Patent classifications
A61K31/216
NOVEL THYROMIMETICS
Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
##STR00001##
PDIA4 INHIBITORS AND USE THEREOF FOR INHIBITING ß-CELL PATHOGENESIS AND TREATING DIABETES
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.
PDIA4 INHIBITORS AND USE THEREOF FOR INHIBITING ß-CELL PATHOGENESIS AND TREATING DIABETES
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.
Autoimmune disorder treatment using RXR agonists
The present specification provides RXR agonist compounds, compositions comprising such RXR agonists, and methods using such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection as well as use of such RXR agonists to manufacture a medicament and use of such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection.
Autoimmune disorder treatment using RXR agonists
The present specification provides RXR agonist compounds, compositions comprising such RXR agonists, and methods using such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection as well as use of such RXR agonists to manufacture a medicament and use of such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection.
Methods of preventing or treating ophthalmic diseases
The present invention relates to a pharmaceutical combination comprising: (a) a PPAR agonist; (b) a p38 kinase inhibitor; and optionally (c) one or more pharmaceutically acceptable diluents, excipients or carriers for use in a method of preventing or treating ophthalmic diseases or disorders in a subject.
Methods of preventing or treating ophthalmic diseases
The present invention relates to a pharmaceutical combination comprising: (a) a PPAR agonist; (b) a p38 kinase inhibitor; and optionally (c) one or more pharmaceutically acceptable diluents, excipients or carriers for use in a method of preventing or treating ophthalmic diseases or disorders in a subject.
TOPICAL COMPOSITIONS COMPRISING PEA PROTEINS AND POLYPHENOLS
The object of the invention is topical compositions comprising pea proteins and polyphenols and the use thereof for the treatment of local or generalised disorders caused by increased permeation of the natural epithelial barriers. Said disorders may be of bacterial, viral, inflammatory, allergic and/or fungal origin, or endogenous or idiopathic.
TOPICAL COMPOSITIONS COMPRISING PEA PROTEINS AND POLYPHENOLS
The object of the invention is topical compositions comprising pea proteins and polyphenols and the use thereof for the treatment of local or generalised disorders caused by increased permeation of the natural epithelial barriers. Said disorders may be of bacterial, viral, inflammatory, allergic and/or fungal origin, or endogenous or idiopathic.
TOPICAL COMPOSITIONS COMPRISING PEA PROTEINS AND POLYPHENOLS
The object of the invention is topical compositions comprising pea proteins and polyphenols and the use thereof for the treatment of local or generalised disorders caused by increased permeation of the natural epithelial barriers. Said disorders may be of bacterial, viral, inflammatory, allergic and/or fungal origin, or endogenous or idiopathic.