Catechol derivatives, and preventive and remedial preparations for regressive disorders in the central nervous system containing the same

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT The present invention is a preventive and remedial preparation for regressive disorders in the central nervous system which comprises as an effective ingredient a catechol derivative having the formula (A): ##STR1## wherein R is two hydrogen atoms, two acyl groups, a --CO-- group, --CO.
multidot.
CO-- group, or --C(CH.
sub.
3).
sub.
2 -- group, and wherein R.
sub.
1 and R.
sub.
2 are each independently a hydrogen atom or lower alkyl group.
Among these derivatives for use in the medicinal compositions, the below described derivative is a novel compound which has not yet been known.
That is, a catechol derivative having the formula (B): ##STR2## wherein R.
sub.
3 is two acyl groups, a --CO-- group, --CO.
multidot.
CO-- group or --C(CH.
sub.
3).
sub.
2 -- group, and R.
sub.
4 is a lower alkyl group, and wherein excluding when R.
sub.
3 is acetyl group and R.
sub.
4 is methyl group and when R.
sub.
3 is --CO.
multidot.
CO-- group and R.
sub.
4 is methyl group.
More practical illustration of the derivative is: (1) A catechol derivative having the formula (C): ##STR3## wherein R.
sub.
5 is an acyl group and R.
sub.
6 is a lower alkyl group, and wherein excluding when R.
sub.
5 is an acetyl group and R.
sub.
6 is a methyl group, (2) a catechol derivative having the formula (D): ##STR4## wherein R.
sub.
7 is a lower alkyl group, (3) a catechol derivative having the formula (E): ##STR5## wherein R.
sub.
8 is a lower alkyl group and wherein excluding when R.
sub.
8 is a methyl group, and (4) a catechol derivative having the formula (F): ##STR6## wherein R.
sub.
9 is a lower alkyl group.
At the first step, neurotransmitters and agonists of their receptors, neuromodulators, etc.
and their structurally related compounds were selected in order to search the active derivative of this invention.
Typical compounds were selected from those exhibiting the activity for accelerating the production and secretion of NGF in the screening system in vitro using cultured cells.
In the experiments in vivo using rats, these typical compounds have induced the production and secretion of NGF in the particular regions of brain even by the peripheral administration