Title:
1,4-DISUBSTITUTED PIPERIDINE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/1997/045414
Kind Code:
A1
Abstract:
1,4-Disubstituted piperidine derivatives represented by general formula (I) and pharmaceutically acceptable salts thereof, wherein Ar represents heteroaryl having one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and optionally fused to aryl or benzene (wherein each hydrogen on the aryl and heteroaryl rings may be substituted by lower alkyl, halogeno, lower alkoxy, amino or hydroxymethyl); R1 represents C3-6 cycloalkyl having one or two hydroxyl groups on the ring; R2 represents heteroarylalkyl having one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and optionally fused to saturated or unsaturated aliphatic C5-15 hydrocarbon, aralkyl, arylalkenyl or benzene (wherein each hydrogen on the aralkyl, arylalkenyl and heteroarylalkyl rings may be substituted by lower alkyl, halogeno, lower alkoxy, amino or hydroxymethyl); and X represents O or NH. Because of having a selective muscarine M3 receptor antagonism, these compounds are useful as safe remedies or preventives with little side effects for respiratory diseases such as asthma, chronic respiratory obstruction and pulmonary fibrosis; urologic diseases in association with urination disorders such as frequent urination, urgency of micturition and urinary incontinence; and digestive diseases such as irritable bowel syndrome and convulsion or motor hyperenergia of digestive tracts.
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Inventors:
TSUCHIYA YOSHIMI (JP)
NOMOTO TAKASHI (JP)
OHSAWA HIROKAZU (JP)
KAWAKAMI KUMIKO (JP)
OHWAKI KENJI (JP)
NISHIKIBE MASARU (JP)
NOMOTO TAKASHI (JP)
OHSAWA HIROKAZU (JP)
KAWAKAMI KUMIKO (JP)
OHWAKI KENJI (JP)
NISHIKIBE MASARU (JP)
Application Number:
PCT/JP1997/001770
Publication Date:
December 04, 1997
Filing Date:
May 27, 1997
Export Citation:
Assignee:
BANYU PHARMA CO LTD (JP)
TSUCHIYA YOSHIMI (JP)
NOMOTO TAKASHI (JP)
OHSAWA HIROKAZU (JP)
KAWAKAMI KUMIKO (JP)
OHWAKI KENJI (JP)
NISHIKIBE MASARU (JP)
TSUCHIYA YOSHIMI (JP)
NOMOTO TAKASHI (JP)
OHSAWA HIROKAZU (JP)
KAWAKAMI KUMIKO (JP)
OHWAKI KENJI (JP)
NISHIKIBE MASARU (JP)
International Classes:
C07D211/58; (IPC1-7): C07D211/58; A61K31/445; C07D401/06
Domestic Patent References:
| WO1996033973A1 | 1996-10-31 |
Foreign References:
| JPH01131145A | 1989-05-24 |
Other References:
INT. J. RADIAT. APPL. INSTRUM., Part B, NUCL. MED. BIOL., 1989, Vol. 16, No. 1, OTTO C.A. et al., "In Vitro and Ex Vivo Evaluation of Cyclic Aminoalkyl Benzilates as Potential Emission Tomography Ligands for the Muscarinic Receptor", pages 51-55.
GEN. PHARMAC., 1991, Vol. 22, No. 3, TANG L.C. et al., "Human Erythrocyte as a Model for Investigating Muscarinicagonists and Antagonists", pages 485-590.
GEN. PHARMAC., 1991, Vol. 22, No. 3, TANG L.C. et al., "Human Erythrocyte as a Model for Investigating Muscarinicagonists and Antagonists", pages 485-590.
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