1426319-55-2Relevant academic research and scientific papers
METHODS AND COMPOSITIONS FOR TREATING HIV-RELATED DISORDERS
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Paragraph 0211, (2016/02/10)
Certain adjunctive therapies comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent for treating HIV-related disorders are provided herein. These disorders include AIDS dementia complex, AIDS-induced encephalopathy, HIV-associated neurocognitive disorder, asymptomatic neurocognitive impairment, minor neurocognitive disorder, minor cognitive motor disorder, vacuolar myelopathy, peripheral neuropathies, and polymyositis. Also provided are pharmaceutical compositions comprising a kynurenine-3- monooxygenase inhibitor and an antiviral agent.
Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntingtons disease
Toledo-Sherman, Leticia M.,Prime, Michael E.,Mrzljak, Ladislav,Beconi, Maria G.,Beresford, Alan,Brookfield, Frederick A.,Brown, Christopher J.,Cardaun, Isabell,Courtney, Stephen M.,Dijkman, Ulrike,Hamelin-Flegg, Estelle,Johnson, Peter D.,Kempf, Valerie,Lyons, Kathy,Matthews, Kimberly,Mitchell, William L.,Oconnell, Catherine,Pena, Paula,Powell, Kendall,Rassoulpour, Arash,Reed, Laura,Reindl, Wolfgang,Selvaratnam, Suganathan,Friley, Weslyn Ward,Weddell, Derek A.,Went, Naomi E.,Wheelan, Patricia,Winkler, Christin,Winkler, Dirk,Wityak, John,Yarnold, Christopher J.,Yates, Dawn,Munoz-Sanjuan, Ignacio,Dominguez, Celia
, p. 1159 - 1183 (2015/03/04)
We report on the development of a series of pyrimidine carboxylic acids that are potent and selective inhibitors of kynurenine monooxygenase and competitive for kynurenine. We describe the SAR for this novel series and report on their inhibition of KMO activity in biochemical and cellular assays and their selectivity against other kynurenine pathway enzymes. We describe the optimization process that led to the identification of a program lead compound with a suitable ADME/PK profile for therapeutic development. We demonstrate that systemic inhibition of KMO in vivo with this lead compound provides pharmacodynamic evidence for modulation of kynurenine pathway metabolites both in the periphery and in the central nervous system.
KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Paragraph 00165, (2013/03/28)
Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and diso
