1190044-23-5Relevant articles and documents
C-2 derivatized 8-sulfonamidoquinolines as antibacterial compounds
Davison, Emma K.,McGowan, John E.,Li, Freda F.,Harper, Andrew D.,Jeong, Joo Young,Mros, Sonya,Harbison-Price, Nichaela,Van Zuylen, Essie M.,Knottenbelt, Melanie K.,Heikal, Adam,Ferguson, Scott A.,McConnell, Michelle A.,Cook, Gregory M.,Krittaphol, Woravimol,Walker, Greg F.,Brimble, Margaret A.,Rennison, David
supporting information, (2020/11/25)
A series of C-2 derivatized 8-sulfonamidoquinolines were evaluated for their antibacterial activity against the common mastitis causative pathogens Streptococcus uberis, Staphylococcus aureus and Escherichia coli, both in the presence and absence of supplementary zinc (50 μM ZnSO4). The vast majority of compounds tested were demonstrated to be significantly more active against S. uberis when in the presence of supplementary zinc (MICs as low as 0.125 μg/mL were observed in the presence of 50 μM ZnSO4). Compounds 5, 34–36, 39, 58, 79, 82, 94 and 95 were shown to display the greatest antibacterial activity against S. aureus (MIC ≤ 8 μg/mL; both in the presence and absence of supplementary zinc), while compounds 56, 58 and 66 were demonstrated to also exhibit activity against E. coli (MIC ≤ 16 μg/mL; under all conditions). Compounds 56, 58 and 66 were subsequently confirmed to be bactericidal against all three mastitis pathogens studied, with MBCs (≥3log10 CFU/mL reduction) of ≤ 32 μg/mL (in both the presence and absence of 50 μM ZnSO4). To validate the sanitizing activity of compounds 56, 58 and 66, a quantitative suspension disinfection (sanitizer) test was performed. Sanitizing activity (>5log10 CFU/mL reduction in 5 min) was observed against both S. uberis and E. coli at compound concentrations as low as 1 mg/mL (compounds 56, 58 and 66), and against S. aureus at 1 mg/mL (compound 58); thereby validating the potential of compounds 56, 58 and 66 to function as topical sanitizers designed explicitly for use in non-human applications.
QUINOLINE SULFONAMIDE COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS
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Page/Page column 68; 73, (2019/07/13)
The invention provides novel quinoline sulfonamide compounds of Formula I: (Formula (I)) and their use for the treatment or prevention of bacterial infections caused by both Gram positive and Gram negative bacteria such as, for example, infections caused by one or more bacteria from the Enterobactericeae, Staphylococcaceae, or Streptococcaceae families. The compounds described and claimed herein may be formulated in one or more pharmaceutical or veterinary compositions for use in animal husbandry, and in particular in relation to the treatment of mastitis by directly targeting mastitis causing bacteria in a bovine herd. In certain embodiments described herein the pharmaceutical or veterinary compositions are formulated as a spray for direct administration to the udder of the bovine animal such as a cow.
NITROGENOUS HETEROCYCLIC COMPOUND, PREPARATION METHOD, INTERMEDIATE, COMPOSITION AND USE
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Paragraph 0267, (2019/01/17)
Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.
INHIBITION OF OLIG2 ACTIVITY
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Paragraph 00362-00363, (2018/03/25)
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.
1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
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Page/Page column 72, (2016/05/24)
The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
SYNERGISTIC COMBINATION OF IMMUNOLOGIC INHIBITORS FOR THE TREATMENT OF CANCER
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Paragraph 00260, (2014/05/24)
In some embodiments, the methods involve the use of a combination of at least two of the following: an inhibitor of indoleamine-2,3-dioxygenase (IDO), an inhibitor of the PD-L1/PD-1 pathway, an inhibitor of CTLA-4, an inhibitor of CD25, or IL-7. The inven
BETA-LACTAMASE INHIBITORS
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Paragraph 00316, (2014/06/24)
Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Chemoselective alkynylation of N-sulfonylamides versus amides and carbamates-Synthesis of tetrahydropyrazines
Aubineau, Thomas,Cossy, Janine
supporting information, p. 3303 - 3305 (2013/06/04)
The chemoselective alkynylation of N-sulfonylamides versus amides and carbamates using TMS-EBX as an alkynylating agent leads to the formation of non-symmetrical tetrahydropyrazines from orthogonally protected diamines. The Royal Society of Chemistry 2013
4-(SUBSTITUTED ANILINO)QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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Page/Page column 18-19, (2012/08/14)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositons and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
4-(Substituted Anilino)-Quinazoline Derivatives Useful as Tyrosine Kinase Inhibitors
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Page/Page column 13, (2012/08/28)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.