608537-88-8Relevant articles and documents
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.
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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Page 136; 139, (2008/06/13)
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
3,4-DI-SUBSTITUTED CYCLOBUTENE-1, 2-DIONES AS CXC-CHEMOKINE RECEPTOR LIGANDS
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Page 137, (2008/06/13)
Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof. Also disclosed is the treatment of chemokine-mediated diseases using compounds of the formula (II)