145485-58-1Relevant academic research and scientific papers
Triazole derivative having HSP90 (Heat Shock Protein) inhibiting activity, as well as preparation method and application of triazole derivative
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, (2017/08/02)
The invention discloses a triazole derivative having an HSP90 (Heat Shock Protein) inhibiting activity, as well as a preparation method and an application of the triazole derivative. Specifically, the invention relates to the triazole derivative having a structure as shown in a formula (I), a stereisomer of the triazole derivative and a pharmaceutically acceptable salt, wherein the definition of each substituent group in the formula (I) and the definition in a description are the same. The compound with a novel structure has the HSP90 inhibiting activity, can be used to cure cancers, neurodegenerative disorders, inflammation diseases, autoimmune diseases, ischemic brain injuries and the like, and has a broad application prospect.
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys
Fischer, Christian,Zultanski, Susan L.,Zhou, Hua,Methot, Joey L.,Shah, Sanjiv,Hayashi, Ikuo,Hughes, Bethany L.,Moxham, Christopher M.,Bays, Nathan W.,Smotrov, Nadya,Hill, Armetta D.,Pan, Bo-Sheng,Wu, Zhenhua,Moy, Lily Y.,Tanga, Flobert,Kenific, Candia,Cruz, Jonathan C.,Walker, Deborah,Bouthillette, Melanie,Nikov, George N.,Deshmukh, Sujal V.,Jeliazkova-Mecheva, Valentina V.,Diaz, Damaris,Michener, Maria S.,Cook, Jacquelynn J.,Munoz, Benito,Shearman, Mark S.
, p. 3488 - 3494 (2015/08/06)
Abstract Synthesis and SAR studies of novel triazolobenzazepinones as gamma secretase modulators (GSMs) are presented in this communication. Starting from our azepinone leads, optimization studies toward improving central lowering of Aβ42 led to the discovery of novel benzo-fused azepinones. Several benzazepinones were profiled in vivo and found to lower brain Aβ42 levels in Sprague Dawley rats and transgenic APP-YAC mice in a dose-dependent manner after a single oral dose. Compound 34 was further progressed into a pilot study in our cisterna-magna-ported rhesus monkey model, where we observed robust lowering of CSF Aβ42 levels.
Synthesis of substituted 1-benzazepin-2-ones via ring-closing olefin metathesis
Hoyt, Scott B.,London, Clare,Park, Min
scheme or table, p. 1911 - 1913 (2009/08/17)
The 1-benzazepin-2-one ring system is an important structural feature of marketed drugs, clinical candidates, and other bioactive molecules. We have developed a new benzazepinone synthesis that employs ring-closing olefin metathesis as a key step. This route provides efficient access to substituted benzazepinones that are difficult to synthesize via existing procedures.
Benzo-fused lactams that promote the release of growth hormone
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, (2008/06/13)
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
