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1. WO2021250648 - NITRILE-CONTAINING ANTIVIRAL COMPOUNDS

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Publication Number WO/2021/250648
Publication Date 16.12.2021
International Application No. PCT/IB2021/057281
International Filing Date 06.08.2021
IPC
C07D 207/267 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18having one double bond between ring members or between a ring member and a non-ring member
22with 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
24Oxygen or sulfur atoms
262-Pyrrolidones
263with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
267with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
C07D 403/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 403/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14containing three or more hetero rings
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
C07D 401/12 2006.1
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
C07D 497/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
497Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61K 31/401
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
401Proline; Derivatives thereof, e.g. captopril
A61K 31/403
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
A61K 31/427
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
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
C07D 207/267
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18having one double bond between ring members or between a ring member and a non-ring member
22with 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
24Oxygen or sulfur atoms
262-Pyrrolidones
263with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
267with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
Applicants
  • PFIZER INC. [US]/[US]
Inventors
  • OWEN, Dafydd Rhys
  • PETTERSSON, Martin Youngjin
  • REESE, Matthew Richard
  • SAMMONS, Matthew Forrest
  • TUTTLE, Jamison Bryce
  • VERHOEST, Patrick Robert
  • WEI, Liuqing
  • YANG, Qingyi
  • YANG, Xiaojing
Agents
  • ZIELINSKI, Bryan C.
Priority Data
63/073,98203.09.2020US
63/143,43529.01.2021US
63/170,15802.04.2021US
63/194,24128.05.2021US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) NITRILE-CONTAINING ANTIVIRAL COMPOUNDS
(FR) COMPOSÉS ANTIVIRAUX CONTENANT DU NITRILE
front page image
Abstract
(EN) The invention relates to compounds of Formula (I'') wherein R, R1, R2, R3, p, q and q' are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS- CoV-2 with the compounds.
(FR) L'invention concerne des composés de formule (I'') dans laquelle R, R1, R2, R3, p, q et q' sont tels que définis dans la description, des compositions pharmaceutiques comprenant les composés, des procédés de traitement d'une infection à coronavirus, telle que la COVID-19 chez un patient, par administration de quantités thérapeutiquement efficaces des composés, et des procédés d'inhibition ou de prévention de la réplication de coronavirus tels que le SARS-CoV-2 avec les composés.
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