| 摘要 |
The pyrazolo[3,4-d]pyrimidine or pyrrolo[2,3-d]pyrimidine derivatives of formula I are used in the manufacture of a medicament to treat, prevent or inhibit a disorder selected from head trauma, spinal cord trauma, ischemic neuronal damage, excitotoxic neuronal damage, epilepsy, stroke, stress induced immune dysfunction, muscular spasm, Parkinson's disease, Huntington's disease, urinary incontinence, multi-infarct dementia, amyotrophic lateral sclerosis, chemical dependence and additions and hypoglycemia in mammals. In formula I: X is =N- or =CR6-; A is -NR1R2, -CR1R2R11, -C(=R2R12)R1, -NH-CR1R2R11, -O-CR1R2R11, -S-CR1R2R11, NHN-R1R2, -CR2R11NHR1, -CR2R11OR1, -CR2R11SR1 or -C(O)R2; R1 is H or optionally substituted alkyl, which may contain one or two double or triple bonds; R2 is optionally substituted alkyl, aryl, alkylene-aryl wherein the aryl is phenyl, naphthyl or a heteroaryl as defined in the specification, cycloalkyl or alkylene-cycloalkyl wherein one or two of the carbons of the cycloalkyl can be replaced by O, S or N-Z which may contain one or two double or triple bonds or R1 and R2 together with the atom to which they are attached may form an optionally saturated 3-8 membered ring wherein one or two or the carbons can be replaced by O, S or N-Z; R3 is H, alkyl, F, Cl, Br, I, OH, amino, -O-alkyl, -mono or di-alkylamino, thiol, -S(O)n-alkyl with n being 0 to 2 wherein the alkyl moieties may contain one or two double or triple bonds and may be substituted; R4 is H, alkyl, F, Cl, Br, I, alkoxy, formyl, mono or di-alkylamino, -S(O)n-alkyl with n being 0 to 2, cyano, OH, carboxy or amido wherein the alkyl moieties may be substituted; R5 is optionally substituted phenyl, naphthyl or a heteroaryl as defined in the specification, cycloalkyl or bicycloalkyl wherein one or two of the carbons of the cycloalkyl can be replaced by O, S or N-Z which may contain one or two double or triple bonds; R6 is H, alkyl, F, Cl, Br, I, OH, amino, -alkoxy, formyl, amino, -mono or di-alkylamino, -S(O)n-alkyl with n being 0 to 2, cyano, OH, carboxy or amido wherein the alkyl moieties may contain one or two double or triple bonds and may be substituted; R11 is H, OH, F, Cl, -COO-alkyl, cyano or -CO-alkyl and Z is H, alkyl, alkanoyl, phenyl or benzyl.
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