1384984-18-2Relevant articles and documents
Second-generation antibacterial benzimidazole ureas: Discovery of a preclinical candidate with reduced metabolic liability
Grillot, Anne-Laure,Tiran, Arnaud Le,Shannon, Dean,Krueger, Elaine,Liao, Yusheng,Odowd, Hardwin,Tang, Qing,Ronkin, Steve,Wang, Tiansheng,Waal, Nathan,Li, Pan,Lauffer, David,Sizensky, Emmanuelle,Tanoury, Jerry,Perola, Emanuele,Grossman, Trudy H.,Doyle, Tim,Hanzelka, Brian,Jones, Steven,Dixit, Vaishali,Ewing, Nigel,Liao, Shengkai,Boucher, Brian,Jacobs, Marc,Bennani, Youssef,Charifson, Paul S.
, p. 8792 - 8816 (2015/03/14)
Compound 3 is a potent aminobenzimidazole urea with broad-spectrum Gram-positive antibacterial activity resulting from dual inhibition of bacterial gyrase (GyrB) and topoisomerase IV (ParE), and it demonstrates efficacy in rodent models of bacterial infec
COMBINATION THERAPY COMPRISING|1 -ETHYL-3-[5-[2-{1 -HYDROXY-1 -METHYL-ETHYL}PYRIMIDIN-5-YL]-7-(TETRA HYDROFURAN-2-|YL}-1 H-BENZIMIDAZOL-2-YL]UREA AND DERIVATIVES THEREOF TO TREAT MYCOBACTERIUM|DISEASES
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, (2014/02/15)
The present invention relates to combination therapies comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhi
SOLID FORMS OF (R)-2-(5-(2-(3-ETHYLUREIDO)-6-FLUORO-7-(TETRAHYDROFURAN-2-YL)-1H-BENZO[D]IMIDAZOL-5-YL)PYRIMIDIN-2-YL)PROPAN-2-YL DIHYDROGEN PHOSPHATE AND SALTS THEREOF
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, (2014/02/15)
The invention relates to solid forms of the Formula (I) wherein X is -PO(OH)2, -PO(OH)O-M+, or -PO(O-)2?2M+,wherein M is a monovalent cation such as Na+, K+, Li+, or NH4+. The invention also provides pharmaceutically acceptable compositions comprising the solid form of he compound and method of using the compositions in the treatment of various disorders.
GYRASE AND TOPOISOMERASE IV INHIBITORS
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, (2012/07/28)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
PROCESS OF MAKING GYRASE AND TOPOISOMERASE IV INHIBITORS
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, (2012/07/28)
The present application is directed to compounds, intermediates and methods for preparing compounds of formula (I) or a pharmaceutically acceptable salts thereof, wherein R is H or F, and each of R3, R4, and R5 are as defined herein. The compounds of formula (I) and pharmaceutical compositions comprising said compounds and salts inhibit bacterial gyrase and/or Topo IV and are useful in treating bacterial infections.
SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[6-FLUORO-5-[2-(1-HYDROXY-1-METHYL-ETHYL)PYRIMIDIN-5-YL]-7-(TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL]UREA
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, (2012/07/28)
The present application is directed to solid forms of compounds of formula I: and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.
PHOSPHATE ESTERS OF GYRASE AND TOPOISOMERASE INHIBITORS
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, (2013/02/28)
The present invention relates to phosphate esters of compounds that inhibit bacterial gyrase and/or Topoisomerase IV and pharmaceutical compositions thereof. These phosphate esters are useful for treating bacterial infections.