JP2025504486A - Ｋｒａｓの標的分解のための化合物及び方法 - Google Patents

Ｋｒａｓの標的分解のための化合物及び方法 Download PDF

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JP2025504486A
JP2025504486A JP2024543238A JP2024543238A JP2025504486A JP 2025504486 A JP2025504486 A JP 2025504486A JP 2024543238 A JP2024543238 A JP 2024543238A JP 2024543238 A JP2024543238 A JP 2024543238A JP 2025504486 A JP2025504486 A JP 2025504486A
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JP2025504486A5 (https=
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ジーザス・ラウル・メディナ
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アルヴィナス・オペレーションズ・インコーポレイテッド
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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
    • A61K31/55—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
    • 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
    • A61K47/54—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 an organic compound
    • A61K47/55—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 an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2024543238A 2022-01-21 2023-01-20 Ｋｒａｓの標的分解のための化合物及び方法 Pending JP2025504486A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202263301887P 2022-01-21 2022-01-21
US63/301,887 2022-01-21
PCT/US2023/060996 WO2023141570A2 (en) 2022-01-21 2023-01-20 Compounds and methods for the targeted degradation of kras

Publications (2)

Publication Number Publication Date
JP2025504486A true JP2025504486A (ja) 2025-02-12
JP2025504486A5 JP2025504486A5 (https=) 2026-01-27

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ID=87349145

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JP2024543238A Pending JP2025504486A (ja) 2022-01-21 2023-01-20 Ｋｒａｓの標的分解のための化合物及び方法

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Country Link
US (1) US20250206732A1 (https=)
EP (1) EP4466277A4 (https=)
JP (1) JP2025504486A (https=)
WO (1) WO2023141570A2 (https=)

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WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
CA3243798A1 (en) 2022-02-09 2023-08-17 Quanta Therapeutics, Inc. Kras Modulators and Their Uses
WO2023230190A1 (en) 2022-05-25 2023-11-30 Quanta Therapeutics, Inc. Pyrimidine based modulators and uses thereof
TW202440597A (zh) 2022-11-30 2024-10-16 美商虎行生物公司 含戊二醯亞胺之pan-kras-突變降解劑化合物及其用途
EP4626554A1 (en) 2022-11-30 2025-10-08 Tiger Biotherapeutics Inc. Glutarimide-containing kras-mutant degrader compounds and uses thereof
WO2024120424A1 (zh) * 2022-12-07 2024-06-13 贝达药业股份有限公司 一种靶向泛kras蛋白降解剂的化合物及其应用
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
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
EP4735438A2 (en) 2023-06-30 2026-05-06 Merck Patent GmbH Heterobifunctional compounds for the degradation of kras
EP4735452A2 (en) 2023-06-30 2026-05-06 Merck Patent GmbH Heterobifunctional compounds for the degradation of kras protein
WO2025024732A1 (en) * 2023-07-26 2025-01-30 Arvinas Operations, Inc. Compounds useful in the treatment of kras mediated disorders
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025039676A1 (zh) * 2023-08-18 2025-02-27 贝达药业股份有限公司 一种靶向泛kras蛋白降解剂的化合物及其应用
US20250127728A1 (en) 2023-10-05 2025-04-24 Capstan Therapeutics, Inc. Constrained Ionizable Cationic Lipids and Lipid Nanoparticles
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025107579A1 (zh) * 2023-11-20 2025-05-30 贝达药业股份有限公司 一种靶向泛kras蛋白降解剂的化合物及其应用
WO2025168051A1 (zh) * 2024-02-08 2025-08-14 润佳（苏州）医药科技有限公司 一种双官能化合物及其用途
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
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
WO2026015801A1 (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
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
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102668696B1 (ko) * 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
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
WO2019195609A2 (en) * 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
US20230002371A1 (en) * 2019-09-13 2023-01-05 Biotheryx, Inc. Ras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
CN115803030A (zh) * 2020-04-06 2023-03-14 阿维纳斯企业公司 用于kras靶向降解的化合物和方法
WO2023077441A1 (en) * 2021-11-05 2023-05-11 Ranok Therapeutics (Hangzhou) Co. Ltd. Methods and compositions for targeted protein degradation

Also Published As

Publication number Publication date
EP4466277A2 (en) 2024-11-27
WO2023141570A3 (en) 2023-09-14
WO2023141570A9 (en) 2024-06-27
EP4466277A4 (en) 2025-12-10
WO2023141570A2 (en) 2023-07-27
US20250206732A1 (en) 2025-06-26

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