| 摘要 |
PROBLEM TO BE SOLVED: To provide pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists.SOLUTION: Compositions of a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof comprises the therapeutically active compound, a non-ionic polymer and an ionic polymer, a binder and a filler, in either form of matrix pellets, matrix tablets or coating pellets to provide a pH independent, in vitro release profile of NMT 70% in 1 hour, NMT 85% in 4 hours, and NLT 80% in 8 hours. The composition is useful for treatment of CNS-related disorders including Treatment Resistant Depression (TRD) and Fragile-X syndrome. In Formula (I), one of A and D is N and the other is C; Ris halogen or cyano; Ris lower alcohol; Ris substituted/non-substituted aryl or heteroaryl; Ris CF, CF, C(O)H, or lower alkyl. |
