Derivatives of (1-hydroxy-2-piperidylalkyl)-indol-2-ones,...

Details Derivatives of (1-hydroxy-2-piperidylalkyl)-indol-2-ones,... Derivatives of (1-hydroxy-2-piperidylalkyl)-indol-2-ones,...

C - Chemistry, Metallurgy

07

D

167/208, 260/254

C07D 401/10 (2006.01) C07D 401/06 (2006.01) C07D 401/14 (2006.01) C07D 491/107 (2006.01)

Patent

CA 1317292

- 38 - ABSTRACT "DERIVATIVES OF (1-HYDROXY-2-PIPERIDYLALKYL)-INDOL-2-ONES, 2-QUINOLINONES, 2-BENZO[B]AZAPINONES, BENZIMIDAZOL-2-ONES, AND QUINAZOLIN-2-ONES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS" A compound, in the form of a pure optical isomer or a mixture thereof, of formula (I): Image in which: Z represents a group of formula -CH2-, -C(CH3)2-, -CH=CH-, -(CH2)2-, -(CH2)3-, -NH- or -N(CH3)CH2-, in which the nitrogen is bonded to the carbonyl group; R1 represents hydrogen or a C1-C4 alkyl group; R2 represents hydrogen or a methyl group; and R3 represents: a phenoxy group which is unsubstituted or substituted by a halogen or a methyl group, a naphthyloxy group, a phenylmethyl group substituted by a halogen or a methyl group, - 39 - an unsubstituted phenylmethyl group when Z does not represent a group of formula -CH=CH- or -(CH2)2-, a bis (4-fluorophenyl)-methyl group, a phenylmethoxy group which is unsubstituted or substituted by a halogen or a methyl group, a (2-naphthyl)methoxy group, a phenoxymethyl group which is unsubstituted or substituted by a halogen or a methyl group, or a pyridinyloxy group, and R4 represents hydrogen; or R3 and R4 form, together and with the piperidine ring to which they are attached, a spiro (2,3-dihydrobenzofuran- 2,4'-piperid-1-yl) group; or a pharmacologically acceptable acid addition salt thereof. These compounds are useful for the treatment of a cerebral disorder, ischaemic attack, cardiac or respiratory arrest, cerebral thrombosis or embolism, cerebral trauma, cerebral senility, dementia following multiple infarcts, senile dementia, Alzheimer's disease, Pick's disease, tinnitus, cancer, schizophrenia or an olivopontocerebellar or other neurodegenerative ailment.

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