| abstract |
Provided are novel 4- (2-furoyl) aminopiperidine represented by the following formula (I), a synthetic intermediate thereof, a preparation method thereof, and a medicament using the same as an active ingredient:n n n [Formula I]n n n n n n n n In the above formula, X is CH or N, Y is a group of the following general formula (II) or (II-a) or (III),n n n [Formula II]n n n n n n n n [Formula II-a]n n n n n n n n [Formula III]n n n n n n n n Where a, b and c are integers from 0 to 6, Z is CH 2 or NH, W is O or S, T is O or NR 15 , R 15 is H, C 1 -C 6 alkyl group, benzyl group , Phenethyl group, R 1 is H, C1-C6 alkoxycarbonyl group, benzyloxycarbonyl group and the like. The 4- (2-furoyl) aminopiperidine derivative obtained by the present invention has an opioid μ-antagonist action and has side effects of opioid μ receptor agonists selected from constipation, nausea, vomiting or pruritus, sudden constipation, and postoperative ileus. It is useful for the prevention or treatment of Usus, Paralytic Ileus, Irritable Bowel Syndrome or Chronic Pruritus. |