62875-50-7Relevant academic research and scientific papers
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 (2007)
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.
Use of ER selective NF-kB inhibitors for the treatment of sepsis
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, (2008/06/13)
The present invention provides methods for treating sepsis, systemic inflammatory response syndrome, severe sepsis, septic shock, and multiple organ dysfunction syndrome by modulating NF-κB transcription with ligands that interact with the estrogen receptor, preferably in the absence of classic estrogenic activity. Other aspects of the invention relate to methods for treating sepsis, systemic inflammatory response syndrome, severe sepsis, septic shock, and multiple organ dysfunction syndrome that comprise administering to a patient suffering therefrom an effective amount of a compound of Formula I:
2-CYANOPROPANOIC ACID AMIDE AND ESTER DERIVATIVES AND METHODS OF THEIR USE
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Page 60, (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.
