Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists

Abstract

The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, Calkyl, Chaloalkyl, Calkoxy, CD3 or halogen; R3 is hydrogen, C(═O)OR7 or Calkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(═O)R7, C(═O)OR7, C(═O)NR8R9, Calkyl, wherein said Calkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with Calkyl or C(═O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ═CHor a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with Calkyl; R7 is hydrogen or Calkyl; R8 and R9 are independently hydrogen or Calkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments.