NOVEL N-SUBSTITUTED PHENOTHIAZINES AND THEIR USE AS MODULATORS OF SERINE HYDROLASE ENZYMES

摘要

The present invention is directed to phenothiazine compounds of formula (I), wherein R is: (a) a branched or straight chain (C1-C6)alkyl group unsubstituted or substituted by phenyl, halo or -NR1R2, wherein R1 and R2 are independently H, a branched or straight chain (C1-C6)alkyl group or R1 and R2 together with the nitrogen atom to which they are bonded form a 5- or 6-membered ring; (b) phenyl; or (c) -NR3R4, wherein R3 and R4 are independently; (i) H, (ii) a branched or straight chain (C1-C6)alkyl group unsubstituted or substituted by (C1-C4)alkoxy, phenyl or -NR5R6, wherein R5 and R6 are independently H, a branched or straight chain (C1-C4)alkyl group, phenothiazine carbonyl or R5 and R6 taken together with the nitrogen atom to which they are bonded form a 5- or 6-membered ring; (v) a (C5-C6)cycloalkyl group; or (iv) R3 and R4 together with the nitrogen atom to which they are bonded form pyrrolidino, piperidino, morpholino, piperazino or 4-methylpiperazino, or a pharmacologically acceptable salt thereof, for use in the treatment of Alzheimer's disease and other conditions. Compounds of formula (I) modulate the activity of serine hydrolase enzymes, for example, they are cholinesterase inhibitors.