1193639-02-9Relevant articles and documents
WDR5-MYC INHIBITORS
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Paragraph 00104; 00144-00145, (2021/05/29)
Substituted N-heteroaryl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject such as cancer cell proliferation.
IMIDAZOLE-CONTAINING INHIBITORS OF ALK2 KINASE
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Page/Page column 634; 635, (2019/01/08)
Disclosed are compounds of formula (I), (II), (III), and (IV), and pharmaceutically acceptable salts thereof. The compounds are inhibitors of ALK2 kinase. Also provided are pharmaceutical compositions comprising a compound of formula (I), (II), (III), or (IV), or pharmaceutically acceptable salt thereof, and methods involving use of the compounds or pharmaceutically acceptable salts thereof and compositions in the treatment and prevention of various diseases and conditions, such as fibrodysplasia ossificans progressiva.
Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease
Helal, Christopher J.,Kang, Zhijun,Lucas, John C.,Gant, Thomas,Ahlijanian, Michael K.,Schachter, Joel B.,Richter, Karl E.G.,Cook, James M.,Menniti, Frank S.,Kelly, Kristin,Mente, Scot,Pandit, Jay,Hosea, Natalie
scheme or table, p. 5703 - 5707 (2010/04/30)
Utilizing structure-based drug design, a 4-aminoimidazole heterocyclic core was synthesized as a replacement for a 2-aminothiazole due to potential metabolically mediated toxicity. The synthetic route utilized allowed for ready synthesis of 1-substituted-4-aminoimidazoles. SAR exploration resulted in the identification of a novel cis-substituted cyclobutyl group that gave improved enzyme and cellular potency against cdk5/p25 with up to 30-fold selectivity over cdk2/cyclin E.
