131747-68-7Relevant articles and documents
Versatility of Terpyridine-Functionalised Aryl Tetrazoles: Photophysical Properties, Ratiometric Sensing of Zinc Cations and Sensitisation of Lanthanide Luminescence
Wright, Phillip J.,Kolanowski, Jacek L.,Filipek, Wojciech K.,Lim, Zelong,Moore, Evan G.,Stagni, Stefano,New, Elizabeth J.,Massi, Massimiliano
, p. 5260 - 5270 (2017)
Four new tetrazole-containing species, in conjugation with terpyridine moieties through phenyl or pyridyl linkers, have been synthesised and characterised. In the series, the tetrazole functional groups are either in their acidic form or are alkylated at the N2 position with a methyl group. The photophysical properties of the species reveal moderate UV or efficient blue fluorescent emission, with photoluminescence quantum yields of around 30 % and 80 % for UV and blue emission, respectively. The spectral profiles can be reversibly modulated through protonation/deprotonation, with changes being consistent with an increase of the electron density on the tetrazole rings upon deprotonation or a decrease of the electron density on the terpyridines through protonation. The tetrazole-containing species were also investigated for fluorescence sensing of biologically and environmentally important metal ions, highlighting a ratiometric response to the presence of Zn2+. Furthermore, this ratiometric response could be well discriminated from that of interfering Cd2+ ions. Lastly, the species have been investigated as ligands for Eu3+ and Yb3+ cations, revealing efficient sensitisation, to give typical red and near-infrared emissions, respectively.
CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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Page/Page column 320, (2016/04/20)
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I): wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula (I), independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and 15 deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimers Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and (III), and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Iminothiadiazine Dioxide Compounds as BACE Inhibitors, Compositions and Their Use
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Paragraph 0581, (2015/11/16)
In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's disease, are also disclosed.
