JP7669556B2 - Ｋｒａｓ阻害剤 - Google Patents

Ｋｒａｓ阻害剤 Download PDF

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Publication number
JP7669556B2
JP7669556B2 JP2024055240A JP2024055240A JP7669556B2 JP 7669556 B2 JP7669556 B2 JP 7669556B2 JP 2024055240 A JP2024055240 A JP 2024055240A JP 2024055240 A JP2024055240 A JP 2024055240A JP 7669556 B2 JP7669556 B2 JP 7669556B2
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cancer
pharma
acceptable salt
compound
optionally substituted
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Japanese (ja)
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JP2024146897A (ja
JP2024146897A5 (https=
Inventor
デイビッド エイブラハム，アデドイン
デ ラ クルス，アルベルト バレロ
リョレンテ，アリシア マルコス
ガルシア，アルバロ エンリケ
グオ，デチィ
ブメ，デスタ
コルディエ，フレデリック ローラン
ジャオ，ガイイン
ガルシア，イサベル ロホ
ロバート ヘンリー，ジェイムズ
エリック ラマー，ジェイソン
アン バスティアン，ジョリー
バレホ，マリア ロウルデス プリエト
バルベリス，マリオ
パトリック バウムガルトナー，マシュー
サンス，ミゲル ガルソン
ラジャマニ，ラムクマール
デュエイン ジョンストン，リチャード
ハズリット，ロバート
マルティン，サンティアゴ カルバリャレス
アロノウ，ショーン
マイケル ウォールズ，シェイン
サンフェリシアーノ，ソニア マリア グティエレス
アンドリューズ，スティーブン
スコット カーチャー，ティモシー
フロレス，ビクトリアノ モレロ
アマドール，ウェンセスラオ ルメラス
ラッシュ スキャッグス，ウィリアム
リンコン，フアン アントニオ
ソレル，フリアン プリエゴ
ロサダ，パブロ ガルシア
ディルガー，アンドリュー
チェン，シャオホン
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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 JP2025067243A priority Critical patent/JP2025111535A/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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • A61K31/535—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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024055240A 2023-03-31 2024-03-29 Ｋｒａｓ阻害剤 Active JP7669556B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025067243A JP2025111535A (ja) 2023-03-31 2025-04-16 Ｋｒａｓ阻害剤

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
EP23382315 2023-03-31
EP23382315 2023-03-31
EP23382531 2023-06-02
EP23382531 2023-06-02
EP23382857 2023-08-18
EP23382857 2023-08-18
EP23382985 2023-09-27
EP23382985 2023-09-27
EP24382267 2024-03-12
EP24382267 2024-03-12

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025067243A Division JP2025111535A (ja) 2023-03-31 2025-04-16 Ｋｒａｓ阻害剤

Publications (3)

Publication Number Publication Date
JP2024146897A JP2024146897A (ja) 2024-10-15
JP2024146897A5 JP2024146897A5 (https=) 2025-03-18
JP7669556B2 true JP7669556B2 (ja) 2025-04-28

Family

ID=90826251

Family Applications (2)

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JP2024055240A Active JP7669556B2 (ja) 2023-03-31 2024-03-29 Ｋｒａｓ阻害剤
JP2025067243A Pending JP2025111535A (ja) 2023-03-31 2025-04-16 Ｋｒａｓ阻害剤

Family Applications After (1)

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JP2025067243A Pending JP2025111535A (ja) 2023-03-31 2025-04-16 Ｋｒａｓ阻害剤

Country Status (16)

Country Link
US (1) US20240368193A1 (https=)
EP (1) EP4688792A1 (https=)
JP (2) JP7669556B2 (https=)
KR (1) KR20250163395A (https=)
CN (1) CN121002032A (https=)
AR (1) AR132295A1 (https=)
AU (1) AU2024241889A1 (https=)
CL (1) CL2025002769A1 (https=)
CO (1) CO2025013134A2 (https=)
DO (1) DOP2025000245A (https=)
IL (1) IL323362A (https=)
JO (1) JOP20250246A1 (https=)
MX (1) MX2025011449A (https=)
PE (1) PE20252444A1 (https=)
TW (1) TWI901059B (https=)
WO (1) WO2024206766A1 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
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
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
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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
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
WO2026015790A1 (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
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

Citations (6)

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WO2022037631A1 (zh) 2020-08-21 2022-02-24 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
WO2022119748A1 (en) 2020-12-04 2022-06-09 Eli Lilly And Company Tricyclic kras g12c inhibitors
CN115611923A (zh) 2021-07-12 2023-01-17 贝达药业股份有限公司 Kras g12d抑制剂及其在医药上的应用
WO2023030517A1 (en) 2021-09-06 2023-03-09 Suzhou Zanrong Pharma Limited Kras g12c inhibitors and uses thereof
CN115785199A (zh) 2021-09-10 2023-03-14 润佳（苏州）医药科技有限公司 一种双官能化合物及其用途
WO2023183585A1 (en) 2022-03-25 2023-09-28 Eli Lilly And Company Kras inhibitors

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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
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ES2929700T3 (es) 2019-12-11 2022-12-01 Lilly Co Eli Inhibidores de KRas g12c
CN116368130A (zh) * 2020-08-28 2023-06-30 金橘生物科技公司 杂环化合物及其用途
US20240166660A1 (en) * 2021-01-15 2024-05-23 Beigene Switzerland Gmbh Kras g12c 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

Patent Citations (6)

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Publication number Priority date Publication date Assignee Title
WO2022037631A1 (zh) 2020-08-21 2022-02-24 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
WO2022119748A1 (en) 2020-12-04 2022-06-09 Eli Lilly And Company Tricyclic kras g12c inhibitors
CN115611923A (zh) 2021-07-12 2023-01-17 贝达药业股份有限公司 Kras g12d抑制剂及其在医药上的应用
WO2023030517A1 (en) 2021-09-06 2023-03-09 Suzhou Zanrong Pharma Limited Kras g12c inhibitors and uses thereof
CN115785199A (zh) 2021-09-10 2023-03-14 润佳（苏州）医药科技有限公司 一种双官能化合物及其用途
WO2023183585A1 (en) 2022-03-25 2023-09-28 Eli Lilly And Company Kras inhibitors

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AU2024241889A1 (en) 2025-09-25
PE20252444A1 (es) 2025-10-20
IL323362A (en) 2025-11-01
WO2024206766A1 (en) 2024-10-03
CL2025002769A1 (es) 2025-11-07
CO2025013134A2 (es) 2025-10-09
KR20250163395A (ko) 2025-11-20
JOP20250246A1 (ar) 2025-09-28
US20240368193A1 (en) 2024-11-07
JP2024146897A (ja) 2024-10-15
DOP2025000245A (es) 2025-11-16
EP4688792A1 (en) 2026-02-11
MX2025011449A (es) 2025-11-03
TWI901059B (zh) 2025-10-11
TW202506688A (zh) 2025-02-16
JP2025111535A (ja) 2025-07-30
CN121002032A (zh) 2025-11-21
AR132295A1 (es) 2025-06-11

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