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1. US20220306646 - Deuterated Angiotensin-Converting Enzyme-2 (ACE-2) Inhibitors

Office
United States of America
Application Number 17215468
Application Date 29.03.2021
Publication Number 20220306646
Publication Date 29.09.2022
Publication Kind A1
IPC
C07D 495/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 233/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
A61K 31/4706
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
47Quinolines; Isoquinolines
47064-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 317/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
317Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08having the hetero atoms in positions 1 and 3
44ortho- or peri-condensed with carbocyclic rings or ring systems
46condensed with one six-membered ring
48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
50with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
60Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
CPC
C07D 233/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 495/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/4706
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
47Quinolines; Isoquinolines
47064-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 317/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
317Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08having the hetero atoms in positions 1 and 3
44ortho- or peri-condensed with carbocyclic rings or ring systems
46condensed with one six-membered ring
48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes unsubstituted on the hetero ring
50with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
60Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07B 2200/05
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
05Isotopically modified compounds, e.g. labelled
Applicants Daljit Singh Dhanoa
Inventors Daljit Singh Dhanoa
Title
(EN) Deuterated Angiotensin-Converting Enzyme-2 (ACE-2) Inhibitors
Abstract
(EN)

The present invention is concerned with novel deuterated Angiotensin-Converting Enzyme-2 (ACE-2) inhibitors of general structural formula I, their optically active enantiomers and diastereoisomers, and pharmaceutical salts and compositions thereof, as well as combination therapies which include compounds of the present invention,

These compounds have high potency and selectivity for Angiotensin-Converting Enzyme-2 (ACE-2) inhibition, and are useful in the treatment of infectious respiratory diseases including the pandemic disease Covid-19, Severe Acute Respiratory Syndrome (SARS-CoV-2), Severe Acute Respiratory Syndrome (SARS-CoV), and other diseases caused by coronaviruses.