Patent classifications
C07H15/23
AMINOGLYCOSIDES AND USES THEREOF IN TREATING GENETIC DISORDERS
A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5 position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.
AMINOGLYCOSIDE DERIVATIVES AND USES THEREOF IN TREATING GENETIC DISORDERS
Novel pseudo-trisaccharide aminoglycosides, represented by Formula I, 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
Novel pseudo-trisaccharide aminoglycosides, represented by Formula I, 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.
Aminoglycosides and uses thereof in treating genetic disorders
A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5 position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.
Selective oxidation of carbohydrates
The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.
Selective oxidation of carbohydrates
The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.
AMINOGLYCOSIDES AND USES THEREOF IN TREATING GENETIC DISORDERS
A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5 position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.
Aminoglycosides and uses thereof in treating genetic disorders
A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5 position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.
Aminoglycosides and uses thereof in treating genetic disorders
A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5 position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.
Substituted biphenyl or phenylheteroaryl-mannosides as antagonists of FimH
Disclosed herein are new O-biphenyl- and O-phenylheteroarylmannoside compounds and compositions and their application as pharmaceuticals for use in the treatment of human disease. Methods of inhibition of FimH activity in human subjects are also provided for the treatment of diseases such as urinary tract infection.