439151-92-5Relevant academic research and scientific papers
Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists
Cherney, Robert J.,Mo, Ruowei,Meyer, Dayton T.,Voss, Matthew E.,Lo, Yvonne C.,Yang, Gengjie,Miller, Persymphonie B.,Scherle, Peggy A.,Tebben, Andrew J.,Carter, Percy H.,Decicco, Carl P.
scheme or table, p. 3418 - 3422 (2010/02/28)
Potent sulfone-containing di- and trisubstituted cyclohexanes were synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the trisubstituted derivative 54, which exhibited excellent binding (CCR2 IC50 = 1.3 nM) and functional antagonism (calcium flux IC50 = 0.5 nM and chemotaxis IC50 = 0.2 nM). The superiority of the trisubstituted scaffold was rationalized to be the result of a conformational rigidification, which provided insight into the bioactive conformation of this chemotype.
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
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Page/Page column 34, (2010/02/11)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
Cyclic derivatives as modulators of chemokine receptor activity
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, (2008/06/13)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and
