BENZOXABOROLE COMPOUNDS SUBSTITUTED AT POSITION 4 AND ASSOCIATED USES

MA41494AInactive Publication Date: 2017-12-19GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO 2) LTD +1
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Patent Information

Application Number
MA41494
Authority / Receiving Office
MA · MA
Patent Type
Applications
Current Assignee / Owner
Priority Date
2016-02-12
Filing Date
2016-02-11
Publication Date
2017-12-19
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Current tuberculosis treatments face challenges such as long duration, poor patient compliance, emergence of multi-drug resistant strains, and adverse interactions, necessitating the development of shorter, more effective regimens that can be taken less frequently and are effective against Mycobacterium tuberculosis, including strains resistant to standard drugs.

Method used

Substituted benzoxaboroles with specific structural features, such as those described in Formula III, exhibit selective inhibition of Mycobacterium tuberculosis replication with sub-micromolar MIC values, potentially used in combination with existing anti-tubercular agents to enhance efficacy and address resistance issues.

Benefits of technology

These compounds demonstrate improved selectivity and efficacy against Mycobacterium tuberculosis, offering a potential solution for shorter treatment durations and reduced resistance development, while being effective against both drug-sensitive and resistant strains.

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Abstract

The present invention relates to substituted benzoxaboroles having the structure comprising formula (iii), wherein r3 is selected from –ch3, –ch2ch3, –ch2=ch2, –ch2ch2ch3, –ch(ch3)2, –ch2ch2=ch2, and a cyclopropyl, r1 and r2 are each independently selected from h, -ch3, -ch2ch3, –ch2ch2ch3, and –ch(ch3)2; compositions containing such compounds, their use in therapy, including their use as antimycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for preparing such compounds.
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