Disulfide-Isomerase A4 (PDIA4) inhibitors and use thereof for inhibiting pancreatic β-cell pathogenesis and treating diabetes are disclosed. Drug candidates that inhibit PDIA4 with IC50 values ranging from 4 μM to 300 nM are identified. The compounds are highly active in augmenting insulin secretion from pancreatic β-cells. The representative compound No. 8 (4,5-dimethoxy-2-propiolamidobenzoic acid), alone or in combination with metformin, is effective in preserving pancreatic β-cell function, treating and/or reversing, returning blood glucose concentration to a normal level in a diabetic.

Novel Styryl Carboxylate derivatives are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases, and diabetes.

Novel Styryl Carboxylate derivatives are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases, and diabetes.

Described herein is an hydrofluorocarboximidate of formula (I) where: R.sub.H is a linear or branched alkyl group comprising 1 or 2 carbon atoms and (a) R.sub.f1 and R.sub.f2 are independent-selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from oxygen, nitrogen, or combinations thereof; or (b) R.sub.f1 and R.sub.f2 are connected to form a ring structure comprising a total of 4-8 carbon atoms and in addition to the nitrogen atom from the carboximidate the ring structure may optionally comprises at least one catenated atom selected from oxygen, nitrogen, or combinations thereof. A method of making the hydrofluorocarboximidate with improved yield is described as well as various uses for the hydrofluorocarboximidate of Formula (I). ##STR00001##

Described herein is an hydrofluorocarboximidate of formula (I) where: R.sub.H is a linear or branched alkyl group comprising 1 or 2 carbon atoms and (a) R.sub.f1 and R.sub.f2 are independent-selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from oxygen, nitrogen, or combinations thereof; or (b) R.sub.f1 and R.sub.f2 are connected to form a ring structure comprising a total of 4-8 carbon atoms and in addition to the nitrogen atom from the carboximidate the ring structure may optionally comprises at least one catenated atom selected from oxygen, nitrogen, or combinations thereof. A method of making the hydrofluorocarboximidate with improved yield is described as well as various uses for the hydrofluorocarboximidate of Formula (I).

##STR00001##

Novel Styryl Carboxylate derivatives are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases, and diabetes.

Novel Styryl Carboxylate derivatives are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases, and diabetes.

The present invention relates to a process for the preparation of 4-aminobenzoamidine (4-AMBA) salts of general formula (I) ##STR00001##
preferably the salts thereof with hydrochloric or hydrobromic acid, particularly preferred the dichloride salt.

The present invention relates to a process for the preparation of 4-aminobenzoamidine (4-AMBA) salts of general formula (I) ##STR00001##
preferably the salts thereof with hydrochloric or hydrobromic acid, particularly preferred the dichloride salt.

The present invention relates to a process for the preparation of 4-aminobenzoamidine (4-AMBA) salts of general formula (I)

##STR00001##

preferably the salts thereof with hydrochloric or hydrobromic acid, particularly preferred the dichloride salt.