Pentanoic acid derivatives

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United States of America Patent

PATENT NO 6201021
SERIAL NO

08681482

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Abstract

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Formula (I) compounds: ##STR1## wherein R.sup.1 is alkyl substituted by fluorine(s); R.sup.2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR.sup.3 R.sup.4, in which R.sup.3, R.sup.4 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 R.sup.3 and R.sup.4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: ##STR2## wherein n is 0 or 1, R.sup.11 is hydrogen and chlorine, R.sup.5 is R.sup.7 --CH.sub.2 -- or R.sup.8, or R.sup.5 and R.sup.11, taken together is alkylidene; R.sup.6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR.sup.9 R.sup.10, in which R.sup.9, R.sup.10 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 R.sup.9 and R.sup.10, taken together is a saturated heterocyclic ring or amino acid residue, R.sup.7 is (i) F--(CH.sub.2)m-- or F.sub.3 C--CH.sub.2 --, (ii) alkyl subsstituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R.sup.8 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).

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Patent Owner(s)

Patent OwnerAddress
ONO PHARMACEUTICAL CO LTDOSAKA-SHI OSAKA 541-8526

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Kishimoto, Kazuo Osaka, JP 32 312
Ohno, Hiroyuki Osaka, JP 88 657
Ohuchida, Shuichi Osaka, JP 44 438
Tateishi, Narito Osaka, JP 9 34

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