Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-10-28
1998-09-15
Bernhardt, Emily
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514255, 514249, 544231, 544379, 544398, 544401, 544403, 544349, A61K 31495, C07D24104, C07D40908
Patent
active
058078550
ABSTRACT:
Trans isomers of 1-piperazino-1,2-dihydroindene compounds having formula (I), ##STR1## wherein X and Y are hydrogen, halogen, trifluoromethyl, alkyl, alkylthio, trifluoromethylthio, alkoxy, hydroxy, alkylsulfonyl, amino, alkylamino, nitro or cyano; Ar is a phenyl, thienyl or furyl group, each optionally substituted; R.sub.1 is hydrogen, or optionally hydroxy substituted alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; R.sub.2 is alkyl, alkenyl, cycloalkyl, or cycloalkylalkyl; or R.sub.1 and R.sub.2 together form a 5 to 7-membered heterocyclic ring fused with the piperazine ring, which ring may be substituted with hydroxy; R.sub.3 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; or R.sub.2 and R.sub.3 together form a 3 to 7-membered carbocyclic ring which is spiro-fused to the piperazine ring; and R.sub.4 is hydrogen or alkyl. The compounds of the invention have potent antagonist action on dopamine D.sub.1 receptors and are useful in the treatment of diseases of the central nervous system, such as psychoses, schizophrenia (positive as well as negative symptoms), anxiety, depression, sleep disturbances, migraine, Parkinson's disease or cocaine abuse.
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B.o slashed.ges.o slashed. Klaus
Bregnedal Peter
Bernhardt Emily
H. Lundbeck A/S
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