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.

Provided herein are novel thyroid hormone receptor (TR) agonists e.g., having Formula I, II, or III. Also provided are methods of preparing the novel TR agonists and method of using the novel TR agonists for treating diseases or disorder modulated by TR agonists, such as NAFLD, NASH, diabetes, hyperlipidemia and/or hypercholesterolemia.

##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.

In the method for producing an optically active 2,3-bisphosphinopyrazine derivative of the present invention, an optically active 2,3-bisphosphinopyrazine derivative represented by the following formula (3) is produced by the step of: preparing solution A containing 2,3-dihalogenopyrazine represented by the following formula (1) ##STR00001##
and a carboxylic acid amide coordinating solvent, lithiating an optically active R- or S-isomer of a hydrogen-phosphine borane compound represented by the following formula (2) ##STR00002##
to give a lithiated phosphine borane compound; adding solution B containing the lithiated phosphine borane compound to the solution A to perform an aromatic nucleophilic substitution reaction; and then performing a deboranation reaction. ##STR00003## (For symbols in the formulas, see the description.)

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.

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.

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.

Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK.sub.1) receptor. The compounds have the general formula (I):

##STR00001##

The present disclosure provides reagents that can be used to label synthetic oligonucleotides with rhodamine dyes or dye networks that contain rhodamine dyes.

The present invention relates to herbicidally active cinnolinium derivatives and formulations comprising such derivatives. The invention further extends to herbicidal mixtures comprising a cinnolinium derivative as described herein and at least one additional herbicidal active ingredient. The use of the afore-mentioned cinnolinium derivatives, formulations and/or herbicidal mixtures in controlling undesirable plant growth: in particular the use for the post-emergence control of weeds, also falls within the scope of the present invention.