Patent ID: 8043601

Claim:
A cycloazapeptide of formula Z: wherein: each Q 1 , Q 2 , Q 3 , Q 4 and Q 5 is independently —CH— or N, provided that at least one Of Q 1 , Q 2 , Q 3 , Q 4 and Q 5 is N; R 1 is hydrogen or is selected from the group consisting of a side chain of a natural amino acid and a side chain of an unnatural amino acid; R 2 and R 3 are each independently selected from the group consisting of —H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkoxyalkyl, aryl, aryl-(C 1 -C 6 alkylene)-, 3- to 7-membered carbocycle, 3- to 7-membered heterocycle, hydroxy-C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy-C 1 -C 6 -alkyl, wherein the alkyl, alkenyl, alkynyl, alkyloxy, alkoxyalkyl, aryl, carbocycle and heterocycle groups are each optionally substituted; R 7 is absent or is selected from the group consisting of H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, aryl, aryl-(C 1 -C 6 alkylene)-, a 3- to 7-membered carbocycle, and a 3- to 7-membered heterocycle, wherein the alkyl, alkenyl, alkynyl, aryl-alkylene, carbocycle and heterocycle groups are each optionally substituted; wherein R 2 , R 3 and R 7 are not all H; R 8 is hydrogen or is selected from the group consisting of a side chain of a natural amino acid and a side chain of an unnatural amino acid; X is a 5 or 6-membered heterocycle or a linker comprising a hydrophilic moiety selected from the group consisting of hydroxyl, carbonyl, amide (—C(O)NH—), sulfonamide, sulfonate, phosphate, polar amino acid moiety, PEG moiety, sugar mimetic and sugar moiety, or a combination thereof; Y is a 5 or 6-membered heterocycle or a linker comprising a hydrophilic moiety selected from the group consisting of hydroxyl, carbonyl, sulfonamide, sulfonate, phosphate, polar amino acid moiety, PEG moiety, sugar mimetic and sugar moiety; where at least one of X and Y is a 5 or 6-membered heterocycle; and w is 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof, optionally in the form of a single stereoisomer or mixture of stereoisomers thereof.