217816-66-5Relevant academic research and scientific papers
Synthesis method of 4-bromo-2-cyano-3-fluorobenzoic acid methyl ester
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Paragraph 0013-0021, (2021/01/29)
The invention belongs to the technical field of medical intermediates, and particularly relates to a synthetic method of 4-bromo-2-cyano-3-fluorobenzoic acid methyl ester. A compound A is used as an initial raw material, and reacts with N-bromo succinimide to form a compound B, and then through subsequent reactions such as the reaction of the compound B, the 4-bromo-2-cyano-3-fluorobenzoic acid methyl ester is formed. The synthesis method of 4-bromo-2-cyano-3-fluorobenzoic acid methyl ester is put forward for the first time.
METALLO-BETA-LACTAMASE INHIBITORS AND METHODS OF USE THEREOF
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, (2019/02/06)
The present invention relates to metallo-β-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
METALLO-BETA-LACTAMASE INHIBITORS AND METHODS OF USE THEREOF
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, (2019/07/20)
The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein RA, R1, and Z are as defined herein. The present invention also relates to compositions whi
METALLO-BETA-LACTAMASE INHIBITORS
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, (2016/12/01)
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
METALLO-BETA-LACTAMASE INHIBITORS
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, (2017/04/04)
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
METALLO-BETA-LACTAMASE INHIBITORS
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, (2015/08/06)
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N′-(2-fluoro-5- methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor
Dai, Yujia,Hartandi, Kresna,Ji, Zhiqin,Ahmed, Asma A.,Albert, Daniel H.,Bauch, Joy L.,Bouska, Jennifer J.,Bousquet, Peter F.,Cunha, George A.,Glaser, Keith B.,Harris, Christopher M.,Hickman, Dean,Guo, Jun,Li, Junling,Marcotte, Patrick A.,Marsh, Kennan C.,Moskey, Maria D.,Martin, Ruth L.,Olson, Amanda M.,Osterling, Donald J.,Pease, Lori J.,Soni, Niru B.,Stewart, Kent D.,Stoll, Vincent S.,Tapang, Paul,Reuter, David R.,Davidsen, Steven K.,Michaelides, Michael R.
, p. 1584 - 1597 (2008/02/01)
In our continued efforts to search for potent and novel receptor tyrosine kinase (RTK) inhibitors as potential anticancer agents, we discovered, through a structure-based design, that 3-aminoindazole could serve as an efficient hinge-binding template for kinase inhibitors. By incorporating an N,N′-diaryl urea moiety at the C4-position of 3-aminodazole, a series of RTK inhibitors were generated, which potently inhibited the tyrosine kinase activity of the vascular endothelial growth factor receptor and the platelet-derived growth factor receptor families. A number of compounds with potent oral activity were identified by utilizing an estradiol-induced mouse uterine edema model and an HT1080 human fibrosarcoma xenograft tumor model. In particular, compound 17p (ABT-869) was found to possess favorable pharmacokinetic profiles across different species and display significant tumor growth inhibition in multiple preclinical animal models.
The synthesis of novel highly substituted benzene derivatives for use in palladium-catalysed cross-coupling reactions
Hird, Michael,Lewis, Robert A.,Toyne, Kenneth J.,West, Jonathan J.,Wilson, Michael K.
, p. 3479 - 3484 (2007/10/03)
A combination of conventional electrophilic aromatic substitution reactions and low-temperature ortho-directed lithiations has been used in the efficient synthesis of some novel highly substituted benzene derivatives containing alkoxy, alkyl, bromo, cyano
