C07H15/234

SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS

The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula:

##STR00001##

where R.sub.1, R.sub.2, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Q, and n are described herein.

SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS

The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula:

##STR00001##

where R.sub.1, R.sub.2, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Q, and n are described herein.

NITRIC OXIDE-RELEASING POLYAMINOGLYCOSIDES AS BIODEGRADABLE ANTIBACTERIAL SCAFFOLDS AND METHODS PERTAINING THERETO
20200030362 · 2020-01-30 ·

Provided herein are hyperbranched polyaminoglycosides, where in some embodiments, the hyperbranched polyaminoglycosides are covalently modified to store and release nitric oxide. Some embodiments pertain to methods of making and use of hyperbranched polyaminoglycosides. In some embodiments, the covalently modified hyperbranched polyaminoglycosides may be tailored to release nitric oxide in a controlled manner and are useful for eradication of both gram positive and gram negative bacteria as well as other microbes.

Kanamycin compound, kanamycin-producing Streptomyces species bacterium, and method of producing kanamycin

Vectors expressing kanA-kanB-kanK and other kanamycin production-related genes, Streptomyces species recombinant bacteria transformed with the vectors, a method of producing kanamycin antibiotics by the bacteria, and a new kanamycin compound produced by the bacterium are provided. With the use of the recombinant bacteria of the present invention, the direct fermentative biosynthesis of amikacin and tobramycin as semi-synthetic kanamycins is possible, and the yield of kanamycin B as a precursor of the semi-synthetic kanamycin is improved.

Kanamycin compound, kanamycin-producing Streptomyces species bacterium, and method of producing kanamycin

Vectors expressing kanA-kanB-kanK and other kanamycin production-related genes, Streptomyces species recombinant bacteria transformed with the vectors, a method of producing kanamycin antibiotics by the bacteria, and a new kanamycin compound produced by the bacterium are provided. With the use of the recombinant bacteria of the present invention, the direct fermentative biosynthesis of amikacin and tobramycin as semi-synthetic kanamycins is possible, and the yield of kanamycin B as a precursor of the semi-synthetic kanamycin is improved.

Potentiation of ?-lactam antibiotics and ?-lactam/?-lactamase inhibitor combinations against multidrug and extensively drug-resistant <i>Pseudomonas aeruginosa </i>using non-ribosomal tobramycin-cyclam conjugates

Herein, we describe the development of non-?-lactam-based potentiator molecules that synergize with ?-lactam antibiotics and ?-lactam-?-lactamase inhibitor combinations against MDR/XDR P. aeruginosa phenotypes. The compound comprises a chemical structure or chemical formula of Formula (A) or a suitable salt form thereof, wherein n is a carbon tether having a length of between about 2-18 carbons.

TRANSCRIPTOME-WIDE DESIGN OF SELECTIVE, BIOACTIVE SMALL MOLECULES TARGETING RNA
20190156912 · 2019-05-23 ·

Methods and computer systems are described herein for identifying small molecules that bind to selected RNA structural features (e.g., to RNA secondary structures). Also described are compounds and compositions that modulate RNA function and/or activity.

TRANSCRIPTOME-WIDE DESIGN OF SELECTIVE, BIOACTIVE SMALL MOLECULES TARGETING RNA
20190156912 · 2019-05-23 ·

Methods and computer systems are described herein for identifying small molecules that bind to selected RNA structural features (e.g., to RNA secondary structures). Also described are compounds and compositions that modulate RNA function and/or activity.

Amphiphilic kanamycin compositions and methods

The present relates to novel bioactive amphiphilic kanamycin compounds having the general formula of: ##STR00001##
where R may be a C.sub.4 to C.sub.20 branched or straight chained alkyl group or a substituted or unsubstituted aryl group. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating and preventing various fungal and bacterial diseases.

Amphiphilic kanamycin compositions and methods

The present relates to novel bioactive amphiphilic kanamycin compounds having the general formula of: ##STR00001##
where R may be a C.sub.4 to C.sub.20 branched or straight chained alkyl group or a substituted or unsubstituted aryl group. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating and preventing various fungal and bacterial diseases.