Highly selective sigma receptor ligands
a sigma receptor, high-selective technology, applied in the field of compounds, can solve the problems of drug abuse, limited pharmacological characterization of the -2 subtype, and protein corresponding to -2 site has not yet been cloned,
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[0028]The generic structures of Formulae I, II, III, IV and V encompasses a diverse range of heterocycles. Embodiments within this genus, for example, include 2(3H)-benzoxazolone (Y=O, Z=O) and 2(3H)-benzothiazolone (Y=S, Z=O) compounds and the sigma receptor affinity shown by these heterocycles. The 2(3H)-benzoxazolone (BOA) and its bioisosteric surrogate 2(3H)-benzothiazolone (BTA) heterocycle is a bicyclic ring system which promotes high versatility in organic synthesis involving N-substitution (either N-alkylation or N-acylation) and aromatic ring electrophilic substitution reactions.
Chemical structures of BOA and BTA
[0029]The present invention relates to compounds having the general formula I
wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine, or isoindoline-1,3-dioneR2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nit...
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