| 摘要 |
Disclosed are compounds of formula (I) e.g. (3aS,9bR)-2-[2-(trans-4-aminocyclohexyl)ethyl]-1,2,3,3a,4,9b-hexahydrochromeno[3,4-c]pyrrole-8-carbonitrile wherein R1 and R2 are defined in the specification, their enantiomers, their diastereoisomers, and also addition salts thereof with a pharmaceutically acceptable acid or base for use in the treatment or prevention of schizophrenia and other psychoses, abuse of drugs, as anxious states and toxicomania, the treatment of bipolar depressive states, impulsive behaviours such as obsessivecompulsive aggressiveness, treatment of Parkinson's disease, memory and other cognitive disorders associated with psychiatric and neurological diseases such as dementias and Alzheimer's disease, adolescents, the treatment of pain, nausea, premature ejaculation and also for renal protection. Also disclosed is a process for the preparation of said compounds characterised in that there is used as starting material bicyclo[2.2.2]oct-5-ene-2-carbonitrile which is subjected to a reductive amination reaction in the presence of a reducing agent, such as sodium triacetoxyborohydride or sodium cyanoborohydride, and an aminocyclohexyl acetalaldehyde compound which is then subjected to a reaction deprotecting the amine function, for example in the presence of trifluoroacetic acid, to yield the desired compound.
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