CN119095853A - Kras抑制剂 - Google Patents

Kras抑制剂 Download PDF

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Publication number
CN119095853A
CN119095853A CN202380030401.9A CN202380030401A CN119095853A CN 119095853 A CN119095853 A CN 119095853A CN 202380030401 A CN202380030401 A CN 202380030401A CN 119095853 A CN119095853 A CN 119095853A
Authority
CN
China
Prior art keywords
cancer
pharmaceutically acceptable
alkyl
acceptable salt
kras
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
CN202380030401.9A
Other languages
English (en)
Chinese (zh)
Inventor
D·A·鲍尔达
J·A·巴斯蒂安
K·W·弗内斯
郭德其
J·R·亨利
R·D·约翰斯顿
J·E·拉马尔
刘韬
M·J·罗德里格斯
A·鲁比奥
斯翀
赵改英
M·S·齐亚-埃布拉希米
M·P·鲍姆加特纳
I·罗约
M·巴尔贝里斯
S·卡拉利亚斯马丁
P·加西亚洛萨达
S·M·古铁雷斯桑费利西亚诺
W·卢默拉斯阿马多
V·莫雷罗弗洛雷斯
M·L·普列托瓦列霍
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN119095853A publication Critical patent/CN119095853A/zh
Pending legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically 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)
CN202380030401.9A 2022-03-25 2023-03-24 Kras抑制剂 Pending CN119095853A (zh)

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

Publications (1)

Publication Number Publication Date
CN119095853A true CN119095853A (zh) 2024-12-06

Family

ID=86331239

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202380030401.9A Pending CN119095853A (zh) 2022-03-25 2023-03-24 Kras抑制剂

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=)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP7676677B2 (ja) 2025-05-14
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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