Patent ID: 6806277
Filing Date: 2004-10-19
Classification: A61P,C07D

Abstract:
A quinolylpropylpiperidine derivative of general formula: in which:R1 is an amino, alkylamino, dialkylamino, hydroxyamino, alkyloxyamino, or alkyl(alkyloxy)amino radical, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is an alkyl radical having 1 to 6 carbon atoms substituted by a substituent selected from the group consisting of a.) a phenylthio radical which, itself, has up to 4 substituents selected from the group consisting of halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano and amino, b.) a cycloalkylthio radical, the cyclic part of which comprises 3 to 7 members, and c.) a 5- to 6-membered heteroarylthio radical comprising 1 to 4 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, oxo, carboxyl, alkyloxycarbonyl, cyano and amino; or, alternatively, R3 is a propargyl radical that is (a) substituted by a phenyl radical which is optionally substituted by 1 to 4 substituents selected from the group consisting of halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano and amino or (b) substituted by a cycloalkyl radical comprising 3 to 7 members or (c) substituted by a 5- to 6-membered heteroaryl radical comprising 1 to 4 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, said heteroaryl radical being optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, oxo, carboxyl, alkyloxycarbonyl, cyano and amino, and R4 is selected from the group consisting of an alkyl radical comprising 1 to 6 carbon atoms, an alkenyl-CH2â€” radical, the alkenyl portion of which comprises 2 to 6 carbon atoms, an alkynyl-CH2â€” radical, the alkynyl portion of which comprise 2 to 6 carbon atoms, a cycloalkyl radical, the cyclic portion of which comprises 3 to 8 members and a (cycloalkyl)alkyl radical, the cyclic portion of which comprises 3 to 8 members, said alkyl radicals being straight- or branched-chain radicals that, unless otherwise specified, comprise 1 to 4 carbon atoms, in its cis and trans forms and/or in its diastereoisomeric forms or their mixtures, and the pharmaceutically acceptable salts thereof.