| 摘要 |
<p>The invention is concerned with novel quinoline derivatives having cardiovascular activities of formula 1 <IMAGE> 1 in which A-B is -CH2-CH2-, -CHOH-CH2, -CH2-CHOH-, -C(O)-CH2-, -CH2-C(O)-, -C(NOR5)-CH2- or -CH2-C(NOR5)-; R1 is hydrogen, hydroxy or lower alkoxy; R2 is lower alkyl, hydroxy, lower alkoxy or CF3; R3 is ethyl or vinyl; R4 is C1-9 alkyl, C2-9 hydroxyalkyl or lower alkoxyalkyl, C5-6 cycloalkyl, C3-6 cycloalkyl lower alkyl, cyano lower alkyl, lower alkenyl, lower alkynyl, tetrahydrofurfuryl, mono- or di-lower alkylamino lower alkyl; mono- or di-lower alkylamino lower hydroxyalkyl; phenyl C1-4 alkyl, phenyl C1-4 hydroxy-alkyl, diphenyl C1-4 alkyl, benzoyl C1-4 alkyl, furyl C1-4 alkyl, thienyl C1-4 alkyl, furoyl C1-4 alkyl or thienoyl C1-4 alkyl, which groups may be optionally substituted in the aromatic nucleus, and R5 is lower alkyl, whereby the substituents at the 3- and 4-positions of the piperidine ring are in the cis-position. The compounds of the formula may be in the form of their optically active enantiomers and/or their therapeutically acceptable salts. Furthermore the invention provides pharmaceutical compositions possessing cardiovascular activities, in which as active compound at least a compound of the above formula is used. Methods for the preparation of the pharmaceutical compositions and of the active compounds are also disclosed and covered by the invention.</p> |
