4- (2-furoyl) aminopiperidines, intermediates in the synthesis thereof, process for producing same and medicinal use thereof

摘要

"4- (2-FUROIL) AMINOPIPERIDINES, INTERMEDIATE IN SYNTHESIS OF THE SAME, PROCESS TO PRODUCE THE SAME AND MEDICAL USE OF THE SAME". The invention relates to novel 4- (2-furoyl) aminopiperidines represented by general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N and Y is a group following the general formula (II), formula (II-a) or formula (III): wherein: a, b and c are each an integer from 0 to 6; Z is CH 2 - 2 or NH; W is O or S; T is O or N-R 15 where R 15 is H, a C 1-6 alkyl group, a benzyl group or a phenethyl group; and R4 is H, a C1 -C6 alkoxycarbonyl group, a benzyloxycarbonyl group or the like. The 4- (2-furoyl) aminopiperidine derivatives according to this invention have Î ± opioid antagonistic activity and are useful for treating or preventing side effects that are caused by Î ± -receptor agonist and are selected from constipation. , nausea / emesis or scabies or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic itching.