Provided are sulfonamide compounds having formula (I):

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or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.

Provided herein are benzenesulfonamide derivatives having Formula (III), pharmaceutical compositions comprising said compounds, and method for using said compounds for disrupting proteins/polypeptides, protein/polypeptide function, and for the treatment of diseases through the disruption of proteins or polypeptides involved in the etiology of the disease. Said compounds comprise fluorinated benzene sulfonamide structures.

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Compounds that may selectively inhibit Oplophorus luciferase-derived bioluminescent complexes, e.g., NanoBiT® bioluminescent complex, are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds.

Compounds that may selectively inhibit Oplophorus luciferase-derived bioluminescent complexes, e.g., NanoBiT® bioluminescent complex, are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds.

Disclosed by the present invention are an SIRT6 small-molecule allosteric activator and the application thereof and provided is an SIRT6 small-molecule allosteric activator that contains a derivative as shown in formula (1) or a pharmacologically acceptable salt thereof as the active ingredient. The SIRT6 small-molecule allosteric activator designed and synthesized in the present invention has high efficacy and low toxicity, may significantly activate SIRT6 activity during in vitro experiments, and has great importance in the development of pharmaceuticals for relevant diseases.

Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.

Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.

The present disclosure describes an anti-cancer drug for treating tumor diseases and providing antibacterial, antivirus, and anti-inflammatory effects. The drug contains a naphthalene dicarboxamide compound with a structural formula as shown in Formula I or a biologically acceptable salt or ester form of the compound with the formula I as an active ingredient. The drug is able to help inhibit the growth of tumor cells and possesses certain antibacterial, antivirus, and anti-inflammatory effects. ##STR00001##

This patent document discloses novel compounds and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds. As direct inhibitors of Keap1-Nrf2 interaction, the compounds disclosed herein are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential dmg candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, Parkinson's, and inflammatory bowel disease including ulcerative colitis.

Disclosed herein is a class of molecules termed remodilins that inhibit serum response factor (SRF). By inhibiting SRF, a number of downstream pathways can be targeted. The remodilins can be used to treat glaucoma, inhibit tumor cell growth, inhibit tumor metastasis, inhibit hypoxia-induced response, and/or reduce cellular metabolism.