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1. WO2022204777 - ANTIVIRAL COMPOUNDS, METHODS FOR THE MANUFACTURING OF COMPOUNDS, ANTIVIRAL PHARMACEUTICAL COMPOSITION, USE OF THE COMPOUNDS AND METHOD FOR THE ORAL TREATMENT OF CORONAVIRUS INFECTION AND RELATED DISEASES THEREOF

Publication Number WO/2022/204777
Publication Date 06.10.2022
International Application No. PCT/BR2022/050120
International Filing Date 01.04.2022
IPC
C07H 19/167 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
16Purine radicals
167with ribosyl as the saccharide radical
C07D 473/34 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
A61K 31/52 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
A61K 31/7076 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
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
CPC
A61K 31/52
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
A61K 31/7076
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
A61P 31/14
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
C07D 473/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
C07H 19/167
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
16Purine radicals
167with ribosyl as the saccharide radical
Applicants
  • CALIXTO, João Batista [BR]/[BR]
  • RABI NALLAR, Jaime Alberto [CL]/[BR]
  • LOPES E SOUZA, Thiago Moreno [BR]/[BR]
Inventors
  • CALIXTO, João Batista
  • RABI NALLAR, Jaime Alberto
  • LOPES E SOUZA, Thiago Moreno
Agents
  • FERREIRA EVANGELISTA, Katia Jane
  • CALABRIA MATTIOLI DANTAS, Paola
Priority Data
PCT/BR2021/05013601.04.2021BR
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) ANTIVIRAL COMPOUNDS, METHODS FOR THE MANUFACTURING OF COMPOUNDS, ANTIVIRAL PHARMACEUTICAL COMPOSITION, USE OF THE COMPOUNDS AND METHOD FOR THE ORAL TREATMENT OF CORONAVIRUS INFECTION AND RELATED DISEASES THEREOF
(FR) COMPOSÉS ANTIVIRAUX, PROCÉDÉS DE FABRICATION DES COMPOSÉS, COMPOSITION PHARMACEUTIQUE ANTIVIRALE, UTILISATION DES COMPOSÉS ET MÉTHODE DE TRAITEMENT PAR VOIE ORALE D'UNE INFECTION À CORONAVIRUS ET DE MALADIES ASSOCIÉES
Abstract
(EN) The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-CoV-2 and MHV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-CoV-2 and of patients with COVID-19, individual infected with SARS-CoV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-CoV-2 was greatly enhanced by inhibiting the 3'-5'-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.
(FR) La présente invention concerne des composés antiviraux choisis parmi les cytokinines, leurs analogues nucléosidiques et nucléotidiques, et leurs promédicaments en tant qu'inhibiteurs de la synthèse d'ARN viral, ou leurs sels, solvates, dérivés ou même combinaisons des composés susmentionnés, pour un traitement prophylactique, un traitement curatif (thérapeutique) ou un traitement atténuant une infection à coronavirus, représentée par le coronavirus humain et vétérinaire, le SARS-CoV-2 et le MHV, et pour le traitement d'individus potentiellement exposés à la COVID-19. La présente invention concerne également des procédés de fabrication de tels composés, une composition pharmaceutique antivirale contenant les composés selon l'invention, ainsi que l'utilisation des composés, des combinaisons de composés et une méthode pour le traitement prophylactique, curatif (thérapeutique) ou un traitement atténuant une infection à coronavirus, représentée par le coronavirus, en particulier le SARS-CoV-2 et des patients atteints de COVID-19, des individus infectés par le SARS-CoV-2 ou potentiellement exposés à ce virus. L'activité antivirale des composés selon la présente invention contre le SARS-CoV-2 a été améliorée de manière considérable par l'inhibition de l'exonucléase 3'-5'. Les résultats synergiques des composés selon la présente invention ont été obtenus à partir de la combinaison avec des médicaments réaffectés.
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