C07H15/224

CHROMATOGRAPHIC MATERIAL HAVING IMPROVED PH STABILITY, METHOD FOR PREPARATION THEREOF AND USES THEREOF
20210213420 · 2021-07-15 ·

A chromatographic material including a substrate having a surface and having a polymeric layer covalently bound to the surface; the polymeric layer comprising polymer molecules covalently attached to the surface of the substrate, each polymer molecule being attached to the surface via multiple siloxane bonds and each polymer molecule being connected to one or more functionalizing compounds that each comprise a functional group, wherein the polymeric layer is formed by covalently attaching polymer molecules to the surface of the substrate via multiple siloxane bonds, each polymer molecule containing multiple first reactive groups, and reacting the first reactive groups of the attached polymer molecules with at least one functionalizing compound that comprises a second reactive group that is reactive with the first reactive groups and that further comprises a functional group. Preferred conditions of reacting the polymer with the substrate include elevated temperature and reduced pressure.

CHROMATOGRAPHIC MATERIAL HAVING IMPROVED PH STABILITY, METHOD FOR PREPARATION THEREOF AND USES THEREOF
20210213420 · 2021-07-15 ·

A chromatographic material including a substrate having a surface and having a polymeric layer covalently bound to the surface; the polymeric layer comprising polymer molecules covalently attached to the surface of the substrate, each polymer molecule being attached to the surface via multiple siloxane bonds and each polymer molecule being connected to one or more functionalizing compounds that each comprise a functional group, wherein the polymeric layer is formed by covalently attaching polymer molecules to the surface of the substrate via multiple siloxane bonds, each polymer molecule containing multiple first reactive groups, and reacting the first reactive groups of the attached polymer molecules with at least one functionalizing compound that comprises a second reactive group that is reactive with the first reactive groups and that further comprises a functional group. Preferred conditions of reacting the polymer with the substrate include elevated temperature and reduced pressure.

MODIFIED AMINOGLYCOSIDE COMPOUNDS AND USES THEREOF IN DISABLING BACTERIAL RIBOSOME

Modified aminoglycoside compounds represented by Formula I as defined and described in the specification are provided. The modified aminoglycosides feature a diamine-containing functional moiety at one or more of positions 3′, 4′ and 6′. Uses of the modified aminoglycosides as antimicrobial (e.g., antibacterial) agents, and in treating medical conditions associated with microorganisms, are also provided.

NEOMYCIN AND PAROMOMYCIN DERIVATIVES

The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6′, C2′ and/or C5″. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.

Aminoglycoside derivatives and uses thereof in treating genetic disorders
10899785 · 2021-01-26 · ·

Novel aminoglycosides, represented by Formulae Ia and Ib, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

Aminoglycoside derivatives and uses thereof in treating genetic disorders
10899785 · 2021-01-26 · ·

Novel aminoglycosides, represented by Formulae Ia and Ib, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I):

##STR00001##

including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q.sub.1, Q.sub.2, Q.sub.3, R.sub.8 and R.sub.9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I):

##STR00001##

including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q.sub.1, Q.sub.2, Q.sub.3, R.sub.8 and R.sub.9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC FOR MULTIDRUG-RESISTANT BACTERIA

A compound represented by the following general formula (I) or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition thereof, and the use thereof to prevent or treat infectious diseases and a method to prevent or treat infectious diseases using those regimen are disclosed. The compound represented by formula (I) has an antibacterial activity against both gram-positive and gram-negative bacteria, and is useful in the prevention or treatment of infectious diseases caused by these bacteria.

##STR00001##

EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC FOR MULTIDRUG-RESISTANT BACTERIA

A compound represented by the following general formula (I) or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition thereof, and the use thereof to prevent or treat infectious diseases and a method to prevent or treat infectious diseases using those regimen are disclosed. The compound represented by formula (I) has an antibacterial activity against both gram-positive and gram-negative bacteria, and is useful in the prevention or treatment of infectious diseases caused by these bacteria.

##STR00001##