发明名称 Terminally-functionalized conjugates and uses thereof
摘要 The present disclosure provides inter alia conjugates of formula (I):;wherein n, R1, R2, Rx, Z, X, Y and Z are as defined herein. A conjugate of formula (I) can also be converted to a conjugate of formulae (II) or (III) as described herein. Without limitation, the conjugates can be used to make controlled release materials and chemical sensors.
申请公布号 US9095623(B2) 申请公布日期 2015.08.04
申请号 US201314095068 申请日期 2013.12.03
申请人 SMARTCELLS, INC. 发明人 Zion Todd C.;Lancaster Thomas M.
分类号 A61K39/12;A61K47/48;A61K38/28 主分类号 A61K39/12
代理机构 代理人 Thampoe Immac J.;Reilly John David
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.
地址 Whitehouse Station NJ US