发明名称 CLEAVABLE DRUG CONJUGATES, COMPOSITIONS THEREOF AND METHODS OF USE
摘要 Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.
申请公布号 US2016129027(A1) 申请公布日期 2016.05.12
申请号 US201614986620 申请日期 2016.01.01
申请人 Nguyen Mark Quang 发明人 Nguyen Mark Quang
分类号 A61K31/704;A61K47/48;A61K31/136;A61K45/06 主分类号 A61K31/704
代理机构 代理人
主权项 1. A compound of Formula (III): or a pharmaceutically acceptable salt thereof, wherein: Q is selected from a ligand having at least one thiol group, a ligand having at least one primary amine group, a ligand having at least one secondary amine group, ligand having at least one biotin-binding group, a ligand having at least one photoreactive group, a ligand having at least one alkyne group, and a ligand having at least one azide group;each Y is independently selected from a covalent bond and a hydrogen bond;each A2 is independently selected from a covalent bond, an amide group, an avidin-binding group, a carbamate group, a carbonyl group, a disulfide group, an ester group, a hydrazone group, an imine group, a succinimide group, a sulfonamide group, a sulfone group, a sulfoxide group, a thioether group, a triazole group, and a urea group;each X1 and X3 is independently selected from a covalent bond, C1-20 alkanediyl, substituted C1-20 alkanediyl, C1-20 heteroalkanediyl, substituted C1-20 heteroalkanediyl, C3-12 cycloalkanediyl, substituted C3-12 cycloalkanediyl, C3-12 heterocycloalkanediyl, substituted C3-12 heterocycloalkanediyl, C4-20 alkanecycloalkanediyl, substituted C4-20 alkanecycloalkanediyl, C4-20 heteroalkanecycloalkanediyl, substituted C4-20 heteroalkanecycloalkanediyl, C6-20 arenediyl, substituted C6-20 arenediyl, C6-20 heteroarenediyl, substituted C6-20 heteroarenediyl, C7-20 alkanearenediyl, substituted C7-20 alkanearenediyl, C6-20 heteroalkanearenediyl, substituted C6-20 heteroalkanearenediyl, and —(CH2)n1—(CH2—CH2—O)n2—(CH2)n3—, wherein: each n1 and n3 is independently an integer selected from 0 to 5; andeach n2 is independently an integer selected from 1 to 25;each X2 is independently selected from a covalent bond, —O—, —S—, —NH—, —N═, —N═N—, —N═CH—, —SO—, —SO2—, —SO2NH—, —SS—, —C(O)—, —C(O)O—, —C(O)NH—, —C(O)S—, —C(O)NH—N═, —OP(O)(OH)O—, —OC(O)O—, —OC(O)NH—, —NHC(O)NH—, and —NHC(S)NH—;each R1 and R2 is independently selected from hydrogen, C1-6 alkyl, substituted C1-6 alkyl, C1-6 heteroalkyl, substituted C1-6 heteroalkyl, C6-10 aryl, substituted C6-10 aryl, C6-10 heteroaryl, and substituted C6-10 heteroaryl;each D is independently selected from therapeutic agent having at least one primary amine group, a therapeutic agent having at least one secondary amine group, a therapeutic agent having at least one hydroxy group, and a therapeutic agent having at least one thiol group; andn6 is an integer selected from 1 to 20.
地址 San Jose CA US