153248-47-6Relevant academic research and scientific papers
Optimization of LpxC Inhibitor Lead Compounds Focusing on Efficacy and Formulation for High Dose Intravenous Administration
Panchaud, Philippe,Surivet, Jean-Philippe,Diethelm, Stefan,Blumstein, Anne-Catherine,Gauvin, Jean-Christophe,Jacob, Lo?c,Masse, Florence,Mathieu, Ga?lle,Mirre, Azely,Schmitt, Christine,Enderlin-Paput, Michel,Lange, Roland,Gnerre, Carmela,Seeland, Swen,Herrmann, Charlyse,Locher, Hans H.,Seiler, Peter,Ritz, Daniel,Rueedi, Georg
, p. 88 - 102 (2020)
LpxC inhibitors were optimized starting from lead compounds with limited efficacy and solubility and with the goal to provide new options for the treatment of serious infections caused by Gram-negative pathogens in hospital settings. To enable the development of an aqueous formulation for intravenous administration of the drug at high dose, improvements in both solubility and antibacterial activity in vivo were prioritized early on. This lead optimization program resulted in the discovery of compounds such as 13 and 30, which exhibited high solubility and potent efficacy against Gram-negative pathogens in animal infection models.
SGC STIMULATORS
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, (2014/09/29)
Compounds of Formulae (I') and (I) are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Page/Page column 83-84, (2011/04/26)
Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): (Formula (I)), including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2, R3, Z1 and Z2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Page/Page column 108-109, (2011/04/26)
Compounds having antibacterial activity are disclosed. The compounds have one of the following structures (I) or (II): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2, R3 and Z1 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES
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Page/Page column 58; 59, (2010/08/05)
The present invention relates to a compound according to formula I, wherein R1, R2 and A are as defined herein, which exhibit PDE4 inhibitory activity and may be used in the treatment of inflammatory diseases or autoimmune diseases,
TREATMENT OF URINARY TRACT INFECTIONS WITH ANTIBACTERIAL AMINOGLYCOSIDE COMPOUNDS
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Page/Page column 214, (2010/12/17)
A method for treating a urinary tract infection in a mammal in need thereof is disclosed, the method comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound.
ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Page/Page column 205, (2009/06/27)
Compounds of structure (I): having antibacterial activity are disclosed, including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
