10 results about "BRD4" patented technology

The application discloses a new use of a BET inhibitor YD-851 or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating pulmonary fibrosis. The application finds that YD-851 can inhibit the expression of BRD4 and fibrosis-related markers in pulmonary fibrosis tissues, reduce the structural damage of bleomycin-induced mouse lung tissues, inflammatory cell infiltration and fibrosis pathological changes, and improve lung function damage. Experimental results show that YD-851 can reduce the pulmonary fibrosis score, inflammation score and area ratio of consolidation, improve the lung imaging abnormalities, and down-regulate the expression of fibrosis-related genes such as Col1a1, Fn1 and Acta2. It is shown that YD-851 has the effect of treating pulmonary fibrosis, and can be used for preparing a drug for treating pulmonary fibrosis, and a new use of YD-851 is developed.

Provided herein are compositions and methods for treating an autoimmune disease or disorder in a subject. In some cases, the compositions and methods use chemical inducers of proximity (CIPs). In some cases, the CIPs include a first moiety having specific binding for a BTB domain-containing protein or a transcriptional repressor expressed in B cell subpopulations and a second moiety having specific binding for a modulator of gene regulation. In some cases, the BTB domain-containing protein comprises BCL6. In some cases, the transcriptional repressor expressed in B cell subpopulations is PRDM1 or IRF4. In some cases the modulator of gene regulation comprises BRD4, CDK9, and / or p300.

The purpose of the present invention is to provide a compound that has an excellent effect of inducing BRD4 protein degradation and is useful as a cancer therapeutic agent, or a pharmaceutically acceptable salt thereof. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof. [In the formula, each symbol is as defined in the description.]

The present disclosure provides a use of a substance targeting BRD4 in the preparation of a product related to diabetes. In the present disclosure, it is found that the expression of BRD4 in human diabetic beta cells is significantly reduced, and BRD4 plays an important role in maintaining beta cell maturation and differentiation, and long-term and acute BRD4 deficiency can lead to reduced insulin secretion and down-regulation of differentiation markers, highlighting the key role of BRD4 in pancreatic beta cells, providing a target BRD4 that has a significant impact on diabetes, so that substances targeting BRD4 can help to assess the susceptibility of diabetes, screening, prevention, intervention and treatment of diabetes.

Disclosed in the present invention are a compound having a BRD4 inhibitory activity, a preparation method therefor and the use thereof. The structure of the compound having the BRD4 inhibitory activity of the present invention is as shown in formula I, and the definition of each substituent is as described in the description and claims. The compound of the present invention has a high bromodomain protein inhibitory activity, in particular a BRD4-targeting inhibitory activity, and can be used for the treatment and / or prevention of related diseases mediated by bromodomain proteins.

Provided herein are methods of treating cancer using a combination of a compound provided herein (e.g., Compound 1, Compound 2, Compound 3, Compound 4, Compound 5, Compound 6, or Compound 7, or a stereoisomer or mixture of stereoisomers, a pharmaceutically acceptable salt, a tautomer, a prodrug, a solvate, a hydrate, a co-crystal, a clathrate, or a polymorph thereof) and a second active agent. The second active agent is one or more of a PLK1 inhibitor, a BRD4 inhibitor, a BET inhibitor, a NEK2 inhibitor, a AURKB inhibitor, a MEK inhibitor, a PHF19 inhibitor, a BTK inhibitor, a mTOR inhibitor, a PIM inhibitor, an IGF-1R inhibitor, an XPO1 inhibitor, a DOT1L inhibitor, an EZH2 inhibitor, a JAK2 inhibitor, a BIRC5 inhibitor, or a DNA methyltransferase inhibitor.

The application discloses a triazolopyridine bromodomain-containing protein 4 (BRD4) small molecule inhibitor and a preparation method and application thereof, a compound or a pharmaceutically acceptable salt or a racemate thereof, the general formula of which is shown as formula (I). The novel synthetic triazolopyridine compound effectively regulates the occurrence and development process of related diseases by inhibiting the activity of BRD4 protein. In addition to the advantage of inhibiting the activity of BRD4 protein, the compound has good water solubility and liver microsomal stability, which means that it can be better absorbed and distributed in the body, thereby improving the therapeutic effect. The compound also has good drugability, so that it can be better applied to various inflammatory, autoimmune diseases and tumor drugs. The application provides a new choice for the treatment of related diseases and is expected to play an important role in clinical practice.

The purpose of the present invention is to provide a compound that has an excellent effect of inducing BRD4 protein degradation and is useful as a cancer therapeutic agent, or a pharmaceutically acceptable salt thereof. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof. [In the formula, each symbol is as defined in the description.]

This invention discloses a CDK8 / BRD4 dual-target inhibitor, its preparation method, pharmaceutical composition, and applications, relating to the field of medicinal chemistry. The multi-target inhibitory compound designed and synthesized in this invention can effectively inhibit BET and kinase protein activity. The preferred compound has an IC50 value of [missing information]. 50 The concentration can reach nanomolar levels and has excellent anti-proliferative activity against colorectal cancer cells, achieving excellent therapeutic effects at the molecular level, with a very wide range of application prospects; at the same time, the compound preparation method provided by this invention is highly versatile and suitable for various structural types.