KR20250093430A - Kras 억제제 - Google Patents

Kras 억제제 Download PDF

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Publication number
KR20250093430A
KR20250093430A KR1020257020079A KR20257020079A KR20250093430A KR 20250093430 A KR20250093430 A KR 20250093430A KR 1020257020079 A KR1020257020079 A KR 1020257020079A KR 20257020079 A KR20257020079 A KR 20257020079A KR 20250093430 A KR20250093430 A KR 20250093430A
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KR
South Korea
Prior art keywords
cancer
kras
mmol
fluoro
mutant
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.)
Pending
Application number
KR1020257020079A
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English (en)
Korean (ko)
Inventor
데이비드 앤서니 바르다
졸리 앤 바스티안
켈리 웨인 퍼네스
데키 구오
제임스 로버트 헨리
리차드 듀엔 존스턴
제이슨 에릭 라마르
타오 리우
마이클 존 로드리게즈
알무데나 루비오
총 시
가이잉 자오
모하메드 사데그 지아-에브라히미
메튜 패트릭 바움가르트너
이자벨 로조
마리오 바르베리스
산티아고 카르발라레스 마틴
파블로 가르시아 로사다
소니아 마리아 구티에레즈 산펠리시아노
웬세슬라오 루메라스 아마도르
빅토리아노 몰레로 플로레즈
마리아 루르데스 프리에토 발레호
Original Assignee
일라이 릴리 앤드 캄파니
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 일라이 릴리 앤드 캄파니 filed Critical 일라이 릴리 앤드 캄파니
Publication of KR20250093430A publication Critical patent/KR20250093430A/ko
Pending legal-status Critical Current

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Classifications

    • 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020257020079A 2022-03-25 2023-03-24 Kras 억제제 Pending KR20250093430A (ko)

Applications Claiming Priority (8)

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
KR1020247035268A KR102847563B1 (ko) 2022-03-25 2023-03-24 Kras 억제제

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020247035268A Division KR102847563B1 (ko) 2022-03-25 2023-03-24 Kras 억제제

Publications (1)

Publication Number Publication Date
KR20250093430A true KR20250093430A (ko) 2025-06-24

Family

ID=86331239

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020257020079A Pending KR20250093430A (ko) 2022-03-25 2023-03-24 Kras 억제제
KR1020247035268A Active KR102847563B1 (ko) 2022-03-25 2023-03-24 Kras 억제제

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020247035268A Active KR102847563B1 (ko) 2022-03-25 2023-03-24 Kras 억제제

Country Status (16)

Country Link
US (2) US12351591B2 (cg-RX-API-DMAC7.html)
EP (1) EP4499233A1 (cg-RX-API-DMAC7.html)
JP (2) JP7676677B2 (cg-RX-API-DMAC7.html)
KR (2) KR20250093430A (cg-RX-API-DMAC7.html)
CN (1) CN119095853A (cg-RX-API-DMAC7.html)
AU (1) AU2023241055A1 (cg-RX-API-DMAC7.html)
CA (1) CA3246810A1 (cg-RX-API-DMAC7.html)
CL (1) CL2024002874A1 (cg-RX-API-DMAC7.html)
CO (1) CO2024012604A2 (cg-RX-API-DMAC7.html)
DO (1) DOP2024000186A (cg-RX-API-DMAC7.html)
IL (1) IL315782A (cg-RX-API-DMAC7.html)
JO (1) JOP20240210A1 (cg-RX-API-DMAC7.html)
MX (1) MX2024011631A (cg-RX-API-DMAC7.html)
PE (1) PE20251071A1 (cg-RX-API-DMAC7.html)
TW (2) TW202438502A (cg-RX-API-DMAC7.html)
WO (1) WO2023183585A1 (cg-RX-API-DMAC7.html)

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TW202430179A (zh) 2022-11-21 2024-08-01 美商樹線生物科學公司 螺環二氫哌喃并嘧啶ＫＲａｓ抑制劑
KR20250164300A (ko) * 2023-03-30 2025-11-24 일라이 릴리 앤드 캄파니 KRas 억제제
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
US20240368193A1 (en) * 2023-03-31 2024-11-07 Eli Lilly And Company Kras inhibitors
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
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025038936A1 (en) 2023-08-17 2025-02-20 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. 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
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
TW202535880A (zh) * 2023-10-30 2025-09-16 大陸商江蘇恆瑞醫藥股份有限公司 稠合雜芳基類化合物、其製備方法及其在醫藥上的應用
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
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
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
WO2026015790A1 (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
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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
WO2026075942A1 (en) * 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors
WO2026075945A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3030582A1 (en) 2015-07-22 2017-01-26 The Royal Institution For The Advancement Of Learning/Mcgill University Compounds and uses thereof in the treatment of cancers and other medical conditions
LT3710439T (lt) 2017-11-15 2023-05-10 Mirati Therapeutics, Inc. Kras g12c inhibitoriai
TW202033518A (zh) * 2018-10-15 2020-09-16 美商美國禮來大藥廠 Kras g12c 抑制劑
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
PT3886991T (pt) 2019-12-11 2022-10-17 Lilly Co Eli Inibidores de kras g12c
WO2021244603A1 (en) * 2020-06-04 2021-12-09 Shanghai Antengene Corporation 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
CA3191279A1 (en) 2020-08-28 2022-03-03 Yi Liu Heterocyclic compounds and uses thereof
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
JP2024510207A (ja) * 2021-03-12 2024-03-06 ブリストル－マイヤーズ スクイブ カンパニー Ｋｒａｓ阻害剤
WO2022261154A1 (en) * 2021-06-09 2022-12-15 Eli Lilly And Company Substituted fused azines as kras g12d inhibitors
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

Also Published As

Publication number Publication date
DOP2024000186A (es) 2024-10-31
JOP20240210A1 (ar) 2024-09-26
IL315782A (en) 2024-11-01
CO2024012604A2 (es) 2024-12-09
KR102847563B1 (ko) 2025-08-20
KR20240160650A (ko) 2024-11-11
US20240043451A1 (en) 2024-02-08
US12351591B2 (en) 2025-07-08
PE20251071A1 (es) 2025-04-10
TWI852436B (zh) 2024-08-11
CN119095853A (zh) 2024-12-06
MX2024011631A (es) 2024-09-30
CL2024002874A1 (es) 2024-12-20
JP2025118729A (ja) 2025-08-13
AU2023241055A1 (en) 2024-10-10
JP2025512811A (ja) 2025-04-22
US20250289830A1 (en) 2025-09-18
CA3246810A1 (en) 2023-09-28
TW202404572A (zh) 2024-02-01
WO2023183585A1 (en) 2023-09-28
TW202438502A (zh) 2024-10-01
JP7676677B2 (ja) 2025-05-14
EP4499233A1 (en) 2025-02-05

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Legal Events

Date Code Title Description
A107 Divisional application of patent
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20250617

Application number text: 1020247035268

Filing date: 20241023

PA0201 Request for examination
PG1501 Laying open of application