Pentanoic acid derivatives

Details Pentanoic acid derivatives Pentanoic acid derivatives

C - Chemistry, Metallurgy

07

C

C07C 53/21 (2006.01) A61K 31/16 (2006.01) A61K 31/19 (2006.01) A61K 31/22 (2006.01) A61K 31/395 (2006.01) C07C 69/63 (2006.01) C07C 233/01 (2006.01) C07C 233/05 (2006.01) C07C 233/11 (2006.01) C07C 233/25 (2006.01) C07C 233/47 (2006.01) C07C 233/54 (2006.01) C07C 323/52 (2006.01) C07D 213/40 (2006.01) C07D 213/75 (2006.01) C07D 295/185 (2006.01)

Patent

CA 2124784

The compound of the formula (I) (see formula I) 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 substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together a saturated heterocyclic ring or amino acid residues; and non-toxic salts thereof and acid addition salts thereof. The compounds of the present invention of the formula (I) and the compounds of the formula (X): (see formula II) 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 a saturated heterocyclic ring or amino acid residues, 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 salts and acid addition salts thereof are useful for prevention and / or treatment for neurodegenerative disease (Alzheimer's disease etc.) and neuronal dysfunction by stroke or traumatic injury (Multiple sclerosis etc.) etc.

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