Piperazine derivatives as 5-ht antagonists

Details Piperazine derivatives as 5-ht antagonists Piperazine derivatives as 5-ht antagonists

1996-10-23

1998-01-20

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142305, 5142358, 514254, 540481, 540598, 544105, 544121, 544357, 544364, 544372, 544376, 544377, A61K 3155, A61K 31495, C07D40514, C07D40510

Patent

active

057101493

ABSTRACT:
This invention concerns compounds of formula (I) ##STR1## where A is a C.sub.1 or C.sub.2 alkylene chain optionally substituted by lower alkyl; Z is a bicyclic oxygen-containing aryl radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl); R is hydrogen or lower alkyl; R.sup.1 is aryl or aryl(lower)alkyl; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, cycloalkyl of 3 to 12 carbon atoms; cycloalkyl(lower)alkyl, aryl or aryl(lower)alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom, and the pharmaceutically acceptable acid addition salts thereof. The compounds are 5-HT.sub.1A -antagonists which may be used, for example, in treating anxiety.

REFERENCES:
patent: 4788290 (1988-11-01), Stack
patent: 4935511 (1990-06-01), Youssefyeh et al.
patent: 4988814 (1991-01-01), Abou-Gharbia et al.
patent: 5340812 (1994-08-01), Cliffe
patent: 5369103 (1994-11-01), Cliffe et al.
patent: 5382583 (1995-01-01), Cliffe
patent: 5430033 (1995-07-01), Cliffe et al.

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