体及びその塩
JP2025013928A (ja) Kif18a阻害剤として有用なヘテロアリールアミド
US20240246968A1 (en) Small molecule inhibitors of kras g12c mutant
KR20250164341A (ko) Kras g12c 억제제 화합물의 주요 중간체의 개선된 합성
TW202128632A (zh) 4-胺基丁-2-烯醯胺衍生物及其鹽
CN116003405A (zh) Kras g12c的抑制剂及其使用方法
KR102953492B1 (ko) Kras g12c 억제제 화합물의 개선된 합성
EA049102B1 (ru) Улучшенный синтез соединения, представляющего собой ингибитор kras g12c
KR20260056313A (ko) Kras g12c 억제제 화합물의 개선된 합성
HK40050247A (en) Improved synthesis of key intermediate of kras g12c inhibitor compound
HK40050247B (en) Improved synthesis of key intermediate of kras g12c inhibitor compound

Legal Events

Date Code Title Description
AA64 Notification of invalidation of claim of internal priority (with term)

Free format text: JAPANESE INTERMEDIATE CODE: A241764

Effective date: 20230131

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230202

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230222

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20231122

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20231122

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20250121

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250417

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20250624

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250702

R150 Certificate of patent or registration of utility model

Ref document number: 7707189

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150