Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1977-05-23
1978-09-26
Milestone, Norma S.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
26029381, 26029384, 424267, 424263, C07D21148, C07D40106
Patent
active
041169638
ABSTRACT:
The present invention encompasses compounds of the formula ##STR1## AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R represents hydrogen, alkanoyl having 1 to 7 carbon atoms, or lower alkyl having 1 to 7 carbon atoms; X and Y represent alkylene having 1 to 3 carbon atoms and Ar, Ar', and Ar" represent phenyl, halosubstituted phenyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1 to 4 carbon atoms; and Ar'" represents phenyl, pyridyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1 to 4 carbon atoms or halosubstituted phenyl. Compounds of the present invention are prepared by reaction of triarylalkanoyl halide with appropriately substituted piperidine followed by subsequent reduction of the resulting amide. Compounds of the present invention are potent antidiarrheal compounds with unexpected separation of antidiarrheal and central nervous system properties.
REFERENCES:
patent: 3438991 (1969-04-01), Janssen
patent: 3462444 (1969-08-01), Beckett et al.
patent: 3979390 (1976-09-01), Sasajima et al.
patent: 3998832 (1976-12-01), Adelstein
G.D. Searle & Co.
McDonnell John J.
Milestone Norma S.
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