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Abstract

The present invention provides diazabicyclooctane derivatives of formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein the group represents ##STR2## R.sup.1 and R.sup.2 are selected independently from H, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)fluoroalkyl, halogen (e.g., F. Cl, Br, I), cyano, nitro, O--(C.sub.1 -C.sub.6)alkyl, O--(C.sub.1 -C.sub.6)fluoroalkyl, --NHC(O)R.sup.4 and --OR.sup.4, where R.sup.4 and R.sup.5 are selected independently from H, (C.sub.1 -C.sub.6)alkyl, and a 5- to 7-membered aryl or heteroaryl ring, or R.sup.1 and R.sup.2 together with the atoms to which they are attached, form a carbocyclic 5- or 6-membered ring or a heterocyclic 5- or 6-membered ring; and R.sup.3 is selected from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, (CH.sub.2).sub.m -aryl or (CH.sub.2).sub.m -heteroaryl, wherein m is an integer from 1 to 4, each aryl or heteroaryl group optionally substituted with Cl, Br, CN, CF.sub.3, O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl, sulfonyl(C.sub.1 -C.sub.6)alkyl, --CO(C.sub.1 -C.sub.6)alkyl, --CONH.sub.2, --CONH(C.sub.1 -C.sub.6)alkyl, --CON((C.sub.1 -C.sub.6)alkyl).sub.2, or CH(OH)(C.sub.1 -C.sub.6)alkyl. The invention also relates to pharmaceutical compositions of a compound of formula (I), and methods of use thereof in the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to processes for the preparation of compounds of formula (I) and intermediates useful therefor.

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First Claim