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Hayward, CA, United States

The present invention provides certain water-soluble O-carbonyl phosphoramidate prodrugs of the following formula I: or pharmaceutically acceptable salts thereof that are therapeutic or antibacterial agents, pharmaceutical compositions containing them, methods for their use, and reagents and methods for preparing these compounds.


Patent
MicuRx Pharmaceuticals | Date: 2012-12-20

Provided herein are antimicrobial tricyclic boron compounds of the following formula I: or pharmaceutically acceptable salts, complexes, or tautomers thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.


News Article | August 22, 2013
Site: www.finsmes.com

The round was led by BVCF, with participation from existing investors Morningside Group and Devon Park Bioventures. In conjunction with the funding, Weixin Xu and Davis Yang of BVCF will join the company’s board of directors. Led by Zhengyu Yuan, Ph.D., president and chief executive officer, MicuRx Pharmaceuticals is developing novel antibiotics to combat infections due to resistant bacteria. The company intends to use the capital to fund the U.S. development of MRX-I, a novel oral oxazolidinone antibiotic targeting infections due to multi-drug resistant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). MicuRx also has research and development facilities in Hayward, CA and Shanghai, China. To date, it has raised $37m in funding.


Li C.-R.,Peking Union Medical College | Zhai Q.-Q.,Peking Union Medical College | Wang X.-K.,Peking Union Medical College | Hu X.-X.,Peking Union Medical College | And 9 more authors.
Antimicrobial Agents and Chemotherapy | Year: 2014

MRX-I is a potent oxazolidinone antibiotic against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), penicillin-intermediate S. pneumoniae (PISP), and vancomycin-resistant enterococci (VRE). In this study, the in vivo efficacy of orally administered MRX-I was evaluated using linezolid as a comparator. MRX-I showed the same or better efficacy than linezolid in both systemic and local infection models against the tested strains. Copyright © 2014, American Society for Microbiology. All Rights Reserved. Source


Ling C.,CAS Shanghai Institute of Materia Medica | Fu L.,CAS Shanghai Institute of Materia Medica | Gao S.,CAS Shanghai Institute of Materia Medica | Chu W.,CAS Shanghai Institute of Materia Medica | And 4 more authors.
Journal of Medicinal Chemistry | Year: 2014

A series of novel thioether pleuromutilin derivatives incorporating various heteroaromatic substituents into the C14 side chain have been reported. Structure-activity relationship (SAR) studies resulted in compounds 52 and 55 with the most potent in vitro antibacterial activity among the series (MIC = 0.031-0.063 μg/mL). Further optimization to overcome the poor water solubility of compound 55 resulted in compounds 87, 91, 109, and 110 possessing good in vitro antibacterial activity with increased hydrophilicity. Compound 114, the water-soluble phosphate prodrug of compound 52, was also prepared and evaluated. Among the derivatives, compound 110 showed moderate pharmacokinetic profiles and good in vivo efficacy in both MSSA and MRSA systemic infection models. Compound 110 was further evaluated in CYP450 inhibition assay and displayed intermediate in vitro inhibition of CYP3A4. © 2014 American Chemical Society. Source

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