C07D275/03

METHODS AND MATERIALS FOR INHIBITING NF-kB ACTIVITY
20230041576 · 2023-02-09 ·

This document provides compounds that are inhibitors of NF-κB activity, as well as the methods of using such compounds for treating diseases and conditions such as cancer, inflammatory conditions, or autoimmune diseases.

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.

HERBICIDAL COMPOUNDS

The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.

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ANTICANCER COMPOUNDS
20230025178 · 2023-01-26 ·

Disclosed are compounds of formula (I):

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and pharmaceutically acceptable salts thereof. The compounds of the invention are BDII-selective inhibitors of BET proteins, and have therapeutic potential for treating cancer, acute kidney disease, and viral infections, among other diseases.

ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

SMYD Inhibitors

The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

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SMYD Inhibitors

The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

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MYST family histone acetyltransferase inhibitors

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

SMYD Inhibitors

The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

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AMIDE COMPOUND CONTAINING SUBSTITUTED ACETOPHENONE STRUCTURAL FRAGMENTS AND PREPARATION METHOD AND APPLICATION THEREOF

The present invention discloses an amide compound containing substituted acetophenone structural fragments, having a structure shown by general formula I:

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The definitions of substituents in the formula are shown in the description. The compound of the present invention has broad-spectrum fungal activity, and has excellent control effects on cucumber downy mildew, wheat powdery mildew, corn rust, cucumber anthracnose, cucumber botrytis and tomato botrytis.