Benzofuran derivatives as D.sub.4 receptor antagonists
AssigneeMerck Sharp & Dohme Corp.
InventorsJanusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer
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Abstract
A class of chemical compounds comprising a benzo [b] furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo [b] furan moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia while manifesting fewer side-effects than those associated with classical neuroleptic drugs.
Claims11
A compound of formula I, or a salt or prodrug thereof:
- ##STR9## wherein A represents hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, cyano or trifluoromethyl;
- Q represents a moiety of formula Qa, Qb, Qc or Qd:
- ##STR10## in which the broken line represents an optional chemical bond;
- R.sup.1 represents hydrogen, or an optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, aryl, aryl(C.sub.1-6)alkyl, aryl(C.sub.1-6)alkoxy, aryl(C.sub.2-6)alkenyl, aryl(C.sub.2-6)alkynyl, C.sub.3-7 heterocydoalkyl(C.sub.1-6)alkyl, heteroaryl, heteroaryl(C.sub.1-6)alkyl, heteroaryl(C.sub.2-6)alkenyl or heteroaryl(C.sub.2-6)alkynyl group;
- R.sup.2 represents an optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, aryl, aryl(C.sub.1-6)aryl, aryloxy(C.sub.1-6)alkyl, aryl(C.sub.1-6)alkoxy, aryl(C.sub.2-6)alkenyl, aryl(C.sub.2-6)alkynyl, C.sub.3-7 heterocycloalkyl(C.sub.1-6)alkyl, heteroaryl, heteroaryl(C.sub.1-6)alkyl, heteroaryl(C.sub.2-6)alkenyl or heteroaryl(C.sub.2-6)alkynyl group;
- R.sup.3, R.sup.4 and R.sup.5 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, --OR.sup.a, --SR.sup.a, --SOR.sup.a, --SO.sub.2 R.sup.a, --SO.sub.2 NR.sup.a R.sup.b, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --COR.sup.a, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;
- Z represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --;
- R.sup.6 represents hydrogen or halogen, or an optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl, aryloxy, aryl(C.sub.1-6)alkyl, aryl(C.sub.1-6)alkoxy or heteroaryl group;
- and
- R.sup.a and R.sup.b independently represent hydrogen, hydrocarbon or a heterocyclic group.
Dependencies are inferred from the claim text.