C07D213/75

2-(3-(2-METHYL-6-(P-TOLYL) PYRIDINE-3-YL) UREIDO) BENZENESULFONAMIDE AND DERIVATIVES AS INHIBITOR OF CARBONIC ANHYDRASE IX FOR THE TREATMENT OF CANCER

2-(3-(2-Methyl-6-(p-tolyl) pyridine-3-yl) ureido) benzenesulfonamide (formula I) compound and related pyridine based sulfonamide derivatives are disclosed. The compound of the invention is a carbonic anhydrase targeted small molecule and also an inhibitor of carbonic anhydrase activity and overexpression. Therefore, the compound is useful, as pharmaceutical agent, especially in the treatment and/or prevention of disorders associated with proliferative diseases, such as cancer.

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2-(3-(2-METHYL-6-(P-TOLYL) PYRIDINE-3-YL) UREIDO) BENZENESULFONAMIDE AND DERIVATIVES AS INHIBITOR OF CARBONIC ANHYDRASE IX FOR THE TREATMENT OF CANCER

2-(3-(2-Methyl-6-(p-tolyl) pyridine-3-yl) ureido) benzenesulfonamide (formula I) compound and related pyridine based sulfonamide derivatives are disclosed. The compound of the invention is a carbonic anhydrase targeted small molecule and also an inhibitor of carbonic anhydrase activity and overexpression. Therefore, the compound is useful, as pharmaceutical agent, especially in the treatment and/or prevention of disorders associated with proliferative diseases, such as cancer.

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KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE

Disclosed herein are kinase inhibitor compounds having the structure (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R.sup.1, R.sup.2, X, L, Q, and Y are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

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MrgprX2 Antagonists and Uses Thereof

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.

MrgprX2 Antagonists and Uses Thereof

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.

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.

DISUBSTITUTED ADAMANTYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION FOR SUPPRESSING CANCER GROWTH COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to: a disubstituted adamantyl derivative or a pharmaceutically acceptable salt thereof, and an anticancer pharmaceutical composition and a kit containing same as an active ingredient. The disubstituted adamantyl derivative according to the present invention suppresses the growth of cancer cells by targeting mitochondria ETC complex I and damaging the metabolism of cancer cells, and thus can be useful as an anticancer pharmaceutical composition that is a powerful therapeutic agent for cancer dependent on oxidative phosphorylation for producing ATP.

Krüppel-Like Factor 15 (KLF15) Small Molecule Agonists in Kidney Disease
20230219893 · 2023-07-13 ·

The present disclosure is concerned with small molecule modulators of KLF15 signaling useful for treating various disorders such as, for example, kidney disease (e.g., chronic kidney disease), heart disease, obesity, or a neurodegenerative disorder (e.g., amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

AKT3 MODULATORS
20230219927 · 2023-07-13 ·

Compounds of Formula 1a, 1b, or Ic, (Ia); (Ib); or (Ic), are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

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AKT3 MODULATORS
20230219927 · 2023-07-13 ·

Compounds of Formula 1a, 1b, or Ic, (Ia); (Ib); or (Ic), are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

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