C07D307/84

T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS
20180003702 · 2018-01-04 ·

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
20180003702 · 2018-01-04 ·

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.

Ligand-Enabled meta-C-H Activation Using a Transient Mediator
20180009739 · 2018-01-11 ·

An alternative approach to formation of a C-C bond at a meta-position of an aromatic compound is disclosed that employs an ethylenically unsaturated bicyclic compound as a transient mediator to achieve meta-selective C-H activation with a simple and common ortho-directing group. The use of a pyridine-based ligand assists in relaying the palladium catalyst to the meta-position by the unsaturated bicyclic compound following initial ortho-C-H activation.

Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors

This invention relates to compounds of Formula (I) wherein Cy.sup.1, L.sup.1, Y, R.sup.1, L.sup.2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions. ##STR00001##

Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors

This invention relates to compounds of Formula (I) wherein Cy.sup.1, L.sup.1, Y, R.sup.1, L.sup.2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions. ##STR00001##

Benzo-fused heterocyclic derivatives useful as agonists of GPR120

The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

Benzo-fused heterocyclic derivatives useful as agonists of GPR120

The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

Fused furans for the treatment of hepatitis C

The disclosure provides compounds of formula I or II, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. ##STR00001##

Fused furans for the treatment of hepatitis C

The disclosure provides compounds of formula I or II, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. ##STR00001##

METHOD OF EXTRACTING NUTRIENTS FROM A PLANT
20170216739 · 2017-08-03 ·

A method of extracting nutrients from a plant includes the steps of: pulverizing a water soluble nutrient-based plant part of a first plant material of the plant so as to form a first pulverized plant part; pulverizing a lipid soluble nutrient-based plant part of a second plant material of the plant so as to form a second pulverized plant part; subjecting the first pulverized plant part to a distillation so as to obtain a distillate and a first residue that contains a water soluble nutrient; and immersing the second pulverized plant part in the distillate to form a first mixture followed by distillation of the first mixture, so as to obtain a second residue that contains a lipid soluble nutrient.