Quinoline derivatives, pharmaceutical compositions containing su

Details Quinoline derivatives, pharmaceutical compositions containing su Quinoline derivatives, pharmaceutical compositions containing su

1981-03-05

1984-04-10

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

546156, 546157, 546168, 546174, 546176, 546177, A61K 3147, C07D40106

Patent

active

044421060

ABSTRACT:
The invention is concerned with novel quinoline derivatives having cardiovascular activities of formula 1 ##STR1## in which A--B is --CH.sub.2 --CH.sub.2 --, --CHOH--CH.sub.2, --CH.sub.2 --CHOH--, --C(O)--CH.sub.2 --, --CH.sub.2 --C(O)--, --C(NOR.sup.5)--CH.sub.2 -- or --CH.sub.2 --C(NOR.sup.5)--; R.sup.1 is hydrogen, hydroxy or lower alkoxy; R.sup.2 is lower alkyl, hydroxy, lower alkoxy or CF.sub.3 ; R.sup.3 is ethyl or vinyl; R.sup.4 is C.sub.1-9 alkyl, C.sub.2-9 hydroxyalkyl or lower alkoxyalkyl, C.sub.5-6 cycloalkyl, C.sub.3-6 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 C.sub.1-4 alkyl, phenyl C.sub.1-4 hydroxy-alkyl, diphenyl C.sub.1-4 alkyl, benzoyl C.sub.1-4 alkyl, furyl C.sub.1-4 alkyl, thienyl C.sub.1-4 alkyl, furoyl C.sub.1-4 alkyl or thienoyl C.sub.1-4 alkyl, which groups may be optionally substituted in the aromatic nucleus, and R.sup.5 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.

REFERENCES:
patent: 3914235 (1975-10-01), Gutzwiller et al.
patent: 3953453 (1976-04-01), Grethe et al.
patent: 4237139 (1980-12-01), Champseix et al.
patent: 4238612 (1980-12-01), Barieux et al.
patent: 4299835 (1981-11-01), Champseix et al.
patent: 4402961 (1983-09-01), Dubroeucq et al.
Grethe et al., Chemical Abstracts, vol. 83, 114,718j (1975).
Heidelberger et al., J. Am. Chem. Soc., vol. 44, pp. 1098-1107 (1922).
Wirth, Chemical Abstracts, vol. 76, 103776f (1972).
Wirth, Chemical Abstracts, vol. 80, 124762w (1974).
Dawes, British J. Pharmacol., 1, pp. 90-111 (1946).

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