Unlock instant, AI-driven research and patent intelligence for your innovation.

Macrolides with modified desosamine sugars and uses thereof

A kind of carbocyclic group, heterocyclic group technology, applied in the macrolide with modified deoxyglucosamine sugar and its application field

Inactive Publication Date: 2018-01-02
PRESIDENT & FELLOWS OF HARVARD COLLEGE
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite greatly enhanced binding to ribosomes, ketolides such as telithromycin and solithromycin have not resolved several of the most recent forms of macrolide resistance that have evolved in hospital settings, especially ribosomes Methylation and RNA point mutations

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Macrolides with modified desosamine sugars and uses thereof
  • Macrolides with modified desosamine sugars and uses thereof
  • Macrolides with modified desosamine sugars and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0794] In order that the invention described herein may be more fully understood, the following examples are set forth. The synthetic and biological examples described in this application are provided to illustrate the compounds, pharmaceutical compositions and methods provided herein and are not to be construed in any way as limiting the scope thereof.

[0795] Macrolide Binding and Drug Resistance

[0796] Macrolide antibiotics (such as figure 1 Exemplary macrolides shown in ) inhibit peptide synthesis by impeding nascent peptide transport through the export channel in bacterial ribosomes. All 13- to 16-membered macrolide antibiotics bind to the nearly identical macrolide (or azalide) conformation in which the hydrophobic face of the molecule (containing several methyl groups group and one ethyl group) engages the walls of the peptidyl exit channel, and the hydrophilic face of the molecule (comprising four C–O and C=O groups) is exposed to the hydrophobic interior of the ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

Provided herein are macrolide compounds of Formula (I) and (I-N) for the treatment of infectious diseases and inflammatory conditions. The 14-membered ketolides and 14-, 15-, and 16-membered azaketolides described herein comprise modified sugars which are desosamine or mycaminose analogs. Pharmaceutical compositions and methods of treating infection diseases and inflammatory conditions using the inventive macrolides are also provided. This disclosure additionally provides methods of preparing the macrolides by the coupling of an eastern and western half.

Description

[0001] related application [0002] This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Applications U.S.S.N. 62 / 138,198, filed March 25, 2015, and U.S.S.N. Reference. Background technique [0003] Emerging resistance to existing antibiotics is rapidly developing into a global crisis, especially for Staphylococcus aureus, Streptococcus pyogenes and Staphylococcus pneumonia infections. Pathogenic bacteria can pass genes encoding antibiotic resistance both vertically (to their offspring) and horizontally (to neighboring bacteria of different lineages), whereby antibiotic resistance can evolve rapidly, especially in hospitals in environment. See, eg, Wright, Chem. Commun. (2011) 47:4055-4061. This year, >99,000 people in the United States will die from care-associated infections, more than all deaths from traffic accidents, HIV, and breast cancer combined, creating an estimated $45 billion burden on U.S. care costs. See, eg, Klevens et al., ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/70A61K31/7042A61K31/7056
CPCC07H1/00C07H15/26C07H17/08A61P29/00A61P31/00A61P31/04A61P33/00
Inventor A.G.迈尔斯I.B.塞普尔Z.张
Owner PRESIDENT & FELLOWS OF HARVARD COLLEGE