Heterocyclic compounds, their preparation and use

Details Heterocyclic compounds, their preparation and use Heterocyclic compounds, their preparation and use

1995-02-08

1998-04-21

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514250, 544337, 544346, A61K 31675, A61K 31495, C07F 9576, C07D48704

Patent

active

057417857

ABSTRACT:
##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are the same or independently are H, alkyl, alkoxy, halogen, NO.sub.2, NH.sub.2, CF.sub.3, CN, SO.sub.2 CH.sub.3, SO.sub.2 CF.sub.3, SO.sub.2 NR'R" or a 5- or 6-membered N-containing heterocyclic ring, optionally substituted, and R', R" are independently H or alkyl; and R.sup.4 is H or CH.sub.2 -R.sup.6 ; and R.sup.6 is H, halogen, POR'"R"", NR.sup.7 R.sup.8 or a 5- or 6-membered N-containing heterocyclic ring optionally substituted, and R'", R"" are independently hydroxy or alkoxy; and ##STR2## R.sup.7, R.sup.8 are the same or independently are H, or alkyl optionally substituted; and n is 1, 2 or 3;
R.sup.5 is ##STR3## and R.sup.9 is OH, alkoxy, H or NR.sup.10 R.sup.11 ; and R.sup.10, R.sup.11 are the same or independently are H, NH.sub.2 or OH; and X is O or S; and Y is O, S or NH.sub.2, and pharmaceutically acceptable salts thereof, have affinity for the AMPA receptors and are antagonists in connection with this type of receptor which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.

REFERENCES:
patent: 4291033 (1981-09-01), Barnes et al.
patent: 5153196 (1992-10-01), McQuaid
Ager et al., J. Med. Chem., vol. 31, pp. 1098-1115 (1988).
D.D. Davey et al., J. Med. Chem., vol. 34, pp. 2671-2677 (1991).
McQuaid et al., J. Med. Chem., vol. 35, pp. 3319-3324 (1992).
Jackson et al., Bioorg. Med. Chem. Lett., vol. 1, No. 12, pp. 751-756 (1991).

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