C07D231/54

PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF INFLAMMATORY DISEASES COMPRISING NAPHTHOQUINONE DERIVATIVE
20220354825 · 2022-11-10 · ·

Provided is a method for the prevention or treatment of inflammatory diseases using a naphthoquinone or benzoindazole compound which increases the ratio of NAD.sup.+ and NAD.sup.+/NADH through activity in NQO1 in vivo, and through this, activates mitochondria, thereby inducing the metabolism of macrophages towards mitochondrial OXPHOS, which is the major metabolic pathway of M2 phenotype macrophages, such that the macrophages are polarized into an anti-inflammatory macrophage M2 phenotype, and consequently is able to inhibit the expression and activity of inflammatory cytokines, or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, diasteromer, tautomer, or prodrug thereof.

TETRACYCLINE COMPOUNDS AND METHODS OF TREATMENT

The present invention is directed to methods of treating hematological cancers, such as acute myleiod leukemia, with tetracyclines, or a pharmaceutically acceptable salt thereof.

Substituted pyridines, pyridazines, pyrimidines, and 1,2,4-triazines as TYK2 inhibitors

Described herein are compounds of Formula (XVII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of Using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity. ##STR00001##

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
20230092163 · 2023-03-23 ·

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., (cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

CRF RECEPTOR ANTAGONISTS AND METHODS OF USE

Compounds are provided herein that antagonize corticotropin-releasing factor (CRF) receptors, in particular CRF receptor 1 (CRF.sub.1), as well as related preparations, compositions and methods for treating diseases and/or disorders that would benefit from the same such as congenital adrenal hyperplasia (CAH).

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CRF RECEPTOR ANTAGONISTS AND METHODS OF USE

Compounds are provided herein that antagonize corticotropin-releasing factor (CRF) receptors, in particular CRF receptor 1 (CRF.sub.1), as well as related preparations, compositions and methods for treating diseases and/or disorders that would benefit from the same such as congenital adrenal hyperplasia (CAH).

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INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX KINASE ("NACK") AND METHODS FOR USE OF THE SAME

Disclosed herein are Notch transcriptional activation complex kinase (“MACK”) inhibitors, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein include compounds of Formula (Ia) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

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INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX KINASE ("NACK") AND METHODS FOR USE OF THE SAME

Disclosed herein are Notch transcriptional activation complex kinase (“MACK”) inhibitors, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein include compounds of Formula (Ia) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

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PYRAZOLE DERIVATIVES WITH ANTICANCER ACTIVITY

The inventors have used a differential nuclear staining (DNS) assay to discover compounds with cytotoxic activity against the CEM cell line that has been determined to be highly sensitive to a variety of anti-cancer compounds. Compounds were synthesized based on a pyrazole backbone structure. Several newly synthesized compounds have been tested to identify the compounds with highest activity. One compound identified is the SSK-3 compound which has been tested on cancer cell lines and determined that it induced apoptosis via phosphatidylserine membrane exposure and activation of caspase 3 in the CEM lymphoma cell line.

PYRAZOLE DERIVATIVES WITH ANTICANCER ACTIVITY

The inventors have used a differential nuclear staining (DNS) assay to discover compounds with cytotoxic activity against the CEM cell line that has been determined to be highly sensitive to a variety of anti-cancer compounds. Compounds were synthesized based on a pyrazole backbone structure. Several newly synthesized compounds have been tested to identify the compounds with highest activity. One compound identified is the SSK-3 compound which has been tested on cancer cell lines and determined that it induced apoptosis via phosphatidylserine membrane exposure and activation of caspase 3 in the CEM lymphoma cell line.