C07C311/44

COMPOUNDS WITH ANTIMICROBIAL ACTIVITY
20200347010 · 2020-11-05 ·

This invention relates to compounds of formula 1, 2 or 3

##STR00001##

a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

Compounds and methods for hematopoietic regeneration

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

Compounds and methods for hematopoietic regeneration

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

METHODS AND COMPOSITIONS FOR TREATMENT OF MUSCLE WASTING, MUSCLE WEAKNESS, AND/OR CACHEXIA

Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

METHODS AND COMPOSITIONS FOR TREATMENT OF MUSCLE WASTING, MUSCLE WEAKNESS, AND/OR CACHEXIA

Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.

4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.

Preparation and use of silver sulfadiazine-immobilized fillers
10736821 · 2020-08-11 · ·

Silver sulfadiazine-immobilized inorganic fillers are described, and their synthesis is presented. The fillers are believed to have utility in dental composites and dental adhesives to achieve potent, long-term, and none-leaching antimicrobial effects.

Preparation and use of silver sulfadiazine-immobilized fillers
10736821 · 2020-08-11 · ·

Silver sulfadiazine-immobilized inorganic fillers are described, and their synthesis is presented. The fillers are believed to have utility in dental composites and dental adhesives to achieve potent, long-term, and none-leaching antimicrobial effects.

SULFONAMIDE OR AMIDE COMPOUNDS, COMPOSITIONS AND METHODS FOR THE PROPHYLAXIS AND/OR TREATMENT OF AUTOIMMUNE, INFLAMMATION OR INFECTION RELATED DISORDERS

The present invention related to novel sulfonamides or amides as TLR-4 antagonists, and pharmaceutical formulations containing the same and the methods of use thereof. Uses of the present novel sulfonamides or amides include, but are not limited to, the prophylaxis and/or treatment of autoimmune, inflammation, or infection related disorders.