2-Arylsubstituted benzimidazoles, quinoxalines, in 3,5-position substituted 2,6-dimethylpyridines, and 1,4-bis(alkylamino)-9,10-anthracenediones are easily prepared under mild conditions by means of benzofuroxan as oxidant. Thus, the preparation of 2-arylbenzimidazoles succeeds in acetonitrile at 50-degrees-C in yields of 65 to 78 %.
Nanoparticles for chemotherapy, targeted therapy, photodynamic therapy, immunotherapy, and any combination thereof
申请人:The University of Chicago
公开号:US11246877B2
公开(公告)日:2022-02-15
Prodrugs containing lipid moieties attached to drug derivatives, such as anti-cancer drug derivatives, via linkers comprising disulfide groups are described. Also described are nanoparticles coated with a lipid layer containing the prodrugs, formulations comprising the nanoparticles, and the use of the nanoparticles in methods of treating diseases, such as cancer, alone or in combination with additional drug compounds, targeting agents, and/or immunotherapy agents, such as immunosuppression inhibitors that target the CTLA-4, PD-1/PD-L1, IDO, LAG-3, CCR-7 or other pathways, or multiple immunosuppression inhibitors targeting a combination of such pathways. Optionally, the nanoparticles can comprise a photosensitizer or a derivative thereof and can be used in methods involving photodynamic therapy. Synergistic therapeutic effects result from combinations of multiple modalities provided by the disclosed nanoparticles and/or nanoparticle formulations.
An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.
NANOPARTICLES FOR CHEMOTHERAPY, TARGETED THERAPY, PHOTODYNAMIC THERAPY, IMMUNOTHERAPY, AND ANY COMBINATION THEREOF
申请人:The University of Chicago
公开号:US20190269706A1
公开(公告)日:2019-09-05
Prodrugs containing lipid moieties attached to drug derivatives, such as anti-cancer drug derivatives, via linkers comprising disulfide groups are described. Also described are nanoparticles coated with a lipid layer containing the prodrugs, formulations comprising the nanoparticles, and the use of the nanoparticles in methods of treating diseases, such as cancer, alone or in combination with additional drug compounds, targeting agents, and/or immunotherapy agents, such as immunosuppression inhibitors that target the CTLA-4, PD-1/PD-L1, IDO, LAG-3, CCR-7 or other pathways, or multiple immunosuppression inhibitors targeting a combination of such pathways. Optionally, the nanoparticles can comprise a photosensitizer or a derivative thereof and can be used in methods involving photodynamic therapy. Synergistic therapeutic effects result from combinations of multiple modalities provided by the disclosed nanoparticles and/or nanoparticle formulations.
Dehydrogenations Using Benzofuroxan as Oxidant
作者:F. Pätzold、F. Zeuner、Th. Heyer、H.-J. Nielas
DOI:10.1080/00397919208021304
日期:1992.1
2-Arylsubstituted benzimidazoles, quinoxalines, in 3,5-position substituted 2,6-dimethylpyridines, and 1,4-bis(alkylamino)-9,10-anthracenediones are easily prepared under mild conditions by means of benzofuroxan as oxidant. Thus, the preparation of 2-arylbenzimidazoles succeeds in acetonitrile at 50-degrees-C in yields of 65 to 78 %.