摘要 |
<p>Cpds. of formula (I) and their therapeutically acceptable acid addition salts, anhydrous or hydrated, and their bioprecursors, are new (the dotted line is an opt. double bond; Ar is 2-,3-, or 4-pyridyl or is of formula (II) where Y is in the 2-, 3- or 4-posn. and is 1-3C alkyl or alkoxy, halogen, CF3, NH2 or mono- or di-(1-3C-alkyl)amino; X is H or a value of Y; R is 1-3C alkyl; R1 is H or R). Also claimed are intermediates of formulae (III)-(X) (R' is H, or 1-3C alkyl, acyl or alkylslphonyl; Z is F, Cl, Br, I or OSO2R'a; R'a is alkyl, aralkyl or aryl; R" and R"' are amino-protecting gps.). (I) are CNS active, partic. antidepressants, tranquillisers and anxiolytic agents. Doses are e.g. 25-250, pref. 50 -150 mg. p.o., or 5-50, pref. 10-30 mg. parenterally, to humans and animals.</p> |