83 results about "Stat3 inhibitor" patented technology

Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and / or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and / or non-inhibition of Stat1 activity are also described herein.

The invention discloses an STAT3 small molecular selective inhibitor and a preparation method and applications thereof, and the STAT3 small molecular selective inhibitor comprises four structure general formulae as shown in formula I, formula II, formula III and formula IV. The preparation comprises the following steps: allowing 2-phenyl substituted quinoline-4-carboxylic acid thionyl chloride or oxalyl chloride to react to generate substituted acyl chloride, reacting with substituted arylamine to generate substituted quinoline-4-amide derivatives. The applications comprise an application in the preparation of medicaments for treating cancers related to abnormally-activated STAT3 pathway, and an application in the preparation of antitumor medicaments where the STAT3 small molecular selective inhibitor is used as an inhibitor of the STAT3 signal pathway. The STAT3 inhibitor of the invention is a small molecular selective inhibitor; based on results obtained by detecting its effect on cancer cells and evaluating its activity, the small molecular STAT3 selective inhibitor of the invention is applicable to the development of related cancer-treatment medicaments, has quite wide applications, and has very good medicine curative effect. The small molecular STAT3 selective inhibitor of the invention has various types, easily available raw materials, a simple preparation method, high product purity, high yield, and strong practicality.

The invention relates to the application of compounds possessing STAT3 inhibitor activity shown in general formula I, isomers and a drug compound containing the compounds and isomers in the prevention or treatment of malignant tumors, AIDS and inflammations and the termination of unexpected pregnancies or the application of tool drugs used for studying the growth, proliferation, differentiation and apoptosis of tumors as well as STAT3-related signaling pathways.

Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed.

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head / neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

Described herein, inter alia, are STAT-binding nucleic acids-including compositions and methods of using the same.

The invention belongs to the technical field of medicine and pharmacy, and discloses an application of a micromolecule compound WZ-2-033 shown as below to medicines for treating breast cancer and stomach cancer. The compound can restrain proliferation, clone formation, migration and invasion of breast cancer cells and stomach cancer cells, and can induce apoptosis of the breast cancer cells and the stomach cancer cells. The compound exerts effects through influencing an STAT3 signal channel, can reduce the phosphorylation level (Y705) of the STAT3, can reduce STAT3 dimer formation, can reduceDNA combining capacity and transcriptional activity of the STAT3, and can further reduce the expression level of STAT3 target genes c-Myc, Bcl-xL and Mcl-1 so as to restrain activation of STAT3 signals and restrain the growth of the breast cancer cells and the stomach cancer cells. In an animal model, the compound can restrain the growth of stomach cancer cell transplanted tumors and has favorableapplication prospects.

The present invention includes methods for the treatment of autoimmune disorders such as autism, schizophrenia, and type 1 diabetes. Flavonoids, luteolin, diosmin, and diosmin's aglycone form, diosmetin, were found to inhibit activation / phosphorylation of STAT3 induced by IL-6 in cultured neuronal cells. Furthermore, mice treated with diosmin showed a significant reduction of autistic phenotype induced by IL-6 through inhibition of STAT3 activation.

The present invention provides small molecules useful to affect cancer cells, along with related methods. The present compounds, formulations, kits and methods are useful for a variety of research, diagnostic and therapeutic purposes. STAT3 inhibitors, particularly LLL12, are disclosed. The STAT3 inhibitors are useful to treat breast cancer in general and breast cancer initiating cells in particular.

The invention discloses a heteroaromatic amide compound and a preparation method and application thereof. According to the heteroaryl amide compound provided by the invention, a preliminary activity research shows that the compound has selectivity to STAT3 and also has very strong tumor cell proliferation inhibition activity; the compound can be used as a series of novel STAT3 inhibitors and can be used for preparing drugs for treating corresponding diseases. The compound has obvious killing effect on human cancer cells, especially human breast cancer cell line MDA-MB-231, human prostate cancer cell line PC-3 and human prostate cancer cell line DU-145, has the potential of being prepared into novel antitumor drugs, and has better market prospect.