Antibiotic compounds
Inventors
Mishra, Prabhu Dutt • Mahajan, Girish Badrinath
Assignees
Foundation For Neglected Disease Research (fndr) • National Centre For Polar And Ocean Research (ncpor)
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Publication Number
US-10501492-B2
Publication Date
2019-12-10
Expiration Date
Abstract
Purified compounds of formula I are described. Compounds include all stereoisomeric forms and all tautomeric forms of the compounds of formula I and pharmaceutically acceptable salts and derivatives. Processes for the production of the antibacterial compounds by fermentation of the microorganism belonging to Streptomyces species (PM0626271/MTCC 5447) and to pharmaceutical compositions containing one or more of the novel compounds as active ingredient and their use in medicines for treatment and prevention of diseases caused by bacterial infections are described.
Core Innovation
The invention relates to novel antibacterial compounds of Formula I, including Formula I(a) and Formula I(b). The disclosure covers all stereoisomers and tautomers of the compounds, as well as pharmaceutically acceptable salts and derivatives, and reports structural identification and complete characterization of the compounds.
The document discloses production of the compounds by cultivating a Streptomyces species identified as PM0626271/MTCC 5447 under submerged aerobic fermentation conditions. The process yields the compounds of Formula I(a) and Formula I(b) in the fermented broth, followed by isolation, extraction, and purification to obtain Formula I(a)/Formula I(b).
The compounds are described as having antibacterial activity against MRSA and VRE/Enterococcus, and as having antimycobacterial activity against MDR Mycobacterium tuberculosis. Antibacterial and antimycobacterial performance is reported using MIC values and % reduction in luciferase reporter RLUs for TB strains.
Claims Coverage
The provided material includes one independent claim. The claim contains three inventive features focused on producing pharmaceutically acceptable salts of Formula I(a) and Formula I(b) via cultivation of a specified Streptomyces microorganism, then isolating, purifying, and converting the compounds to pharmaceutically acceptable salts.
Submerged aerobic cultivation of Streptomyces PM0626271/MTCC 5447 to produce Formula I(a) and Formula I(b)
A process producing the compound of Formula I(a) and the compound of Formula I(b) in the fermented broth by cultivating Streptomyces species PM0626271/MTCC 5447 under submerged aerobic conditions in a nutrient medium containing sources of carbon, nitrogen and inorganic salts.
Isolation and purification of Formula I(a) and Formula I(b) from fermented broth
Isolating the compound of Formula I(a) and the compound of Formula I(b) from the fermented broth obtained after cultivating Streptomyces species PM0626271/MTCC 5447, followed by purifying the isolated compound of Formula I(a) and the isolated compound of Formula I(b).
Conversion of purified Formula I(a) or Formula I(b) to pharmaceutically acceptable salts
Converting the purified compound of Formula I(a) or the purified compound of Formula I(b) prepared by the purification step to its pharmaceutically acceptable salt.
Overall, the claim scope covers cultivation of Streptomyces species PM0626271/MTCC 5447 to produce Formula I(a) and Formula I(b), isolation and purification of both compounds, and conversion of the purified compounds to corresponding pharmaceutically acceptable salts.
Stated Advantages
Antibacterial activity against MRSA and VRE/Enterococcus.
Antimycobacterial activity against MDR Mycobacterium tuberculosis.
Complete characterization of the compounds using HPLC, HRMS, IR, and NMR.
Documented Applications
Therapeutic/prophylactic use as a medicament for bacterial infections in mammals/humans.
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