81015-49-8Relevant academic research and scientific papers
VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 0221; 0225, (2020/01/24)
Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
NOVEL NUCLEOSIDE PHOSPHORAMIDATE COMPOUND AND USE THEREOF
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Paragraph 0084, (2015/11/24)
The present invention provides a novel nucleoside phosphoramidate compound, or a stereoisomer, salt, hydrate, solvate or crystal thereof for the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The present invention also provides the pharmaceutical composition comprising a compound of the present invention, or a stereoisomer, salt, hydrate, solvate or crystal thereof and a use of the compound or the composition of the present invention in the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The compound of the present invention has a good anti-HCV effect.
Design, synthesis, and in vitro antitumor evaluation of novel diaryl ureas derivatives
Sun, Min,Wu, Xiaoqing,Chen, Junqing,Cai, Jin,Cao, Meng,Ji, Min
experimental part, p. 2299 - 2306 (2010/07/05)
Two series of novel diaryl ureas have been designed and synthesized, with their in vitro antitumor effect screened on human non-small cell lung cancer (NSCLC) cell line A549 and human breast cancer cell line MDA-MB-231. Some target compounds demonstrated significant inhibitory activities against both cell lines. Compared to contrast drug Sorafenib, 1b, 1d, 1f, 1i were found to demonstrate more potent antitumor activities. The structures of all the newly synthesized compounds were determined by 1H, 13C NMR, MS, IR and elementary analysis.
ARYL AMINO ACID DERIVATIVES AS INHIBITORS FOR TREATING INFLAMMATION
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Page/Page column 7; 16, (2008/06/13)
The present invention relates to a chemical genus of 3-(triaryl)-2-aminopropanol derivative inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention of inflammatory diseases and disorders. The compounds have general formula III: A particular embodiment is
BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
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Page/Page column 78, (2008/06/13)
The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is
New potent C2-symmetric malaria plasmepsin I and II inhibitors.
Oscarsson, Karin,Oscarson, Stefan,Vrang, Lotta,Hamelink, Elizabeth,Hallberg, Anders,Samuelsson, Bertil
, p. 1235 - 1246 (2007/10/03)
A series of malaria plasmepsin (Plm) I and II inhibitors containing a C(2)-symmetric core structure have been synthesised and tested for protease inhibition activity. These compounds can be prepared using a straightforward synthesis involving a phenol nuc
Preparation of 2- and 5-aryl substituted thiazoles via palladium-catalyzed Negishi cross-coupling
Jensen,Skj?rb?k,Veds?
, p. 128 - 134 (2007/10/03)
2-Aryl substituted thiazoles 3a-k were prepared by oxidative insertion of zinc into 2-bromothiazole (1) followed by palladium(0)-catalyzed Negishi cross-coupling in a one-pot procedure. 5-Aryl substituted thiazoles 6a-i were prepared by regioselective C-5 lithiation of 2-(trimethylsilyl)thiazole (4) followed by transmetalation with zinc chloride and palladium(0)-catalyzed Negishi cross-coupling in a one-pot procedure. The synthetic sequences were combined to give 2,5-diaryl substituted thiazoles 8a,b and 10 via stepwise C-2 and C-5 arylation and vice versa.
β1-Selective Adrenoceptor Antagonists: Examples of the 2-phenyl>imidazole Class. 2
Baldwin, John J.,Christy, Marcia E.,Denny, George H.,Habecker, Charles N.,Freedman, Mark B.,et al.
, p. 1065 - 1080 (2007/10/02)
An attempt to develop a highly cardioselective β-adrenoceptor antagonist devoid of intrinsic sympathomimetic activity (ISA) focused on exploring structure-activity relationships around (S)--amino>-2-hydroxypropoxy>phen
