6-POSITION-SUBSTITUTED INDOLINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF

Disclosed are a 6-position-substituted indolinone derivative, a preparation method therefor, and a medical use thereof. The present invention belongs to the field of medicinal chemistry; the 6-position-substituted indolinone derivative of the present invention is a CSF-1R inhibitor having a novel st...

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Hauptverfasser: RONG, Quanjin, PAN, Xiang, LV, Qi, HU, Lihong, WANG, Junwei, WANG, Dan
Format: Patent
Sprache:chi ; eng ; fre
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Zusammenfassung:Disclosed are a 6-position-substituted indolinone derivative, a preparation method therefor, and a medical use thereof. The present invention belongs to the field of medicinal chemistry; the 6-position-substituted indolinone derivative of the present invention is a CSF-1R inhibitor having a novel structure. The described derivative has strong CSF-1R inhibitory activity, can achieve immunotherapy for a variety of solid tumors by means of specifically inhibiting the chemotaxis of macrophages to tumors and inducing the repolarization of M2-type TAMs to the M1 phenotype. In particular, the effective dose for the treatment of colorectal cancer is relatively low, and the tumor inhibition rate at the same dose is significantly better than that of PLX3397. In addition, said derivative has a good synergistic effect in combination with a PD-L1 monoclonal antibody. L'invention concerne un dérivé d'indolinone substitué en position 6, son procédé de préparation et son utilisation médicale. La présente invention relève du