HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY

    公开(公告)号:EP3892305A1

    公开(公告)日:2021-10-13

    申请号:EP21175538.4

    申请日:2016-01-29

    IPC分类号: A61K47/68 C07K5/02 A61P35/00

    摘要: 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.