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Title:
NOVEL 4−&lpar 2−FUROYL&rpar AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME, PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME
Document Type and Number:
WIPO Patent Application WO/2003/035645
Kind Code:
A1
Abstract:
Novel 4−(2−furoyl)aminopiperidines represented by the following general formula (I), intermediates in synthesizing the same, a process for producing the same and medicines containing the same as the active ingredient: (I) wherein X represents CH or N&semi and Y represents a group represented by the following general formula (II), (II−a) or (III): (II) (II−a) (III) (wherein a, b and c are each an integer of 0 to 6&semi Z represents CH2 or NH&semi W represents O or S&semi T represents O or N−R15 (wherein R15 represents H, C1−6 alkyl, benzyl or phenethyl)&semi and R1 represents H, C1−6 alkoxycarbonyl, benzyloxycarbonyl, etc. Because of having an antagonism to opioid μ, these 4−(2−furoyl)aminopiperidine derivatives are useful in preventing or treating side effects of opioid μ receptor agonists selected from among constipation, nausea, vomiting and itch, constipation subitum, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic itch.

Inventors:
FUKUTOMI RYUUTA (JP)
INOUE HITOSHI (JP)
KAWAMURA KOJI (JP)
KISHIMOTO TAKUYA (JP)
SUZUKI MASASHI (JP)
SHIBAYAMA RIE (JP)
KOJIMA KAZUKO (JP)
HAGIHARA KOUICHIROU (JP)
Application Number:
PCT/JP2002/010449
Publication Date:
May 01, 2003
Filing Date:
October 08, 2002
Export Citation:
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Assignee:
KYORIN SEIYAKU KK (JP)
NISSHIN PHARMA INC (JP)
FUKUTOMI RYUUTA (JP)
INOUE HITOSHI (JP)
KAWAMURA KOJI (JP)
KISHIMOTO TAKUYA (JP)
SUZUKI MASASHI (JP)
SHIBAYAMA RIE (JP)
KOJIMA KAZUKO (JP)
HAGIHARA KOUICHIROU (JP)
International Classes:
A61P1/04; A61P1/08; A61P1/10; A61P17/04; A61P43/00; C07D211/58; C07D401/12; C07D405/12; C07D405/14; C07D413/14; (IPC1-7): C07D405/14; C07D413/14; C07D401/12; C07D405/12; C07D211/58; A61K31/443; A61K31/4525; A61K31/453; A61K31/454; A61K31/4545; A61K31/497; A61K31/5377; A61P1/04; A61P1/08; A61P1/10; A61P17/04; A61P43/00
Domestic Patent References:
WO1994027967A11994-12-08
Foreign References:
EP0277794A21988-08-10
EP0160422A11985-11-06
Other References:
See also references of EP 1443046A4
Attorney, Agent or Firm:
Takagi, Chiyoshi (10 Kojimachi 1-chom, Chiyoda-ku Tokyo, JP)
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