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.

Suppressors of Premature Termination Codons as Therapeutics and Methods for Their Use

This invention discloses the use of aminoglycoside antibiotics such as gentamicin B1 to suppress premature termination codons during translation and promote the full length read-through of transcripts such as p53 that incorporate nonsense mutations and to treat disease conditions such as cancer caused by such genetic mutations.

##STR00001##

Suppressors of Premature Termination Codons as Therapeutics and Methods for Their Use

This invention discloses the use of aminoglycoside antibiotics such as gentamicin B1 to suppress premature termination codons during translation and promote the full length read-through of transcripts such as p53 that incorporate nonsense mutations and to treat disease conditions such as cancer caused by such genetic mutations.

##STR00001##

Selective oxidation of carbohydrates

The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.

Selective oxidation of carbohydrates

The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.

Arbekacin derivative, and production and use thereof

It has been found that adding carbon dioxide or the like to a solution containing arbekacin free base makes it possible to produce arbekacin derivatives including arbekacin carbonate and carbamic acid of arbekacin. Moreover, it has been found that the arbekacin derivatives have a high stability, and that the use thereof enables efficient productions of highly-pure arbekacin free base and pharmaceutically acceptable salt thereof.

Arbekacin derivative, and production and use thereof

It has been found that adding carbon dioxide or the like to a solution containing arbekacin free base makes it possible to produce arbekacin derivatives including arbekacin carbonate and carbamic acid of arbekacin. Moreover, it has been found that the arbekacin derivatives have a high stability, and that the use thereof enables efficient productions of highly-pure arbekacin free base and pharmaceutically acceptable salt thereof.

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.