280752-96-7Relevant academic research and scientific papers
ACRYLAMIDE DERIVATIVES AS VLA-1 INTEGRIN ANTAGONISTS AND USES THEREOF
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Page/Page column 150-151, (2010/02/10)
Compounds that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds, and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-1 integrin.
Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
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, (2008/06/13)
The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
HYDROXY-BIPHENYL-CARBALDEHYDE OXIME DERIVATIVES AND THEIR USE AS ESTROGENIC AGENTS
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Page 18; 39, (2008/06/13)
This invention provides estrogen receptor modulators having the structure formula (I): wherein R1 to R6 and R8 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
ERβ ligands. Part 2: Synthesis and structure-activity relationships of a series of 4-hydroxy-biphenyl-carbaldehyde oxime derivatives
Yang, Cuijian,Edsall Jr., Richard,Harris, Heather A.,Zhang, Xiaochun,Manas, Eric S.,Mewshaw, Richard E.
, p. 2553 - 2570 (2007/10/03)
A series of biphenyl carbaldehyde oximes (6) was prepared and shown to have significant selectivity for the estrogen receptor-β (ERβ). The exploitation of the oxime moiety as a hydrogen bond donating group, which mimicked the C-ring of genistein makes these compounds unique. Molecular modeling studies showed the oxime moiety hydrogen bonding to the histidine residue, which was supported by the structure-activity relationships. The most potent compounds in this study had IC50 values in a radioligand binding assay of between 8-35nM. Among the most selective compounds were 6i and 6s (49- and 31-fold ERβ selective, respectively).
Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
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Page 74, (2010/02/07)
The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
Amino(oxo) acetic acid protein tyrosine phosphatase inhibitors
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, (2008/06/13)
Compounds of formula (I) or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure - Activity relationship of substituents on the benzene ring of the cinnamide
Winn,Kester,Von Geldern,Leitza,Devries,Dickinson,Mussatto,Okasinski,Reilly,Liu,Huth,Jae,Freeman,Pei,Xin,Lynch
, p. 4393 - 4403 (2007/10/03)
We have shown that p-arylthio cinnamides can inhibit the interaction of LFA-1 and ICAM-1, which is involved in cell adhesion and the inflammatory process. We now show that 2,3-disubstitution on the aryl portion of the cinnamide results in enhanced activit
Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists
Link, James T.,Sorensen, Bryan,Liu, Gang,Pei, Zhonghua,Reilly, Edward B.,Leitza, Sandra,Okasinski, Greg
, p. 973 - 976 (2007/10/03)
Diarylsulfide cyclopropylamides were synthesized and evaluated as LFA-1/ICAM-1 interaction antagonists. A substituent pattern was identified which maximized potency and minimized protein binding as exemplified by antagonist 30 (IC50 = 5 nM).
