GABA esters and GABA analog esters

Details GABA esters and GABA analog esters GABA esters and GABA analog esters

1990-05-07

1991-09-24

Friedman, Stanley J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514533, 514538, 514539, 514540, 514551, 260399, 260400, 260401, 260402, 2604025, 260404, 2604045, A61K 31225, A61K 31235, A61K 3124, A61K 3122

Patent

active

050514482

ABSTRACT:
Ester derivatives of gamma-aminobutyric acid (GABA) and GABA analogues which cross the blood-brain barrier are disclosed, as well as methods of synthesizing and using the compounds.
The ester derivatives have the formula: ##STR1## where A is a radical compound having at least one esterifiable OH group; n varies from one to the total number of esterifiable OH group contained in A; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or a substituent.

REFERENCES:
Chemical Abstracts; vol. 103, (1985) #64867r; Shashoua.
Chemical Abstracts; vol. 100 (1984), #156960g; Shashoua.
Chemical Abstracts; vol. 88 (1978), #7325k; Fominova et al.
Chemical Abstracts; vol. 85 (1976), #108263g; Shmuilovich et al.
Chemical Abstracts; vol. 84 (1976), #30348w; Shmuilovich et al.
Chemical Abstracts; vol. 79 (1973), #73657k; Ostrovskaya et al.
Chemical Abstracts; vol. 68 (1968) #113074z; Berteui et al.
Jacob, J. N., Journal of Medicinal Chemistry, 1985, vol. 28, No. 1, pp. 106-110, Lipid Esters of GABA Penetrate Blood-Brain Barrier.
Hesse, G. W., et al., Neuropharmacology, vol. 24, No. 2, pp. 139-146, 1985, Cholesteryl-GABA inhibition.

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