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1. WO2021205298 - COMPOUNDS AND METHODS FOR THE TREATMENT OF COVID-19

Publication Number WO/2021/205298
Publication Date 14.10.2021
International Application No. PCT/IB2021/052741
International Filing Date 01.04.2021
IPC
C07F 9/6558 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6558containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
A61K 31/662 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
662Phosphorus acids or esters thereof having P-C bonds, e.g. foscarnet, trichlorfon
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 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 47/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
08containing oxygen, ; e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
12Carboxylic acids; Salts or anhydrides thereof
A61K 47/26
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 9/19
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
19lyophilised ; , i.e. freeze-dried, solutions or dispersions
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
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
Applicants
  • PFIZER INC. [US]/[US]
Inventors
  • BEZAWADA, Padmavani
  • HAWKING, Emma Louise
  • HOFFMAN, Robert Louis
  • JAINI, Rohit
  • KANIA, Robert Steven
  • KULKARNI, Samir
  • LILLIS, Jonathan Richard
  • LUTHRA, Suman
  • O'BRIEN LARAMY, Matthew Nathan
  • OWEN, Dafydd Rhys
  • PENCHEVA, Klimentina Dimitrova
  • PETTERSSON, Martin Youngjin
  • RANE, Anil Mahadeo
  • SAMMONS, Matthew Forrest
  • SULLIVAN, Bradley Paul
  • THIEL, Andrew John
  • TICEHURST, Martyn David
  • TUTTLE, Jamison Bryce
Agents
  • ZIELINSKI, Bryan C.
Priority Data
63/005,40705.04.2020US
63/038,45412.06.2020US
63/061,62805.08.2020US
63/065,65814.08.2020US
63/073,14501.09.2020US
63/114,28916.11.2020US
63/163,63519.03.2021US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS AND METHODS FOR THE TREATMENT OF COVID-19
(FR) COMPOSÉS ET MÉTHODES DESTINÉS AU TRAITEMENT DE LA COVID-19
Abstract
(EN) The invention relates to compounds of formula I wherein R1, R2 and ----- are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.
(FR) L'invention concerne des composés de formule I, dans laquelle R1, R2 and ----- sont tels que définis dans la description, ainsi que des compositions pharmaceutiques les comprenant et des méthodes de traitement de la COVID-19 chez un patient, par administration de quantités thérapeutiquement efficaces desdits composés, ainsi que des méthodes destinées à inhiber ou à prévenir la réplication du SARS-CoV-2 au moyen desdits composés.
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