| 摘要 |
PURPOSE: Novel fluorinated 1,4-bisubstituted piperidine derivatives and pharmaceutically acceptable salts thereof are provided which is useful for treatment or prophylaxis of various kinds of diseases in respiratory organ, urinary system, and digestive system. CONSTITUTION: Novel fluorinated 1,4-bisubstituted piperidine derivatives are represented by general formula (I), wherein Ar represents aryl or heteroaryl having 1 or 2 heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur in which one to three hydrogen atoms on the aryl or heteroaryl ring may be substituted by lower alkyl, etc.; R1 represents C3 to C6 cycloalkyl in which one to four arbitrary hydrogen atoms may be substituted by fluorine; R2 represents saturated or unsaturated, aliphatic C5 to C15 hydrocarbon in which one to six arbitrary hydrogen atoms may be substituted by fluorine, aralkyl, arylalkenyl, or heteroarylalkyl or heteroarylalkenyl having one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, in which one to three hydrogen atoms on the aralkyl, arylalkenyl, heteroarylalkyl or heteroarylalkenyl ring may be substituted by lower alkyl, trifluoromethyl, cyano, hydroxy, nitro, lower alkoxycarbonyl, halogeno, lower alkoxy, amino, etc.; and X represents O or NH, provided that at least one of R1 and R2 has one or more fluorine atoms. Because of having selective muscarinic receptor antagonism and being excellent in oral activity, persistence of the action and dynamic in vivo, these compounds are useful as efficacious and safe remedies or preventives with little side effects for respiratory, urologic and digestive diseases.
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