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1. WO2020108720 - NOVEL TETRAZINE COMPOUNDS FOR IN VIVO IMAGING

Publication Number WO/2020/108720
Publication Date 04.06.2020
International Application No. PCT/DK2019/050374
International Filing Date 29.11.2019
IPC
C07D 257/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
257Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
08Six-membered rings
A61K 51/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
C07D 401/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
A61K 31/395 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
CPC
A61K 51/044
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
041Heterocyclic compounds
044having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
A61K 51/0495
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0495Pretargeting
C07B 59/002
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59Introduction of isotopes of elements into organic compounds ; ; Labelled organic compounds per se
002Heterocyclic compounds
C07D 257/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
257Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
08Six-membered rings
C07D 401/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
Applicants
  • KØBENHAVNS UNIVERSITET [DK]/[DK]
  • RIGSHOSPITALET [DK]/[DK]
Inventors
  • KJÆR, Andreas
  • PETERSEN, Ida Nymann
  • HERTH, Matthias Manfred
  • KRISTENSEN, Jesper Langgard
Agents
  • CHAS. HUDE A/S
Priority Data
PA 2018 7079130.11.2018DK
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL TETRAZINE COMPOUNDS FOR IN VIVO IMAGING
(FR) NOUVEAUX COMPOSÉS DE TÉTRAZINE POUR L'IMAGERIE IN VIVO
Abstract
(EN)
The present invention relates to novel tetrazine compounds of formula I, wherein one of R1-R5 is 18F, for use in pretargeted in vivo imaging. The compounds are suitable for use in click chemistry, i.e. reactions that join a targeting molecule and a reporter molecule. The invention further relates to precursors to formula I, wherein one of R1-R5 is SnR3, B(OR)2, B(0H)2. Formula (I).
(FR)
La présente invention concerne de nouveaux composés de tétrazine de formule I, dans laquelle l'un de R1 à R5 est 18F, destiné à être utilisé dans une imagerie in vivo préciblée. Les composés sont appropriés pour une utilisation en chimie click, c'est-à-dire des réactions qui relient une molécule de ciblage et une molécule rapporteur. L'invention concerne en outre des précurseurs de formule I, dans laquelle l'un de R1 à R5 est SnR3, B(OR)2, B(0H)2. Formule (I).
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