Kyorin Pharmaceutical Co., Ltd.

Nisshin Seifun Group Inc.

Nisshin Pharma Inc.

Takuya Kishimoto

Masashi Suzuki

Koji Kawamura

Hitoshi Inoue

Rie Shibayama

Tomokazu Fujimoto

Kazuko Kojima

Yukiko Muraki

Ryuuta Fukutomi

Kouichirou Hagihara

There are provided compounds represented by the following general formula (I): [where Ris 5-methylpyridin-2-yl, p-tolyl or mesityl, Ris one of the following general formulas (II)-(IX): (where Ris C1-C4 alkyl, Ris H or C1-C4 alkyl, Ris H, 3-pyridylmethyl or 4-pyridylmethyl, and Ris 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when Ris mesityl, Ris the following formula (X)], and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.

4-(2-furoyl)aminopiperidine compound useful as therapeutic agent for itching

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):  The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid &#x3bc; antagonistic activity and are useful for the treatment or prevention of side effects which are caused by &#x3bc; 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.

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

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Fujimino, Japan

Takuya Kishimoto