| abstract |
The present invention provides diazabicyclooctane derivatives formula (1): (see formula) and pharmaceutically acceptable salts thereof, wherein the group: represents (see formula) R1 and R2 are independently selected from H, alkyl of 1 to 6 atoms of carbon, fluoroalkyl of 1 to 6 carbon atoms, halogen (for example, F, CI, Br, l), cyano, nitro, O-alkyl of 1 to 6 carbon atoms, O-fluoroalkyl of 1 to 6 carbon atoms , -NHC (O) R4 and ûOR56, wherein R4 and R5 are independently selected from H, alkyl of 1 to 6 carbon atoms, and an aryl or heteroaryl ring of 5 to 7 members or Rl or R 2 together with the atoms to which they are attached, form a carbocyclic ring of 5 or 6 members, or a heterocyclic ring of 5 to 6 members; and R3 is selected from the group consisting of H. alkyl of 1 to 6 carbon atoms, (CH2) m aryl or (CH2) m heteroaryl wherein m is an integer from 1 to 4, each aryl or heteroaryl group optionally substituted with CI, Br, CN, CF3, O-alkyl of 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, sufonyl alkyl of 1 to 6 carbon atoms, -CO-alkyl of 1 to 6 carbon atoms, - CONH2, -CONH-alkyl of 1 to 6 carbon atoms-CON (alkyl of 1 to 6 carbon atoms) 2, or CH (OH) -alkyl of 1 to 6 carbon atoms. The invention relates to pharmaceutical compositions of a compound of the formula (1) and methods of use thereof in the treatment of diseases, conditions or disorders of the central nervous system. In addition, the present invention is directed to processes for the preparation of compounds of the formula (1) and useful intermediates for them. |