Pfizer Corporation

Christopher John Burns

David Alker

Sandra Marina Monaghan

Quaternary ammonium compounds

The present invention provides a compound of formula (I) wherein R is phenyl, C,-C,cycloalkyl or heteroaryl, each of which being optionally benzo- or C,-C,cycloalkyl-fused and optionally substituted, including in the benzo- or C,-C,cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C,-C,alkyl, fluoro(C,-C,)alkyl, C,-C,alkoxy, fluoro(C,-C,)alkoxy, phenoxy, C,-C,alkanoyl, halo, C,-C,alkoxycarbonyl, C,-C,cycloalkyl, &mdash;S(O),(C,-C,alkyl), cyano, &mdash;NR,R,, &mdash;S(O),NR,R,, &mdash;NR,(C,-C,alkanoyl) and &mdash;CONR,R,, or R is 2,3-dihydrobenzo&lsqb;b&rsqb;furanyl or chromanyl; R,is H or C,-C,alkyl; W is a direct link, methylene or ethylene; X is unbranched C,-C,alkylene; Y is phenyl, naphthyl, benzyl, pyridyl, thienyl or C,-C,cycloalkyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C,-C,alkyl, fluoro(C,-C,)alkyl, C,-C,alkoxy, fluoro(C,-C,)alkoxy, halo and cyano; Ar is phenyl, naphthyl, benzyl, thienyl, benzo&lsqb;b&rsqb;thienyl or indolyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C,-C,alkyl, fluoro(C,-C,)alkyl, C,-C,alkoxy, fluoro(C,-C,)alkoxy, halo and cyano, or Ar is 1,3-benzodioxolan-4 or 5-yl or 1,4-benzodioxan-5 or 6-yl; Z,is a pharmaceutically acceptable anion; with the proviso that when W is a direct link and R is optionally fused and optionally substituted heteroaryl, said heteroaryl is linked by a ring carbon atom to the carbonyl group. The compounds are tachykinin antagonists.

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Sydney, Australia

Christopher John Burns