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 US2014294851(A1) 申请公布日期 2014.10.02
申请号 US201313854296 申请日期 2013.04.01
申请人 NGUYEN MARK QUANG 发明人 NGUYEN MARK QUANG
分类号 A61K47/48;A61K45/06 主分类号 A61K47/48
代理机构 代理人
主权项 1. A compound of Formula (II):or a salt thereof, wherein: each A1 is independently selected from a thiol-reactive group, an amine-reactive group, an avidin-binding group, a photoreactive group, an alkyne-reactive group, and an azide-reactive 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—, —N—, —N═, —N═N—, —N═C—, —SO—, —SO2—, —SO2N—, —SS—, —C(O)—, —C(O)O—, —C(O)N—, —C(O)S—, —C(O)N—N═, —OP(O)(OH)O—, —OC(O)O—, —OC(O)N—, —NC(O)N—, and —NC(S)N; 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; D is selected from a 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; and n5 is an integer selected from 1 to 20.
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