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1. WO2022072975 - COMPOSITIONS AND METHODS OF TREATMENT FOR SARS-COV-2 THROUGH PAPAIN PROTEASE INHIBITION

Publication Number WO/2022/072975
Publication Date 07.04.2022
International Application No. PCT/US2021/071439
International Filing Date 14.09.2021
IPC
A61K 31/445 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
C07D 213/02 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
C07D 409/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
A61K 31/445
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
C07D 213/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
C07D 409/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. [US]/[US]
Inventors
  • PEGAN, Scott
  • DURIE, Ian
  • FREITAS, Brendan
  • TRIPP, Ralph
  • CUMMINGS, Brian
  • CRICH, David
  • AHIADORME, Daniil
  • SUBEDI, Yagya
  • ONOBUN, Emmanuel
  • HILL, Jarvis
  • UPADHYAYA, Kapil
  • PIRRONE, Mike
  • BAGUL, Rahul
Agents
  • BUCKLEY, Ragan
Priority Data
63/086,13701.10.2020US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) COMPOSITIONS AND METHODS OF TREATMENT FOR SARS-COV-2 THROUGH PAPAIN PROTEASE INHIBITION
(FR) COMPOSITIONS ET MÉTHODES DE TRAITEMENT DU SRAS-COV-2 PAR INHIBITION DE PROTÉASE À PAPAÏNE
Abstract
(EN) In one aspect, the disclosure relates to viral papain protease inhibitors, methods of making the same, pharmaceutical compositions comprising the same, and methods of treating and/or preventing COVID-19 and other coronavirus diseases using the same. In one aspect, the papain protease inhibitors have a core or linker structure featuring at least one nitrogen atom and substituted or unsubstituted cycloalkyl, aromatic, or heteroaromatic groups on either side of the core structure. In another aspect the papain protease inhibitors are capable of ablating viral deubiquitination and/or deISGase activity. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
(FR) Selon un aspect, l'invention concerne des inhibiteurs de protéase à papaïne virale, leurs procédés de fabrication, des compositions pharmaceutiques les comprenant, et des méthodes de traitement et/ou de prévention de la COVID-19 et autres maladies à coronavirus en ayant recours à ceux-ci. Selon un aspect, les inhibiteurs de protéase à papaïne ont une structure de noyau ou de lieur caractérisant au moins un atome d'azote et des groupes cycloalkyle, aromatiques ou hétéroaromatiques substitués ou non substitués de chaque côté de la structure de noyau. Selon un autre aspect, les inhibiteurs de protéase à papaïne sont capables d'effectuer l'ablation de la désubiquitination virale et/ou de l'activité de la déISGase. Le présent abrégé est destiné à servir d'outil d'exploration à des fins de recherche dans ce domaine technique particulier et ne se limite pas à la présente invention.
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