Benzoxazines for enhancing synaptic response
AssigneeThe Regents of the University of California
InventorsGary A. Rogers, Gary S. Lynch
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Abstract
Compounds based on the benzoxazine ring system are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating schizophrenia, and for improving memory encoding.
Claims38
A compound having the formula ##STR13## in which:
- R.sup.1 and R.sup.2 are independently selected from the group consisting of H and R.sup.4 O such that at least one of R.sup.1 and R.sup.2 is R.sup.4 O, in which R.sup.4 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- or
- R.sup.1 and R.sup.2 together form a single divalent moiety selected from the group consisting of ##STR14## in which:
- R.sup.6 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- R.sup.7 is a member selected from the goup consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- and
- R.sup.8 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- R.sup.3 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- and
- n is 1,2,3 or 4.
A method for the treatment of a subject to enhance synaptic response mediated by AMPA receptors, said method comprising administering to said subject an effective amount of a compound having the formula ##STR18## in which:
- R.sup.1 and R.sup.2 are independently selected from the group consisting of H and R.sup.4 O such that at least one of R.sup.1 and R.sup.2 is R.sup.4 O, in which R.sup.4 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 C.sub.6 alkyl;
- or
- R.sup.1 and R.sup.2 together form a single divalent moiety selected from the group consisting of ##STR19## in which:
- R.sup.6 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- R.sup.7 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- and
- R.sup.8 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- R.sup.3 is a member selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl and halo-substituted C.sub.1 -C.sub.6 alkyl;
- and
- n is 1,2,3 or 4.
Dependencies are inferred from the claim text.