JP7039489B2 - Ｋｒａｓ ｇ１２ｃ阻害剤 - Google Patents

Ｋｒａｓ ｇ１２ｃ阻害剤 Download PDF

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JP7039489B2
JP7039489B2 JP2018560589A JP2018560589A JP7039489B2 JP 7039489 B2 JP7039489 B2 JP 7039489B2 JP 2018560589 A JP2018560589 A JP 2018560589A JP 2018560589 A JP2018560589 A JP 2018560589A JP 7039489 B2 JP7039489 B2 JP 7039489B2
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mmol
alkyl
piperazine
cancer
optionally substituted
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JP2019516718A5 (enExample
JP2019516718A (ja
Inventor
フィッシャー，ジョン・ピー
フェル，ジェイ・ブラッドフォード
ブレイク，ジェームズ・エフ
ヒンクリン，ロナルド・ジェイ
メヒア，マセドニオ・ジェイ
ヒッケン，エリック・ジェームズ
チカレリ，マーク・ジョゼフ
ガウディーノ，ジョン・ジェイ
ビジャーズ，ガイ・ピー・エイ
バージェス，ローレンス・イー
マークス，マシュー・アーノルド
クリステンセン，ジェームズ・ゲイル
リー，マシュー・ランドルフ
サベチェンコフ，パベル
ゼッカ，ヘンリー・ジェイ
タン，トニー・ピー
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Mirati Therapeutics Inc
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Mirati Therapeutics Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (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 Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2018560589A 2016-05-18 2017-05-17 Ｋｒａｓ ｇ１２ｃ阻害剤 Active JP7039489B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662338116P 2016-05-18 2016-05-18
US62/338,116 2016-05-18
US201762444614P 2017-01-10 2017-01-10
US62/444,614 2017-01-10
PCT/US2017/033099 WO2017201161A1 (en) 2016-05-18 2017-05-17 Kras g12c inhibitors

Publications (3)

Publication Number Publication Date
JP2019516718A JP2019516718A (ja) 2019-06-20
JP2019516718A5 JP2019516718A5 (enExample) 2019-07-25
JP7039489B2 true JP7039489B2 (ja) 2022-03-22

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Country Status (12)

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US (3) US11267812B2 (enExample)
EP (1) EP3458445B1 (enExample)
JP (1) JP7039489B2 (enExample)
KR (1) KR102444509B1 (enExample)
CN (1) CN109843856B (enExample)
AU (1) AU2017266911B2 (enExample)
CA (1) CA3024523A1 (enExample)
ES (1) ES2863873T3 (enExample)
IL (1) IL262867B (enExample)
MX (1) MX382339B (enExample)
SG (1) SG11201810171SA (enExample)
WO (1) WO2017201161A1 (enExample)

Families Citing this family (220)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102444509B1 (ko) 2016-05-18 2022-09-19 미라티 테라퓨틱스, 인크. Kras g12c 억제제
CN110366550A (zh) 2016-12-22 2019-10-22 美国安进公司 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物
AU2018273356B2 (en) 2017-05-22 2021-09-16 Amgen Inc. KRAS G12C inhibitors and methods of using the same
AU2018329920B2 (en) 2017-09-08 2022-12-01 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
LT3710439T (lt) * 2017-11-15 2023-05-10 Mirati Therapeutics, Inc. Kras g12c inhibitoriai
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
EP3842433B1 (en) 2018-01-19 2023-11-01 Medshine Discovery Inc. Pyridone-pyrimidine derivative acting as krasg12c mutein inhibitor
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) * 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
EP3788053B1 (en) 2018-05-04 2024-07-10 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3098574A1 (en) * 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
MA52564A (fr) 2018-05-10 2021-03-17 Amgen Inc Inhibiteurs de kras g12c pour le traitement du cancer
US11096939B2 (en) 2018-06-01 2021-08-24 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
AU2019320945C1 (en) 2018-08-16 2021-09-30 F. Hoffmann-La Roche Ag Fused ring compounds
ES2961253T3 (es) * 2018-08-31 2024-03-11 Mirati Therapeutics Inc Inhibidores de KRas G12C
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
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
ES3017461T3 (en) * 2018-09-10 2025-05-13 Mirati Therapeutics Inc Combination of dasatinib and adagrasib for use in the treatment of non-small cell lung cancer
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
CR20210175A (es) 2018-09-18 2021-06-01 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2)
CN114042070A (zh) 2018-09-30 2022-02-15 凯瑞康宁生物工程（武汉）有限公司 作为神经元组胺受体-3拮抗剂的化合物及其用途
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
PE20260440A1 (es) 2018-11-09 2026-02-19 Hoffmann La Roche Compuestos de anillo fusionado
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
AU2019384118B2 (en) 2018-11-19 2025-06-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
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
US20220152026A1 (en) 2019-02-12 2022-05-19 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
KR102934231B1 (ko) 2019-03-05 2026-03-06 아스트라제네카 아베 항암제로 유용한 융합 삼환식 화합물
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
JP7502337B2 (ja) * 2019-05-20 2024-06-18 カリフォルニア インスティチュート オブ テクノロジー Ｋｒａｓ ｇ１２ｃインヒビター及びその使用
WO2020236947A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
AU2020277398B2 (en) 2019-05-21 2026-01-29 Amgen Inc. Solid state forms
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
TW202110837A (zh) * 2019-05-24 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 氫化吡啶并嘧啶類衍生物、其製備方法及其在醫藥上的應用
WO2020239077A1 (zh) * 2019-05-29 2020-12-03 上海翰森生物医药科技有限公司 含氮杂环类衍生物调节剂、其制备方法和应用
CN112047939B (zh) * 2019-06-06 2023-05-02 江苏先声药业有限公司 一种具有抗肿瘤活性的四氢吡啶并嘧啶类化合物
WO2021000885A1 (zh) * 2019-07-01 2021-01-07 江苏恒瑞医药股份有限公司 喹唑啉酮类衍生物、其制备方法及其在医药上的应用
CN112300153B (zh) * 2019-07-26 2023-06-13 博瑞生物医药（苏州）股份有限公司 一种杂环化合物、药物组合物和用途
CN112390788A (zh) * 2019-08-13 2021-02-23 苏州闻天医药科技有限公司 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途
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
CN112390796B (zh) * 2019-08-19 2023-06-27 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
CN112430234B (zh) * 2019-08-26 2023-04-28 信达生物制药(苏州)有限公司 一种新型kras g12c蛋白抑制剂及其制备方法和用途
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021043322A1 (zh) * 2019-09-06 2021-03-11 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
US20220402916A1 (en) * 2019-09-18 2022-12-22 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN112538084B (zh) * 2019-09-23 2023-06-20 信达生物制药(苏州)有限公司 新颖的kras g12c蛋白抑制剂及其制备方法和用途
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
CN114555586B (zh) * 2019-10-10 2023-06-23 信达生物制药(苏州)有限公司 Krasg12c蛋白抑制剂及其制备方法和用途
CN112694475B (zh) 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
AU2020377925A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
IL322454A (en) 2019-11-04 2025-09-01 Revolution Medicines Inc ras inhibitors
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
CN112778301A (zh) * 2019-11-07 2021-05-11 苏州泽璟生物制药股份有限公司 四氢吡啶并嘧啶类抑制剂及其制备方法和应用
CN114630832A (zh) * 2019-11-15 2022-06-14 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
CN112824410A (zh) * 2019-11-21 2021-05-21 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
EP4065231A1 (en) * 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
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
CN112979664B (zh) * 2019-12-02 2024-03-01 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
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
CN113045565A (zh) * 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
CN112094269B (zh) * 2020-01-01 2021-12-07 上海凌达生物医药有限公司 一类饱和六元环并杂环类化合物、制备方法和用途
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
CN115135650A (zh) * 2020-02-20 2022-09-30 贝达医药公司 作为kras抑制剂的吡啶并嘧啶衍生物
AU2021233058B2 (en) * 2020-03-12 2024-05-16 D3 Bio(Wuxi) Co., Ltd Pyrimidoheterocyclic compounds and application thereof
TWI811656B (zh) * 2020-04-22 2023-08-11 大陸商德昇濟醫藥（無錫）有限公司 嘧啶并雜環類化合物及其應用
WO2021219072A1 (zh) * 2020-04-30 2021-11-04 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
CN113666923A (zh) * 2020-05-15 2021-11-19 苏州泽璟生物制药股份有限公司 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用
CN113683616B (zh) * 2020-05-18 2025-12-30 广州百霆医药科技有限公司 Kras g12c突变蛋白抑制剂
JP7808058B2 (ja) * 2020-06-02 2026-01-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング がんを治療するための縮合環化２－アミノ－３－シアノチオフェン及び誘導体
CN111646910A (zh) * 2020-06-15 2020-09-11 中国药科大学 一种盐酸达泊西汀消旋体的制备方法
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
CN115942936A (zh) 2020-06-24 2023-04-07 勃林格殷格翰国际有限公司 包含sos1抑制剂和kras g12c抑制剂的抗癌组合疗法
CN113912608B (zh) * 2020-07-10 2023-07-14 江苏恒瑞医药股份有限公司 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用
CN113980014B (zh) * 2020-07-27 2023-05-12 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
US20250195521A1 (en) 2020-09-03 2025-06-19 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
WO2022052895A1 (zh) 2020-09-11 2022-03-17 南京明德新药研发有限公司 氮杂环丁烷取代化合物的晶型
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
US20230357277A1 (en) * 2020-09-22 2023-11-09 Mirati Therapeutics, Inc. Kras g12d inhibitors
JP2023544450A (ja) 2020-09-23 2023-10-23 エラスカ・インコーポレイテッド 三環式ピリドン及びピリミドン
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
MX2023004373A (es) * 2020-10-14 2023-07-07 Ranok Therapeutics Hangzhou Co Ltd Metodos y composiciones para la degradacion dirigida de proteinas.
US20240059703A1 (en) 2020-10-20 2024-02-22 Amgen Inc. Heterocyclic spiro compounds and methods of use
WO2022087375A1 (en) * 2020-10-22 2022-04-28 Spectrum Pharmaceuticals, Inc. Novel heterocyclic compounds
WO2022087371A1 (en) * 2020-10-22 2022-04-28 Spectrum Pharmaceuticals, Inc. Novel bicyclic compounds
WO2022105855A1 (en) * 2020-11-20 2022-05-27 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
EP4247807A4 (en) * 2020-11-23 2024-10-16 Merck Sharp & Dohme LLC 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT
KR102503336B1 (ko) 2020-11-23 2023-02-23 동의대학교 산학협력단 음성지원이 가능한 반려동물의 배변 처리 패드
CN116829151A (zh) * 2020-12-15 2023-09-29 米拉蒂治疗股份有限公司 氮杂喹唑啉泛KRas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
WO2022133345A1 (en) 2020-12-18 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2022140472A1 (en) 2020-12-22 2022-06-30 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
US20240092803A1 (en) * 2021-01-08 2024-03-21 Beigene Switzerland Gmbh 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.
CN116600808B (zh) * 2021-02-09 2024-10-22 苏州阿尔脉生物科技有限公司 一类作为kras突变体g12c抑制剂的四氢萘啶类衍生物、其制备方法及其应用
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
JP2024509280A (ja) * 2021-03-10 2024-02-29 ベータ・ファーマ・インコーポレイテッド Ｋｒａｓ阻害物質としてのピリドピリミジン誘導体
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
WO2022204112A1 (en) 2021-03-22 2022-09-29 Incyte Corporation Imidazole and triazole kras inhibitors
CN115124524A (zh) * 2021-03-26 2022-09-30 浙江海正药业股份有限公司 三环类衍生物及其制备方法和用途
WO2022216648A1 (en) 2021-04-08 2022-10-13 Mirati Therapeutics, Inc. Combination therapies using prmt5 inhibitors for the treatment of cancer
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
JP2024514127A (ja) 2021-04-09 2024-03-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 抗がん剤療法
EP4322954A4 (en) * 2021-04-16 2025-01-29 Merck Sharp & Dohme LLC SMALL MOLECULAR INHIBITORS OF THE KRAS G12D MUTANT
EP4322945A4 (en) * 2021-04-16 2025-07-16 Mirati Therapeutics Inc KRAS G12C INHIBITORS
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
CN117203207A (zh) * 2021-04-30 2023-12-08 江苏恒瑞医药股份有限公司 桥环类化合物、其制备方法及其在医药上的应用
TW202309052A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ｒａｓ抑制劑
KR20240017811A (ko) 2021-05-05 2024-02-08 레볼루션 메디슨즈, 인크. 암의 치료를 위한 ras 억제제
US12280055B2 (en) 2021-05-27 2025-04-22 Mirati Therapeutics, Inc. Combination therapies
EP4347041A1 (en) * 2021-05-28 2024-04-10 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
WO2022261210A1 (en) * 2021-06-08 2022-12-15 Quanta Therapeutics, Inc. Kras modulators and uses thereof
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2022271823A1 (en) * 2021-06-23 2022-12-29 Newave Pharmaceutical Inc. Mutant kras modulators and uses thereof
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途
EP4359081A1 (en) 2021-06-23 2024-05-01 Novartis AG Pyrazolyl derivatives as inhibitors of the kras mutant protein
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
MX2024000357A (es) 2021-07-07 2024-02-12 Incyte Corp Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras).
WO2023287896A1 (en) 2021-07-14 2023-01-19 Incyte Corporation Tricyclic compounds as inhibitors of kras
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
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
US12441742B2 (en) 2021-08-31 2025-10-14 Incyte Corporation Naphthyridine compounds as inhibitors of KRAS
KR20240055778A (ko) 2021-09-01 2024-04-29 노파르티스 아게 Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도
EP4389751A1 (en) * 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2023040989A1 (en) * 2021-09-16 2023-03-23 Suzhou Zanrong Pharma Limited Kras g12c inhibitors and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
MX2024004846A (es) 2021-10-22 2024-05-03 Jiangsu Hengrui Pharmaceuticals Co Ltd Compuesto tetraciclico que contiene nitrogeno, metodo de preparacion del mismo y uso medico del mismo.
IL312381A (en) * 2021-11-05 2024-06-01 Frontier Medicines Corp KRAS G12C inhibitors
WO2023099624A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN117940436A (zh) * 2021-12-02 2024-04-26 上海和誉生物医药科技有限公司 一种7-(萘-1-基)吡啶并[4,3-d]嘧啶衍生物及其制备和应用
WO2023098425A1 (zh) * 2021-12-02 2023-06-08 上海和誉生物医药科技有限公司 一种kras抑制剂及其制备和在药学上的应用
CN119212994A (zh) 2021-12-17 2024-12-27 建新公司 作为shp2抑制剂的吡唑并吡嗪化合物
TW202340202A (zh) 2021-12-22 2023-10-16 美國加利福尼亞大學董事會 Gtp酶抑制劑及其用途
WO2023117681A1 (en) 2021-12-22 2023-06-29 Boehringer Ingelheim International Gmbh Heteroaromatic compounds for the treatment of cancer
CN116410145A (zh) * 2021-12-29 2023-07-11 上海泓博智源医药股份有限公司 一种mrtx849中间体的制备方法
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
WO2023137223A1 (en) * 2022-01-17 2023-07-20 Newave Pharmaceutical Inc. Pan-kras inhibitors and uses thereof
CN118556063A (zh) * 2022-01-21 2024-08-27 上海湃隆生物科技有限公司 杂环类化合物、药物组合物及其应用
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
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
JP2025510572A (ja) 2022-03-08 2025-04-15 レボリューション メディシンズ インコーポレイテッド 免疫不応性肺癌を治療するための方法
CN116891514A (zh) * 2022-04-06 2023-10-17 润佳（苏州）医药科技有限公司 一种双官能化合物及其用途
CN119053595A (zh) 2022-03-28 2024-11-29 尼坎治疗公司 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰氨基衍生物
EP4504203A1 (en) 2022-04-04 2025-02-12 Sanofi Therapeutic combination of kras g12c inhibitor and tead inhibitor
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
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
WO2023220421A1 (en) * 2022-05-13 2023-11-16 Ranok Therapeutics (Hangzhou) Co. Ltd. Inhibitors of kras(g12d)
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
CN119790053A (zh) 2022-06-08 2025-04-08 霖康疗法公司 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰胺衍生物
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250024833A (ko) * 2022-06-14 2025-02-19 미라티 테라퓨틱스, 인크. 테트라하이드로피리도피리미딘 PAN-Kras 억제제
JP2025525356A (ja) * 2022-06-15 2025-08-05 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
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds
JP2025531491A (ja) * 2022-09-28 2025-09-19 ミラティ セラピューティクス， インコーポレイテッド 併用療法
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer
CN120659773A (zh) 2022-11-09 2025-09-16 锐新医药公司 化合物、复合物以及其制备方法和用途
AU2023375457A1 (en) 2022-11-11 2025-05-01 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
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
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
CN121464140A (zh) 2023-04-14 2026-02-03 锐新医药公司 Ras抑制剂的结晶形式、含有其的组合物及其使用方法
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
KR20240168510A (ko) * 2023-05-22 2024-12-02 주식회사 이노파마스크린 Kras g12d 및 g12v 돌연변이 표적 화합물 및 그 용도
CN116640104B (zh) * 2023-05-24 2024-04-02 杭州科耀医药科技有限公司 一种替洛利生的工业合成方法
EP4720678A1 (en) 2023-05-31 2026-04-08 Boehringer Ingelheim International GmbH Survivin as a biomarker for predicting the responsiveness of cancer treatment
EP4721766A1 (en) 2023-06-02 2026-04-08 Daiichi Sankyo Company, Limited Combination of (anti-her3 antibody)-drug conjugate and rasg12c inhibitor
CN116675690B (zh) * 2023-06-02 2026-03-27 北京康立生医药技术开发有限公司 一种肺癌治疗药物的制备方法
WO2025016899A1 (en) 2023-07-19 2025-01-23 Bayer Aktiengesellschaft Spirocyclic compounds for the treatment of cancer
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
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors
TW202529768A (zh) 2023-09-29 2025-08-01 大陸商德昇濟醫藥（無錫）有限公司 癌症治療的療法
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
TW202527955A (zh) 2023-11-27 2025-07-16 美商尼坎醫療公司 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶２和週期蛋白依賴性激酶４的含有２，５－取代的嘧啶衍生物的雙功能化合物
WO2025117981A1 (en) 2023-12-02 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
US20250205238A1 (en) 2023-12-20 2025-06-26 Boehringer Ingelheim International Gmbh Anti-cancer combination therapy
WO2025145207A1 (en) 2023-12-29 2025-07-03 Bristol-Myers Squibb Company Combination therapy of kras inhibitor and treg-depleting agent
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025212828A1 (en) 2024-04-03 2025-10-09 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025240536A1 (en) 2024-05-15 2025-11-20 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026003808A1 (en) 2024-06-28 2026-01-02 Assia Chemical Industries Ltd. Solid state form of adagrasib and process for preparation
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
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
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
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007512364A (ja) 2003-11-21 2007-05-17 アレイ バイオファーマ、インコーポレイテッド Ａｋｔプロテインキナーゼインヒビター
WO2012171015A2 (en) 2011-06-10 2012-12-13 Translational Genomics Research Institute Therapeutic combination for cancer treatment
JP2014506930A (ja) 2011-02-28 2014-03-20 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼインヒビター
WO2014152588A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
US20140288045A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c
JP2015519308A (ja) 2012-04-10 2015-07-09 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア 癌治療用組成物および方法

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002053558A1 (en) 2001-01-02 2002-07-11 F.Hoffman-La Roche Ag Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
US20080051387A1 (en) 2006-06-09 2008-02-28 Yuelian Xu Tetrahydropyrido[3,4-d]pyrimidines and related analogues
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
EP2518063B1 (en) 2006-12-21 2017-02-01 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
WO2008103470A2 (en) 2007-02-21 2008-08-28 Trustees Of Columbia University In The City Of New York Oncogenic-ras-signal dependent lethal compounds
US20100298289A1 (en) 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
JP2011516494A (ja) 2008-04-07 2011-05-26 ギリアード サイエンシーズ， インコーポレイテッド ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するための２Ｈ−ベンゾ［ｂ］［１，４］オキサジン−３（４Ｈ）−オン誘導体
CA2729045A1 (en) 2008-07-31 2010-02-04 Philippe Bergeron Pyrimidine compounds, compositions and methods of use
WO2010120996A1 (en) * 2009-04-17 2010-10-21 Wyeth Llc 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2518064A1 (en) 2009-12-25 2012-10-31 Mochida Pharmaceutical Co., Ltd. Novel aryl urea derivative
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
US9695133B2 (en) 2012-07-13 2017-07-04 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-RAS-selective lethal compounds and their use
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
JP6279963B2 (ja) 2014-04-15 2018-02-14 株式会社神戸製鋼所 チタンまたはチタン合金からなるスラブの連続鋳造装置
MA40074A (fr) 2014-05-30 2015-12-03 Univ Columbia Composés liant ras multivalents
WO2016025650A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinations of an erk inhibitor and a cdk4/6 inhibitor and related methods
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 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インヒビター
US10017540B2 (en) 2015-03-11 2018-07-10 California Institute Of Technology Cyclic peptide binder against oncogenic K-Ras
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
US10421764B2 (en) 2015-04-24 2019-09-24 H. Lee Moffitt Cancer Center And Research Institute, Inc. Mutant KRas inhibitors
AU2016258192B2 (en) 2015-05-06 2021-07-29 Leidos Biomedical Research, Inc. K-Ras modulators
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
CN108513588A (zh) 2015-09-24 2018-09-07 Ionis制药公司 Kras表达的调节剂
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
EP3365686A4 (en) 2015-10-22 2019-03-27 The Scripps Research Institute REACTIVE CYSTEINSONS AND USES THEREOF
WO2017080980A1 (en) 2015-11-09 2017-05-18 Astrazeneca Ab Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
WO2017079864A1 (en) 2015-11-12 2017-05-18 Hangzhou Yier Biotech Co., Ltd. Treatment of cancers related to chronically active ras
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
KR102444509B1 (ko) 2016-05-18 2022-09-19 미라티 테라퓨틱스, 인크. Kras g12c 억제제
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
WO2018069871A2 (en) 2016-10-13 2018-04-19 Sorrento Therapeutics, Inc. Anti-kras binding proteins
US12150934B2 (en) 2016-11-30 2024-11-26 Bantam Pharmaceutical, Llc Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
CA3081983A1 (en) 2016-11-30 2018-06-07 Bantam Pharmaceutical, Llc Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases
KR20190095355A (ko) 2016-12-15 2019-08-14 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 암의 치료를 위한 조성물 및 방법
EP3558979B1 (en) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
CN110366550A (zh) 2016-12-22 2019-10-22 美国安进公司 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3573966A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused n-heterocyclic compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
EP3612526A2 (en) 2017-04-20 2020-02-26 The Regents of the University of California K-ras modulators
AU2018329920B2 (en) 2017-09-08 2022-12-01 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
LT3710439T (lt) * 2017-11-15 2023-05-10 Mirati Therapeutics, Inc. Kras g12c inhibitoriai
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007512364A (ja) 2003-11-21 2007-05-17 アレイ バイオファーマ、インコーポレイテッド Ａｋｔプロテインキナーゼインヒビター
JP2014506930A (ja) 2011-02-28 2014-03-20 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼインヒビター
WO2012171015A2 (en) 2011-06-10 2012-12-13 Translational Genomics Research Institute Therapeutic combination for cancer treatment
JP2015519308A (ja) 2012-04-10 2015-07-09 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア 癌治療用組成物および方法
WO2014152588A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
US20140288045A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Bioorganic & Medicinal Chemistry Letters，2014年，24 (12)，2635-2639

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