Compounds effective in the treatment of circadian rhythms and re

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548507, A61K 3140, C07D20914

Patent

active

055524281

ABSTRACT:
The novel compounds of formula: ##STR1## in which R is isopropyl, cyclohexyl, phenyl, CH.sub.3, Br or I; or H R.sub.1 is CH.sub.3 or cyclopropyl and R.sub.2 is H or Br, and when R.sub.1 is cyclopropyl and R.sub.2 is H, R is other than H, and when R.sub.1 is CH.sub.3 and R.sub.2 is H, R is other than H, and when R.sub.1 is CH.sub.3 and R.sub.2 is H, R is other than I, and when R is CH.sub.3 and R.sub.2 is H, R.sub.1 is other than CH.sub.3, and when R is phenyl and R.sub.2 is H, R.sub.1 is other than CH.sub.3, exhibit superior activity in the treatment of pathologies which interfere with the circadian rhythm. A novel method of preparation is described according to which the pharmaceutical compositions containing the novel compounds, as well as compounds already known, are administered transdermally. The novel method of administration results in sustained peripheral blood level. Novel pharmaceutical compositions are described suitable for transdermal administration.

REFERENCES:
patent: 4087444 (1978-04-01), Flaugh et al.
patent: 5242941 (1993-09-01), Lewy et al.
patent: 5264219 (1993-11-01), Godbey et al.
patent: 5284660 (1994-02-01), Lee et al.

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