Peptide-drug conjugates

申请公布号：

US9579317(B2)

申请号：

US201514726897

申请日期：

2015.06.01

申请公布日期：

2017.02.28

申请人：

Jiarui Biopharmaceuticals, Ltd.

发明人：

Chu Shaosong

分类号：

A61K38/00;A61K47/00;A61K38/14;C07K9/00;A61K38/06;C07K5/00;C07K7/00;C07K16/00;C07K17/00;A61K31/4745;A61K31/407;A61K31/704;A61K47/48

主分类号：

A61K38/00

代理机构：

Fish & Richardson P.C.

代理人：

Fish & Richardson P.C.

地址：

Yixing CN

摘要：

Peptide-drug conjugates comprising p-aminobenzyl carbamoyl or p-aminobenzolyl carbonate self-immolating linkers are disclosed. The peptide-drug conjugates comprise a peptide moiety that can be cleaved by cellular proteases, bound to the self-immolating linker, which linker is bound to a cytotoxic drug moiety. Upon cleavage of the peptide moiety, the linker self-immolates, releasing the cytotoxic drug in active form. Dimeric structures of the peptide drug conjugates comprising two molecules of cytotoxic drug per conjugate are also disclosed.

主权项：

1. A peptide-drug conjugate, which is Nα-succinamic acid-Ala-Ala-Asn-PABC-mitomycin; or a pharmaceutically acceptable salt thereof, wherein the mitomycin is bonded to PABC at a C-1″ aziridine nitrogen of the mitomycin; and PABC is a p-aminobenzyl carbamoyl linker moiety.