473733-03-8Relevant academic research and scientific papers
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.
THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
-
Page 263, (2008/06/13)
Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
-
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
-
Page 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.
