JP7676677B2 - Ｋｒａｓ阻害剤 - Google Patents

Ｋｒａｓ阻害剤 Download PDF

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Publication number
JP7676677B2
JP7676677B2 JP2024556680A JP2024556680A JP7676677B2 JP 7676677 B2 JP7676677 B2 JP 7676677B2 JP 2024556680 A JP2024556680 A JP 2024556680A JP 2024556680 A JP2024556680 A JP 2024556680A JP 7676677 B2 JP7676677 B2 JP 7676677B2
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Japan
Prior art keywords
cancer
alkyl
pharma
compound
acceptable salt
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Japanese (ja)
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JP2025512811A (ja
Inventor
アンソニー バーダ，デイビッド
アン バスティアン，ジョリー
ウェイン ファーネス，ケリー
グオ，デチィ
ロバート ヘンリー，ジェイムズ
デュエイン ジョンストン，リチャード
エリック ラマー，ジェイソン
リウ，タオ
ジョン ロドリゲス，マイケル
ルビオ，アルムデナ
シ，チョン
ジャオ，ガイイン
サデグ ジア－エブラヒミ，モハメド
パトリック バウムガルトナー，マシュー
ロホ，イサベル
バルベリス，マリオ
マルティン，サンティアゴ カルバリャレス
ロサダ，パブロ ガルシア
サンフェリシアーノ，ソニア マリア グティエレス
アマドール，ウェンセスラオ ルメラス
フロレス，ビクトリアノ モレロ
バレホ，マリア ロウルデス プリエト
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イーライ リリー アンド カンパニー
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Priority to JP2025075148A priority Critical patent/JP2025118729A/ja
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024556680A 2022-03-25 2023-03-24 Ｋｒａｓ阻害剤 Active JP7676677B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025075148A JP2025118729A (ja) 2022-03-25 2025-04-30 Ｋｒａｓ阻害剤

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202263323607P 2022-03-25 2022-03-25
US63/323,607 2022-03-25
US202263406906P 2022-09-15 2022-09-15
US63/406,906 2022-09-15
US202263386404P 2022-12-07 2022-12-07
US63/386,404 2022-12-07
PCT/US2023/016257 WO2023183585A1 (en) 2022-03-25 2023-03-24 Kras inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025075148A Division JP2025118729A (ja) 2022-03-25 2025-04-30 Ｋｒａｓ阻害剤

Publications (2)

Publication Number Publication Date
JP2025512811A JP2025512811A (ja) 2025-04-22
JP7676677B2 true JP7676677B2 (ja) 2025-05-14

Family

ID=86331239

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2024556680A Active JP7676677B2 (ja) 2022-03-25 2023-03-24 Ｋｒａｓ阻害剤
JP2025075148A Pending JP2025118729A (ja) 2022-03-25 2025-04-30 Ｋｒａｓ阻害剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025075148A Pending JP2025118729A (ja) 2022-03-25 2025-04-30 Ｋｒａｓ阻害剤

Country Status (16)

Country Link
US (2) US12351591B2 (https=)
EP (1) EP4499233A1 (https=)
JP (2) JP7676677B2 (https=)
KR (2) KR102847563B1 (https=)
CN (1) CN119095853A (https=)
AU (1) AU2023241055A1 (https=)
CA (1) CA3246810A1 (https=)
CL (1) CL2024002874A1 (https=)
CO (1) CO2024012604A2 (https=)
DO (1) DOP2024000186A (https=)
IL (1) IL315782A (https=)
JO (1) JOP20240210A1 (https=)
MX (1) MX2024011631A (https=)
PE (1) PE20251071A1 (https=)
TW (2) TWI852436B (https=)
WO (1) WO2023183585A1 (https=)

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WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2024206747A1 (en) * 2023-03-30 2024-10-03 Eli Lilly And Company Kras inhibitors
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
EP4688792A1 (en) * 2023-03-31 2026-02-11 Eli Lilly and Company Kras inhibitors
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
AU2024323424A1 (en) 2023-08-17 2026-03-05 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
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
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025092798A1 (zh) * 2023-10-30 2025-05-08 江苏恒瑞医药股份有限公司 稠合杂芳基类化合物、其制备方法及其在医药上的应用
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547457A (zh) * 2024-04-08 2025-12-16 大陸商江蘇恆瑞醫藥股份有限公司 二氫呋喃并[3,4-f]喹唑啉類化合物、其製備方法及其在醫藥上的應用
WO2025214344A1 (zh) * 2024-04-09 2025-10-16 上海和誉生物医药科技有限公司 一种kras抑制剂及其在药学上的应用
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
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
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026059955A1 (en) * 2024-09-11 2026-03-19 Eli Lilly And Company (3-((6-(2-amino-benzo[d]thiazol-4-yl)-3-(pyrrolidin-1-yl)-7,9-dihydrofuro[3,4-f]quinazolin-1-yl)amino)- piperidin-2-one derivatives as kras inhibitors for the treatment of cancer
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
US12600733B2 (en) * 2024-10-01 2026-04-14 Eli Lilly And Company KRAS inhibitors
WO2026075942A1 (en) * 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors

Citations (2)

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WO2021118877A1 (en) 2019-12-11 2021-06-17 Eli Lilly And Company Kras g12c inhibitors
WO2022047260A1 (en) 2020-08-28 2022-03-03 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof

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US10844051B2 (en) 2015-07-22 2020-11-24 The Royal Institution For The Advancement Of Learning/Mcgill University Substituted oxazoles for the treatment of cancer
HRP20230377T1 (hr) 2017-11-15 2023-06-23 Mirati Therapeutics, Inc. Inhibitori mutacije kras g12c
TW202033518A (zh) * 2018-10-15 2020-09-16 美商美國禮來大藥廠 Kras g12c 抑制劑
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
EP4161934A1 (en) * 2020-06-04 2023-04-12 Antengene Discovery Limited Inhibitors of kras g12c protein and uses thereof
CN113880827B (zh) * 2020-07-03 2024-10-01 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
US20240166660A1 (en) 2021-01-15 2024-05-23 Beigene Switzerland Gmbh Kras g12c inhibitors
WO2022184178A1 (en) 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
CA3210383A1 (en) * 2021-03-12 2022-09-15 Bristol-Myers Squibb Company Kras inhibitors
CN117500799A (zh) 2021-06-09 2024-02-02 伊莱利利公司 作为kras g12d抑制剂的取代的稠合吖嗪
WO2023061294A1 (zh) 2021-10-13 2023-04-20 再鼎医药(上海)有限公司 含氮杂环类衍生物调节剂、其制备方法及应用

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2021118877A1 (en) 2019-12-11 2021-06-17 Eli Lilly And Company Kras g12c inhibitors
WO2022047260A1 (en) 2020-08-28 2022-03-03 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof

Also Published As

Publication number Publication date
AU2023241055A1 (en) 2024-10-10
US20250289830A1 (en) 2025-09-18
WO2023183585A1 (en) 2023-09-28
EP4499233A1 (en) 2025-02-05
CN119095853A (zh) 2024-12-06
JP2025118729A (ja) 2025-08-13
KR102847563B1 (ko) 2025-08-20
PE20251071A1 (es) 2025-04-10
TW202438502A (zh) 2024-10-01
JP2025512811A (ja) 2025-04-22
US12351591B2 (en) 2025-07-08
US20240043451A1 (en) 2024-02-08
TW202404572A (zh) 2024-02-01
KR20240160650A (ko) 2024-11-11
MX2024011631A (es) 2024-09-30
IL315782A (en) 2024-11-01
CL2024002874A1 (es) 2024-12-20
KR20250093430A (ko) 2025-06-24
CO2024012604A2 (es) 2024-12-09
TWI852436B (zh) 2024-08-11
CA3246810A1 (en) 2023-09-28
JOP20240210A1 (ar) 2024-09-26
DOP2024000186A (es) 2024-10-31

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