N-acyl-pyrazoles of the formula ##SPC1## Wherein A is alkylene of one to four carbon atoms; Ar is phenyl, unsubstituted or substituted by one or more of alkyl and alkoxy of one to four carbon atoms, trifluoromethyl and halogen, and Q is ##SPC2## R being saturated or unsaturated alkyl or aralkyl of up to 10 carbon atoms, aryl of up to 10 carbon atoms, unsubstituted or substituted by one or more of alkyl, of 1-4 carbon atoms, amino and methoxy, --NH.sub.2, --N(CH.sub.3).sub.2 or alkoxy of 1-4 carbon atoms, and the physiologically acceptable salts thereof, possess valuable pharmacological properties, especially CNS-depressive activity, e.g., one or more of narcosis-prolonging, tranquilizing and neuroleptic properties.
The present invention relate to the use of heterocyclic compounds of the following formula: where Het, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D.sub.3 receptor and can therefore be used to treat disorders which respond to dopamine D.sub.3 ligands.
This disclosure describes novel pyrazolylpiperazines useful as hypotensive agents in mammals and as intermediates for the preparation of certain pyrazolo[1,5-a]pryrimidines.
Compounds of the general formula ##STR1## wherein X is a C.sub.1 -C.sub.6, straight chain saturated or unsaturated hydrocarbyl group, the group R.sup.4 and the group Y are situated in any position in this chain and wherein at least one of the hydrogen atoms in X can be a heavy isotope of hydrogen; R.sup.4 is hydrogen or an alkyl, alkoxy, hydroxy, aryl, aryloxy, aralkyl, aralkoxy, aralkylamino, or morpholino group wherein the alkyl or aryl part of any one of said groups may be substituted by one or more halogeno groups; or R.sup.4, together with at least one carbon atom of the group X, forms a carbocyclic or heterocyclic ring of 5 to 6 ring atoms; Y is an acidic or related group giving rise to one or more electronegative sites in the group; or R.sup.4 --X--Y represents a carboxylic acyl group; R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl; R.sup.1 is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group; R.sup.2 R.sup.3 and R.sup.5 which may be the same or different is each hydrogen or an alkyl, hydroxy, alkoxy, carboxy, alkyloxycarbonyl, halo, aryl, haloaryl or aryloxycarbonyl group; or R.sup.2 and R.sup.3 together with the carbon atoms to which they are attached form a ring system or R.sup.3 and R.sup.4 together and/or R.sup.3 and X together form one or more than one ring systems, or a physiologically acceptable salt thereof have activity in the central nervous system.
This invention is related to compositions and methods for the treatment of central nervous system disorders comprising compounds of the general formula ##STR1## wherein X, Y, and the R groups are defined in the disclosure.
Triazole compounds of the following formula: ##STR1## where Ar.sup.1, A, B and Ar.sup.2 have the meanings given in the description, possess a high affinity for the dopamine D.sub.3 receptor and can therefore be used for treating diseases which respond to dopamine D.sub.3 ligands.
