Aryl-and heteroaryl piperazinyl carboxamides having central nervous system activity
US5254552A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 16, 1992 |
| Grant date | Oct 19, 1993 |
| Priority date | — |
| Expiry date | Mar 16, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D295/13
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof. The compounds of this invention which demonstrate selectivity at the 5-HT.sub.1A and 5-HT.sub.2 versus D.sub.2 receptor binding sites are useful as potential anxiolytic-antidepressant agents. Compounds of this invention with equal high affinity for the 5-HT.sub.1A and D.sub.2 -receptor binding sites are useful as mixed antipsychotic-anxiolytic agents. Compounds of this invention which demonstrate central cholinergic activity are useful in the treatment of senile dementia of the Alzheimer type (SDAT) and Huntingdon's chorea.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.