4-(2-furoyl) aminopiperidines, intermediates in synthesizing...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S207000

Reexamination Certificate

active

10492065

ABSTRACT:
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.In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III):whereina, b and c are each an integer of 0-6;Z is CH2or NH;W is O or S;T is O or N—R15wherein R15is H, a C1-C6 alkyl group,a benzyl group or a phenethyl group; andR1is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like.The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ 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.

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