CD73 INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

    公开(公告)号:EP4272836A2

    公开(公告)日:2023-11-08

    申请号:EP23196737.3

    申请日:2020-04-27

    IPC分类号: A61P35/00

    摘要: A CD73 inhibitor having the structure represented by formula (I), a preparation method therefor and an application thereof. The series of compounds can be widely applied in the preparation of drugs for treating cancers or tumors that are at least partially mediated by CD73, autoimmune diseases and disorders and metabolic diseases, in particular drugs for treating melanoma, colon cancer, pancreatic cancer, breast cancer, prostate cancer, lung cancer, leukemia, brain tumor, lymphoma, ovarian cancer and Kaposi's sarcoma. A new generation of CD73 inhibitor drugs is expected to be developed.

    FGFR4 INHIBITOR ACID SALT, PREPARATION METHOD THEREFOR, AND USE THEREOF

    公开(公告)号:EP4450499A1

    公开(公告)日:2024-10-23

    申请号:EP22906521.4

    申请日:2022-12-12

    摘要: The present invention relates to an FGFR4 inhibitor acid salt, a preparation method therefor, and a use thereof. The FGFR4 inhibitor is a compound N -((35,45)-3-((6-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(3-methoxy-3-methylazetidin-1-yl)pyrido[3,4- d ]pyrimidin-2-yl)amino)tetrahydro-2 H -pyran-4-yl)acrylamide having the structure represented by formula (I), and the acid salt is p -toluenesulfonate. The physical and chemical properties such as the solubility and bioavailability of the compound represented by formula (I) in the free form are greatly increased, and the development requirements of clinical medicine preparations can be met. The present invention has vital clinical application value for p-toluenesulfonate and has the prospect of developing into a new generation of FGFR4 small-molecule inhibitors.