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The new chemical space has the potential to generate new functions and properties previously not available.
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Functionalized Azaborine Compounds for Disease Therapy Background: Boron-containing compounds have recently received significant attention in the synthetic community. In particular, the strategy of substituting the organic C=C unit with the isosteric inorganic B-N bond in organic molecules (BN/CC isosterism) has emerged as a viable strategy for broadening the chemical diversity of compounds relevant to materials science and biomedical research. The new chemical space has the potential to generate new functions and properties previously not available. Invention: Azaborines are isostructural (have the same structure) and isoelectronically (have the same number of electrons) equivalent to benzene. The invention provides: 1) novel methods for syntheses and functionalization of azaborine compounds, azaborine-containing biarylcarboxylic acids and biarylcarboxamides, and 2) their bioactivities and ADME (absorption, distribution, metabolism, and excretion) information. These novel azaborine-containing compounds show unique physical and biological properties when compared to their corresponding all-carbon compounds, and have potential to be used for disease therapies and treatment and as well as in materials science. Features/Advantages of the Compounds: Possess aromaticity, fluorescence properties, water and air stability Show unique biological properties including: nanomolar biological activity, improved solubility, reduced toxicity, novel metabolism, and new binding modes Applications: Compounds may be used as: Basic research tools, building blocks for biologically active compounds, therapeutic agents in human health, chemical compounds in material science Publication: J. Am. Chem. Soc. 2015, 137, in press, Angew. Chem. Int. Ed. 2013, 52, 2599-2601. Angew. Chem. Int. Ed. 2009, 48, 6817-6819. Lead Inventor: Shih-Yuan Liu, Professor, Department of Chemistry, Boston College Patent Information: Patent Cooperation Treaty (PCT) Application has been filed Licensing Status: Available for exclusive or non-exclusive license Looking for Partners: For sponsored collaboration research to develop and commercialize this invention