Abstract: The invention relates to phosphoric acid esters of polyether-modified alkyl alcohols, to their preparation and to a use of phosphoric acid esters of polyether-modified alkyl alcohols for generating shine on a surface.

Abstract: Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.

Abstract: The present invention relates to various salts of inositol tripyrophosphate including the calcium, lithium, beryllium, magnesium, potassium, strontium, barium, rubidium and cesium salts of inositol tripyrophosphate, compositions comprising these salts, methods of making the various salts, and methods of use of the above salts. Methods of use include administering the above salts in an effective amount in individuals for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis.

Abstract: The invention relates to an isoprene oligomer that contains a trans structural moiety and a cis structural moiety, which can be represented by the following formula (1), wherein at least 1 atom or group in the trans structural moiety is replaced by another atom or group. The invention also relates to a polyisoprene, which is biosynthesized using the isoprene oligomer and isopentenyl diphosphate. Further, this invention provides a rubber composition comprising the isoprene oligomer and/or the polyisoprene, and a pneumatic tire, including tire components (e.g., treads and sidewalls) formed from the rubber composition.

Abstract: Mitigation of photo-induced damage in excitation illuminated reactions and analyses utilizing such reactions results in an enhanced performance for the reactions and the analyses. There is provided a novel class of triplet-state quenchers for mitigating photo-induced damage which are both simple in structure and effective at preventing and/or reducing photo-induced damage to reaction components of excitation illuminated reaction mixtures. Also provided are methods of using the compounds of the invention, devices and kits incorporating the compounds of the invention.

Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.

Abstract: The present invention is directed to polyphosphorylated and pyrophosphate derivatives of cyclitols. More particularly, the invention relates to polyphosphorylated and pyrophosphate derivatives of inositols. The invention also relates to compositions of the polyphosphorylated and pyrophosphate derivatives of inositol and other similar, more lipophilic derivatives, and their use as allosteric effectors, cell-signaling molecule analogs, and therapeutic agents.

Abstract: Phosphate depletion, a physiological condition commonly seen in certain patient populations, including alcoholics, malnourished, acutely ill patients, patients receiving parenteral nutrition, patients being re-fed after prolong fasting, and dialysis patients, requires intravenous supplementation when oral repletion is not feasible. This invention provides a method and pharmaceutical composition for therapeutic administration of pyrophosphate, instead of phosphate, for phosphate or pyrophosphate repletion. During hemodialysis or peritoneal dialysis significant removal of phosphate and pyrophosphate occurs. Pyrophosphate depletion predisposes patients to vascular calcification. This invention further provides a method and pharmaceutical composition for therapeutic administration of pyrophosphate for phosphate or pyrophosphate repletion by addition of pyrophosphate to hemodialysis or peritoneal dialysis solutions.

Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.

Abstract: The present invention relates to a method of producing a polymerizable phosphate containing at least one selected from polymerizable phosphates represented by formula (II), (III) or (IV) by a batch reaction, including a step of adding a compound represented by formula (I) into a mixture of a polymerizable phosphate reaction product containing at least one selected from polymerizable phosphates represented by formula (II), (III) or (IV), obtained by a pre-batch reaction, and phosphoric acid anhydride to react them: wherein R1 represents H or a C1-4 alkyl group, R2 represents a C2-6 alkylene group and n denotes an integer from 1 to 3.

Abstract: The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, ?-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.

Abstract: Compounds and related methods as can be used for selective mevalonate pathway inhibitors.

Abstract: Fluoroalkyl phosphates containing a tertiary carbon and a nonfluorinated chain are provided. The fluoroalkyl phosphates are useful as surfactants and additives for coating compositions and as treatment agents to impart various surface properties to substrates.

Abstract: The subject matters of the invention are: a crystallographic model of the binding site and a modulator regulating the catalytic activity of phosphofructokinase (PFK), a method of designing, selecting and producing a PFK modulator, a computer-based method for the analysis of the interaction between the modulator and PFK and for the analysis of molecular structures, a computer-based method of drug design, a method of assessing the ability of the potential modulator to interact in the binding site on the PFK surface, a method of providing data for generating structures and/or performing design for drugs that bind PFK, PFK homologues or analogues, complexes of PFK with a potential modulator, or complexes of PFK homologues or analogues with potential modulators, a computer system.

Abstract: The present invention relates to a new class of compounds having ?? T cells activating properties referred to herein as angelyl or tiglyl phosphoesters, compositions comprising any of these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.

Abstract: The present invention relates to a new class of compounds having ?? T cells activating properties referred to herein as angelyl or tiglyl phosphoesters, compositions comprising any of these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.

Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.

Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.

Abstract: A composition of formula I [Rf(CH2)m(O)n]x-A wherein Rf is a straight or branched perfluoroalkyl group having from about 2 to about 20 carbon atoms, or a mixture thereof, m is a positive integer equal to or greater than 3, n is 0 or 1, x is 1 to about 3, and A is —P(O)(OR1)y(OM+)3?y?x, —C(O)CH(SO3?M+)CH2C(O)?, ?(CH2CH2O)d(CH2CHR2O)eR3, or ?SO2B, M+ is an alkali metal ion, NH4+, or NH2(CH2CH2OH)2, B is N(R)2 or N(CH2CH3)(CH2CH2OH), R1 is C1 to C3 alkyl, and R2 is C1 to C4 alkyl, R3 is H or CH3, y is 0 to about 1, d is 0 to about 16, e is 0 to about 16, provided that (d+e) is from about 3 to about 16 is disclosed.

Abstract: The present invention provides methods and compositions for monitoring cofactors and metabolites of a metabolic pathway of interest. The subject compositions and methods are particularly suited for monitoring the mevalonate pathway in a variety of cells. The invention also provides fermentation methods for the production of isoprenoids.

Abstract: Novel phosphonate compounds are provided including a phosphonoglyoxylamide ester, an ?-keto phosphonophosphinate ester, a carbonylbisphosphonate analog of a nucleotide, and a diazomethylenebisphosphonate analog of a nucleotide, as well as methods of making synthetically and medically useful ?-keto phosphonate compounds.

Abstract: The present invention describes organophosphorus compounds of general formula (I) their preparation and their uses in the activation of gamma/delta T-cells, in the screening of GcpE and LytB enzyme inhibitors and in the prophylaxis and treatment of diseases in humans and animals.

Abstract: The present invention relates to a new class of compounds having ?? T cells activating properties referred to herein as angelyl or tiglyl phosphoesters, compositions comprising any of these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.

Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.

Abstract: The invention provides compounds comprising at least one phosphoepoxide group of the formula: where R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.

Abstract: A pharmaceutically acceptable salt of 2-methyl-3-butenyl-l-pyrophosphoric acid; an agent for treating lymphocytes which comprises at least one of 2-methyl-3-butenyl-l-pyrophosphoric acid, a pharmaceutically acceptable salt thereof, and a hydrate thereof; V?2V?2 type T cells treated by the same; and a medicine containing the same specifically stimulate and proliferate the human V?2V?2 type T cells, and also induce and enhance an antitumor activity thereof.

Abstract: The invention provides compounds of formula I: 1

Abstract: The invention provides compounds of formula I: wherein X, R1, R2, and n have any of the values defined in the specification, and their pharmaceutically acceptable salts. The compounds are useful, for example, for blocking prenylation transferase enzymes, for probing or diagnosing protein prenylation processes, and for treating cancer in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and intermediates useful for the synthesis of compounds of formula I.

Abstract: The invention relates to trans carotenoid salt compounds, methods for making them, methods for solubilizing them and uses thereof. These compounds are useful in improving diffusivity of oxygen between red blood cells and body tissues in mammals including humans.

Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T&ggr;9&dgr;2 lymphocytes.

Abstract: Farnesyl diphosphate analogs, specifically the 3-substituted alcohol precursors of the diphosphate analogs, 3-allylfarnesol and 3-vinylfarnesol, are potent inhibitors of mammalian protein fanesyltransferase (FTase). 3-allylgeranylgeraniol is a highly specific cellular inhibitor of protein geranylgeranylation (GGTase I). Furthermore, these compounds are able to efficiently block the anchorage-dependent growth of ras transformed cells. While 3-allylfarnesol inhibits protein farnesylation in situ, 3-vinylfarnesol instead leads to the abnormal prenylation of proteins with the 3-vinylfarnesyl group. In a similar manner, treatment with 3-allylgeranylgeraniol inhibits protein geranylgeranylation while 3-vinylgeranylgeraniol restores protein geranylgeranylation in cells.

Abstract: A description is given of compounds of the formula in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.

Abstract: The post-translational addition of a farnesyl moiety to the Ras oncoprotein is essential for its membrane localization and is required for both its biological activity and ability to induce malignant transformation. The present invention describes design and synthesis of a farnesylpyrophosphate (FPP) analog, 8-anilinogeranyl pyrophosphate (AGPP) that is transferred to Ras by farnesyltransferase (FTase), in which the &ohgr;-terminal isoprene unit of the farnesyl group has been replaced with an aniline functionality. AGPP potently inhibited FTase activity in vitro (IC50=0.6 &mgr;M) and is highly selective showing little inhibitory activity against either geranylgeranyl-protein transferase type I (GGTase I) (IC50=31 &mgr;M) or the utilization of FPP by the enzyme squalene synthase (IC50=1000 &mgr;M). Kinetic analyses suggest that AGPP acts as a competitive inhibitor of FTase with respect to FPP.

Abstract: The present invention provides phosphonylating agents and phosphonylation conditions that are compatible with the acid- and base-sensitive compounds and which promote a regioselective and reproducible conversion to a phosphonate compound. Also provided are intermediates that may be used to prepare phosphonate derivatives of cyclic peptides antifungal agent and a process for converting the phosphonates to the desired phosphonic acid prodrugs.

Abstract: The present invention is directed to presqualene diphosphate (PSDP) analogs having an active region of natural PSDP and a metabolic transformation region resistant to rapid intracellular inactivation in vivo. For example, PSDP and its stable analogs can inhibit neutrophil signal transduction events in cellular activation that result in the generation of active oxygen species, regulation of leukocyte adherence, both homotypic (leukocyte-leukocyte) or heterotypic adherence with leukocytes and epithelial cells of mucosal origin or endothelial cells of vascular origin. These analogs can also be used to regulate leukocyte-dependent tissue injury.

Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.

Abstract: A description is given of compounds of the formula ##STR1## in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II ##STR2## in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.

Abstract: A composition of lactoferrin, ovotransferrin or serotransferrin in combination with desferrioxamine methanesulfonate or other low molecular weight chelators for treating viral infections, and methods of treatment utilizing these compositions, is described.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

Abstract: Novel bisoxazoline monomers and novel bisoxazoline-novolak thermoset polymeric systems made therewith which have increased flame resistance.

Abstract: Compounds are disclosed for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and human immunodeficiency virus (HIV) by means of lipid derivatives of antiviral agents. The compounds consist of lipid derivatives of phosphonoacids having antiviral activity which are linked, commonly through the phosphate group of the phosphonoacid, to one of a selected group of lipids.The lipophilic nature of these compounds provides advantages over the use of the phosphonoacids alone. It also makes it possible to incorporate them into the lamellar structure of liposomes when combined with similar molecules. In the form of liposomes, these antiviral molecules are preferentially taken up by macrophages and monocytes, cells which have been found to harbor the target human immunodeficiency virus (HIV).