Ono Pharmaceutical Co., Ltd.

Kazuo Kishimoto

Shuichi Ohuchida

Hiroyuki Ohno

Narito Tateishi

Formula (I) compounds: wherein Ris alkyl substituted by fluorine(s); Ris hydroxy, alkoxy, alkoxy substituted by phenyl, NRR, in which R, Ris (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 Rand R, 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, Ris hydrogen and chlorine, Ris R&#x2014;CH&#x2014; or R, or Rand R, taken together is alkylidene; Ris hydroxy, alkoxy, alkoxy substituted by phenyl, NRR, in which R, Ris (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 Rand R, taken together is a saturated heterocyclic ring or amino acid residue, Ris (i) F&#x2014;(CH)m- or FC&#x2014;CH&#x2014;, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; Ris 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).

Pentanoic acid derivatives

Formula (I) compounds: wherein Ris alkyl substituted by fluorine(s); Ris hydroxy, alkoxy, alkoxy substituted by phenyl, NRR, in which R, Ris (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 Rand R, 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, Ris hydrogen and chlorine, Ris R&#x2014;CH&#x2014; or R, or Rand R, taken together is alkylidene; Ris hydroxy, alkoxy, alkoxy substituted by phenyl, NRR, in which R, Ris (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 Rand R, taken together is a saturated heterocyclic ring or amino acid residue, Ris (i) F&#x2014;(CH)m- or FC&#x2014;CH&#x2014;, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; Ris 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).

The compound of the formula (I): wherein Ris alkyl substituted by fluorine(s); The compounds of the present invention of the formula (I) and the compounds of the formula (X): wherein n is 0 or 1,

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Osaka, Japan

Kazuo Kishimoto