NOVEL 4-(2FUROYL)AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME, PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME

摘要

There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. <CHEM> In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): <CHEM> <CHEM> <CHEM> wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N-R<15> wherein R<15> is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R<1> is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like. <??>The 4-(2-furoyl) aminopiperidine derivatives according to this invention possess opioid mu antagonistic activity and are useful for the treatment or prevention of side effects which are caused by mu receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.