| 摘要 |
PURPOSE: Benzothiazine and benzothiadiazine compounds, a preparation process thereof and pharmaceutical compositions containing the same are provided. The compounds have higher pharmacological activity on AMPA current than that of conventional compounds having similar structures, and are useful as AMPA modulators for treatment or prevention of the memory and recognition disorders associated with aging, the anxious or depressive syndromes, progressive neurodegenerative diseases, Alzheimer's disease, Pick's disease, Huntington's chorea, schizophrenia, after-effects of acute neurodegenerative diseases, after-effects of ischemia and after-effects of epilepsy. CONSTITUTION: The benzothiazine and benzothiadiazine compounds represented by the formula(I), enantiomers or partial stereoisomers thereof, or pharmaceutically acceptable addition salts with acid or base are provided, wherein R1 is hydrogen, halogen or linear or branched C1-C6 alkyl; R1a is hydrogen or linear or branched C1-C6 alkyl; R2 is hydrogen, halogen or hydroxy; A is CR4R5 group or NR4 group or is nitrogen and forms a N-containing ring with -CHR3- group in which m is 1, 2 or 3; R3 is hydrogen, linear or branched C1-C6 alkyl or C3-C7 cycloalkyl; R4 is hydrogen or linear or branched C1-C6 alkyl; R5 is hydrogen or halogen; X is NR6R7, S(O)nR8 or OR'8 or heterocyclic; R6 is hydrogen, linear or branched C1-C6 alkyl, S(O)pR9, COR9 or P(O)OR9OR10; R7 is hydrogen, or linear or branched C1-C6 alkyl; R6 and R7 form heterocyclic with nitrogen; R8, R9 and R10 are the same or different, and hydrogen, linear or branched C1-C6 alkyl optionally substituted with one or more halogen, aryl C1-C6 alkyl wherein aryl is linear or branched, or aryl; R'8 is linear or branched C1-C6 alkyl, or linear or branched C1-C6 acyl; and n and p is the same or different, and 1 or 2.
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