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    Compounds useful as RET inhibitors
    11.
    发明授权
    Compounds useful as RET inhibitors 有权

    公开(公告)号：US11680068B2

    公开(公告)日：2023-06-20

    申请号：US17738278

    申请日：2022-05-06

    Applicant: Cancer Research Technology Limited

    Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

    IPC: C07D487/04

    CPC classification number: C07D487/04

    Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity:




    wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.

    FUSION PROTEINS WITH ARGINASE ACTIVITY
    16.
    发明申请
    FUSION PROTEINS WITH ARGINASE ACTIVITY 有权

    公开(公告)号：US20220378828A1

    公开(公告)日：2022-12-01

    申请号：US17621182

    申请日：2020-06-29

    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

    Inventor： Francis Jay Mussai ,  Carmela De Santo

    IPC: A61K35/17 ,  C07K14/725 ,  C07K14/705 ,  C07K16/30 ,  C07K16/28 ,  C07K16/18 ,  C12N9/78

    Abstract: The invention relates to fusion target-binding proteins, such as chimeric antigen receptors (CARs), that comprise a target binding moiety, an intracellular signalling region, and an arginase domain. These proteins confer advantages that include improved cell killing and increased proliferation. The invention also relates to nucleic acids encoding the fusion target-binding proteins and cells expressing such proteins. The invention relates to pharmaceutical compositions, medical uses, and methods of treatment, all using the fusion target-binding proteins, cells, or nucleic acids disclosed. The medical uses and methods of treatment are of particular benefit in cancer therapy.

    Compounds Useful as RET Inhibitors
    17.
    发明申请
    Compounds Useful as RET Inhibitors 有权

    公开(公告)号：US20220348585A1

    公开(公告)日：2022-11-03

    申请号：US17738278

    申请日：2022-05-06

    Applicant: Cancer Research Technology Limited

    Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

    IPC: C07D487/04

    Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.

    MODIFIED ANTIBODIES CONTAINING MODIFIED IGG2 DOMAINS WHICH ELICIT AGONIST OR ANTAGONISTIC PROPERTIES AND USE THEREOF
    19.
    发明申请
    MODIFIED ANTIBODIES CONTAINING MODIFIED IGG2 DOMAINS WHICH ELICIT AGONIST OR ANTAGONISTIC PROPERTIES AND USE THEREOF 有权

    公开(公告)号：US20210347907A1

    公开(公告)日：2021-11-11

    申请号：US17327837

    申请日：2021-05-24

    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

    Inventor： Martin J. Glennie ,  Ann White

    IPC: C07K16/28 ,  C07K16/30

    Abstract: Through a combination of in vitro and in vivo approaches, the inventors show that human lgG2 (h2) delivers unique FcγR-independent agonistic activity to anti-CD40 antibodies and to antibodies specific to other immunostimulatory receptors, including 4-1BB and CD28. Investigation of an anti-human CD40 mAb, LOB7.4, revealed that the unique activity of h2 was dependent upon the precise arrangement of hinge and CH1 disulfide bonds. Chemical ‘shuffling’ or mutagenesis to ‘lock’ LOB7.4 into either a more flexible ‘h2A’ or more compact ‘h2B’ conformation endowed antagonistic and agonistic properties, respectively. Engineering of h2 in this way allows development of reagents with either immunostimulatory or immunosuppressive characteristics, with direct implication for the design of therapeutic mAb agents and fusion proteins.

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