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1. WO2022129376 - 6-6 OR 5-6 FUSED BICYCLIC COMPOUNDS COMPRISING A PYRI(MI)DINE RING USEFUL IN THE|TREATMENT OF INFECTIOUS DISEASES

Publication Number WO/2022/129376
Publication Date 23.06.2022
International Application No. PCT/EP2021/086262
International Filing Date 16.12.2021
IPC
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 473/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
C07D 473/40 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
40with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 495/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 31/12 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
CPC
A61P 31/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
A61P 33/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
33Antiparasitic agents
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 473/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
C07D 473/40
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
40with halogen atoms or perhalogeno-alkyl radicals directly attached in positions 2 or 6
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) [FR]/[FR]
  • ECOLE POLYTECHNIQUE [FR]/[FR]
  • UNIVERSITE DE BORDEAUX [FR]/[FR]
  • INSTITUT PASTEUR [FR]/[FR]
  • CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE [FR]/[FR]
Inventors
  • CHIARAVALLI, Jeanne
  • GUILLON, Jean
  • LAVIGNE, Marc
  • MUNIER-LEHMANN, Hélène
  • MERGNY, Jean-Louis
  • MEYER, Björn
  • SAVRIMOUTOU, Solène
Agents
  • CABINET NONY
Priority Data
20306606.318.12.2020EP
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 6-6 OR 5-6 FUSED BICYCLIC COMPOUNDS COMPRISING A PYRI(MI)DINE RING USEFUL IN THE|TREATMENT OF INFECTIOUS DISEASES
(FR) COMPOSÉS BICYCLIQUES FUSIONNÉS EN 6-6 OU 5-6 COMPRENANT UN CYCLE PYRI(MI)DINE UTILES DANS LE TRAITEMENT DE MALADIES INFECTIEUSES
Abstract
(EN) The present invention relates to new specific 6-6 or 5-6 fused bicyclic compounds comprising pyrimidine or pyridine useful in the prevention and/or treatment of infectious diseases. In particular, the present invention relates to a compound of formula (I) wherein : Ar1 is a (C5-C11)arylene or (C5-C11)heteroarylene group, X is -CH-, -S-, -NR5 or -N-, Y is -CH-, -NR5 -S- or -NR6-CH2-, T is -CH- and Q is -CH- or T is -N- and Q is -CR10- or -N-, provided that one or two of X, Q and Y comprise a heteroatom, and with the proviso that, at least one of R1, R2, and, if present, R5 or R6, contains a group -NH-Alk-NR3R4. The inventors showed that compounds of formula (I) present an activity against both W2 and 3D7 Plasmodium falciparum strains, an activity against T. brucei brucei but also an activity against SARS-CoV-2 virus, and that they are positive for G4 recognition. The invention also relates to the preparation process and to the therapeutic uses of the compounds of formula (I).
(FR) La présente invention porte sur de nouveaux composés bicycliques fusionnés en 6-6 ou 5-6 spécifiques comprenant une pyrimidine ou une pyridine utiles dans la prévention et/ou le traitement de maladies infectieuses. En particulier, la présente invention porte sur un composé de formule (I) dans laquelle : Ar1 représente un groupe arylène (C5 à C11) ou hétéroarylène (C5 à C11), X représente -CH-, -S-, -NR5 ou -N-, Y représente -CH-, -NR5-S- ou -NR6-CH2-, T représente -CH- et Q représente -CH- ou T représente -N- et Q représente -CR10- ou -N-, à condition qu'un ou deux constituants parmi X, Q et Y comprennent un hétéroatome, et à condition que, au moins un constituant parmi R1, R2, et, si présent, R5 ou R6, contient un groupe -NH-Alk-NR3R4. Les inventeurs ont montré que les composés de formule (I) présentent une activité à la fois contre les souches W2 et 3D7 de Plasmodium falciparum, une activité contre T. brucei brucei mais également une activité contre le virus du SARS-CoV-2, et sont positifs pour la reconnaissance G4. L'invention porte également sur le procédé de préparation et sur les utilisations thérapeutiques des composés de formule (I).
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