α-aminocyclolactam ligands for G-protein coupled receptors

A pharmaceutical composition comprising, as active ingredient, a compound of formula (I):

• wherein y is any integer from 1 to 8;
• z is any integer from 1 to 8 with the proviso that y and z cannot simultaneously be 1;
• X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n;
• k is 0 or 1;
• Y is a cycloalkyl, polycyloalkyl, cycloalkenyl or polycycloalkenyl group;
• each R1 is independently selected from an alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl, or charged alkylcarboxylate radical of 1 to 20 carbon atoms;
• or each R1 is independently selected from charged aminotrialkyl, or carboxylate radical;
• and
• n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y;
• and, where R1 is charged, one or more suitable counter-ions are present,
• or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient and/or carrier.

A compound of formula (II)

• wherein:
• the bridge Q in formula (II) represents a bridging group independently selectable from the group consisting of alkenylene and alkylene substituted by halo, amino, aminoalkyl, aminodialkyl, charged trialkylamino, charged carboxylate or hydroxy moieties having a carbon chain length of from 1 to 8;
• z is any integer from 1 to 8;
• X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n;
• k is 0 or 1;
• Y is a cycloalkyl, polycyloalkyl, cycloalkenyl or polycycloalkenyl group;
• each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms;
• or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical;
• and
• n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y;
• or
• alternatively R1 may be a peptido radical having from 1 to 4 peptidic moieties linked together by peptide bonds;
• wherein the 1 to 4 peptidic moieties are selected from the 20 naturally occurring amino acids
• and, where one or more of R1 and the bridging group is charged, one or more suitable counter-ions are present.