BENZIMIDAZOLINYL PIPERIDINES AS CGRP LIGANDS

摘要

A compound of formula I, wherein: R<1> is naphthyl or benzothienyl which is unsubstituted or substituted at up to three substitutable positions independently by C1-6 alkyl, halogen, C1-6 alkoxy, CF3, OCF3, NO2, CN, methylenedioxy or ethylenedioxy; R<2> is hydrogen, C1-8 alkyl, -(CH2)t-aryl wherein aryl is selected from phenyl, biphenyl and naphthyl, -(CH2)t-heteroaryl wherin heteroaryl is selected from tetrazolyl, oxadiazolyl, thiadiazolyl, triazolyl and pyrazinyl, -(CH2)qC(O)OR<6>, -(CH2)qOR<6>, -(CH2)qOC(O)R<6>, -(CH2)qC(O)R<6>, -(CH2)qC(O)(CH2)taryl, -(CH2)qN(R<6>)C(O)R<6>, -(CH2)qC(O)N(R<6>)2, -(CH2)qN(R<6>)SO2R<6>, -(CH2)qN(R<6>)C(O)N(R<6>)2, -(CH2)qOC(O)N(R<6>)2, -(CH2)qN(R<6>)C(O)OR<6>, -(CH2)qN(R<6>)SO2N(R<6>)2 and -(CH2)qS(O)mR<6>; R<3> is NH2; R<4> is hydrogen, C1-6 alkyl, C1-6 alkoxy, halogen, OCF3 or CF3; R<5> is hydrogen, C1-6 alkyl, C1-6 alkoxy, halogen, OCF3 or CF3; R<6> is hydrogen, C1-8 alkyl or C3-7 cycloalkyl, and when two R<6> groups are present and both represent C1-8 alkyl they may optionally together with the atom to which they are both attached form a C3-8 ring; Q is -(CH2)x-C(R<7>)(R<7a>)-(CH2)y- or -(CH2)x-V-(CH2)y-; R<7> and R<7a> are independently chosen from hydrogen, CF3, halogen, C1-6 alkyl and C1-6 alkoxy; V is a C3-8 non-aromatic cyclic or bicyclic ring or an aromatic ring which is benzene or naphthalene, said ring being unsubstituted or substituted at up to three substitutable positions independently by C1-6 alkyl, C1-6 alkoxy, halogen, OCF3, CF3, CN, NO2, methylenedioxy or ethylenedioxy; m is 0, 1 or 2; q is 0, 1, 2, 3 or 4; t is 0, 1, 2 or 3; x and y are independently 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof; useful as CGRP (calcitonin gene-related peptide) receptor ligands, processes for their preparation, their use in therapy, pharmaceutical compositions comprising them and methods of treatment using them.