- Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of duchenne muscular dystrophy
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Figure Presented. A series of novel 2-arylbenzoxazoles that upregulate the production of utrophin in murine H2K cells, as assessed using a luciferase reporter linked assay, have been identified. This compound class appears to hold considerable promise as a potential treatment for Duchenne muscular dystrophy. Following the delineation of structure-activity relationships in the series, a number of potent upregulators were identified, and preliminary ADME evaluation is described. These studies have resulted in the identification of 1, a compound that has been progressed to clinical trials.
- Chancellor, Daniel R.,Davies, Kay E.,De Moor, Olivier,Dorgan, Colin R.,Johnson, Peter D.,Lambert, Adam G.,Lawrence, Daniel,Lecci, Cristina,Maillol, Carole,Middleton, Penny J.,Nugent, Gary,Poignant, Séverine D.,Potter, Allyson C.,Price, Paul D.,Pye, Richard J.,Storer, Richard,Tinsley, Jonathon M.,Van Well, Renate,Vickers, Richard,Vile, Julia,Wilkes, Fraser J.,Wilson, Francis X.,Wren, Stephen P.,Wynne, Graham M.
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supporting information; experimental part
p. 3241 - 3250
(2011/07/06)
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- Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors
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An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity.
- Geng, Bolin,Comita-Prevoir, Janelle,Eyermann, Charles J.,Reck, Folkert,Fisher, Stewart
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body text
p. 5432 - 5435
(2011/10/12)
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- COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS
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The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
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Page/Page column 107
(2010/11/25)
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- Metallized phenyl-azo-naphthol compounds
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Metallized azo dyes of the formula STR1 wherein A is a sulfonyl, sulfonamido or carboxamido group, D is the residue of a phenol or naphthol, E is the residue of acetoacetanilide, a phenyl or naphthyl pyrazolone or the residue of a naphthol and M is a cation. The dyes are suitable for dyeing natural and synthetic polyamides, demonstrating good all-around fastness properties.
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