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US 10,538,525 B2Granted
1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones as PDE1 inhibitors
AssigneeH. Lundbeck A/S
InventorsKarsten Juhl, Mikkel Jessing, Morten Langgård, Paulo Jorge Vieira Vital, Mauro Marigo, Jan Kehler, Lars Kyhn Rasmussen
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Abstract
The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Claims15
A compound of formula (I):
- wherein:
- Y is N or CH;
- R1 is selected from the group consisting of linear or branched C2-C8 alkyl, saturated monocyclic C3-C8 cycloalkyl, oxetanyl, tetrahydrofuranyl and tetrathydropyranyl;
- all of which can be substituted one or more times with one or more substituents selected from the group consisting of methyl, fluorine, hydroxy, cyano and methoxy;
- R2 is:
- (a) selected from the group consisting of linear or branched C1-C8 alkyl, phenyl, benzo[1,3]dioxole and saturated monocyclic C3-C8 cycloalkyl;
- or
- (b) phenyl substituted one or more times with one or more substituents selected from the group consisting of halogen, C1-C3 alkyl and methoxy;
- or
- (c) pyridyl substituted with a substituent selected from the group consisting of halogen, C1-C3 alkyl, C1-C3 alkoxy, C1-C3 fluoroalkoxy, C3-C4 cycloalkoxy and C4-C5 methylcycloalkoxy;
- or
- (d) selected from the group consisting of 5-membered heteroaryls substituted with C1-C3 alkyl;
- and
- R3 is selected from the group consisting of linear or branched C1-C3 alkyl and saturated monocyclic C3-C8 cycloalkyl;
- which can each be optionally substituted with a substituent selected from halogen, C1-C3 alkoxy, phenyl, dialkylamine and oxetane;
- or a tautomer or pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.