1, 2, 3, 5 -TETRAHYDROBENZO`C!AZEPIN-4-ONE DERIVATIVES HAVING MUSCARINIC ANTAGONIST ACTIVITY

摘要

There is disclosed a compound having the formula or a pharmaceutically acceptable salt thereof, wherein: R1a, R1b and R1c are independently fluorine or hydrogen; R2 is C1 to C12 alkyl being straight or branched chain, saturated or unsaturated, mono-substituted or unsubstituted, said substituents being selected from piperidine,pyrroliding, morpholine, thiomorpholine and cycloalkyl of 3 to 7 carbon atoms; a cycloalkyl of 3 to 9 carbon atoms; a cycloalkyl of 3 to 9 carbon atoms having a C1 to C6 alkyl substituent; a polycycloalkyl of 2 to 3 rings having 7 to 12 carbons; and phenyl or phenyl substituted with halogen, hydroxy, C1 to C6 alkoxy, C1 to C6 alkyl, nitro, methylene dioxy or trifluoromethyl; and R3 is a moiety selected from: (I), (II) or a pyrrolidin-3-yl moiety of the formula (III). The compounds are disclosed for use as muscarinic antagonists with M3 selectivity.