Pyrudyl and pyrimidylpiperazine derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S218000, C514S235800, C514S253090, C514S253120, C514S253130, C514S217050, C514S252140, C540S575000, C544S121000, C544S295000, C544S360000, C544S364000, C544S365000

Reexamination Certificate

active

06326371

ABSTRACT:

BACKGROUND
There is an urgent need for efficient drugs in the treatment of mental disorders which are more effective and which have fewer side effects than the drugs in clinical use today. Antipsychotic drugs in current use produce a range of troublesome extrapyratidal movement disorders (e.g. acute dystonic reactions and tardive dyskinesia) and are poor in ameliorating the negative symptoms (e.g. restricted or blunted emotional arousal) of schizophrenia. The main disadvantage of the anti-depressants is that they fail to alleviate depression in 30 to 40% of patients. Anxioltyics are commonly associated with addictive properties.
PRIOR ART
Various pyridyl- and pyrimidyl-piperazine derivates pharmacologically active in the central nervous system are known in the art. Some representative examples can be mentioned. Azaperone, a neuroleptic drug of the butyrophenone series, is a sedative for pigs. Buspirone is an aixiolytic. The anxiolytic effect is thought to be mediated via effects on the 5HT-receptors.
In the U.S. Pat. No. 4,937,245, compounds of the general formula C is disclosed
wherein A is selected from pyridyl or pyrimidyl group, e.g.
 wherein preferably R6 is hydrogen and R7 is cyano, amides, methoxy or hydrogen substituent in the 3-position of the pyridyl ring, useful for the treatment of mental disorders such as psychoses, depression and anxiety.


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