Technion Research & Development Foundation Ltd

Tagra Biotechnologies Ltd.

Valery Belakhov

Timor Baasov

Jeyakumar Kandasamy

Dana Atia-Glikin

Mariana Hainrichson

Varvara Pokrovskaya

Micha Fridman

Emma Kvitnitsky

Yury Shapiro

Vladimir Babtsov

Sima Yaron

Boris Smolkin

Alina Khononov

Michal Shavit Kishkober

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.

Modified aminoglycoside compounds and uses thereof in disabling bacterial ribosome

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: or a pharmaceutically acceptable salt thereof, wherein Ris 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&#x2033; 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: or a pharmaceutically acceptable salt thereof, wherein Ris selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

Provided herein are antimicrobial conjugates of two antibiotic agents, exhibiting improved activity also against resistant bacteria, compared to each of the agents separately or their mixture, and having substantially no resistance emerged thereagainst, as well as processes for preparation the same, compositions containing the same, and uses thereof in medical treatments against pathogenic microorganisms. The disclosed antimicrobial conjugates are composed of aminoglycosides and non-ribosomal active antibiotics. Some of the antimicrobial conjugates are prepared via 'click' chemistry.

Conjugated antimicrobial agents

A novel group of aminoglycosides which share some structural features of currently available aminoglycosides with regard to the backbone, while also having significant structural differences, is disclosed. The similarity enables these aminoglycosides to be highly potent and effective antibiotics, while the significant differences enable these aminoglycosides to reduce or even block antibiotic resistance. The aminoglycosides of the present invention are suitable for inhibition of antrax lethal factor, hence are suitable for use as a cure for anthrax.

Bifunctional antibiotics for targeting rRNA and resistance-causing enzymes and for inhibition of anthrax lethal factor

Novel derivatives of ascorbic acid and compositions comprising them are provided. The novel derivatives are of the following general formula (I): where R1 is a C2&#x2013;C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1&#x2013;C17 alkyl ; R2 is a group of the following formula (II) wherein R5 or R6 are the same or different and represent hydrogen, a C1&#x2013;C4 alkyl, or R5 is C1&#x2013;C4 alkyl group and R6 is a metal cation or ammonium cation; R3 or R4 are the same or different and represent hydrogen, C2&#x2013;C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1&#x2013;C17 alkyl.

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Haifa, Israel

Valery Belakhov