JOP20250246A1 - مثبطات kras - Google Patents

مثبطات kras

Info

Publication number
JOP20250246A1
JOP20250246A1 JOJO/P/2025/0246A JOP20250246A JOP20250246A1 JO P20250246 A1 JOP20250246 A1 JO P20250246A1 JO P20250246 A JOP20250246 A JO P20250246A JO P20250246 A1 JOP20250246 A1 JO P20250246A1
Authority
JO
Jordan
Prior art keywords
kras inhibitors
pharmaceutically acceptable
acceptable salts
kras
inhibitors
Prior art date
Application number
JOJO/P/2025/0246A
Other languages
Arabic (ar)
English (en)
Inventor
Sean Aronow
Steven Andrews
Garcia Alvaro Enriquez
Adedoyin David Abraham
Mario Barberis
Jolie Anne Bastian
Soler Julian Priego
Vallejo Maria Lourdes Prieto
Desta Bume
Matthew Patrick Baumgartner
Gaiying Zhao
Xiaohong Chen
Richard Duane Johnston
Andrew Dilger
Ramkumar Rajamani
Garcia Isabel Rojo
Cabezudo Juan Antonio Rincon
William Rush Scaggs
Sanz Miguel Garzón
Losada Pablo Garcia
Sanfeliciano Sonia Maria Gutierrez
Deqi Guo
De La Cruz Alberto Valero
Martin Santiago Carballares
Timothy Scott Kercher
Jason Eric Lamar
Cordier Frederic Laurent
Amador Wenceslao Lumeras
Llorente Alicia Marcos
Florez Victoriano Molero
Robert Hazlitt
James Robert Henry
Shane Michael Walls
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of JOP20250246A1 publication Critical patent/JOP20250246A1/ar

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • 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)
  • 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)
JOJO/P/2025/0246A 2023-03-31 2025-09-28 مثبطات kras JOP20250246A1 (ar)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP23382315 2023-03-31
EP23382531 2023-06-02
EP23382857 2023-08-18
EP23382985 2023-09-27
EP24382267 2024-03-12
PCT/US2024/022154 WO2024206766A1 (en) 2023-03-31 2024-03-29 Kras inhibitors

Publications (1)

Publication Number Publication Date
JOP20250246A1 true JOP20250246A1 (ar) 2025-09-28

Family

ID=90826251

Family Applications (1)

Application Number Title Priority Date Filing Date
JOJO/P/2025/0246A JOP20250246A1 (ar) 2023-03-31 2025-09-28 مثبطات kras

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

Family Cites Families (15)

* 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
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
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
TWI880049B (zh) 2020-12-04 2025-04-11 美商美國禮來大藥廠 Kras g12c抑制劑
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
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
CN117222654A (zh) 2021-09-06 2023-12-12 苏州赞荣医药科技有限公司 Kras g12c抑制剂和其用途
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
JP7676677B2 (ja) 2022-03-25 2025-05-14 イーライ リリー アンド カンパニー Kras阻害剤

Also Published As

Publication number Publication date
JP7669556B2 (ja) 2025-04-28
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
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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