Naphth[1,2-d]imidazoles
AssigneeGruppo Lepetit S.p.A.
InventorsAmedeo Omodei-Sale, Emilio Toia
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AssigneeGruppo Lepetit S.p.A.
InventorsAmedeo Omodei-Sale, Emilio Toia
Estimating the term…
Naphth[1,2-d]imidazoles and naphth[2,1-d]oxazoles of formula ##STR1## wherein R and R.sub.1 are hydrogen, halogen, alkyl or alkoxy, R.sub.2 is hydrogen or halogen and A is one of the following moieties ##STR2## wherein R.sub.3 is alkyl, cycloalkyl, or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group in which n is 1,2 or 3, R.sub.5 is hydrogen or alkyl, R.sub.6 is alkyl or R.sub.5 and R.sub.6 taken together with the adjacent nitrogen atom are a 4- to 7-membered saturated hetero ring which may contain a further hetero atom and optionally may be substituted, e.g., with phenyl or substituted phenyl, R.sub.4 is hydrogen, alkyl, cycloalkyl or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group, provided that one of R.sub.3 and R.sub.4 is a --(CH.sub.2).sub.n --NR.sub.5 R.sub.6 group, and R.sub.7 is --(CH.sub.2).sub.n --NR.sub.5 R.sub.6, or a pharmaceutically-acceptable acid addition salt thereof. They are made by contacting a corresponding naphth[1,2-d]imidazole or a naphth[2,1-d]oxazole wherein one of R.sub.3 and R.sub.4 or R.sub.7 is a --(CH.sub.2).sub.n X group wherein X is the residue of a reactive ester with an appropriate amine of the formula HNR.sub.5 R.sub.6 in the presence of an acid acceptor. The new compounds are useful as CNS-depressant agents.
A compound of the formula ##STR14## wherein R and R.sub.1, each independently, are selected from the group consisting of hydrogen, halogen, (C.sub.1 -C.sub.6)alkyl and (C.sub.1 -C.sub.6)alkoxy;
Dependencies are inferred from the claim text.