Piperazine derivatives, their preparation and uses

专利名称：Piperazine derivatives, their preparation and

uses in therapy (5ht1b receptor activity)

发明人：Howard Marshall,Mervyn Thompson,Paul

Adrian Wyman

申请号：US10471432申请日：20040309

公开号：US20040132720A1公开日：20040708

摘要：Compounds of formula (I) or a pharmaceutically acceptable salt thereof aredisclosed: in which Ris a group of formula (i) wherein Pis phenyl, naphthyl or heteroaryl;Ris halogen, Calkyl, Ccycloalkyl, COCalkyl, Calkoxy, hydroxy, hydroxyCalkyl, nitro,haloCalkyl, cyano, SR, SOR, SOR, SONRR, COR, CONRR, OCONRCOR, NRr, NRCOR, NRCOR,NRSOR, NRCONRR, CHNRCOR, CHNRCOR, CHNRSOR, CR═NORwhere R, Rand Rareindependently hydrogen or Calkyl, a is 1, 1, 2, or 3; or Ris a group of formula (ii) where Pisphenyl, naphthyl, heteroaryl or a 5 to 7 membered heterocyclic ring; Pis phenyl, naphthylor heteroaryl; Ris a defined above for Rin formula (I) or Ris heteroaryl optionallysubstituted By Calkyl, halogen or COCalkyl or is a 5-7 membered heterocyclic ringoptionally substituted by oxo; Ris halogen, Calkyl, Ccycloalkyl, Calkyl, COCalkyl, hydroxy,intro, haloCalkyl, cyano, COR, CONRR, NRRwhere Rand Rare as defined above; b and c areindependently 0, 1, 2, or 3; Y is a single bond, CHor NH; X is oxygen, sulfur or N—RwhereRis hydrogen or Calkyl; Ris hydrogen, halogen, Calkyl, haloCalkyl, COCalkyl or cyano; Rishydrogen or Calkyl. Processes for their preparation, pharmaceutical compositionscontaining them and their use in therapy as 5-HTreceptor antagonists, for diseases such

as depression, are also disclosed.

申请人：MARSHALL HOWARD,THOMPSON MERVYN,WYMAN PAUL ADRIAN

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