| 主权项 |
1. A conjugate of the formula Cys159-linker-inhibitor moiety, wherein the Cys159 is Cys159 of HCV protease, wherein the inhibitor moiety is of formula A: or a pharmaceutically acceptable salt thereof, wherein: one of Ra and Rb is hydrogen and the other is —OH or —OC(O)R′, or Ra and Rb are taken together to form an oxo group; R′ is an optionally substituted group selected from C1-6 aliphatic, C3-7 cycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 4-7 membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R1 is an optionally substituted group selected from C1-6 aliphatic or C3-7 cycloalkyl(C1-3 alkyl); R2 is hydrogen or an optionally substituted group selected from C1-6 aliphatic or C3-7 cycloalkyl; Rx and Ry are taken together to form an optionally substituted C3-7 membered ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R4 is —NHC(O)NHR5, —NHC(O)OR6, or R5 is an optionally substituted group selected from C1-6 aliphatic, bridged bicyclic, 6-10 membered aryl, 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 4-7 membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R6 is an optionally substituted group selected from C1-6 aliphatic, bridged bicyclic, 6-10 membered aryl, 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 4-7 membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R7 is an optionally substituted group selected from C1-6 aliphatic, bridged bicyclic, 6-10 membered aryl, 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 4-7 membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; and R is hydrogen or an optionally substituted group selected from C1-6 aliphatic, C3-7 cycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 4-7 membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur. |
