Provided herein are certain compounds useful as HTT modulators. Such compound are useful in the treatment of Huntington's disease.
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Page/Page column 114-115
(2021/11/20)
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors
A high-throughput screening (HTS) of the Genentech/Roche library identified a novel, uncharged scaffold as a KDM5A inhibitor. Lacking insight into the binding mode, initial attempts to improve inhibitor potency failed to improve potency, and synthesis of
Liang, Jun,Labadie, Sharada,Zhang, Birong,Ortwine, Daniel F.,Patel, Snahel,Vinogradova, Maia,Kiefer, James R.,Mauer, Till,Gehling, Victor S.,Harmange, Jean-Christophe,Cummings, Richard,Lai, Tommy,Liao, Jiangpeng,Zheng, Xiaoping,Liu, Yichin,Gustafson, Amy,Van der Porten, Erica,Mao, Weifeng,Liederer, Bianca M.,Deshmukh, Gauri,An, Le,Ran, Yingqing,Classon, Marie,Trojer, Patrick,Dragovich, Peter S.,Murray, Lesley
supporting information
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Structure-selectivity relationship in alkyllithium-aldehyde condensations using 3-aminopyrrolidine lithium amides as chiral auxiliaries
A nonracemizing route to a set of chiral 3-aminopyrrolidines, based on 4-hydroxy-(L)-proline, is described. The induction potential of the lithium amides derived from these diamines has then been investigated in the asymmetric addition of alkyllithium com
Corruble, Aline,Valnot, Jean-Yves,Maddaluno, Jacques,Duhamel, Pierre
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