| 摘要 |
LIGANDS FOR G-PROTEIN COUPLED RECEPTORS Abstract X N NH (1) The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I) wherein y is any integer from 1 to 8; z is one integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1; X is -CO-(Y)k-(R'), or S0 2 -(Y)k-(R'),,; k is 0 or 1; y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or y is a 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 I to 20 carbon atoms; or each R' is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and n is any integer from I to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or alternatively R' may be selected from a peptido radical, for example having from I to 4 peptidic moieties linked together by peptide bonds (for example a peptido radical of I to 4 amino acid residues). 5614259_1 |
