Effective aminoglycoside antibiotic for multidrug-resistant bacteria

Patent metadata

Field	Value
Publication number	US-11135234-B2
Application number	US-202016749191-A
Country	US
Kind code	B2
Filing date	Jan 22, 2020
Priority date	Jul 30, 2015
Publication date	Oct 5, 2021
Grant date	Oct 5, 2021

Abstract

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.

First claim

The invention claimed is:

1. A method for the treatment of bacterial infectious disease comprising administering a therapeutically effective dose of a compound represented by a formula (I) or a pharmaceutically acceptable salt or hydrate thereof:

wherein,
R 1 is a hydrogen atom or a hydroxyl group,
R 2 is a hydrogen atom or an amino group,
R 3 is a hydrogen atom, a halogen atom, a hydroxyl group or an amino group,
R 4 is a hydrogen atom, a halogen atom or an amino group,
wherein R 1 and R 4 may form a double bond together,
R 5 is a hydrogen atom, a hydroxyl group or an amino group,
R 6 is a hydrogen atom, a hydroxyl group or an amino group,
R 7 is a hydrogen atom, a hydroxyl group or an amino group,
R 8 is a hydrogen atom, a hydroxyl group or an amino group,
R 9 and R 10 are each independently a hydrogen atom, a C 1-6 alkyl group, an amino-C 1-6 alkyl group, a guanidino-C 1-6 alkyl group, an amino-C 3-7 cycloalkyl group, an amino-C 3-7 cycloalkyl-C 1-6 alkyl group, an amidino group, an azetidino group optionally substituted with a C 1-6 alkyl group, a glycyl group, a sarcosyl group, an L-alanyl group, a D-alanyl group, an L-seryl group, a D-seryl group, a β-alanyl group, an L-isoseryl group or a D-isoseryl group; and
R 11 is a hydrogen atom, a hydroxyl group or a fluorine atom,
except when
(i) R 5 , R 8 , and R 11 are hydroxyl groups, R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , R 9 , and R 10 are hydrogen atoms, or
(ii) R 1 , R 5 , R 8 , and R 11 are hydroxyl groups, R 2 , R 3 , R 4 , R 6 , R 7 , R 9 , and R 10 are hydrogen atoms.

Assignees

• Microbial Chem Res Found
• Meiji Seika Pharma Co Ltd

Inventors

• Takahashi Yoshiaki
• Umemura Eijiro
• Ida Takashi
• Igarashi Masayuki

Classifications

• Y02A50/30

  Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change · CPC title

• A61K31/7036 Primary

  having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins · CPC title

• A61P31/04

  Antibacterial agents · CPC title

• C07H15/224

  with only one saccharide radical directly attached to the cyclohexyl radical, e.g. destomycin, fortimicin, neamine · CPC title

• C07H15/12 Primary

  attached to a nitrogen atom of the saccharide radical · CPC title