Abstract
A method for preparing a series of exatecan derivatives containing a hydroxylamine structure substitution and pharmaceutically acceptable salts thereof, and the use thereof in the field of anti-tumor are provided. These exatecan derivatives not only have a good activity of inhibiting the growth of tumor cells, but also have a good capability of permeating cell membranes or bystander effect, and can be used as monotherapy, combination therapy, or as toxin components of ADC for the treatment of tumors.
Full Text
What is claimed is:
A method for preparing a series of exatecan derivatives containing a hydroxylamine structure substitution and pharmaceutically acceptable salts thereof, and the use thereof in the field of anti-tumor are provided. These exatecan derivatives not only have a good activity of inhibiting the growth of tumor cells, but also have a good capability of permeating cell membranes or bystander effect, and can be used as monotherapy, combination therapy, or as toxin components of ADC for the treatment of tumors.
Timeline
Filed
03/13/2026Published
07/16/2026Granted
Not AvailableIPC Codes(5)
C07D 491/22:in which the condensed system contains four or more hetero rings
A61K 31/4745:condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines (yohimbine derivatives, vinblastine A61K 31/475; ergoline derivatives A61K 31/48)
A61K 47/68:the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment