C07D213/74

NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS

The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

HOST MATERIAL, COMPOSITION, AND ORGANIC ELECTROLUMINESCENT ELEMENT
20230113918 · 2023-04-13 ·

To improve the emission efficiency, the driving voltage and the lifetime of an organic light-emitting device using a delayed fluorescent material. A host material for a delayed fluorescent material, containing a compound represented by the following general formula: R.sup.1 to R.sup.5 each are a substituent not containing a cyano group. n1 to n5 each are 0 to 4, Ar is a monocyclic arylene group or a monocyclic heteroarylene group.

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SUBSTITUTED PYRIDINE AND PYRAZINE COMPOUNDS AS PDE4 INHIBITORS

The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders, including inflammatory and renal disorders.

SUBSTITUTED PYRIDINE AND PYRAZINE COMPOUNDS AS PDE4 INHIBITORS

The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders, including inflammatory and renal disorders.

BROMODOMAIN INHIBITORS
20220315601 · 2022-10-06 · ·

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

BROMODOMAIN INHIBITORS
20220315601 · 2022-10-06 · ·

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

CHARGED ION CHANNEL BLOCKERS AND METHODS FOR USE
20230107360 · 2023-04-06 ·

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts 5 thereof:

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The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.

HETEROAROMATIC ACETAMIDE DERIVATIVE, AND PREPARATION AND USE THEREOF

Provided in the present invention are a heteroaromatic acetamide derivative and the preparation and the use thereof, wherein the heteroaromatic acetamide derivative is a heteroaromatic acetamide compound as shown in general formula (I), or a pharmaceutically acceptable salt and/or solvate thereof. According to the present invention, experiments have confirmed that the heteroaromatic acetamide derivative of the present invention can specifically bind to transient receptor potential ankyrin 1 (TRPA1) and inhibit or reduce the activity thereof, and can be used for treating diseases mediated by TRPA1. The present invention further provides a method for preparing the heteroaromatic acetamide derivative, and a drug and pharmaceutical composition containing the heteroaromatic acetamide derivative.

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COMPOUND FOR TREATING ALZHEIMERS DISEASE

Provided in the present invention are a compound as shown in formula I, various crystal forms thereof, a hydrate, a solvate or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition. The compound of the present invention can effectively treat Alzheimer's disease or Down's syndrome, especially cognitive function impairment caused by Alzheimer's disease or Down's syndrome. Also disclosed in the present invention is use of a ubiquitin specific protease USP25 encoded and expressed by chromosome 21 for preventing, treating or ameliorating Alzheimer's disease or Down's syndrome.

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COMPOUND FOR TREATING ALZHEIMERS DISEASE

Provided in the present invention are a compound as shown in formula I, various crystal forms thereof, a hydrate, a solvate or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition. The compound of the present invention can effectively treat Alzheimer's disease or Down's syndrome, especially cognitive function impairment caused by Alzheimer's disease or Down's syndrome. Also disclosed in the present invention is use of a ubiquitin specific protease USP25 encoded and expressed by chromosome 21 for preventing, treating or ameliorating Alzheimer's disease or Down's syndrome.

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