957056-06-3Relevant academic research and scientific papers
The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists
Matthews, Jay M.,Qin, Ning,Colburn, Raymond W.,Dax, Scott L.,Hawkins, Mike,McNally, James J.,Reany, Laura,Youngman, Mark A.,Baker, Judith,Hutchinson, Tasha,Liu, Yi,Lubin, Mary Lou,Neeper, Michael,Brandt, Michael R.,Stone, Dennis J.,Flores, Christopher M.
, p. 2922 - 2926 (2012/06/04)
A series of benzothiophene-based phosphonates was synthesized and many analogs within the series were shown to be potent antagonists of the TRPM8 channel. The compounds were obtained as a racemic mixture in 5 synthetic steps, and were tested for TRPM8 antagonist activity in a recombinant, canine TRPM8-expressing cell line using a fluorometric imaging plate reader (FLIPR) assay. Structure-activity relationships were developed initially by modification of the core structure and subsequently by variation of the aromatic substituents and the phosphonate ester. Compound 9l was administered intraperitoneally to rats and demonstrated engagement of the TRPM8 target in both prevention and reversal-modes in an icilin-induced 'wet-dog' shake model.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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Page/Page column 53, (2012/03/12)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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Page/Page column 53, (2012/07/28)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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Page/Page column 168-169; 170, (2008/06/13)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
