Bicyclic nonane and decane compounds having dopamine receptor affinity

Abstract

Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from O, S, SO, SO.sub.2, CH.sub.2, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, and C.dbd.CHCN; X.sub.2 --- is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O)--; n is 1 or 2; R.sub.1 is selected from H and the .alpha.-carbon side chain of an amino acid; R.sub.2 and R.sub.3 are selected independently from H, OH, --NH.sub.2, --C(O)NH.sub.2 .dbd.O, .dbd.S,halo,cyano, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, C.sub.1-4 alkylS--, C.sub.1-4 alkylSO--, C.sub.1-4 alkylSO.sub.2 --, phenoxy, benzyloxy and piperonyloxy; and H* is in either the R- or the S-configuration, and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.

Dependencies are inferred from the claim text.