Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders. [electronic resource]
Producer: 20130226Description: 9045-54 p. digitalISSN:- 1520-4804
- 3',5'-Cyclic-AMP Phosphodiesterases -- antagonists & inhibitors
- Amyloid beta-Protein Precursor -- genetics
- Animals
- Brain -- metabolism
- Catalytic Domain
- Cognition Disorders -- drug therapy
- Crystallography, X-Ray
- Cyclic GMP -- metabolism
- Dogs
- Drug Design
- Hippocampus -- drug effects
- Humans
- Long-Term Potentiation -- drug effects
- Maze Learning -- drug effects
- Mice
- Mice, Transgenic
- Microsomes, Liver -- metabolism
- Models, Molecular
- Protein Conformation
- Pyrazoles -- chemical synthesis
- Pyrimidinones -- chemical synthesis
- Rats
- Stereoisomerism
- Structure-Activity Relationship
- Synapses -- drug effects
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Publication Type: Journal Article
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