A61K31/422

EXOGENOUS NITRIC OXIDE FOR IMPROVED SUSCEPTIBILITY AND LOWERED ANTIBIOTIC RESISTANCE IN RESISTANT RESPIRATORY BACTERIA
20230082968 · 2023-03-16 ·

Disclosed are antimicrobial compositions and formulations directed against a broad range of bacteria and Pseudomonas aeruginosa biofilms. In an aspect, the compositions and formulations do not engender resistance. In an aspect, in combination with antibiotics, the compositions and formulations slow the development of antibiotic-resistance and greatly improve bacterial susceptibility to multiple classes of antibiotics.

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
20220331297 · 2022-10-20 ·

The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
20220331297 · 2022-10-20 ·

The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Anat Inhibitors and Methods of Use Thereof
20230128972 · 2023-04-27 ·

Inhibitors of a critical brain enzyme, N-acetyltransferase (ANAT), and methods of discovering, making and using the same for the treatment of disease are disclosed.

NEW INHIBITORS FOR THE KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION

Described herein are compounds, compositions and methods useful for inhibiting Kelch-like ECH-associated protein 1 (KEAP1). The compounds, compositions and methods described herein are useful for treating diseases, disorders or conditions associated with KEAP1.

NEW INHIBITORS FOR THE KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION

Described herein are compounds, compositions and methods useful for inhibiting Kelch-like ECH-associated protein 1 (KEAP1). The compounds, compositions and methods described herein are useful for treating diseases, disorders or conditions associated with KEAP1.

METHODS AND PHARMACEUTICAL COMPOSITIONS OF THROMBOXANE A2 RECEPTOR ANTAGONIST FOR THE TREATMENT OF COVID-19
20230129262 · 2023-04-27 ·

The present invention is related to the use of thromboxane A2 receptor antagonists (e.g., 3-[2-[[(1S,2R,3S,4R)-3-[4-(pentylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid (Ifetroban), or one, or a mixture of more than one pharmaceutically acceptable salts thereof) in the treatment of SARS-CoV-2 infection in humans, and pharmaceutical compositions for the same comprising thromboxane A2 receptor antagonists (e.g., ifetroban) in an effective amount to treat and/or prevent conditions resulting from such infection.

METHODS AND PHARMACEUTICAL COMPOSITIONS OF THROMBOXANE A2 RECEPTOR ANTAGONIST FOR THE TREATMENT OF COVID-19
20230129262 · 2023-04-27 ·

The present invention is related to the use of thromboxane A2 receptor antagonists (e.g., 3-[2-[[(1S,2R,3S,4R)-3-[4-(pentylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid (Ifetroban), or one, or a mixture of more than one pharmaceutically acceptable salts thereof) in the treatment of SARS-CoV-2 infection in humans, and pharmaceutical compositions for the same comprising thromboxane A2 receptor antagonists (e.g., ifetroban) in an effective amount to treat and/or prevent conditions resulting from such infection.

Fused imidazole derivatives as IL-17 modulators

A series of substituted fused bicyclic imidazole derivatives, including benzimidazole derivatives and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

Fused imidazole derivatives as IL-17 modulators

A series of substituted fused bicyclic imidazole derivatives, including benzimidazole derivatives and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.