Abstract: A cyclic dinucleotide compound of Formula (I): wherein X1 is H or F; X2 is H or F; at least one among X1 and X2 is a fluorine atom; Z is OH, OR1, SH or SR1, wherein: R1 is Na or NH4, or R1 is an enzyme-labile group which provides OH or SH in vivo such as pivaloyloxymethyl; B1 and B2 are bases chosen from Adenine, Hypoxanthine or Guanine, and B1 is a different base than B2 and a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the cyclic dinucleotide, as well as their use in the treatment of a bacterial infection, a viral infection or a cancer are also described.
Abstract: The present invention provides a method of treating or preventing type 2 diabetes and hyperlipidemia in a subject in need thereof, comprising administrating to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a pharmaceutical composition for treatment or prevention of type 2 diabetes and hyperlipidemia, comprising a compound of formula I and a pharmaceutically acceptable carrier. Through down-regulation of PEPCK, G6Pase, 11?-HSD1, DGAT2, and GPAT, up-regulation of PPAR? and adiponectin, and promotion of membrane GLUT4 expression and phosphorylation of AMPK and Akt, the compound of formula I of the present invention exerts antidiabetic and antihyperlipidemic effects, including reduced weight of visceral fat, decreased blood levels of triglycerides, free fatty acids, glucose, insulin, and leptin as well as decreased hepatic levels of total lipid and triacylglycerol. The compound of formula I also inhibits adipocyte hypertrophy and hepatic ballooning.
Abstract: A compound represented by the following Structural Formula (A) or a salt thereof. The compound or the salt thereof is suitably produced from a microorganism belonging to the genus Saccharothrix and can be suitably used as a prostaglandin production inhibitor.
Abstract: Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action.
Abstract: This invention relates to hydrolase fluorogenic substrates with improved cell permeability, methods for the preparation thereof, and methods of measuring activities of hydrolases, particularly in cell-based assays. The substrates easily diffuse into the cells, where they are enzymatically processed to yield photostable fluorescent products, and are particularly fitted for visualising enzyme-derived activities in cell-based assays.
Abstract: The invention provides compounds having increased or reduced immunostimulatory effect, said compounds comprising a CpG dinucleotide and an immunomodulatory moiety wherein the increased or reduced immunomodulatory effect is relative to a similar compound lacking the immunomodulatorv moiety.