The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Apr. 10, 1984

Filed:

Mar. 05, 1981
Applicant:
Inventors:

Hans B Trijzelaar, Zeist, NL;

Ronus de Bode, Bilthoven, NL;

Hendricus B Welle, Maarssen, NL;

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K / ; C07D / ;
U.S. Cl.
CPC ...
424258 ; 546156 ; 546157 ; 546168 ; 546174 ; 546176 ; 546177 ;
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.


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