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1. WO2020127059 - USE OF SULCONAZOLE AS A FURIN INHIBITOR

Publication Number WO/2020/127059
Publication Date 25.06.2020
International Application No. PCT/EP2019/085361
International Filing Date 16.12.2019
IPC
A61K 31/4174 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 45/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/28 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
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
A61K 31/4174
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
Applicants
  • INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) [FR]/[FR]
  • UNIVERSITÉ DE BORDEAUX [FR]/[FR]
  • INSTITUT BERGONIÉ [FR]/[FR]
Inventors
  • KHATIB, Abdel-Majid
  • TOME MONTESINOS, Maria Mercedes
  • SOULET, Fabienne
  • EVRARD, Serge
  • SIEGFRIED, Géraldine
  • VILLOUTREIX, Bruno
Agents
  • INSERM TRANSFERT
Priority Data
18306702.417.12.2018EP
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) USE OF SULCONAZOLE AS A FURIN INHIBITOR
(FR) UTILISATION DE SULCONAZOLE EN TANT QU'INHIBITEUR DE LA FURINE
Abstract
(EN) The proprotein convertases (PCs) are implicated in the activation of various precursor proteins that play a crucial role in various cancers. Using structure-based virtual screening and a compound collection containing FDA approved drugs; the inventors identified Sulconazole as a small molecule able to repress furin activity. Moreover, the inventor show that Sulconazole is particularly suitable for repressing the expression of immune checkpoint protein (e.g. PD-1). 10 Therefore, Sulconazole would be particularly suitable for the treatment of disease involving furin activity in particular for the treatment of cancers.
(FR) Les proprotéines convertases (PC) sont impliquées dans l'activation de diverses protéines précurseurs qui jouent un rôle crucial dans divers cancers. A l'aide d'un criblage virtuel basé sur une structure et une collection de composés contenant des médicaments approuvés par la FDA; les inventeurs ont identifié le Sulconazole en tant que petite molécule capable de réprimer l'activité de la furine. De plus, l'inventeur montre que le Sulconazole est particulièrement approprié pour réprimer l'expression d'une protéine de point de contrôle immunitaire (par exemple PD-1). Par conséquent, le Sulconazole serait particulièrement approprié pour le traitement d'une maladie mettant en jeu une activité furine en particulier pour le traitement de cancers.
Related patent documents
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