32 results about "BET inhibitor" patented technology

The present invention relates to covalent conjugates of BET inhibitors and alpha amino acid esters, processes for their preparation, compositions containing them, and to their use in the treatment of various disorders in particular inflammatory and autoimmune diseases, such as rheumatoid arthritis; and cancers.

The present disclosure provides BET inhibitors of the formula: wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of treating a patient comprising administering a bromo- and extra-terminal (BET) domain inhibitor for the treatment of FSHD which modulates DUX4 expression. In some embodiments, the present methods comprise using one or more BET inhibitors as a therapeutic agent for the treatment of FSHD patients including patients who are being treated with one or more palliative treatments such as therapy and / or agents which lead to increased muscle mass.

The invention relates to application of a BET inhibitor BMS-986158, in particular to application of the BET inhibitor BMS-986158 in preparation of an anti-HIV-1 medicine. Researches show that the BET inhibitor BMS-986158 can be used for remarkably activating expression of HIV-1 in an HIV-1 latent cell line J-Lat, OM10.1 and ACH2 cells; when the the BET inhibitor BMS-986158 is combined with other types of latent activators, a synergistic effect is shown; the activation effect is not influenced by anti-HIV drugs, and activities of the anti-HIV drugs can be improved; and in peripheral blood mononuclear cells separated from a body of an HIV-1 patient receiving ART treatment for a long time, the BMS-986158 also shows a remarkable latent activation effect. Toxicity experiment of the BMS-986158 on PBMC shows that CC50 is greater than 100 [mu] M, indicating that the BMS-986158 less toxic to cells. The BMS-9861658 has low toxicity and high latent activation HIV-1 activity, and can enhance an antiviral effect of an anti-viral drug in vitro. Therefore, the BMS-9861658 can be used for preparing an anti-HIV-1 latency medicine and can be combined with an anti-HIV medicine to be used for treating the AIDS, and a new intervention way and strategy are provided for thoroughly curing AIDS.

The invention relates to the field of immunotherapy, more in particular to a composition for use in the treatment of cancer. The invention also relates to a composition obtainable by such a method, such as a pharmaceutical composition. More in particular, the invention relates to an ex vivo method for obtaining a composition suitable for the treatment of cancer in a subject, comprising the steps of providing primary tumor cells derived from the subject, and ex vivo contacting the tumor cells with an inhibitor of a bromodomain and extra-terminal domain family member (BET inhibitor).

Bromodomain and extra terminal protein (BET) resistant leukemic cell lines and methods for producing such cell lines are described as are methods for using such cell lines in screening assays to identify therapeutic agents. The cell lines can be generated from haematopoietic stem and progenitor cells (HSPCs) that are clonally enriched by serially exposing c-kit positive cells to a BET inhibitor.

The invention discloses a tetravalent platinum complex containing a BET inhibitor. The structure of the tetravalent platinum complex is as shown in a general formula I, wherein substituent groups are defined in the specification. The advantages of the tetravalent platinum complex are utilized, and the synergistic anti-tumor effect of the BET inhibitor and cis-platinum is exerted. The tetravalent platinum complex containing the BET inhibitor shows broad-spectrum and excellent in-vitro anti-tumor activity, the activity of the tetravalent platinum complex is obviously superior to that of cis-platinum, the BET inhibitor and the mixture of the cis-platinum and the BET inhibitor according to the ratio of 1: 1, and the tetravalent platinum complex has huge potential of being developed into a novel broad-spectrum anti-tumor drug.