66952-65-6Relevant academic research and scientific papers
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
, (2021/09/20)
Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
3,4-DISUBSTITUTED 3-CYCLOBUTENE-1,2-DIONES AND USE THEREOF
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Paragraph 0414; 0415, (2019/02/24)
Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula: The compounds are useful for treating inflammatory and autoimmune diseases.
Bicyclo[2.2.1]heptane containing: N, N ′-diarylsquaramide CXCR2 selective antagonists as anti-cancer metastasis agents
Che, Jin-Xin,Wang, Zhi-Long,Dong, Xiao-Wu,Hu, You-Hong,Xie, Xin,Hu, Yong-Zhou
, p. 11061 - 11069 (2018/03/26)
CXCR1 and CXCR2 are CXC chemokine receptors (CXCRs), corresponding to cytokines of the CXC chemokine family. CXCR2 was found to be 77% homologous to CXCR1. Antagonism of the chemokine receptor CXCR2 has been proposed as a new strategy for the treatment of
Probing the activity of a non-oxime reactivator for acetylcholinesterase inhibited by organophosphorus nerve agents
Cadieux, C. Linn,Wang, Haoyu,Zhang, Yuchen,Koenig, Jeffrey A.,Shih, Tsung-Ming,McDonough, John,Koh, John,Cerasoli, Douglas
, p. 133 - 141 (2016/12/09)
Currently fielded treatments for nerve agent intoxication include atropine, an acetylcholine receptor antagonist, and pralidoxime (2PAM), a small molecule reactivator of acetylcholinesterase (AChE). 2PAM reactivates nerve agent-inhibited AChE via direct n
NOVEL DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED DISEASES
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Paragraph 0151, (2015/03/31)
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds corresponding to general formula (I) are disclosed. Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
NOVEL DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED DISEASES
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Paragraph 0101, (2014/10/16)
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the tr
DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED PATHOLOGIES
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Paragraph 0110; 0114, (2014/10/29)
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the
NOVEL HYDRAZINO-CYCLOBUT-3-ENE-1, 2-DIONE DERIVATIVES AS CXCR2 ANTAGONISTS
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Page/Page column 23, (2010/09/03)
The present invention relates to novel hydrazino-cyclobut-3-ene-1,2-dione compounds of Formula (I) as selective CXCR2 antagonists, pharmaceutical compositions containing the novel compounds, as well as methods for treating or preventing chemokine mediated
ANTI -INFLAMMATORY SUBSTITUTED CYCLOBUTENEDIONE COMPOUNDS
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Page/Page column 26, (2009/01/24)
The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists
Chao, Jianhua,Taveras, Arthur G.,Chao, Jianping,Aki, Cynthia,Dwyer, Michael,Yu, Younong,Purakkattle, Biju,Rindgen, Diane,Jakway, James,Hipkin, William,Fosetta, James,Fan, Xuedong,Lundell, Daniel,Fine, Jay,Minnicozzi, Michael,Phillips, Jonathan,Merritt, J. Robert
, p. 3778 - 3783 (2008/02/10)
A novel series of cyclobutenedione centered C(4)-alkyl substituted furanyl analogs was developed as potent CXCR2 and CXCR1 antagonists. Compound 16 exhibits potent inhibitory activities against IL-8 binding to the receptors (CXCR2 Ki = 1 nM, IC50 = 1.3 nM; CXCR1 Ki = 3 nM, IC50 = 7.3 nM), and demonstrates potent inhibition against both Gro-α and IL-8 induced hPMN migration (chemotaxis: CXCR2 IC50 = 0.5 nM, CXCR1 IC50 = 37 nM). In addition, 16 has shown good oral pharmacokinetic profiles in rat, mouse, monkey, and dog.
