A method for preparing a β-amino phosphonic acid derivative includes: dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate, and potassium carbonate in a solvent and reacting at room temperature to obtain (2-benzamido-1-arylvinyl)dialkyl-phosphonate derivative; and hydrolyzing (2-benzamido-1-arylethyl)dialkylphosphonate derivative to obtain β-amino phosphonic acid derivative. The N-(arylvinyl)benzamide derivative is used as starting material. The raw materials are easy to obtain and are of many different types. A method of preparing β-aminophosphonic acid derivative includes: dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate and potassium carbonate in a solvent, reacting at room temperature to obtain (2-benzamide-1-arylvinyl) dialkyl phosphonate derivative, and then reducing and hydrolyzing the compound to obtain β-aminophosphonic acid derivative. The method of the invention has the advantages of short synthesis route, mild reaction conditions, simple reaction operation and post-treatment process, good yield, and is suitable for large-scale production.

The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias.

An electrochromic element including a first electrode, second electrode facing the first electrode with gap, electrolyte layer between the first and second electrodes, and layer including a compound represented by General Formula (1) where the layer is on or above the first electrode,

##STR00001##

where R.sub.1 to R.sub.4 are each a monovalent organic group wherein no hydrogen atom is at a benzyl site where the monovalent group may include a polymerizable functional group; and R.sub.5 to R.sub.28 are each a hydrogen atom, alkyl or alkoxy group where R.sub.25 and R.sub.28, or R.sub.26 and R.sub.27 may be bonded to form a structure represented by General Formula (2),

##STR00002##

where R.sub.29 and R.sub.30 are each an alkyl, alkoxy or aryl group, and R.sub.29 and R.sub.30 may be bonded via a common bond to form a cyclic structure when R.sub.29 and R.sub.30 are aryl groups.

A method for preparing a β-amino phosphonic acid derivative includes: dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate, and potassium carbonate in a solvent and reacting at room temperature to obtain (2-benzamido-1-arylvinyl)dialkyl-phosphonate derivative; and hydrolyzing (2-benzamido-1-arylethyl) dialkylphosphonate derivative to obtain β-amino phosphonic acid derivative. The N-(arylvinyl) benzamide derivative is used as starting material. The raw materials are easy to obtain and are of many different types. A method of preparing β-aminophosphonic acid derivative includes: dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate and potassium carbonate in a solvent, reacting at room temperature to obtain (2-benzamide-1-arylvinyl) dialkyl phosphonate derivative, and then reducing and hydrolyzing the compound to obtain β-aminophosphonic acid derivative. The method of the invention has the advantages of short synthesis route, mild reaction conditions, simple reaction operation and post-treatment process, good yield, and is suitable for large-scale production.

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

The present invention discloses a compound with the following formula (I), or a tautomer, mesomer, racemate, enantiomer, and diastereoisomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt thereof, or a prodrug molecule thereof, wherein D is selected from:

##STR00001##

The invention further discloses the use of the compound in the preparation of drugs for preventing and/or treating cancers, and the use of the compound in the preparation of drugs for inhibiting cancer metastasis. The compound of the present invention can effectively inhibit the proliferation and metastasis of cancer cells by adjusting the acidity of a tumor microenvironment to achieve a better effect in clinical cancer treatment, and has broad application prospects.

##STR00002##

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a STAT3 or STAT5-dependent cancer using said compounds; or a pharmaceutically acceptable salt, solvate or prodrug thereof.

##STR00001##

A compound or a polymer is claimed. A first formula can be ##STR00001##
wherein X is H, CH.sub.3, CN, phenyl, substituted phenyl, (CH.sub.2).sub.mZ, or phenyl(CH.sub.2).sub.mZ; T is O, N, S or NH; m equals 1 to 20; n equals 1-100; and Z is CN, NH.sub.2, Thiol, OH, or CO.sub.2H. The second formula is: ##STR00002##
wherein X is H, CH.sub.3, CN, phenyl, substituted phenyl, (CH.sub.2).sub.mZ, or phenyl(CH.sub.2).sub.mZ; and Z is CN, NH.sub.2, Thiol, OH, or CO.sub.2H. The third formula is ##STR00003##
wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently: H, CH.sub.3, OH, or a halogen.