- FUSED TRICYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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Page/Page column 129; 130; 150; 151
(2015/06/25)
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- Second-generation antibacterial benzimidazole ureas: Discovery of a preclinical candidate with reduced metabolic liability
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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
- 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.
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p. 8792 - 8816
(2015/03/14)
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- Antibacterial Compounds
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The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
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Paragraph 0493-0494
(2013/10/07)
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