Piperidine derivatives, their preparation and use in medicine.

摘要

1. Claims for the Contracting States BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Piperidine derivatives of Formula (I) see diagramm : EP0077427,P8,F1 wherein R represents either a hydrogen atom, or a (C1-4 ) alkyl radical or a hydroxy (C1-4 )alkyl radical, or a (C1-4 )alkoxycarbonyl radical, or a benzyl radical optionally bearing a substituent selected from halogen atoms and (C1-4 )alkoxy radicals, or the phenethyl radical or the 3-phenyl-propyl radical, X represents one or more hydrogen or halogen atoms or (C1-4 )alkyl, (C1-4 )alkoxy, trifluoromethyl, methylenedioxy radicals, or X together with the phenyl ring forms a naphthyl radical, provided that R and X do not represent simultaneously hydrogen atoms, and their pharmaceutically acceptable acid addition salts. 1. Claim for the Contracting State : AT Process for the preparation of piperidine derivatives of Formula (I) see diagramm : EP0077427,P8,F2 wherein R represents either a hydrogen atom, or a (C1-4 ) alkyl radical or a hydroxy (C1-4 )alkyl radical, or a (C1-4 )alkoxycarbonyl radical, or a benzyl radical optionally bearing a substituent selected from halogen atoms and (C1-4 )alkoxy radicals, or the phenethyl radical or the 3-phenyl-propyl radical, X represents one or more hydrogen or halogen atoms or (C1-4 )alkyl, (C1-4 )alkoxy, trifluoromethyl, methylenedioxy radicals, or X together with the phenyl ring forms a naphthyl radical, provided that R and X do not represent simultaneously hydrogen atoms, and their pharmaceutically acceptable acid addition salts, process characterized in that a compound (II) see diagramm : EP0077427,P8,F4 wherein R' represents a protecting radical for the nitrogen, such as a 4-nitro-benzoyl radical, optionally substituted benzoyl radical, optionally substituted benzyl radical or alkyl radical, is reacted with a compound (III) see diagramm : EP0077427,P8,F6 wherein Y represents a reactive radical such as bromine or chlorine ; then the protecting radical R' is either eliminated when it does not correspond to a R radical, or the protecting, optionally substituted, benzoyl group is reduced, either a compound (I) see diagramm : EP0077427,P8,F8 is reacted with a compound RZ, wherein Z is a reactive group, so as to graft the R radical.