Patent classifications
C07D209/08
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.
BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS
The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.
BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS
The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.
SYNTHESIS OF CYCLOPROPYL INDOLES AND CYCLOHEPTA[B]INDOLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHOD OF USING THEM
Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst.
SYNTHESIS OF CYCLOPROPYL INDOLES AND CYCLOHEPTA[B]INDOLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHOD OF USING THEM
Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst.
SPIRO-TYPE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT COMPRISING SAME
The present specification provides a compound having a spiro structure, and an organic light emitting device including the same.
SPIRO-TYPE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT COMPRISING SAME
The present specification provides a compound having a spiro structure, and an organic light emitting device including the same.
DEUTERATED ORGANIC COMPOUND, MIXTURE AND COMPOSITION CONTAINING SAID COMPOUND, AND ORGANIC ELECTRONIC DEVICE
The present disclosure discloses a deuterated organic compound and a formulation and an organic electronic device containing the same, wherein the deuterated organic compound has the following structural formula:
##STR00001##
wherein Ar is an aromatic or heteroaromatic structural unit, D is an electron donor group, A is an electron acceptor group, n and m are an integer between 1 and 6; and wherein for the organic compound, (S1-T1)≦0.25 eV, and at least one H atom of the organic compound is substituted by deuterium. The present disclosure achieves the improvement of the electroluminescence quantum efficiency and the lifetime of the organic compound by replacing the H atom in the organic compound with deuterium and having (S1-T1)≦0.35 eV, and the material of the present disclosure has a great application potential and application range due to its low cost and relatively simple synthesis process.
Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors
Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity. ##STR00001##
ARYL RECEPTOR MODULATORS AND METHODS OF MAKING AND USING THE SAME
The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.