Piperazine derivatives
AssigneeJohn Wyeth & Brother Limited
InventorsIan A. Cliffe, Christopher I. Brightwell, Howard L. Mansell, Alan C. White
Life of this patent
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Abstract
Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, A is an optionally substituted alkylene chain, Z is a specified bicyclic nitrogen containing heteroaromatic radical, R is hydrogen or lower alkyl, R.sup.1 is aryl or aryl(lower)alkyl and R.sup.2 and R.sup.3 are hydrogen or specified organic radicals or --NR.sup.2 R.sup.3 represents a heterocyclic ring. ##STR1##
Claims13
A compound of the formula ##STR5## or a pharmaceutically acceptable acid addition salt thereof, wherein A is a C.sub.1 -C.sub.2 alkylene chain, optionally substituted by one or more C.sub.1 -C.sub.6 alkyl groups, Z is a bicyclic nitrogen containing heteroaromatic radical selected from the group consisting of indolyl, isoindolyl, quinolinyl, isoquinolinyl, indazolyl and benzotriazolyl, which may be optionally substituted bv one or two substitutents selected from C.sub.1 -C.sub.6 alkyl, halogen, trifluoromethyl, nitro, cyano, oxo, hydroxy, C.sub.1 -C.sub.6 alkoxy, hydroxy -C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 acyl, C.sub.1 -C.sub.6 acyl-C.sub.1 -C.sub.6 alkyl, carboxamido, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, mono- or di-C.sub.1 -C.sub.6 alkylamino;
- R represents H or one or two same or different C.sub.1 -C.sub.6 alkyl groups;
- R.sup.1 is an aryl radical or aryl-C.sub.1 -C.sub.6 alkyl where aryl is phenyl or naphthyl, optionally substituted by 1 or 2 groups selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, cyano, amino, mono- or di-C.sub.1 -C.sub.6 alkylamino;
- R.sup.2 and R.sup.3 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring having 4 to 8 members, one of which can be an additional heteroatom selected from oxygen, sulfur, or nitrogen wherein said ring may be optionally substituted by C.sub.1 -C.sub.6 alkyl, phenyl or phenyl-C.sub.1 -C.sub.6 alkyl.
Dependencies are inferred from the claim text.