- DERIVATIVES OF SUBSTITUTED 3-PHENYL-1-(PHENYLTHIENYL)PROPAN-1-ONES AND OF 3-PHENYL-1-(PHENYLFURANYL) PROPAN-1-ONES, PREPARATION AND USE
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The present invention relates to compounds derived from substituted 3-phenyl-1-(thien-2-yl)propan-1-ones, pharmaceutical compositions comprising them as well as their therapeutic applications, notably in the field of human and animal health.
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Page/Page column 12-13
(2010/03/02)
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- ERβ ligands. Part 2: Synthesis and structure-activity relationships of a series of 4-hydroxy-biphenyl-carbaldehyde oxime derivatives
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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).
- Yang, Cuijian,Edsall Jr., Richard,Harris, Heather A.,Zhang, Xiaochun,Manas, Eric S.,Mewshaw, Richard E.
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p. 2553 - 2570
(2007/10/03)
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- HYDROXY-BIPHENYL-CARBALDEHYDE OXIME DERIVATIVES AND THEIR USE AS ESTROGENIC AGENTS
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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.
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Page 18; 38-39
(2008/06/13)
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- Phenoxyacetic acid derivatives composition and use
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Novel phenoxyacetic acid derivatives of the formula: STR1 wherein A is a substituted or unsubstituted 5-pyrazolyl group, R1 is hydrogen atom or a lower alkyl group, R2 is hydrogen atom or a lower alkenyl group, X is a halogen atom and Z is oxygen atom or methylene group, and salts thereof have potent diuretic, saluretic and uricosuric activities.
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- Synthesis and Spectroscopic Data of Chlorinated 4-Hydroxybenzaldehydes
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All chlorinated 4-hydroxybenzaldehydes including three hitherto unknown compounds have been synthesized from chlorinated phenols by applying the Reimer-Tiemann method. (1)H NMR, (13)C NMR, and mass-spectral data on all compounds are reported.
- Knuutinen, Juha S.,Kolehmainen, Erkki T.
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p. 139 - 141
(2007/10/02)
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- [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids, their analogs, esters, salts, and derivatives
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The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acid and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthe
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