Patent classifications
C07C235/54
T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS
The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.
T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS
The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.
Inhibitors of the WNT/beta-catenin pathway
The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY
The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
Anti-inflammatory compounds
Synthetic kava analog compounds of formula I are disclosed. Specifically, kava analogs of the structural type 3-oxoclclohex-1-en-1-yl benzoates, and corresponding benzamides are disclosed. The compounds of the within invention are useful in the inhibition of cytokine TNF-α, the management of chronic inflammation such as but not limited to Porphyromonas gingivalis induced periodontitis, and in infective arthritis, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other anti-inflammatory active pharmaceutical ingredients. Methods of treating chronic inflammation such as periodontitis and infective arthritis are also disclosed.
PROCESS OF MAKING A CRYSTALLINE EDG-2 RECEPTOR ANTAGONIST
Described herein are methods of making crystalline Form 1 of 2-(4-methoxy-3-(3-methylphenethoxy)benzamido)-2,3-dihydro-1H-indene-2-carboxylic acid.
PROCESS OF MAKING A CRYSTALLINE EDG-2 RECEPTOR ANTAGONIST
Described herein are methods of making crystalline Form 1 of 2-(4-methoxy-3-(3-methylphenethoxy)benzamido)-2,3-dihydro-1H-indene-2-carboxylic acid.
CRYSTALLINE EDG-2 RECEPTOR ANTAGONIST AND METHODS OF MAKING
Described herein are crystalline forms of 2-(4-methoxy-3-(3-methylphenethoxy)benzamido)-2,3-dihydro-1H-in-dene-2-carboxylic acid and methods of making the same. Such forms of 2-(4-methoxy-3-(3-methylphenethoxy)benzamido)-2,3-dihydro-1H-indene-2-carboxylic acid are useful in the preparation of pharmaceutical compositions for the treatment of diseases or conditions that would benefit by administration with an EDG-2 receptor antagonist compound.