796853-76-4Relevant articles and documents
Estrogen receptor dependent inhibitors of NF-κB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: Pathway selective inhibitors of NF-κB, a potential treatment for rheumatoid arthritis
Caggiano, Thomas J.,Brazzale, Antony,Ho, Douglas M.,Kraml, Christina M.,Trybulski, Eugene,Chadwick, Christopher C.,Chippari, Sue,Borges-Marcucci, Lisa,Eckert, Amy,Keith, James C.,Kenney, Thomas,Harnish, Douglas C.
, p. 5245 - 5248 (2008/03/14)
Pathway selective ligands of the estrogen receptor inhibit transcriptional activation of proinflammatory genes mediated by NF-κB. Substituted 2-cyanopropanoic acid derivatives were developed leading to the discovery of WAY-204688, an orally active, pathway selective, estrogen receptor dependent anti-inflammatory agent. This propanamide was shown to be orally active in preclinical models of inflammatory diseases, such as rheumatoid arthritis, without the proliferative effect associated with traditional estrogens.
2-CYANOPROPANOIC ACID AMIDE AND ESTER DERIVATIVES AND METHODS OF THEIR USE
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Page 46, (2008/06/13)
This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof that are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
