848092-84-2Relevant articles and documents
HISTONE METHYLTRANSFERASE INHIBITORS
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Page/Page column 56, (2017/09/08)
The present disclosure provides certain compounds of formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinpathies such as beta-thalassemia and sickle cell disease. Also provided are pharmaceutical compositions containing such compounds as well as processes and intermediates for preparing such compounds.
CONJUGATES FOR TREATING DISEASES
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Page/Page column 114, (2016/10/04)
The present disclosure relates to pyrrolobenzodiazepine (PBD) prodrugs and conjugates thereof. The present disclosure also relates to pharmaceutical compositions of the conjugates described herein, methods of making and methods of using the same.
Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization
Tasler, Stefan,Mueller, Oliver,Wieber, Tanja,Herz, Thomas,Pegoraro, Stefano,Saeb, Wael,Lang, Martin,Krauss, Rolf,Totzke, Frank,Zirrgiebel, Ute,Ehlert, Jan E.,Kubbutat, Michael H.G.,Schaechtele, Christoph
supporting information; experimental part, p. 6728 - 6737 (2009/12/09)
Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range.