| abstract |
The present invention provides diazabicyclooctane derivatives of formula (I):n nand pharmaceutically acceptable salts thereof, wherein the groupn nrepresentsn n R 1 and R 2 are selected independently from H, (C 1 -C 6 )alkyl, (C 1 -C 6 )fluoroalkyl, halogenn(e.g., F, Cl, Br, I), cyano, nitro, O-(C 1 -C 6 )alkyl, O-(C 1 -C 6 )fluoroalkyl, -NHC(O)R 4 and -OR 4 ,nwhere R 4 and R 5 are selected independently from H, (C 1 -C 6 )alkyl, and a 5- to 7-membered arylnor heteroaryl ring, or R 1 and R 2 together with the atoms to which they are attached, form ancarbocyclic 5- or 6-membered ring or a heterocyclic 5- or 6-membered ring; and R 3 is selected from the group consisting of H, (C 1 -C 6 )alkyl, (CH 2 ) m -aryl orn(CH 2 ) m -heteroaryl, wherein m is an integer from 1 to 4, each aryl or heteroaryl group optionallynsubstituted with Cl, Br, CN, CF 3 , O-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, sulfonyl(C 1 -C 6 )alkyl,n-CO(C 1 -C 6 )alkyl, -CONH 2 , -CONH(C 1 -C 6 )alkyl, -CON((C 1 -C 6 )alkyl) 2 , or CH(OH)(C 1 -C 6 )alkyl. n The invention also relates to pharmaceutical compositions of a compound of formulan(I), and methods of use thereof in the treatment of diseases, conditions or disorders of thencentral nervous system. Further, the present invention is also directed to processes for thenpreparation of compounds of formula (I) and intermediates useful therefor. |