| 摘要 |
Naphth(1,8-de)-2,3-dihydro-1,2-thiazine derivatives of formula (I) and their enantiomers, diastereomers and salts are disclosed, wherein: R1 can be H, C1-C6 alkyl (optionally substituted by 1 or more halogen atoms), SO2H, C1-C6 alkyl-sulfinyl or -sulfonyl, C1-C6 alkylcarbonyl, O, C1-C4 alkyl substituted by phenyl, NR6R7 or C1-C4 alkoxy, or 3-6C cycloalkyl; R2, R3 (independently) may be H, C1-C6 alkyl (optionally substituted by 1 or more halo), halo, SO2H, C1-C6 alkyl-sulfinyl or -sulfonyl, C1-C6 alkylcarbonyl, OH, C1-C6 alkoxy or alkylthio, C1-C4 alkyl substituted NR<6>R<7> or C1-C4 alkoxy, or 3-6C cycloalkyl; or R1 and R2 together are a C4-C6 alkylene bridge; R6, R7 are independently selected from H, C1-C4 alkyl or C1-C4 alkylcarbonyl; R4, R5 are independently selected from C1-C6 alkyl (optionally substituted with 1 or more halo), phenyl(C1-C4)alkyl, halo, CN, NO2, SO2H, SO3H, C1-C6 alkyl-sulfinyl, C1-C6 alkyl-sulfonyl, SO2NR6R7, carboxy, C1-C6 alkylcarbonyl, C1-C4 alkylcarbonyloxy, C1-C4 alkocycarbonyl, C1-C4 alkoxycarbonyloxy, CON R6R7, OH, C1-C6 alkoxy, C1-C6 alkylthio, NR6R7, or aryl (optionally substituted by one or more halo, NO2, SO2H or C1-C4 alkyl); and N and m are independently 0-3; provided that naptho(1,8-de)-2,3-dihydro-1,2-thiazine-1,1-dioxide is excluded. Such compositions are useful as pharmaceuticals, particularly for the treatment of neurodegenerative diseases and/or cerebral ischemia, such as schizophrenia, memory disorders and dementias.
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