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

摘要

Novel 4-(2-furoyl)aminopiperidines represented by the following general formula (I), intermediates in synthesizing the same, a process for producing the same and medicines containing the same as the active ingredient: (I) wherein X represents CH or N; and Y represents a group represented by the following general formula (II), (II-a) or (III): (II) (II-a) (III) (wherein a, b and c are each an integer of 0 to 6; Z represents CH2 or NH; W represents O or S; T represents O or N-R15 (wherein R15 represents H, C1-6 alkyl, benzyl or phenethyl); and R1 represents H, C1-6 alkoxycarbonyl, benzyloxycarbonyl, etc . Because of having an antagonism to opioid .mu., these 4-(2- furoyl)aminopiperidine derivatives are useful in preventing or treating side effects of opioid .mu. receptor agonists selected from among constipation, nausea, vomiting and itch, constipation subitum, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic itch.