Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof

    公开(公告)号:US11498921B1

    公开(公告)日:2022-11-15

    申请号:US17499230

    申请日:2021-10-12

    Inventor: Yueheng Jiang

    Abstract: The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. See e.g., Formula I below. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).

    PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF

    公开(公告)号:US20210261543A1

    公开(公告)日:2021-08-26

    申请号:US17231581

    申请日:2021-04-15

    Inventor: Yueheng Jiang

    Abstract: The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).

    EGFR inhibitors
    8.
    发明授权

    公开(公告)号:US12227491B2

    公开(公告)日:2025-02-18

    申请号:US18187430

    申请日:2023-03-21

    Abstract: Provided herein are compounds, salts, solid forms, and pharmaceutical compositions that are related to EGFR inhibitors, such as N-(2-((2-(dimethylanino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-(2,2,2-trifluoroethyl)-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide, as well as methods of preparing the same. Also provided herein are methods of using the compounds, salts, solid forms, and pharmaceutical compositions for the treatment of diseases or disorders, such as cancer.

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