Ethanobicyclic amine derivatives for CNS disorders

Details Ethanobicyclic amine derivatives for CNS disorders Ethanobicyclic amine derivatives for CNS disorders

1990-04-30

1992-02-18

Shen, Cecilia

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514255, 544403, 546203, 546204, A61K 31445, A61K 31495, C07D21106, C07D29500

Patent

active

050895060

ABSTRACT:
Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;
wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl wherein each of R.sup.12 and R.sup.13 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R.sup.3, R.sup.4, ring-position two, and ring-position three; or the pharmaceutically-acceptable salts thereof.

REFERENCES:
patent: 3821249 (1974-06-01), Malen et al.
A. F. Gilman et al., The Pharmacological Basis of Therapeutics 7th Edn., p. 403 (1985).
S. M. Rothman et al., Annals of Neurology, 19(2), 105-111 (1986).
C. Carter et al., J. Pharm Exp. Ther., 247(3), 1222-1232 (1988).
R. M. Bartholow et al., J. Pharm. Exp. Ther., 202(3) 532-543 (1977).
S. M. Knepper et al., J. Pharmacol. Exp. Ther., 247(2), 487-494 (1988).
H. E. Katerinopoulos et al., Eur. J. Med. Chem., 23(4), 391-396 (1988).

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