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1. WO2021204896 - MACROCYCLIC DIAMINE DERIVATIVES AS ENT INHIBITORS FOR THE TREATMENT OF CANCERS, AND COMBINATION THEREOF WITH ADENOSINE RECEPTOR ANTAGONISTS

Publication Number WO/2021/204896
Publication Date 14.10.2021
International Application No. PCT/EP2021/059096
International Filing Date 07.04.2021
IPC
C07D 491/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic 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/-C07D459/290
02in which the condensed system contains two hetero rings
08Bridged systems
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/551 2006.1
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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
Applicants
  • ITEOS BELGIUM SA [BE]/[BE]
Inventors
  • DELIGNY, Michael
  • CROSIGNANI, Stefano
  • HOUTHUYS, Erica Joke Katelijne Heleen
Agents
  • ICOSA
Priority Data
63/006,62907.04.2020US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MACROCYCLIC DIAMINE DERIVATIVES AS ENT INHIBITORS FOR THE TREATMENT OF CANCERS, AND COMBINATION THEREOF WITH ADENOSINE RECEPTOR ANTAGONISTS
(FR) DÉRIVÉS DE DIAMINE MACROCYCLIQUE SERVANT D'INHIBITEURS D'ENT POUR LE TRAITEMENT DE CANCERS, ET LEUR COMBINAISON AVEC DES ANTAGONISTES DU RÉCEPTEUR DE L'ADÉNOSINE
Abstract
(EN)
The present invention relates to macrocyclic diamine derivatives of formula II, including pharmaceutically acceptable salts and solvates thereof. Compounds of the invention are inhibitors of ENT family transporter, especially of ENT1, and are useful as therapeutic compounds for the treatment of cancers. The invention also relates to the combined use of the macrocyclic diamine derivatives with an adenosine receptor antagonist, for the treatment of cancers.
(FR)
La présente invention concerne des dérivés de diamine macrocyclique de formule II, comprenant des sels ou solvates pharmaceutiquement acceptables de ceux-ci. Les composés selon l'invention sont des inhibiteurs du transporteur de la famille des ENT, en particulier ENT1, et sont utiles en tant que composés thérapeutiques pour le traitement de cancers. L'invention concerne également l'utilisation combinée des dérivés de diamine macrocyclique avec un antagoniste du récepteur de l'adénosine, pour le traitement de cancers.
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