| 摘要 |
1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: <CHEM> wherein X represents oxygen or sulphur; R<1> represents a non-aromatic azacyclic or azabicyclic ring system; and R<2> represents hydrogen, halogen, -CF3, -OR<7>, -NR<7>R<8>, -NHOR<7>, -NHNH2, -CN, -CO2R<7> or -CONR<7>R<8>, or a substituted or unsubstituted, saturated or unsaturated hydrocarbon group; wherein R<7> and R<8> independently represent hydrogen or C1-2 alkyl; provided that: (a) when R<2> is hydrogen and R<1> is in the 2-position, then R<1> is in the endo configuration; and (b) when R<2> is methyl and R<1> is in the 2-position, then R<1> does not represent an unsubstituted exo-1-azabicyclo[2.2.1]hept-3-yl, exo-1-azabicyclo[3.2.1]oct-3-yl or exo-1-azabicyclo[3.2.1]oct-6-yl group; stimulate central muscarinic acetylcholine receptors and are therefore useful in the treatment of neurological and mental illnesses whose clinical manifestations are due to involvement of cholinergic neurones; these compounds are also of benefit in the treatment of severe painful conditions. 1,3-Oxazole and 1,3-thiazole compounds of formula II, and salts and prodrugs thereof: <CHEM> wherein X is oxygen or sulphur; R<1><1> represents a non-aromatic azacyclic or azabicyclic ring system; and R<1><2> represents hydrogen, halogen, -CF3, -OR<7>, -NR<7>R<8>, -NHOR<7>, -NHNH2, -CN, -CO2R<7> or -CONR<7>R<8> or an optionally substituted, saturated or unsaturated hydrocarbon group; wherein R<7> and R<8> are as defined above; provided that when R<1><2> is present in the 2-position and represents amino, alkylamino, dialkylamino or alkylcarbonylamino, then R<1><1>, when present in the 4-position, does not represent optionally N-substituted piperidin-3-yl or 1,2,5,6-tetrahydropyridin-3-yl; provided also that: (a) when R<1><2> is hydrogen and R<1><1> is in the 2-position, then R<1><1> is in the endo configuration; and (b) when R<1><2> is methyl and R<1><1> is in the 2-position, then R<1><1> does not represent an unsubstituted exo-1-azabicyclo[2.2.1]hept-3-yl, exo-1-azabicyclo[3.2.1]oct-3-yl or exo-1-azabicyclo[3.2.1]oct-6-yl group; are novel compounds; processes for preparing the novel compounds are described, as also are pharmaceutical compositions containing the novel compounds.
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