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1. WO2017220799 - COMPOUNDS FOR TREATING DISORDERS SENSITIVE TO SEROTONINERGIC REGULATION CONTROLLED BY THE 5-HT1A RECEPTORS

Publication Number WO/2017/220799
Publication Date 28.12.2017
International Application No. PCT/EP2017/065585
International Filing Date 23.06.2017
IPC
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 405/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 211/38 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with 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
38Halogen atoms or nitro radicals
A61K 31/44 2006.01
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
A61K 31/4427 2006.01
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
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 25/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
22Anxiolytics
A61P 25/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
24Antidepressants
C07D 211/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with 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
38Halogen atoms or nitro radicals
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
Applicants
  • NEUROLIXIS [FR]/[FR]
  • UNIVERSITE JAGELLONNE [PL]/[PL]
Inventors
  • SNIECIKOWSKA, Joanna
  • BUCKI, Adam
  • NEWMAN-TANCREDI, Adrian
  • VARNEY, Mark Andrew
Agents
  • REGIMBEAU
Priority Data
16305769.824.06.2016EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS FOR TREATING DISORDERS SENSITIVE TO SEROTONINERGIC REGULATION CONTROLLED BY THE 5-HT1A RECEPTORS
(FR) COMPOSÉS POUR LE TRAITEMENT DE TROUBLES SENSIBLES À LA RÉGULATION SÉROTONINERGIQUE RÉGULÉE PAR LES RÉCEPTEURS 5-HT1A
Abstract
(EN)
The invention concerns compounds that possess a high affinity at 5-HT 1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.
(FR)
L'invention concerne des composés qui possèdent une affinité élevée pour les récepteurs 5-HT1A et une efficacité agoniste, telle que mesurée par des valeurs Emax provenant d'un essai d'activation cellulaire, qui est supérieure à celle des composés décrits dans l'état de la technique. L'aptitude des composés de l'invention à activer un complexe de protéines effectrices est supérieure à celle de l'agoniste le plus efficace décrit dans l'état de la technique. Les composés de l'invention présentent également une sélectivité exceptionnellement élevée (rapport Ki supérieur à 1000 fois) par rapport, en particulier, aux récepteurs D2 de la dopamine et aux récepteurs adrénergiques du sous-type alpha1. Cette sélectivité constitue un avantage important étant donné qu'elle signifie que les composés éviteront l'induction d'effets (centraux et périphériques) associés à l'activation ou à l'inhibition de ces récepteurs
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