| abstract |
The NK1 and NK2 receptor antagonist compounds of formula (I) of the present invention are R, phenyl, cycloalkyl or heteroaryl, which may be fused to and substituted with a benzo or cycloalkyl group, wherein the substituents are (substituted) alkyl, (substituted) alkoxy, phenoxy, alkanoyl, alkoxycarbonyl, cycloalkyl, -S (O) m-alkyl, cyano, -NR 2 R 3, -S (O) m NR 2 R 3, -NR 4 alkanoyl and -CONR 2 R 3 or R 2,3-dihydrobenzo [b ] furanyl or chromanyl; R1, R2, R3 and R4 are each independently hydrogen or alkyl, or R2 and R3 together are alkylene; W is a covalent bond or a methylene or ethylene group; X is alkylene; Y is phenyl, naphthyl, benzyl, pyridyl, thienyl or cycloalkyl, which may be substituted, wherein the substituents may be alkyl, alkoxy, fluoro-substituted alkyl or alkoxy, halogen and cyano; Ar is phenyl, naphthyl, benzyl, thienyl, benzo [b] thienyl or indolyl which may be substituted and the substituents may be (substituted) alkyl, (substituted) alkoxy, halo, and cyano, or Ar is 1,3-. benzodioxolan-4-or-5-yl or 1,4-benzodioxan-5 or -6-yl; m is 0, 1 or 2; and ZA is a pharmaceutically acceptable anion. The invention further relates to the preparation of the above compounds, to pharmaceutical compositions containing them, to their use and to their application. HE |