申请人:SUTRO BIOPHARMA, INC.
公开号:US20160257709A1
公开(公告)日:2016-09-08
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, W
1
, W
4
, W
5
, SG, and R are as described herein.
本文提供了半天然菌素衍生物及其共轭物,包含这些衍生物或共轭物的组合物,制备这些衍生物和共轭物的方法,以及使用这些衍生物,共轭物和组合物治疗细胞增殖的方法。这些衍生物,共轭物和组合物在治疗和预防细胞增殖和癌症的方法中有用,用于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。在一个实施例中,半天然菌素衍生物如公式1000所示:或其药学上可接受的盐,溶剂或互变异构体,其中Ar,L,W1,W4,W5,SG和R如本文所述。