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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
C07D 205/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
C07D 205/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
12condensed with carbocyclic rings or ring systems
C07D 211/62
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
62attached in position 4
C07D 265/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
265Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
021,2-Oxazines; Hydrogenated 1,2-oxazines
C07D 271/113
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
271Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02not condensed with other rings
101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
113with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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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