申请人:SUTRO BIOPHARMA, INC.
公开号:US10844090B2
公开(公告)日:2020-11-24
Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000:
or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W1, W4, W5, SG, and R are as described herein.
本文提供了半胱氨酸衍生物、其共轭物、包含其衍生物或共轭物的组合物、生产其衍生物和共轭物的方法,以及使用其衍生物、共轭物和组合物治疗细胞增殖的方法。这些衍生物、共轭物和组合物可用于细胞增殖和癌症的治疗和预防方法、细胞增殖和癌症的检测方法以及细胞增殖和癌症的诊断方法。在一个实施方案中,半马斯特林衍生物符合式 1000:
或其药学上可接受的盐、溶液或同系物,其中 Ar、L、W1、W4、W5、SG 和 R 如本文所述。