C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/277.3
C07D 401/06 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01)
Patent
CA 1157473
ABSTRACT OF THE DISCLOSURE The invention provides quinicine and cinchonicine derivatives having cardiovascular activities of the formula Image or pharmaceutically acceptable salts thereof in which A-B is -CH2-CH2, -CHOH-CH2-, -CH2-CHOH-, -C(O)-CH2-, -CH2-C(O)-, -C(NOR4)-CH2- or -CH2-C(NOR4)-; R1 is hydrogen, hydroxy or lower alkoxy; R2 is ethyl or vinyl; R3 is C2-8 alkyl, C1-8 hydroxyalkyl, lower alkoxy-alkyl or lower alkanoyloxyalkyl, C3-6 cycloalkyl, hydroxy C3-C6 cycloalkyl, C3-C6 cycloalkyl lower alkyl; cyano, cyano lower alkyl, lower alkenyl, lower alkynyl, tetrahydrofuryl, di-lower alkylamino lower alkyl, di- lower alkylamino lower hydroxy alkyl; phenyl, phenyl lower alkyl or phenyl hydroxy lower alkyl, diphenyl lower alkyl, phenyl lower alkenyl, benzoyl or benzoyl lower alkyl, in which groups the phenyl moiety may be substituted with one to three halogen atoms or lower alkoxy groups and 1 or 2 hydroxy groups, thienoyl or thienoyl lower alkyl; R4 is lower alkyl, and Z is hydrogen, or Z and R3 together with the carbon atom to which they are attached form a C3-6 cycloalkyl group, whereby the substituents at the 3- and 4-position of the piperidine ring are in the cis-position, excluding N-[C2-6 alkyl, C2-6 hydroxy- alkyl, NN-di-lower alkylamino lower alkyl, optionally substi- tuted C7-11 aralkyl] substituted derivatives of quinicine and cinchonicine. The compounds of the formula may be in the form of their optically active enantiomers and/or their therapeuti- cally acceptable salts. Methods for the preparation of the compounds of the formula are also disclosed and form part of the invention.
363749
de Bode Ronus
Trijzelaar Hans B.
Welle Hendricus B. A.
Acf Chemiefarma N.v.
Marks & Clerk
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