JP7789906B2 - Ｒａｓ阻害剤 - Google Patents

Ｒａｓ阻害剤

Info

Publication number
JP7789906B2
JP7789906B2 JP2024520911A JP2024520911A JP7789906B2 JP 7789906 B2 JP7789906 B2 JP 7789906B2 JP 2024520911 A JP2024520911 A JP 2024520911A JP 2024520911 A JP2024520911 A JP 2024520911A JP 7789906 B2 JP7789906 B2 JP 7789906B2
Authority
JP
Japan
Prior art keywords
ras
optionally substituted
inhibitor
mmol
compound
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
JP2024520911A
Other languages
English (en)
Japanese (ja)
Other versions
JP2024538705A5 (enExample
JP2024538705A (ja
Inventor
バックル、アンドレアス
バーネット、ジー．レスリー
クレッグ、ジェームズ
ブイ． エドワーズ、アン
エル． ギル、エイドリアン
イー． ノックス、ジョン
エス． コルトゥン、エレナ
リュー、ヤン
セムコ、クリストファー
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.)
Revolution Medicines Inc
Original Assignee
Revolution Medicines Inc
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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of JP2024538705A publication Critical patent/JP2024538705A/ja
Publication of JP2024538705A5 publication Critical patent/JP2024538705A5/ja
Priority to JP2025244552A priority Critical patent/JP2026048800A/ja
Application granted granted Critical
Publication of JP7789906B2 publication Critical patent/JP7789906B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • 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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2024520911A 2021-10-08 2022-10-07 Ｒａｓ阻害剤 Active JP7789906B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025244552A JP2026048800A (ja) 2021-10-08 2025-12-10 Ｒａｓ阻害剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163254013P 2021-10-08 2021-10-08
US63/254,013 2021-10-08
PCT/US2022/077784 WO2023060253A1 (en) 2021-10-08 2022-10-07 Ras inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025244552A Division JP2026048800A (ja) 2021-10-08 2025-12-10 Ｒａｓ阻害剤

Publications (3)

Publication Number Publication Date
JP2024538705A JP2024538705A (ja) 2024-10-23
JP2024538705A5 JP2024538705A5 (enExample) 2025-10-16
JP7789906B2 true JP7789906B2 (ja) 2025-12-22

Family

ID=84044950

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2024520911A Active JP7789906B2 (ja) 2021-10-08 2022-10-07 Ｒａｓ阻害剤
JP2025244552A Pending JP2026048800A (ja) 2021-10-08 2025-12-10 Ｒａｓ阻害剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025244552A Pending JP2026048800A (ja) 2021-10-08 2025-12-10 Ｒａｓ阻害剤

Country Status (17)

Country Link
US (2) US12202845B2 (enExample)
EP (1) EP4413008A1 (enExample)
JP (2) JP7789906B2 (enExample)
KR (1) KR20240074849A (enExample)
CN (2) CN118679169A (enExample)
AR (1) AR127308A1 (enExample)
AU (2) AU2022360536B2 (enExample)
CA (1) CA3234100A1 (enExample)
CL (2) CL2024001023A1 (enExample)
CO (1) CO2024005879A2 (enExample)
CR (1) CR20240156A (enExample)
IL (1) IL311840A (enExample)
MX (1) MX2024004247A (enExample)
PE (1) PE20241476A1 (enExample)
TW (1) TW202315616A (enExample)
WO (1) WO2023060253A1 (enExample)
ZA (1) ZA202402878B (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
KR20240017811A (ko) * 2021-05-05 2024-02-08 레볼루션 메디슨즈, 인크. 암의 치료를 위한 ras 억제제
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250085767A (ko) 2022-09-29 2025-06-12 광조우 조요 파마테크 컴퍼니 리미티드 거대고리 유도체 및 이의 적용
CN118047797A (zh) * 2022-11-16 2024-05-17 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
CN120813588A (zh) 2023-02-14 2025-10-17 豪夫迈·罗氏有限公司 用于治疗癌症的三环化合物
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
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
CN116376844B (zh) * 2023-05-31 2023-08-11 四川大学华西医院 包含shp2 sh2结构域的靶向her2阳性肿瘤的car-t及制备方法和应用
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024354932A1 (en) 2023-10-03 2026-04-09 Revolution Medicines, Inc. Synthesis of ras inhibitors
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
WO2025093625A1 (en) 2023-11-01 2025-05-08 F. Hoffmann-La Roche Ag Macrocycle compounds for the treatment of cancer
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
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
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026010866A1 (en) * 2024-07-01 2026-01-08 Apertor Pharmaceuticals, Inc. Hetero-bifunctional molecules
WO2026015740A1 (en) * 2024-07-11 2026-01-15 Treeline Biosciences, Inc. Macrocyclic 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
WO2026021499A1 (zh) * 2024-07-24 2026-01-29 苏州泽璟生物制药股份有限公司 卤代亚烷基取代环烷基或杂环基类抑制剂及其制备方法和应用
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)

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JP2022520154A (ja) 2018-12-21 2022-03-29 レボリューション メディシンズ インコーポレイテッド 協同的結合に関与する化合物及びその使用
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WO2022251292A1 (en) 2021-05-25 2022-12-01 Revolution Medicines, Inc. Methods for inhibiting ras
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