1-azabicyclo(2.2.2.)oct-3-yl-(2,4,5,6-tetrahydro 1H-benz(de)isoquinoline-1-one and 1,2,4,5,6,7-hexahydro cyclohept(de)isoquinoline-1-one) as 5-HT 3 antagonists

摘要

The present invention is directed to new pharmaceutically active compounds with 5-HT3 receptor antagonist activity of Formula I: in which the dashed line denotes an optional double bond; n is 1, 2 or 3; p is 0, 1, 2 or 3; q is 0, 1 or 2; each R<1> is halogen, hydroxy, alkoxy (optionally substituted with phenyl), alkyl, nitro, amino, amino carbonyl, (alkyl)amino, di(alkyl)amino, and (alkanoyl)amino; each R<2> is alkyl; and R<3> is in which u, x, y, and z are all independently an integer from 1 to 3; and R<4> and R<5> are independently alkyl, cycloalkyl, cycloalkylalkyl, or a group (CH2)tR6 where t is 1 or 2 and R6 is thienyl, pyrrolyl or furyl optionally further substituted by one or two substituents selected from alkyl, alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and alkyl (optionally substituted).