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1. WO2020089400 - PIPERAZINYL AND PIPERIDINYL QUINAZOLIN-4(3H)-ONE DERIVATIVES HAVING ACTIVITY AGAINST PAIN

Publication Number WO/2020/089400
Publication Date 07.05.2020
International Application No. PCT/EP2019/079846
International Filing Date 31.10.2019
IPC
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 403/06 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
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/14 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
14containing three or more hetero rings
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
A61K 31/517 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 401/14
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 403/06
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
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/14
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
14containing three or more hetero rings
Applicants
  • ESTEVE PHARMACEUTICALS, S.A. [ES]/[ES]
Inventors
  • FERNÁNDEZ-DONIS, Ariadna
  • DÍAZ-FERNÁNDEZ, Jose, Luís
  • ALMANSA-ROSALES, Carmen
  • LORENTE-CRIVILLÉ, Adriana
Agents
  • GONZALEZ PECES, Gustavo Adolfo
Priority Data
18382772.431.10.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PIPERAZINYL AND PIPERIDINYL QUINAZOLIN-4(3H)-ONE DERIVATIVES HAVING ACTIVITY AGAINST PAIN
(FR) DÉRIVÉS DE PIPÉRAZINYLE ET DE PIPÉRIDINYL QUINAZOLIN-4 (3H)-ONE AYANT UNE ACTIVITÉ CONTRE LA DOULEUR
Abstract
(EN)
The present invention relates to piperazinyl and piperidinyl quinazolin-4(3H)-one derivatives having pharmacological activity towards the (formula (I)) subunit, in particular the (formula (2)) subunit, of the voltage-gated calcium channel, in particular having dual pharmacological activity towards both the (formula (I)) subunit, in particular the (formula (2)) subunit, of the voltage-gated calcium channel and the µ-opioid receptor. The present invention also relates to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
(FR)
La présente invention concerne des dérivés de pipérazinyle et de pipéridinyl quinazolin-4(3H)-one ayant une activité pharmacologique vis-à-vis de la sous-unité de (formule (I)), en particulier la sous-unité de (formule (2)), du canal calcique dépendant de la tension, en particulier ayant une double activité pharmacologique vis-à-vis de la sous-unité de (formule (I)), en particulier la sous-unité de (formule (2)), du canal calcique dépendant de la tension et à la fois du récepteur μ-opioïde. La présente invention concerne en outre des procédés de préparation de ces composés, des compositions pharmaceutiques les comprenant, ainsi que leur utilisation thérapeutique, en particulier pour le traitement de la douleur.
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