| 摘要 |
PURPOSE: Provided are new 6-amino- or 6-hydrazino-sulfonyl-3-quinolylphosphonic acid compounds and compositions containing them, which are useful as a therapeutic agent for the acute, and also chronic, treatment of neurological and psychological disorders involving those amino acids, for example degenerative disorders such as cerebrovascular accident, cerebral or spinal traumatism, epilepsy, chronic neurodegenerative diseases such as Alzheimer's disease, schizophrenia, lateral amyotrophic sclerosis or Huntington's chorea. CONSTITUTION: The compound is represented by the formula(I), wherein R1 represents halogen or trifluoromethyl, R2 represents hydrogen or alkyl or cycloalkyl, R3 represents alkyl, cycloalkyl, aryl, arylalkyl, alkoxy, aryloxy, arylalkoxy, hydroxy, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkylcarbonyl, arylcarbonyl or arylalkylcarbonyl or NHR6 (wherein R6 represents hydrogen or alkyl, cycloalkyl, aryl, alkylcarbonyl, arylcarbonyl, arylalkyl or arylalkylcarbonyl), or R2 and R3 together form with the nitrogen atom carrying them a ring having 5 or 6 carbon atoms, in which one of the carbon atoms can be replaced by oxygen, nitrogen or sulphur or by SO, SO2 or NRa (wherein Ra represents hydrogen or alkyl, cycloalkyl, aryl or arylalkyl), R4 and R5, which may be identical or different, represent hydrogen or alkyl, cycloalkyl, aryl or arylalkyl or a group of formula (wherein R7 and R8, which may be identical or different, represent hydrogen or alkyl, cycloalkyl or aryl), it being understood that: alkyl is understood to mean a linear or branched alkyl group containing from 1 to 6 carbon atoms, alkoxy is understood to mean a linear or branched alkoxy group containing from 1 to 6 carbon atoms, cycloalkyl is understood to mean a cyclic alkyl group containing from 3 to 8 carbon atoms, aryl is understood to mean the groups phenyl or naphthyl, it being possible for those groups to be unsubstituted or substituted by from 1 to 3 groups selected from alkyl, cycloalkyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, polyhaloalkyl, SO2NR9R10 (wherein R9 and R10, which may be identical or different, represent a hydrogen atom or an alkyl, cycloalkyl or aryl group) and halogen atoms, their enantiomers and diastereoisomers and addition salts thereof with a pharmaceutically acceptable acid or base.
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