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1. WO2021220137 - PANNEXIN-1 INHIBITORS FOR THE TREATMENT OF SARS-COV-2 INFECTED COVID-19 PATIENTS WITH OR WITHOUT AN ASSOCIATED ACUTE RESPIRATORY SYNDROME

Publication Number WO/2021/220137
Publication Date 04.11.2021
International Application No. PCT/IB2021/053426
International Filing Date 26.04.2021
IPC
A61K 39/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
A61K 39/12 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
12Viral antigens
A61K 39/215 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
12Viral antigens
215Coronaviridae, e.g. avian infectious bronchitis virus
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
A61P 31/14 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
14for RNA viruses
C07H 21/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
04with deoxyribosyl as saccharide radical
CPC
A61K 31/195
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
A61K 31/353
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
352condensed with carbocyclic rings, e.g. cannabinols, methantheline
3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
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
Applicants
  • SAPIR PHARMACEUTICALS INC. [US]/[US]
Inventors
  • LECANU, Laurent
Priority Data
63/015,96027.04.2020US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PANNEXIN-1 INHIBITORS FOR THE TREATMENT OF SARS-COV-2 INFECTED COVID-19 PATIENTS WITH OR WITHOUT AN ASSOCIATED ACUTE RESPIRATORY SYNDROME
(FR) INHIBITEURS DE PANNEXINE-1 POUR LE TRAITEMENT DE LA COVID-19 DE PATIENTS INFECTÉS PAR LE SRAS-COV-2 AVEC OU SANS SYNDROME RESPIRATOIRE AIGU ASSOCIÉ
Abstract
(EN) The present invention relates to the use of probenecid and other pannexin-1 blockers for the treatment of novel coronavirus infection with or without an associated acute respiratory syndrome. Probenecid may be administered either alone or in combination with drugs interfering with the viral replication like, but not limited to, RNA-dependent RNA polymerase inhibitors or with the drugs interfering with the lung hyperinflammation like, but not limited to, IL-6 pathway inhibitors. In particular, the present invention includes the use of probenecid in combination with quercetin, a flavonoid described to reduce lung hyperinflammation, IL-6 production and bronchoconstriction. Further, the present relates to a pharmaceutical composition comprising a combination of an amount of a Pannexin-1 inhibitor with an additional polyphenol in an amount effective to treat a coronavirus infection in a human subject in combination with a pharmaceutically acceptable carrier, additive or excipient wherein the polyphenol includes Epigallocatechin gallate (EGCG).
(FR) La présente invention concerne l'utilisation de probénécide et d'autres bloqueurs de pannexine-1 pour le traitement d'une nouvelle infection à coronavirus avec ou sans syndrome respiratoire aigu associé. Le probénécide peut être administré seul ou en combinaison avec des médicaments interférant avec la réplication virale comme, mais sans s'y limiter, des inhibiteurs d'ARN polymérase dépendant de l'ARN ou avec les médicaments interférant avec une hyperinflammation pulmonaire comme, mais sans s'y limiter, des inhibiteurs de la voie IL-6. En particulier, la présente invention fait appel à l'utilisation de probénécide en combinaison avec de la quercétine, un flavonoïde décrit pour réduire l'hyperinflammation pulmonaire, la production d'IL-6 et la bronchoconstriction. En outre, la présente invention concerne une composition pharmaceutique comprenant une combinaison d'une quantité d'un inhibiteur de pannexine-1 avec un polyphénol supplémentaire en une quantité efficace pour traiter une infection à coronavirus chez un sujet humain en combinaison avec un véhicule, un additif ou un excipient pharmaceutiquement acceptables, le polyphénol comprenant du gallate d'épigallocatéchine (EGCG).
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