Isotopically-stabilized tetronimide compounds

    公开(公告)号:US10961211B2

    公开(公告)日:2021-03-30

    申请号:US16791252

    申请日:2020-02-14

    IPC分类号: C07D307/66 A61P35/04

    摘要: Isotopically-stabilized tetronimide compounds comprising one or more deuterium atoms, derivatives, and intermediates, thereof, including methods for their synthesis, pharmaceutical compositions thereof, and methods of using these compounds to interact with target molecules in cell-free samples, cell- and tissue-based assays, animal models, and in a subject are disclosed. One aspect relates to molecules that modulate the expression or catalytic activity of aspartyl (asparaginyl) β-hydroxylase (ASPH) within or on the surface of a cell. Other aspects of the invention relate to use of the molecules disclosed herein to diagnose, ameliorate, or treat cell proliferation disorders and related diseases. Related aspects include uses of the compounds to modulate the activity of viruses, as anti-hyperlipidemia agents, and as agents to ameliorate or treat thrombosis and related cardiovascular and metabolic disorders.

    Derivatives of korormicin useful as antibiotics

    公开(公告)号:US10166213B2

    公开(公告)日:2019-01-01

    申请号:US15500006

    申请日:2016-04-22

    摘要: An antibiotic compound is of formula (I): R1-R3, R5 and R6 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH2, or SH; R4 is H, alkyl group or substituted alkyl group. X1-X2 are independently selected from O, S, NH, H, alkyl, halogen, OH, SH, or NH2. Y is an acyclic hydrocarbon chain having 4 to 20 carbon atoms or a substituted acyclic hydrocarbon chain having 4 to 20 carbon atoms, but does not include an oxygen atom. Z is CH3 or any neutral or positively charged group. The compound can also be a salt or stereoisomer of formula (I). The compounds are useful in treating bacterial diseases.