University System of Maryland

Carlo Erba S.p.a.

Pharmacia & Upjohn S.p.a.

Farmitalia Carlo Erba S.p.a.

Pharmacia S.p.a.

Arturo Della Torre

Piero Melloni

Alessandro Rossi

Mario Varasi

Robert Schwarcz

Alberto Bianchetti

Francesco Lauria

Carmela Speciale

Raffaele Tommasini

Norina Passerini

Giovanni C Carniel

Substituted kynurenines and process for their preparation

The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).

The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT). The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, and

Substituted morpholine derivatives, such as, for instance the compound 2-[.alpha.-(3,4-methylendioxy-phenoxy)-benzyl]-morpholine are disclosed. The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.

Substituted morpholine derivatives and pharmaceutical compositions

Novel N-tricyclic derivatives of azetidine are disclosed of the general formula ##STR1## where A is a C.sub.1 -C.sub.3 alkylene group, a C.sub.2 -C.sub.3 alkenylene group or a cyclopropylene group, the remaining substituents being defined in the specification. Such compounds are useful for their anti-depressant, anti-convulsant and anxiolytic activities. The compound 1-[5-(10, 11-dihydro-5H-dibenzo [a,d]cyclopheptenyl)]-3-methyl-amino-azetidine is illustrative.

N-tricyclic derivatives of azetidine and process for their preparation

Novel N-tricyclic derivatives of azetidine of the formula: ##STR1## wherein A is a --CH.sub.2 --O-- or an --O--CH.sub.2 group, and the remaining substituents being defined in the specification are disclosed. An illustrative compound is 1-[11-(6,11-dihydro-dibenzo [b,e] oxepinyl)]-3-methylamino-azetidine. The compounds are useful for their anti-depressant, anti-convulsant and anxiolytic activities.

N-tricyclic derivatives of azetidine

Novel N-tricyclic derivatives of azetidine are disclosed of the general formula: ##STR1## WHERE A is a --CH.sub.2 --S-- or --S--CH.sub.2 -- group, the remaining substituents being defined in the specification. Illustrative is the compound 1-[11-(6,11-dihydro-dibenzo [b,e] thiopinyl)]-3-methylamino-azetidine. The compounds are useful for their anti-depressant, anti-convulsant and anxiolytic activities.

Growing community of inventors

Gallarate, Italy

Arturo Della Torre