HETEROCYCLIC DERIVATIVE AND USE THEREOF
    6.
    发明公开

    公开(公告)号:EP4036086A1

    公开(公告)日:2022-08-03

    申请号:EP20868130.4

    申请日:2020-09-23

    摘要: Disclosed are a TAM family kinase /and Ron kinase inhibitor compound as shown in general formula (I), a pharmaceutically acceptable salt, an ester, a stereoisomer and a tautomer thereof, a pharmaceutical composition and a pharmaceutical preparation containing same, and the use thereof. The compound can selectively inhibit TAM family tyrosine kinase /and Ron kinase, and can be used for the treatment and/or prevention of diseases mediated by the abnormal expression of a receptor of TAM family kinase /and Ron kinase and/or a ligand thereof. By means of targeted inhibition of the TAM family kinase /and Ron kinase, the compound can reverse the immunosuppressive environment in a tumor microenvironment, inhibit the growth, migration and/or drug resistance performance of tumors, and exert anti-tumor immunological effects and anti-tumor efficacy.

    The definition of each group in the formula is described in the specification.

    NOVEL USE OF MULTIKINASE INHIBITOR
    7.
    发明公开

    公开(公告)号:EP4112619A1

    公开(公告)日:2023-01-04

    申请号:EP21760436.2

    申请日:2021-02-23

    摘要: The present invention belongs to the technical field of medicines, relates to novel use of a multi-kinase inhibitor, and particularly relates to a compound of general formula (I) or a pharmaceutically acceptable salt, or a stereoisomer or a crystal form thereof for use in the treatment of biliary tract cancer, a pharmaceutical composition comprising the compound, a method for treating biliary tract cancer by using the compound, use of the compound in the treatment of biliary tract cancer, and use of the compound in the preparation of a medicament for treating biliary tract cancer. The variables in the general formula are defined in the specification. Research shows that the multi-kinase inhibitor compound of general formula (I) or the pharmaceutically acceptable salt, or the stereoisomer or the crystal form thereof have a treatment effect on biliary tract cancer, and especially on cholangiocarcinoma, so that the compound of the present invention has huge clinical application potential.

    PDE9 INHIBITOR AND USE THEREOF
    8.
    发明公开

    公开(公告)号:EP3915992A1

    公开(公告)日:2021-12-01

    申请号:EP20744765.7

    申请日:2020-01-20

    发明人: WU, Frank

    摘要: The present invention relates to the technical field of pharmaceuticals, and particularly to a PDE9 inhibitor compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a deuterated compound, a metabolite or a prodrug thereof. The present invention also relates to pharmaceutical formulations, pharmaceutical compositions and use thereof. X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , ring A, L and m are as defined in the specification. The compound of the present invention can be used in the manufacture of a medicament for treating or preventing a PDE9-mediated related disease.