主权项 |
1. A conjugate having a formula selected from the group consisting of: wherein: R1 and R2 are independently selected from the group consisting of optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, or optionally substituted heteroaryl; Rx is hydrogen or optionally substituted C1-6 alkyl; Z is an optionally substituted bivalent C1-10 hydrocarbon chain, wherein 1, 2, 3, 4 or 5 methylene units of Z are optionally and independently replaced with one or more groups selected from —S—, —O—, —NRa—, —(C═NRa)—, —(C═O)—, —(S═O)—, —S(═O)2—, —(CRb═CRb)—, —(N═N)—, an optionally substituted arylene moiety or an optionally substituted heteroarylene moiety, wherein Ra is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, or a suitable amino protecting group; and Rb is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl; each instance of X is independently —ORc or —N(Rd)2, wherein Rc is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, a suitable hydroxyl protecting group, a cation group, or an affinity ligand, and each Rd is, independently, hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, a suitable amino protecting group, or an affinity ligand, wherein at least two occurrences of X include an affinity ligand selected from aminoethylglucose (AEG), aminoethylmannose (AEM), aminoethylbimannose (AEBM) and aminoethyltrimannose (AETM); Y is hydrogen, halogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, —ORe or —SRe wherein Re is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, or optionally substituted heteroaryl; and n is an integer between 5-25, inclusive; wherein: Rx is hydrogen or optionally substituted C1-6 alkyl; Z is an optionally substituted bivalent C1-10 hydrocarbon chain, wherein 1, 2, 3, 4 or 5 methylene units of Z are optionally and independently replaced with one or more groups selected from —S—, —O—, —NRa—, —(C═NRa)—, —(C═O)—, —(S═O)—, —S(═O)2—, —(CRb═CRb)—, —(N═N)—, an optionally substituted arylene moiety or an optionally substituted heteroarylene moiety, wherein Ra is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, or a suitable amino protecting group; and Rb is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl; each instance of X is independently —ORc or —N(Rd)2, wherein Rc is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, a suitable hydroxyl protecting group, a cation group, or an affinity ligand, and each Rd is, independently, hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, a suitable amino protecting group, or an affinity ligand, wherein at least two occurrences of X include an affinity ligand selected from aminoethylglucose (AEG), aminoethylmannose (AEM), aminoethylbimannose (AEBM) and aminoethyltrimannose (AETM); Y is hydrogen, halogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, —ORe or —SRe wherein Re is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, or optionally substituted heteroaryl; and n is an integer between 5-25, inclusive; and wherein: W is a covalently conjugated drug or detectable label; corresponds to a single or double bond; Rx is hydrogen or optionally substituted C1-6 alkyl; Z is an optionally substituted bivalent C1-10 hydrocarbon chain, wherein 1, 2, 3, 4 or 5 methylene units of Z are optionally and independently replaced with one or more groups selected from —S—, —O—, —NRa—, —(C═NRa)—, —(C═O)—, —(S═O)—, —S(═O)2—, —(CRb═CRb)—, —(N═N)—, an optionally substituted arylene moiety or an optionally substituted heteroarylene moiety, wherein Ra is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, or a suitable amino protecting group; and Rb is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl; each instance of X is independently —ORc or —N(Rd)2, wherein Rc is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, a suitable hydroxyl protecting group, a cation group, or an affinity ligand, and each Rd is, independently, hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, a suitable amino protecting group, or an affinity ligand, wherein at least two occurrences of X include an affinity ligand selected from aminoethylglucose (AEG), aminoethylmannose (AEM), aminoethylbimannose (AEBM) and aminoethyltrimannose (AETM); Y is hydrogen, halogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, —ORe or —SRe wherein Re is hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, or optionally substituted heteroaryl; and n is an integer between 5-25, inclusive. |