EP4784573A2 - Agents de ciblage fap dimériques comprenant une structure de base (4-quinoinolyl)glycinyl-2-cyanopyrrolidine, un groupe de liaison 1,3,5-triazine ou -triazinane, et un agent thérapeutique ou diagnostique pour le diagnostic ou le traitement des tumeurs - Google Patents

Agents de ciblage fap dimériques comprenant une structure de base (4-quinoinolyl)glycinyl-2-cyanopyrrolidine, un groupe de liaison 1,3,5-triazine ou -triazinane, et un agent thérapeutique ou diagnostique pour le diagnostic ou le traitement des tumeurs

Info

Publication number
EP4784573A2
EP4784573A2 EP24777065.4A EP24777065A EP4784573A2 EP 4784573 A2 EP4784573 A2 EP 4784573A2 EP 24777065 A EP24777065 A EP 24777065A EP 4784573 A2 EP4784573 A2 EP 4784573A2
Authority
EP
European Patent Office
Prior art keywords
amino
acid
bis
efap
compound
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
EP24777065.4A
Other languages
German (de)
English (en)
Inventor
Yann SEIMBILLE
Hanyue MA
Le Li
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.)
Erasmus MC
Original Assignee
Erasmus MC
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
Priority claimed from PCT/NL2023/050491 external-priority patent/WO2024063648A1/fr
Application filed by Erasmus MC filed Critical Erasmus MC
Publication of EP4784573A2 publication Critical patent/EP4784573A2/fr
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/04—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
    • C07D251/54—Three nitrogen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des agents de ciblage de FAP dimère ayant un noyau central comprenant une fraction 1,3,5-triazine ou un 1,3,5-triazinane. En particulier, l'invention concerne un composé, ou un sel pharmaceutiquement acceptable de celui-ci comprenant un noyau 1,3,5-triazine ou un noyau 1,3,5-triazinane qui est relié à deux fractions de liaison FAP par l'intermédiaire de lieurs L1 et L2, et à une charge utile par l'intermédiaire du lieur L3. La charge utile peut être un radio-isotope, un colorant fluorescent, un médicament cytotoxique ou similaire.
EP24777065.4A 2023-09-21 2024-09-23 Agents de ciblage fap dimériques comprenant une structure de base (4-quinoinolyl)glycinyl-2-cyanopyrrolidine, un groupe de liaison 1,3,5-triazine ou -triazinane, et un agent thérapeutique ou diagnostique pour le diagnostic ou le traitement des tumeurs Pending EP4784573A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/NL2023/050491 WO2024063648A1 (fr) 2022-09-21 2023-09-21 Plateforme et échafaudage pour agents de ciblage de fap
EP24165351 2024-03-21
PCT/NL2024/050516 WO2025063849A2 (fr) 2023-09-21 2024-09-23 Agents de ciblage de fap dimère

Publications (1)

Publication Number Publication Date
EP4784573A2 true EP4784573A2 (fr) 2026-08-05

Family

ID=91248266

Family Applications (1)

Application Number Title Priority Date Filing Date
EP24777065.4A Pending EP4784573A2 (fr) 2023-09-21 2024-09-23 Agents de ciblage fap dimériques comprenant une structure de base (4-quinoinolyl)glycinyl-2-cyanopyrrolidine, un groupe de liaison 1,3,5-triazine ou -triazinane, et un agent thérapeutique ou diagnostique pour le diagnostic ou le traitement des tumeurs

Country Status (2)

Country Link
EP (1) EP4784573A2 (fr)
WO (1) WO2025063849A2 (fr)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011059586A2 (fr) * 2009-10-30 2011-05-19 The Regents Of The University Of Michigan Petites molécules multifonctionnelles
JP2021500373A (ja) 2017-10-23 2021-01-07 ザ・ジョンズ・ホプキンス・ユニバーシティ 線維芽細胞活性化タンパク質α(FAP−α)を標的とする撮像剤および放射線療法用薬剤
WO2019154859A1 (fr) 2018-02-06 2019-08-15 Universität Heidelberg Inhibiteur de fap
AU2019469641B2 (en) 2018-11-13 2025-04-03 Provincial Health Services Authority Radiolabeled bombesin-derived compounds for in vivo imaging of gastrin-releasing peptide receptor (GRPR) and treatment of GRPR-related disorders
PL3997103T3 (pl) 2019-07-08 2025-03-24 3B Pharmaceuticals Gmbh Związki zawierające ligand białka aktywującego fibroblasty i ich zastosowanie
KR20220154111A (ko) 2020-02-12 2022-11-21 필로켐 아게 표적 전달 적용들을 위한 섬유아세포 활성화 단백질 리간드들
DE102021114711B4 (de) * 2021-06-08 2023-11-02 Medianezia GmbH Trislinker-konjugierte dimere Markierungsvorläufer und daraus abgeleitete Radiotracer
EP4342890A1 (fr) * 2022-09-21 2024-03-27 Erasmus University Rotterdam Medical Center Plate-forme et échafaudage pour agents de ciblage fap

Also Published As

Publication number Publication date
WO2025063849A2 (fr) 2025-03-27
WO2025063849A3 (fr) 2025-05-08

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