The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.

The present disclosure relates to novel synthetic method of making 1, 4-diazo N-heterocycles via intermolecular amphoteric diamination of allenes, and to the compounds made by the novel synthetic method.

Fosnetupitant chloride hydrochloride having improved stability, characterized by the following chemical structure: ##STR00001##

A new class of small anti-cancer molecules derived from ethacrynic acid (symbolized by AE) is presented. AE analogues are synthesized and then the in vitro cytotoxic activities thereof are evaluated on the P815 tumour cell line using the MIT test. The AE derivative which exhibited the best in vitro cytotoxicity is then tested in vivo using the DBA2/P815 (H.sub.2d) mouse model. At 30 mg/kg, the effective dose, the animals showed general tolerance with a percentage survival of around 80%, and no significant weight loss is observed.

The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Selected compounds in this class promote apoptosis in senescent cells, and are being developed for treating senescent-related conditions. Selected compounds in this class promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.

The present invention relates to compounds of formula (Ia) and the use thereof as inhibitors of P. aeruginosa virulence factor LasB. Formula (Ia). These compounds are useful in the treatment of bacterial infections, especially caused by P. aeruginosa.

##STR00001##

The present invention provides a charge-reversible phospholipid that is not positively charged at a pH of the body fluid (typically in the neutral range) and has low cytotoxicity.

The present invention provides a phospholipid represented by formula (1):

##STR00001##

wherein m represents a natural number of 9 to 25, n represents a natural number of 10 to 15, X.sub.1, X.sub.2, and X.sub.3 are the same or different and each represent H or OH, and R.sup.1 represents the following formula (i) or (ii):

##STR00002##

wherein p represents 1 or 2, q represents 1 or 2, and r represents an integer of 1 to 4; or

##STR00003##

wherein s represents an integer of 1 to 3, and R.sup.2 represents a hydrogen atom or a hydrocarbon group.

Provided is a charge-reversible and ethanol-soluble phospholipid suitable for the preparation of lipid particles. A phospholipid represented by formula (1):

##STR00001##

wherein R.sup.1 and R.sup.2 are the same or different and each represent a chain hydrocarbon group, R.sup.3 represents a hydrogen atom or a hydrocarbon group, and m represents an integer of 1 to 3.

Compounds of the general Formula A-D-Y are disclosed with activity towards treating diseases related to inflammation, cancer, neurodegenerative diseases, and cardiovascular diseases. Pharmaceutical compositions, methods of making, and methods of use thereof are also described.

This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.