Patent classifications
C07F9/6552
INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE 1 (DGAT-1) AND USES THEREOF
This invention pertains to the use of fused bicycle heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
NEW SYNTHETIC AGONISTS OF TLR4 RECEPTOR
The present invention relates to new synthetic molecules with agonist activity of human Toll-like Receptor 4 (TLR4), compositions comprising them and uses thereof for the treatment of diseases in which it is useful to induce or increase an immune response. These new syntethic molecules differ from other similar agonists due to the simplicity of the formula, the ease and cheapness of preparation and the possibility of further chemical processing to modify the physicochemical properties and allow conjugation to other molecules (for example protein antigens).
FUNCTIONALIZED CYCLIC ETHERS FOR LITHIUM-ION BATTERIES
The present disclosure relates to a functionalized cyclic ether that is useful for stable cycling, storage of lithium-ion cells at high temperatures, and performance at low temperatures, an electrolyte containing the functionalized cyclic ether, and an electrochemical energy storage device containing the electrolyte.
Additive for nonaqueous electrolyte, nonaqueous electrolyte, and electricity storage device
The present invention aims to provide an additive for a non-aqueous electrolyte solution with excellent storage stability capable of forming a stable SEI on the surface of an electrode to improve cell performance such as a cycle performance, a discharge/charge capacity, and internal resistance, when the additive is used for electrical storage devices such as non-aqueous electrolyte solution secondary cells and electric double layer capacitors. The present invention also aims to provide a non-aqueous electrolyte solution containing the additive for a non-aqueous electrolyte solution and to provide an electrical storage device using the non-aqueous electrolyte solution. The present invention is an additive for a non-aqueous electrolyte solution, comprising a compound that has a structure represented by the formula (1-1) or (1-2): ##STR00001##
in which A represents C.sub.mH.sub.(2mn)Z.sub.n, m being an integer of 1 to 6, n being an integer of 0 to 12, and Z representing a substituted or unsubstituted alkyl group, a silyl group, a phosphonic acid ester group, an acyl group, a cyano group, or a nitro group, the compound having a lowest unoccupied molecular orbital energy of 3.0 to 0.4 eV, a standard enthalpy of formation of 220 to 40 kcal/mol, and an enthalpy change with hydrolysis reaction of 5 to 5 kcal/mol.
MACROCYCLIZATION REACTIONS AND INTERMEDIATES AND OTHER FRAGMENTS USEFUL IN THE SYNTHESIS OF HALICHONDRIN MACROLIDES
The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
NUCLEOTIDE PRECURSORS, NUCLEOTIDE ANALOGS AND OLIGOMERIC COMPOUNDS CONTAINING THE SAME
The present disclosure relates to novel nucleotide precursors and nucleotide analogs that can be incorporated into oligonucleotides, including double-stranded oligonucleotides such as siRNAs. Oligonucleotides containing these analogs have superior biological activity, for example, increased in vitro stability and improved in vivo potency especially duration of action. The improved oligonucleotides are useful for silencing (e.g., reducing or eradicating) the expression of a target gene. In particular embodiments, this invention encompasses specific nucleotide analogs to be included in double-stranded RNAs (dsRNAs), and especially in siRNAs, that can hybridize to messenger RNAs (mRNAs) of interest, so as to reduce or block the expression of target genes of interest.
NATURAL LIPIDS CONTAINING NON-OXIDIZABLE FATTY ACIDS
Provided herein is technology relating to natural lipids containing non--oxidizable fatty acids and particularly, but not exclusively, to compositions and methods related to the production and use of natural lipids containing non--oxidizable fatty acids.
Zanamivir phosphonate congeners with anti-influenza activity and determining oseltamivir susceptibility of influenza viruses
Methods and compositions for detection of drug resistant pathogens and treatment against infections thereof are provided. Methods for detection of oseltamivir-resistant influenza viruses by competitive binding assays utilizing non-oseltamivir influenza virus neuraminidase inhibitors and oseltamivir carboxylate are provided. Influenza virus neuraminidase inhibitors coupled to sensors and useful for employment in the methods of the invention are disclosed. Novel phosphonate compounds active as neuraminidase inhibitors against wild-type and oseltamivir-resistant influenza strains of H1N1, H5N1 and H3N2 viruses are disclosed. An enantioselective synthetic route to preparation of these phosphonate compounds via sialic acid is provided.
ELECTRONIC SWITCHING DEVICE
The present invention relates to an electronic switching device, in particular to tunnel junctions, comprising an organic molecular layer for use in memory, sensors, field-effect transistors or Josephson junctions. More particularly, the invention is included in the field of random access non-volatile memristive memories (RRAM). Another aspect of the invention relates to a compound of formula I
##STR00001##
in which the occurring groups have the meanings defined in claim 1, for use in the molecular layer. The invention further relates to the use of said molecular layer and to processes for the production and operation of the electronic switching element and components based thereon.
Gold (I)-Phosphine Compounds as Anti-Bacterial Agents
A compound of formula (I) for use in the prevention or treatment of a bacterial infection wherein R.sup.P1 is either methyl, ethyl, isopropyl, cyclohexyl or phenyl; R.sup.P2 is selected from methyl, ethyl, isopropyl, cyclohexyl and phenyl; R.sup.P3 is either ethyl, isopropyl, cyclohexyl, phenyl or pyridyl; A is either S or Se; R.sup.A is selected from wherein each of Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.9 is independently selected from CH or N, wherein at least three of Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.9 are CH; V is selected from O, CHOR.sup.O1, NCO.sub.2R.sup.C2 or NR.sup.N2; one of V, Y.sup.6, Y.sup.7 and Y.sup.8 is selected from CH and N, and the others are CH; X is selected from NH, S or O; R.sup.C1 is selected from OR.sup.O2 or NHR.sup.N1; R.sup.O1 is selected from H and C.sub.1-3 unbranched alkyl; R.sup.O2 is C.sub.1-3 unbranched alkyl; R.sup.N1 is selected from H and C.sub.1-3 unbranched alkyl; R.sup.N2 is C.sub.1-3 unbranched alkyl; R.sup.C2 is either C.sub.1-3 unbranched alkyl or C.sub.3-4 branched alkyl; R.sup.C3 is selected from C.sub.1-3 unbranched alkyl and C.sub.2H.sub.4CO.sub.2H; R.sup.C4 is either H or Me; R.sup.C5 is either H or Me; R.sup.C6 represents one or two optional methyl substituents; and n is an integer from 2 to 8.
##STR00001##