EP4746874A2 - Kleinmolekülige proteinabbauer einer kras-g12d-mutante - Google Patents

Kleinmolekülige proteinabbauer einer kras-g12d-mutante

Info

Publication number
EP4746874A2
EP4746874A2 EP24844046.3A EP24844046A EP4746874A2 EP 4746874 A2 EP4746874 A2 EP 4746874A2 EP 24844046 A EP24844046 A EP 24844046A EP 4746874 A2 EP4746874 A2 EP 4746874A2
Authority
EP
European Patent Office
Prior art keywords
methyl
compound
pharmaceutically acceptable
acceptable salt
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.)
Pending
Application number
EP24844046.3A
Other languages
English (en)
French (fr)
Inventor
Charles S. Yeung
Thomas Bara
Raphaelle BERGER
Qingmei Hong
Ping LAN
Remond Moningka
Yuping Zhu
Anandan Palani
Toshihiro Sakamoto
Takao Uno
Patrick SCHÖPF
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.)
Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp & Dohme LLC
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 Merck Sharp & Dohme LLC filed Critical Merck Sharp & Dohme LLC
Publication of EP4746874A2 publication Critical patent/EP4746874A2/de
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP24844046.3A 2023-07-20 2024-07-19 Kleinmolekülige proteinabbauer einer kras-g12d-mutante Pending EP4746874A2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202363527954P 2023-07-20 2023-07-20
PCT/US2024/038853 WO2025019819A2 (en) 2023-07-20 2024-07-19 Small molecule protein degraders of kras g12d mutant

Publications (1)

Publication Number Publication Date
EP4746874A2 true EP4746874A2 (de) 2026-05-27

Family

ID=94282702

Family Applications (1)

Application Number Title Priority Date Filing Date
EP24844046.3A Pending EP4746874A2 (de) 2023-07-20 2024-07-19 Kleinmolekülige proteinabbauer einer kras-g12d-mutante

Country Status (2)

Country Link
EP (1) EP4746874A2 (de)
WO (1) WO2025019819A2 (de)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021085653A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
EP4067343A4 (de) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. Neuartige phenolverbindung oder salz davon
WO2021215544A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
WO2022109487A1 (en) 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant
KR20260096846A (ko) 2023-10-20 2026-06-24 머크 샤프 앤드 돔 엘엘씨 Kras 단백질의 소분자 억제제

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11707452B2 (en) * 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
US20220370416A1 (en) * 2020-04-06 2022-11-24 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
US20240239788A1 (en) * 2021-04-16 2024-07-18 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12d mutant
US20260200925A1 (en) * 2021-11-24 2026-07-16 Merck Sharp & Dohme Llc Small molecule inhibitors of kras mutated proteins

Also Published As

Publication number Publication date
WO2025019819A3 (en) 2025-05-01
WO2025019819A2 (en) 2025-01-23

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