Pentanoic acid derivatives

摘要

Formula (I) compounds: wherein R¹ is alkyl substituted by fluorine(s); R² is hydroxy, alkoxy, alkoxy substituted by phenyl, NR³R⁴, in which R³, R⁴ is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R³ and R⁴, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R¹¹ is hydrogen and chlorine, R⁵ is R⁷-CH₂- or R⁸, or R⁵ and R¹¹, taken together is alkylidene; R⁶ is hydroxy, alkoxy, alkoxy substituted by phenyl, NR⁹R¹⁰, in which R⁹, R¹⁰ is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R⁹ and R¹⁰, taken together is a saturated heterocyclic ring or amino acid residue, R⁷ is (i) F-(CH₂)m- or F₃C-CH₂-, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R⁸ is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).