DIARYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS

摘要

N-diarylaminoalkyl-substituted piperazine/4-aminopiperidine compounds of formula (1) are disclosed, wherein each of A and B is independently a 6-membered aromatic or nonaromatic, carbocyclic or heterocyclic moiety or is an aminoalkyl and wherein one and only one of A and B may be H or alkyl (1-8C) or wherein A and B together form an optionally substituted 6-membered aromatic of nonaromatic, carbocyclic or heterocyclic moiety; R<1> is H or alkyl (1-8C), Z is N or CHNR<2> wherein R<2> is H or alkyl (1-8C), X is straight chain alkylene (1-4C) wherein optionally at least one carbon adjacent to a nitrogen is in the form of C=0; each R<3> is an independent substituent; n=0-2; Ar is a six-membered aromatic or heteroaromatic ring; wherein each cyclic moiety included in A or B each Ar moiety in formula (1) may be substituted by one or more substituents. These compounds and salts or conjugated thereof are able to block N-type and T-type calcium channels and are useful for treating conditions mediated by calcium ion channel activity such as chronic pain.