摘要 |
The present disclosure relates generally to the field of phosphodiesterase 10 (PDE10) enzyme inhibition by cinnoline compounds of Formulas: (I) and (II); wherein R'-R<SUP>3</SUP> and R<SUP>15</SUP>-R<SUP>18 </SUP>are as defined herein. Still further, the present invention provides methods for synthesizing compounds with such activity and selectivity, as well as methods of and corresponding pharmaceutical compositions for treating a patient, e.g., mammals, including humans, in need of PDE inhibition. Treatment is preferably for a disease state that involves elevated intracellular PDE10 levels or decreased cAMP and/or cGMP levels, e.g., involving neurological or psychiatric syndromes, especially those states associated with psychoses, most especially schizophrenia or bipolar disorder, obsessive-compulsive disorder, and/or Parkinson's disease. In particular, such psychoses, obsessive-compulsive disorder, and/or Parkinson's disease are due at least in part to catabolism of intracellular cAMP and/or cGMP levels by PDE10 enzymes or where such an impaired condition can be improved by increasing cAMP and/or cGMP levels.
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申请人 |
MEMORY PHARMACEUTICALS CORPORATION;ARRINGTON, MARK, PHILLIP;LIU, RUIPING;CONTICELLO, RICHARD, D.;GAUSS, CARLA, MARIA;HOPPER, ALLEN;NGUYEN, TRUC, MINH;TEHIM, ASHOK |
发明人 |
ARRINGTON, MARK, PHILLIP;LIU, RUIPING;CONTICELLO, RICHARD, D.;GAUSS, CARLA, MARIA;HOPPER, ALLEN;NGUYEN, TRUC, MINH;TEHIM, ASHOK |