PURPOSE: To obtain new piperidine derivatives useful in therapy and prevention of diseases related to 5-HT3 and 5-T4 receptors, such as emesis, central nervous diseases, disorder of cognition and dyskinesia.
CONSTITUTION: Compounds of formula I (R is H or alkyl; Ar is halogen, amino, alkoxy, cycloalkylalkoxy, phenyl or heteroaryl, except compounds wherein R is H and Ar is phenyl or 4-chlorophenyl) and their pharmaceutically acceptable acid addition salts, such as 1-(3,5-dichlorobenzoyl)-4-(1H-imidazol-4-yl) piperidine are provided. A compd. of the formula I is obtained by reacting a compd. of formula II (X is halogen or OH) with a piperidine derivative of formula III. The medicaments are effective for pain, migraine, headache, disorders related to alcohol-or drug-dependence or withdrawal syndrome, disorders of gastrointestinal functions, cardiovascular disorders and respiratory disorders as well as diarrhea and irritable colon, in addition to the above- mentioned diseases.
ICHIYATSUKU ENJIERU
TOOMASU PAASERU
YOHANESU SHIEEMAAKAA
