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1. WO2022234271 - HETEROARYL COMPOUNDS USEFUL IN THE TREATMENT OF COGNITIVE DISORDERS

Publication Number WO/2022/234271
Publication Date 10.11.2022
International Application No. PCT/GB2022/051132
International Filing Date 04.05.2022
IPC
C07D 401/14 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
14containing three or more hetero rings
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 413/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61P 25/28 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07D 413/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 417/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14containing three or more hetero rings
CPC
A61K 31/4178
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
41641,3-Diazoles
4178not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4192
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
41921,2,3-Triazoles
A61K 31/422
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
42Oxazoles
422not condensed and containing further heterocyclic rings
A61K 31/4439
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
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/495
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
A61K 31/4985
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
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
Applicants
  • UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED [GB]/[GB]
Inventors
  • WARD, Simon
  • ATACK, John
  • ASHALL-KELLY, Alexander
  • BALDWIN, Alex
  • FOLEY, David
  • JONES, Heulyn
  • YU, Wai Leung
  • BRAND, Stephen
  • NATARAJAN, Srinivasan
Agents
  • HGF LIMITED
Priority Data
2106385.405.05.2021GB
2201949.115.02.2022GB
Publication Language English (en)
Filing Language English (en)
Designated States
Title
(EN) HETEROARYL COMPOUNDS USEFUL IN THE TREATMENT OF COGNITIVE DISORDERS
(FR) COMPOSÉS HÉTÉROARYLE POUVANT ÊTRE UTILISÉS DANS LE TRAITEMENT DE TROUBLES COGNITIFS
Abstract
(EN) The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salts thereof: wherein X1, X2, X3, R3, Ring A and Ring B are as described herein. The compounds have affinity for α5-subunit-containing GABAA receptors. The invention further provides the manufacture of the compounds of formula (I), pharmaceutical compositions comprising the compounds and their use as medicaments for the treatment of diseases and disorders associated with α5-GABAA receptors, including depression and cognitive impairment, for example, congintive impairment associated with a psychotic disorder such as schizophrenia.
(FR) La présente invention concerne des composés de formule (I), ainsi que des sels pharmaceutiquement acceptables de ces derniers, dans laquelle X1, X2, X3, R3, cycle A et cycle B sont tels que définis dans l’invention. Les composés présentent une affinité pour les récepteurs de GABAA contenant la sous-unité α5. L’invention porte en outre sur la fabrication des composés de formule (I), des compositions pharmaceutiques comprenant les composés et leur utilisation comme médicaments pour le traitement de maladies et de troubles associés aux récepteurs de α5-GABAA, y compris la dépression et le trouble cognitif, par exemple le trouble cognitif associé à un trouble psychotique tel que la schizophrénie.

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