TY - GEN AU - Verhoest,Patrick R AU - Fonseca,Kari R AU - Hou,Xinjun AU - Proulx-Lafrance,Caroline AU - Corman,Michael AU - Helal,Christopher J AU - Claffey,Michelle M AU - Tuttle,Jamison B AU - Coffman,Karen J AU - Liu,Shenpinq AU - Nelson,Frederick AU - Kleiman,Robin J AU - Menniti,Frank S AU - Schmidt,Christopher J AU - Vanase-Frawley,Michelle AU - Liras,Spiros TI - 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 SN - 1520-4804 PY - 2013///0226 KW - 3',5'-Cyclic-AMP Phosphodiesterases KW - antagonists & inhibitors KW - Amyloid beta-Protein Precursor KW - genetics KW - Animals KW - Brain KW - metabolism KW - Catalytic Domain KW - Cognition Disorders KW - drug therapy KW - Crystallography, X-Ray KW - Cyclic GMP KW - Dogs KW - Drug Design KW - Hippocampus KW - drug effects KW - Humans KW - Long-Term Potentiation KW - Maze Learning KW - Mice KW - Mice, Transgenic KW - Microsomes, Liver KW - Models, Molecular KW - Protein Conformation KW - Pyrazoles KW - chemical synthesis KW - Pyrimidinones KW - Rats KW - Stereoisomerism KW - Structure-Activity Relationship KW - Synapses N1 - Publication Type: Journal Article UR - https://doi.org/10.1021/jm3007799 ER -