The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds, as well as to related intermediates, and crystal forms thereof, useful in such methods.

The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds, as well as to related intermediates, and crystal forms thereof, useful in such methods.

Various aspects of the invention relate to compositions comprising C-2a gentamicin. A composition may be substantially free from one or more of C-1 gentamicin, C-1a gentamicin, C-2 gentamicin, C-2b gentamicin, gentamicin A, gentamicin B, and gentamicin X. In some aspects, the invention relates to a method for treating a condition in a subject, comprising administering a composition comprising C-2a gentamicin to the subject. The condition may be, for example, a bacterial infection, genetic disease or disorder, or cancer.

Various aspects of the invention relate to compositions comprising C-2a gentamicin. A composition may be substantially free from one or more of C-1 gentamicin, C-1a gentamicin, C-2 gentamicin, C-2b gentamicin, gentamicin A, gentamicin B, and gentamicin X. In some aspects, the invention relates to a method for treating a condition in a subject, comprising administering a composition comprising C-2a gentamicin to the subject. The condition may be, for example, a bacterial infection, genetic disease or disorder, or cancer.

Reformulations of gentamicin for treatment of infections are provided with the goal to reduce current side effects such as ototoxicity, while maintaining antimicrobial activity. The reformulation is a mixture of three of the C-components of gentamicin: C1a, C2a and C2b, while excluding as much as possible, C1 and C2. Specifically, to the objective of this invention a mixture is formulated having gentamicin C1a ranging from 10-30%, gentamicin C2a ranging from 0-30%, and gentamicin C2b ranging from 40-90%, where the mixture totals a 100% of the gentamicin C-components, defined as C1, C1a, C2, C2a and C2b only. The formulations of this invention increase the probability of a more favorable outcome for the patients exposed to gentamicin, i.e., reduced risk of the side-effect of hearing loss.

Field of application: The invention relates to combinatorial chemistry, pharmacy and cosmetology, allows to synthesize new combinatorial libraries of derivatives of antibiotics for use in pharmacy, cosmetology and pharmacy.

Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.

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.

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.

The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds, as well as to related intermediates, and crystal forms thereof, useful in such methods.

Methods of using and pharmaceutical compositions comprising (2R,3S,4R,5R,6S)-5-amino-6-(((1R,2S,3S,4R,6S)-4,6-diamino-3-(((2R,3R,4R,5R)-3,5-dihydroxy-5-methyl-4-(methylamino)tetrahydro-2H-pyran-2- yl)oxy)-2-hydroxycyclohexyl)oxy)-2-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diol are disclosed, including methods of treating or preventing a nonsense mutation mediated disease associated with premature translation termination or a premature stop codon resulting from a germline or somatic nonsense mutation.