发明名称 Dual Acting Prodrugs
摘要 The present invention relates to a prodrug which comprises at least two different pharmaceutically and/or diagnostically active compounds independently bound by cleavable linkers and a protein-binding moiety which is capable of binding to carrier a molecule.
申请公布号 US2016346396(A1) 申请公布日期 2016.12.01
申请号 US201615236691 申请日期 2016.08.15
申请人 KTB Tumorforschungsgesellschaft MBH 发明人 KRATZ Felix;MERFORT Irmgard
分类号 A61K47/48;A61K31/4745;A61K49/00;A61K31/337;A61K31/704;A61K31/4164;A61K38/06 主分类号 A61K47/48
代理机构 代理人
主权项 1. A prodrug comprising (i) at least a first pharmaceutically and/or diagnostically active compound, (ii) at least a second pharmaceutically and/or diagnostically active compound, (iii) two or more cleavable linkers, and (iv) a protein-binding moiety, wherein the first and the second pharmaceutically and/or diagnostically active compounds are each bound to a cleavable linker, and wherein the first and the second pharmaceutically and/or diagnostically active compounds are different from each other, wherein the first pharmaceutically and/or diagnostically active compound is a cytokine, wherein the two or more cleavable linkers can independently be cleaved hydrolytically and/or enzymatically and/or pH-dependently, and wherein the protein-binding moiety binds in situ to cysteine-34 of albumin and is selected from the group consisting of a maleinimide group, a halogenacetamide group, a halogenacetate group, a pyrildylthio group, a vinylcarbonyl group, an aziridin group, a disulfide group, an substituted or unsubstituted acetylene group, or an N-hydroxysuccininide ester group.
地址 Freiburg im Breisgau DE