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1. WO2013000924 - 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES

Publication Number WO/2013/000924
Publication Date 03.01.2013
International Application No. PCT/EP2012/062381
International Filing Date 26.06.2012
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/4985 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
4985Pyrazines or piperazines ortho- or peri-condensed with 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
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
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
A61K 51/0463
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
041Heterocyclic compounds
044having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
0463having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
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
Applicants
  • JANSSEN PHARMACEUTICA NV [BE]/[BE] (AllExceptUS)
  • ANDRÉS-GIL, José, Ignacio [ES]/[ES] (UsOnly)
  • ROMBOUTS, Frederik, Jan, Rita [BE]/[BE] (UsOnly)
  • TRABANCO-SUÁREZ, Andrés, Avelino [ES]/[ES] (UsOnly)
  • VANHOOF, Greta, Constantia, Peter [BE]/[BE] (UsOnly)
  • DE ANGELIS, Meri [IT]/[DE] (UsOnly)
  • BUIJNSTERS, Peter, Jacobus, Johannes, Antonius [NL]/[NL] (UsOnly)
  • GUILLEMONT, Jerôme, Emile, Georges [FR]/[FR] (UsOnly)
  • BORMANS, Guy, Maurits R. [BE]/[BE] (UsOnly)
  • CELEN, Sofie, Jeanne, Leopoldine [BE]/[BE] (UsOnly)
  • VLIEGEN, Maarten [BE]/[BE] (UsOnly)
Inventors
  • ANDRÉS-GIL, José, Ignacio
  • ROMBOUTS, Frederik, Jan, Rita
  • TRABANCO-SUÁREZ, Andrés, Avelino
  • VANHOOF, Greta, Constantia, Peter
  • DE ANGELIS, Meri
  • BUIJNSTERS, Peter, Jacobus, Johannes, Antonius
  • GUILLEMONT, Jerôme, Emile, Georges
  • BORMANS, Guy, Maurits R.
  • CELEN, Sofie, Jeanne, Leopoldine
  • VLIEGEN, Maarten
Common Representative
  • JANSSEN PHARMACEUTICA NV
Priority Data
11171519.927.06.2011EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES
(FR) DÉRIVÉS DE 1-ARYL-4-MÉTHYL-[1,2,4]TRIAZOLO[4,3-A]QUINOXALINE
Abstract
(EN)
The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
(FR)
La présente invention concerne de nouveaux dérivés de 1-aryl-4-méthyl-[1,2,4]triazolo[4,3-a]-quinoxaline comme inhibiteurs de phosphodiestérase 2 (PDE2) et dans une moindre mesure de phosphodiestérase 10 (PDE10) ou comme inhibiteurs des deux phosphodiestérases, 2 et 10. L'invention concerne également des compositions pharmaceutiques comprenant de tels composés, des procédés pour préparer de tels composés et de telles compositions et l'utilisation de tels composés et de telles compositions pour la prévention et le traitement de troubles dans lesquels la PDE2 est impliquée ou de troubles dans lesquels à la fois la PDE2 et la PDE10 sont impliquées, tels des troubles neurologiques et psychiatriques, et des maladies endocrines ou métaboliques. La présente invention concerne également des composés radiomarqués qui peuvent être utiles en imagerie et pour la quantification de l'enzyme PDE2 dans des tissus, à l'aide de la tomographie par émission de positons (TEP). L'invention concerne également : des compositions comprenant de tels composés; des procédés pour préparer de tels composés et de telles compositions; l'utilisation de tels composés et de telles compositions pour l'imagerie d'un tissu, de cellules ou d'un hôte, in vitro ou in vivo; et des précurseurs desdits composés.
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