88095-61-8Relevant academic research and scientific papers
Design and synthesis of anti-tumor compounds containing ferulic acid-pyrazole skeleton
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Paragraph 0024-0025; 0027-0028; 0031-0032; 0034, (2021/04/28)
The invention discloses design and a preparation method of an anti-tumor compound containing a ferulic acid-pyrazole skeleton. The structure of the anti-tumor compound is shown as a formula in the specification.
COMPOUNDS AND USES THEREOF
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Paragraph 0853; 1110, (2019/11/11)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAFV600E inhibitors
Wang, Chen-Ru,Wang, Ze-Feng,Shi, Lu,Wang, Zhong-Chang,Zhu, Hai-Liang
supporting information, p. 2382 - 2390 (2018/06/25)
With the increasingly acquired resistance, relapse and side effects of known marketed BRAFV600E inhibitors, it's significant to design the more effective and novel drugs. In this study, a series of novel pyrazole derivatives containing acetamid
Identification and Biological Evaluation of Novel Type II B-RafV600E Inhibitors
Wang, Peng-Fei,Wang, Ze-Feng,Qiu, Han-Yue,Huang, Yue,Hu, Hui-Min,Wang, Zhong-Chang,Zhu, Hai-Liang
, p. 2558 - 2566 (2018/11/23)
The mitogen-activated protein kinase (MAPK) pathway plays a vital role in signal transduction networks. Severe diseases may be triggered if it is disturbed by mutated components, especially the kinase B-RafV600E. New inhibitors of the kinase ar
C-H arylation of nitroimidazoles and nitropyrazoles guided by the electronic effect of the nitro group
Jung, Haeun,Bae, Seri,Jang, Ha-Lim,Joo, Jung Min
, p. 3009 - 3014 (2014/12/11)
A palladium-catalyzed C-H arylation reaction of nitroimidazoles and nitropyrazoles was developed using aryl bromides as arene donors. The electron-withdrawing effect of the nitro group allows for direct C-H arylation reactions of the nitro diazoles with h
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible t-cell kinase inhibitors
Burch, Jason D.,Lau, Kevin,Barker, John J.,Brookfield, Fred,Chen, Yong,Chen, Yuan,Eigenbrot, Charles,Ellebrandt, Claire,Ismaili, M. Hicham A.,Johnson, Adam,Kordt, Daniel,Mackinnon, Colin H.,McEwan, Paul A.,Ortwine, Daniel F.,Stein, Daniel B.,Wang, Xiaolu,Winkler, Dirk,Yuen, Po-Wai,Zhang, Yamin,Zarrin, Ali A.,Pei, Zhonghua
, p. 5714 - 5727 (2014/08/05)
Interleukin-2 inducible T-cell kinase (ITK), a member of the Tec family of tyrosine kinases, plays a major role in T-cell signaling downstream of the T-cell receptor (TCR), and considerable efforts have been directed toward discovery of ITK-selective inhibitors as potential treatments of inflammatory disorders such as asthma. Using a previously disclosed indazole series of inhibitors as a starting point, and using X-ray crystallography and solubility forecast index (SFI) as guides, we evolved a series of tetrahydroindazole inhibitors with improved potency, selectivity, and pharmaceutical properties. Highlights include identification of a selectivity pocket above the ligand plane, and identification of appropriate lipophilic substituents to occupy this space. This effort culminated in identification of a potent and selective ITK inhibitor (GNE-9822) with good ADME properties in preclinical species.
Faujasite catalyzed nitrodeiodination of iodopyrazoles
Ravi,Tewari, Surya P.
, p. 35 - 39 (2013/09/12)
Nitrodeiodination of iodopyrazoles using nitric acid/Faujasite has been investigated. The present procedure is simple, rapid and convenient and requires no sulfuric acid or oleum and may be applied for the synthesis of several nitropyrazoles in good yield
Silica-sulfuric acid catalyzed nitrodeiodination of iodopyrazoles
Ravi,Gore, Girish M.,Sikder, Arun K.,Tewari, Surya P.
experimental part, p. 3463 - 3471 (2012/09/22)
We report here the synthesis of nitropyrazoles in good to excellent yields from iodopyrazoles over silica-sulfuric acid catalyst for the first time. The present procedure require less acid, offers a simplified workup procedure, and may be applied for the
HETEROCYCLIC GAMMA SECRETASE MODULATORS
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Page/Page column 27-28, (2010/06/11)
The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise ad
