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1. WO2020117075 - ARYLSULFONAMIDES OF 2-ARYLPYRROLE-3-CARBOXAMIDES FOR THE TREATMENT OF CNS DISORDERS

Publication Number WO/2020/117075
Publication Date 11.06.2020
International Application No. PCT/PL2018/050064
International Filing Date 06.12.2018
IPC
C07D 403/12 2006.01
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 401/14 2006.01
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 401/12 2006.01
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 409/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 471/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
18Bridged systems
A61P 25/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
CPC
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
C07D 401/12
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 401/14
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
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 C07D401/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 409/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 471/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
12in which the condensed system contains three hetero rings
18Bridged systems
Applicants
  • JAGIELLONIAN UNIVERSITY [PL]/[PL]
  • INSTITUTE OF PHARMACOLOGY POLISH ACADEMY OF SCIENCES [PL]/[PL]
  • THE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE [FR]/[FR]
  • THE UNIVERSITY OF MONTPELLIER [FR]/[FR]
  • INSERM TRANSFERT, SOCIÉTÉ ANONYME A DIRECTOIRE ET CONSEIL DE SURVEILLANCE [FR]/[FR]
  • THE UNIVERSITY OF CLERMONT AUVERGNE [FR]/[FR]
  • THE ECOLE NATIONALE SUPERIEURE DE CHIMIE DE MONTPELLIER [FR]/[FR]
Inventors
  • ZAJDEL, Paweł
  • DROP, Marcin
  • CANALE, Vittorio
  • PAWŁOWSKI, Maciej
  • SATAŁA, Grzegorz
  • BOJARSKI, Andrzej
  • SUBRA, Gilles
  • MARTINEZ, Jean
  • BANTREIL, Xavier
  • LAMATY, Fréderic
  • MARTIN, Pierre-Yves
  • COURTEIX, Christine
  • CHAUMONT-DUBEL, Séverine
  • MARIN, Philippe
Agents
  • WITEK, Rafał
Priority Data
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ARYLSULFONAMIDES OF 2-ARYLPYRROLE-3-CARBOXAMIDES FOR THE TREATMENT OF CNS DISORDERS
(FR) ARYLSULFONAMIDES DE 2-ARYLPYRROLE-3-CARBOXAMIDES POUR LE TRAITEMENT DE TROUBLES DU SNC
Abstract
(EN)
The inventions relates to novel arylsulfonamides of 2-aryl-2,5-dihydro-7H-pyrrole-3-carboxamide derivatives of general formula (I): A wherein: Ar represent 5-6 membered aromatic/heteroaromatic ring optionally substituted with halogen atoms, an alkyl group substituted with one or more halogen atoms, or C1-C2 alkoxy group; A represents unsubstituted aryl (5-6 membered), biaryl (8-10 membered), heteroaryl (5-6 membered), heteroaryl (8- 10 membered) having 1 or 2 heteroatoms independently selected from the group consisting of N or S, optionally substituted with one or more substituents selected from an alkyl (C1-C3) group, an alkyl (Ci- C3) group substituted with one or more halogen atoms, an alkoxy (C1-C3) group, an alkoxy (C1-C3) group substituted with one or more halogen atoms, cyano; Ri represents alicyclic amines selected from differently substituted azetidine, pyrrolidine, piperidine, azepine, tropane. Compounds of the invention display high affinity for the 5-HT6 receptors and affect receptor constitutive activity. Compounds of the invention are useful for the treatment of cognitive deficits related to neuropsychiatric disorders, dementia associated with neurodegenerative disorders, neuropathic pain, and/or other disorders where modification of the constitutive activity of the 5-HT6 receptor is preferable.
(FR)
L'invention concerne de nouveaux arylsulfonamides de dérivés de 2-aryl-2,5-dihydro-7H-pyrrole-3-carboxamide de formule générale (I) : dans laquelle : Ar représente un cycle aromatique/hétéroaromatique de 5 à 6 chaînons éventuellement substitué par des atomes d'halogène, un groupe alkyle substitué par un ou plusieurs atomes d'halogène, ou un groupe alcoxy en C1-C2 ; A représente un aryle non substitué (de 5 à 6 chaînons), un biaryle (de 8 à 10 chaînons), un hétéroaryle (de 5 à 6 chaînons), un hétéroaryle (de 8 à 10 chaînons) ayant 1 ou 2 hétéroatomes sélectionnés indépendamment dans le groupe constitué par N ou S, éventuellement substitué par un ou plusieurs substituants choisis parmi un groupe alkyle en (C1-C3), un groupe alkyle en (Ci-C3) substitué par un ou plusieurs atomes d'halogène, un groupe alcoxy en (C1-C3), un groupe alcoxy en (C1-C3) substitué par un ou plusieurs atomes d'halogène, cyano ; Ri représente des amines alicycliques sélectionnées parmi l'azétidine, pyrrolidine, pipéridine, azépine, tropane. Les composés selon l'invention présentent une affinité élevée pour les récepteurs 5-HT6 et affectent l'activité constitutive du récepteur. Les composés selon l'invention sont utiles pour le traitement de déficits cognitifs liés à des troubles neuropsychiatriques, la démence associée à des troubles neurodégénératifs, la douleur neuropathique et/ou d'autres troubles dont la modification de l'activité constitutive du récepteur 5-HT6 est préférable.
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