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

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United States of America Patent

PATENT NO 7375115
APP PUB NO 20050085508A1
SERIAL NO

10492065

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Abstract

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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. ##STR00001## 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): ##STR00002## wherein a, b and c are each an integer of 0-6; Z is CH.sub.2 or NH; W is O or S; T is O or N--R.sup.15 wherein R.sup.15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R.sup.1 is 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 .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.

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Patent Owner(s)

Patent OwnerAddress
NISSHIN PHARMA INCTOKYO JAPAN TOKYO METROPOLIS
KYORIN PHARMACEUTICAL CO LTDCHIYODA-KU

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Fukutomi, Ryuuta Iruma-gun, JP 2 5
Hagihara, Kouichirou Iruma-gun, JP 2 5
Inoue, Hitoshi Iruma-gun, JP 129 1831
Kawamura, Koji Iruma-gun, JP 139 947
Kishimoto, Takuya Iruma-gun, JP 56 411
Kojima, Kazuko Iruma-gun, JP 4 7
Shibayama, Rie Iruma-gun, JP 2 5
Suzuki, Masashi Iruma-gun, JP 202 1793

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