109859-99-6Relevant articles and documents
HISTONE METHYLTRANSFERASE INHIBITORS
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Page/Page column 92, (2018/07/29)
The present disclosure provides certain angular tricyclic compounds that are histone methyltransi erases 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 (e.g., beta- thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Substituted aryl malonamates as new serine β-lactamase substrates: Structure-activity studies
Adediran,Cabaret,Lohier,Wakselman,Pratt
experimental part, p. 282 - 291 (2010/04/05)
A series of substituted aryl malonamates have been prepared. These compounds are analogues of aryl phenaceturates where the amido side chain has been replaced by a retro-amide. Like the phenaceturates, these compounds are substrates of typical class A and class C β-lactamases, particularly of the latter, and of soluble DD-peptidases. The effect of substituents α to the ester carbonyl group on turnover by these enzymes is similar to that in the phenaceturates. On the other hand, N-alkylation of the side chain amide of malonamates, but not of phenaceturates, retains the susceptibility of the compounds to hydrolysis by β-lactamases. This reactivity is not enhanced, however, by bridging the amide nitrogen and Cα atoms. A phosphonate analogue of the malonamates was found to be an irreversible inhibitor of the β-lactamases. These results, therefore, provide further evidence for the covalent access of compounds bearing retro-amide side chains to the active sites of β-lactam-recognizing enzymes.
Cyclic amine derivatives, pharmaceutical compositions containing these compounds and methods for preparing them
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, (2008/06/13)
Disclosed are new cyclic amine derivatives of the formula I STR1 wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
