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Abstract

The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R.sub.1).sub.n represents 0, 1, or 2 substituents, which can be the same or different, from the group C.sub.1-3 -alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C.sub.1-2)-amino, sulfonyl-(C.sub.1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C.sub.1-2)-amino, X is O, S, NH or NCH.sub.3, Y represents CH.sub.2, or (CH.sub.2).sub.2, (R.sub.2).sub.m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R.sub.2).sub.m is a methylene bridge or ethylene bridge, A is a group --CH.sub.2 --(CRH).sub.p -- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-.sub.1-3 -alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono-or dialkyl (C.sub.1-2)amino, sulfonyl-(C.sub.1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C.sub.1-2)-amino. ##STR1##

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First Claim