C07C259/06

NOVEL THYROMIMETICS
20230048992 · 2023-02-16 ·

Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.

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NOVEL THYROMIMETICS
20230048992 · 2023-02-16 ·

Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.

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Derivatives of sobetirome

Compounds are provided that function as thyromimetics, which compounds have utility for treating diseases such as neurodegenerative disorders. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation. Such compounds have the structure of Formula (I) as shown herein, or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof.

SYNTHETIC METHODS FOR PREPARATION OF 4-(2-CHLORO-4-METHOXY-5-METHYLPHENYL)-N-[(1S)-2-CYCLOPROPYL-1-(3-FLUORO-4-METHYLPHENYL)ETHYL]-5-METHYL-N-PROP-2-YNYL-1,3-THIAZOL-2-AMINE

The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thi-azol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).

ASPARAGINE DERIVATIVES AND METHODS OF USING SAME

The present disclosure relates to compounds of formulas (A) and (I), pharmaceutically acceptable salts thereof, and solvates of any of the foregoing, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer, such as colorectal cancer, using the same.

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INDENE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS

Provided herein are an indene compound, e.g., a compound of Formula (I), and a pharmaceutical composition thereof. Also provided herein is a method of their use for treating, preventing, or ameliorating one or more symptoms of a fibrotic disease.

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INDENE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS

Provided herein are an indene compound, e.g., a compound of Formula (I), and a pharmaceutical composition thereof. Also provided herein is a method of their use for treating, preventing, or ameliorating one or more symptoms of a fibrotic disease.

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A CONTINUOUS FLOW PROCESS FOR THE SYNTHESIS OF HYDROXAMIC ACID
20230002312 · 2023-01-05 ·

The present invention relates to a process for the synthesis of hydroxamic acids by continuous flow process wherein said process comprising reacting alkyl ester with hydroxyl amine salt in presence of base in a microreactor system and continuously producing hydroxamic acid.

A CONTINUOUS FLOW PROCESS FOR THE SYNTHESIS OF HYDROXAMIC ACID
20230002312 · 2023-01-05 ·

The present invention relates to a process for the synthesis of hydroxamic acids by continuous flow process wherein said process comprising reacting alkyl ester with hydroxyl amine salt in presence of base in a microreactor system and continuously producing hydroxamic acid.

Inhibitors of histone lysine specific demethylase (LSD1) and histone deacetylases (HDACS)

A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.