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1. WO2012110440 - 6 - CYCLOBUTYL - 1, 5 - DIHYDRO - PYRAZOLO [3, 4-D] PYRIMIDIN- 4 - ONE DERIVATIVES THEIR USE AS PDE9A INHIBITORS

Publication Number WO/2012/110440
Publication Date 23.08.2012
International Application No. PCT/EP2012/052378
International Filing Date 13.02.2012
IPC
C07D 487/04 2006.1
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 31/519 2006.1
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
519ortho- or peri-condensed with heterocyclic rings
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
CPC
A61K 31/519
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
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 15/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
08for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 21/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
Applicants
  • BOEHRINGER INGELHEIM INTERNATIONAL GMBH [DE]/[DE] (AllExceptUS)
  • HEINE, Niklas [DE]/[DE] (UsOnly)
  • GIOVANNINI, Riccardo [IT]/[IT] (UsOnly)
  • FERRARA, Marco [IT]/[IT] (UsOnly)
Inventors
  • HEINE, Niklas
  • GIOVANNINI, Riccardo
  • FERRARA, Marco
Agents
  • HAMMANN, Heinz
Priority Data
11154397.114.02.2011EP
PCT/EP2011/06370509.08.2011EP
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 6 - CYCLOBUTYL - 1, 5 - DIHYDRO - PYRAZOLO [3, 4-D] PYRIMIDIN- 4 - ONE DERIVATIVES THEIR USE AS PDE9A INHIBITORS
(FR) DÉRIVÉS DE 6 - CYCLOBUTYL - 1, 5 - DIHYDRO - PYRAZOLO [3, 4-D] PYRIMIDIN- 4 - ONE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE PDE9A
Abstract
(EN) The invention relates to novel pyrazolopyrimidinones according to formula (I), wherein R1 is a pyridyl or pyrimidinyl group and D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3-or 4-pyridyl. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.
(FR) La présente invention concerne de nouveaux pyrazolopyrimidinones de formule (I) dans laquelle R1 est un groupe pyridyle ou pyrimidinyle et D est cyclopentyle, cyclohexyle, tétrahydrofuranyle, tétrahydropyranyle ou 2-, 3-ou 4-pyridyle éventuellement substitué. Les nouveaux composés sont destinés à être utilisés en tant que principe actif de médicaments ou pour la fabrication de médicaments respectivement, en particulier des médicaments pour le traitement de conditions concernant des déficiences de perception, de concentration, d'apprentissage ou de mémoire. De telles conditions peuvent par exemple être associées à la maladie d'Alzheimer, la schizophrénie et d'autres maladies. Les nouveaux composés sont également utilisés par exemple pour la fabrication de médicaments et/ou pour le traitement de ces maladies, en particulier la détérioration cognitive associée à une telle maladie. Les composés selon l'invention présentent des propriétés inhibitrices de PDE9.
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