| 摘要 |
Compounds of the given formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, -OR1, C1-C6 alkyl optionally substituted with up to three groups selected independently from halogen and hydroxy, or -NR2R3; or X is phenyl, naphthyl, 1-(5,6,7,8-tetrahydro)naphthyl or 4-(1, 2-dihydro) indenyl, pyridinyl, pyrimidyl, isoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, benzofuranyl, or benzothienyl, each of which is optionally substituted with up to three groups selected from halogen, C1-C6 alkyl, C1-C4 alkoxy, C1-C6 alkylthio, hydroxy, amino, mono or di(C1-C6)alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; or X represents a carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen, where the X carbocyclic group is optionally substituted with one or more groups selected from halogen, C1-C6 alkoxy, mono- or di (C1-C6)alkylamino, sulfonamide, aza (C3-C7) cycloalkyl, C3-C7 cycloalkylthio, C1-C6 alkylthio, phenylthio, or a heterocyclic group; Y is lower alkyl having 1-8 carbon atoms optionally substituted with up to two groups selected from halogen, C3-C7 cycloalkyl, C1-C6 alkoxy, mono- or di(C1-C6)alkylamino, sulfonamide, aza(C3-C7)cycloalkyl, C3-C7cycloalkylthio, C1-C6 alkylthio, phenylthio, a heterocyclic group, -OR4,-NR5R6, SR7, or optionally substituted aryl; or Y is a carbocyclic group having from 3-7 members atoms, where up to three of which members are optionally hetero atoms selected from oxygen and nitrogen and where any member of the Y carbocyclic group is optionally substituted with halogen, -OR4,-NR5R6, SR7, aryl or a heterocyclic group; R1 is hydrogen, lower alkyl having 1-6 carbon atoms, or cycloalkyl having 3-7 carbon atoms, where each alkyl may be optionally substituted with -OR4, or -NR5R6; R2 and R3 are the same or different and represent hydrogen, lower alkyl optionally mono- or di substituted with alkoxy, aryl, halogen, or mono- or di-lower alkyl; aryl or aryl(C1-C6)alkyl where each aryl is optionally substituted with up to three groups selected from halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, or mono or di(C1-C6)alkylamino; cycloalkyl having 3-7 carbon atoms optionally mono or disubstituted with halogen, alkoxy, or mono- or di lower alkyl; or -SO2R8; R4 is as defined for R1; R5 and R6 carry the same definitions as R2 and R3, respectively; R7 is hydrogen, lower alkyl having 1-6 carbon atoms, or cycloalkyl having 3-7 carbon atoms; and R8 is lower alkyl having 1-6 carbon atoms, cycloalkyl having 3-7 carbon atoms, or optionally substituted phenyl. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
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