Tetrahydropyridine derivatives as dopamine receptor subtype ligands
AssigneeMerck Sharp & Dohme Corp.
InventorsNeil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Kevin William Moore, Andrew Pate Owens, Martin Richard Teall
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Abstract
A class of 1,2,3,6-tetrahydropyridine derivatives, substituted in the 4-position by a fused bicyclic heteroaromatic moiety and in the 1-position by an optionally substituted benzyl moiety, are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
Claims8
A method for the prevention and/or treatment of schizophrenia which method comprises administering to a patient in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof:
- ##STR6## wherein X represents sulphur;
- Y represents nitrogen;
- and
- R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, halogen, cyano, nitro, trifluoromethyl, C.sub.1-6 alkyl or C.sub.1-6 alkoxy.
A method for the prevention and/or treatment of schizophrenia which method comprises administering to a patient in need of such treatment an effective amount of a compound selected from the following:
- 4-(benzothiazol-2-yl)-1-benzyl-1,2,3,6-tetrahydropyridine;
- 4-(benzothiazol-2-yl)-1-(4-chlorobenzyl)-1,2,3,6-tetrahydropyridine;
- 4-(benzothiazol-2-yl)-1-(3-chlorobenzyl)-1,2,3,6-tetrahydropyridine;
- 4-(benzothiazol-2-yl)-1-(2-chlorobenzyl)-1,2,3,6-tetrahydropyridine;
- 4-(benzothiazol-2-yl)-1-(4-cyanobenzyl)-1,2,3,6-tetrahydropyridine;
- 1-benzyl-4-(5-chlorobenzothiazol-2-yl)-1,2,3,6-tetrahydropyridine;
- 4-(5-chlorobenzothiazol-2-yl)-1-(4-chlorobenzyl)-1,2,3,6-tetrahydropyridine ;
- 4-(5-chlorobenzothiazol-2-yl)-1-(3-chlorobenzyl)-1,2,3,6-tetrahydropyridine ;
- 4-(5-chlorobenzothiazol-2-yl)-1-(2-chlorobenzyl)-1,2,3,6-tetrahydropyridine ;
- 1-benzyl-4-(5-trifluoromethylbenzothiazol-2-yl)-1,2,3,6-tetrahydropyridine.
Dependencies are inferred from the claim text.