| 摘要 |
Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function. The compound has one of following structures:Preferred compounds are ones wherein one of four substituents of R<1>, R<2>, R<3 >and R<4 >must be C1-C3-alkylthio group, the other substituents are independently H, R<11>O-, R<11>S-, halogen (F, Cl, Br), or C1-C3-alkyl; R<2 >and R<3 >taken together can be -SCH2S-, -SCH2O-, or -OCH2S-; R<7 >is R<13>R<14>NCO-, R<13>R<14>NCS-, R<13>R<14>N(CR<15>)-, R<15>OCO-, R<13>CO-, or H; R<8 >and R<9 >are independently H, H2N- or CH3CONH-; and pharmaceutically acceptable salts thereof.
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