KR102847563B1 - Kras 억제제 - Google Patents

Kras 억제제

Info

Publication number
KR102847563B1
KR102847563B1 KR1020247035268A KR20247035268A KR102847563B1 KR 102847563 B1 KR102847563 B1 KR 102847563B1 KR 1020247035268 A KR1020247035268 A KR 1020247035268A KR 20247035268 A KR20247035268 A KR 20247035268A KR 102847563 B1 KR102847563 B1 KR 102847563B1
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KR
South Korea
Prior art keywords
alkyl
pharmaceutically acceptable
acceptable salt
cancer
mmol
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
KR1020247035268A
Other languages
English (en)
Korean (ko)
Other versions
KR20240160650A (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
Priority to KR1020257020079A priority Critical patent/KR20250093430A/ko
Publication of KR20240160650A publication Critical patent/KR20240160650A/ko
Application granted granted Critical
Publication of KR102847563B1 publication Critical patent/KR102847563B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
    • 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

Landscapes

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

Priority Applications (1)

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

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
KR1020257020079A Division KR20250093430A (ko) 2022-03-25 2023-03-24 Kras 억제제

Publications (2)

Publication Number Publication Date
KR20240160650A KR20240160650A (ko) 2024-11-11
KR102847563B1 true KR102847563B1 (ko) 2025-08-20

Family

ID=86331239

Family Applications (2)

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

Family Applications After (1)

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

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

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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
ES2929700T3 (es) 2019-12-11 2022-12-01 Lilly Co Eli Inhibidores de KRas g12c
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
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
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

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
JP7676677B2 (ja) 2025-05-14
JP2025118729A (ja) 2025-08-13
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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