Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.

Abstract: The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Abstract: Phospholipid-analogous compounds of the general formula (I) in which a is b is where R1 and R2 are, independently of one another, hydrogen, a saturated or unsaturated acyl or alkyl radical which can optionally be branched or/and substituted, where the total of the carbon atoms in the acyl and alkyl is 16 to 44 C atoms, s is an integer from 0 to 8, c is a radical of a primary or secondary alcohol of the formula RO—, where R is a saturated or unsaturated alkyl radical, mainly with cis double bond, of froth 12 to 30 carbon atoms, n is an integer from 2 to 8, R3 a can be 1,2-dihydroxypropyl or b can be alkyl with 1 to 3 C atoms when z is >0 or c can be alkyl with 1 to 3 carbon atoms when n?2 and z=0, m is 1 or 2, x is an integer from 0 to 8, y is 1 for z=1 to 5 or is 1 to 4 for z=1 z is an integer from 0 to 5, are novel and are suitable as liposome constituents, solubilizers and pharmaceuticals.

Abstract: A method for the manufacture of aminopolyalkylene phosphonic acid of a specific general formula is described. In particular, a mixture of specifically defined ranges of reactants to wit: phosphorous acid; an amine; formaldehyde and an aminopolyalkylene phosphonic acid, having the same general formula as the compound to be manufactured, are reacted to thus yield a product of outstanding selectivity and purity with substantially reduced levels of non-desirable by-products.

Abstract: Described herein are nitrated lipids and methods of making and using the nitrated lipids.

Abstract: New diacylglycerol-polyethylene glycol (DAG-PEG) conjugates are described. A variety of linkers between the PEG chain and glycerol backbone of the DAG-PEGs may be selected to optimize liposomal formulations of pharmaceuticals and cosmetics.

Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.

Abstract: The present invention contemplates the creation of a low fluoride oil processed from a phospholipid-protein complex (PPC) formed immediately upon a crustacean (i.e., for example, krill) catch. The process comprises disintegrating the crustaceans into smaller particles, adding water, heating the result, adding enzyme(s) to hydrolyze the disintegrated material, deactivating the enzyme(s), removing solids from the enzymatically processed material to reduce fluoride content of the material, separating and drying the PPC material. Then, using extraction with supercritical CO2 and ethanol as solvents, inter alia krill oil is separated from the PPC. In the extraction the krill oil can be separated almost wholly from the feed material. The products have low fluoride content. The manufacturing costs in the extraction process are relatively low.

Abstract: Disclosed are processes for development and recovery of lipids from biomass. A plant or microorganism-based biomass can be developed to encourage a desired lipid profile. Following development, ecologically friendly normally gaseous fluids such as carbon dioxide can be pressurized to a supercritical state followed by rapid expansion. The fluid is first contacted with a biomass source including oil-containing microorganisms and/or agricultural products. For instance, fungi or algae can be bioconverted from another biomass sources such as canola seed or corn syrup and then contacted with the high pressure fluid. During a contact period, the fluid can diffuse into the biomass, and in particular through the cell walls of the biomass. The fluid undergoes rapid release of pressure and opens the cell structure for improved release of oil. The fluid can optionally be utilized for extraction following the explosion process. For instance, the fluid can be re-pressurized in the same vessel for extraction processes.

Abstract: Phospholipid-analogous compounds of the general formula (I) in which a is b is where R1 and R2 are, independently of one another, hydrogen, a saturated or unsaturated acyl or alkyl radical which can optionally be branched or/and substituted, where the total of the carbon atoms in the acyl and alkyl is 16 to 44 C atoms, s is an integer from 0 to 8, c is a radical of a primary or secondary alcohol of the formula RO—, where R is a saturated or unsaturated alkyl radical, mainly with cis double bond, of froth 12 to 30 carbon atoms, n is an integer from 2 to 8, R3 a can be 1,2-dihydroxypropyl or b can be alkyl with 1 to 3 C atoms when z is >0 or c can be alkyl with 1 to 3 carbon atoms when n?2 and z=0, m is 1 or 2, x is an integer from 0 to 8, y is 1 for z=1 to 5 or is 1 to 4 for z=1 z is an integer from 0 to 5, are novel and are suitable as liposome constituents, solubilizers and pharmaceuticals.

Abstract: The present invention relates to polymer conjugated releasable lipids and nanoparticle compositions containing the same for the delivery of nucleic acids and methods of modulating gene expression using the same. In particular, this invention relates to releasable polymeric lipids containing an acid-labile linker based on a ketal or acetal-containing linker, or an imine-containing linker.

Abstract: The present invention relates to releasable fusogenic lipids and nanoparticle compositions containing the same for the delivery of oligonucleotides and methods of modulating gene expression using the same. In particular, this invention relates to releasable fusogenic lipids containing an imine linker and a zwitterionic moiety.

Abstract: Isolated nucleic acid fragments and recombinant constructs comprising such fragments encoding a delta-8 desaturase along with a method of making long-chain polyunsaturated fatty acids (PUFAs) using this delta-8 desaturase in plants and oleaginous yeast are disclosed.

Abstract: The present invention provides lipid compounds for delivering therapeutic amounts of active agents in response to enzymatic activities of cancer tissues. Lipid compositions may include one or more drugs, or a biologically-active agent, encapsulated within liposomes.

Abstract: Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.

Abstract: Described herein are nitrated lipids and methods of making and using the nitrated lipids.

Abstract: The present invention relates to a new class of compounds having ?? T cells activating properties of Formula (I), a composition comprising these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.

Abstract: The preparation and use of fluorescent cell markers of the structure F—S1-S2-L is described where F is a fluorophore, S1-S2 is a spacer linking F to L, and L is a diacyl lipid.

Abstract: Pharmaceutical, cosmetic and dietetic compositions and functional foods, constituted by: A) phospholipid mixtures containing N-acyl-phosphatidyl-ethanolamines (NAPEs) and/or B) phospholipid mixtures containing N-acyl-ethanol amines (NAEs) together with phosphatidic acids (PAs) and/or lysophosphatidic acids (LPAs) with the proviso that said N-acyl-phosphatidyl-ethanolamines (NAPEs) do not include N-oleoyl-phosphatidyl-ethanolamine. New phosphobioflavonic complexes of NAPE or NAE with one or more bioflavonoids are also disclosed.

Abstract: New diacylglycerol-polyethylene glycol (DAG-PEG) conjugates are described. A variety of linkers between the PEG chain and glycerol backbone of the DAG-PEGs may be selected to optimize liposomal formulations of pharmaceuticals and cosmetics.

Abstract: The present invention includes a novel polyethylene glycol derivative; a drug carrier comprising the derivative; and a pharmaceutical composition comprising the drug carrier having a pharmacologically active substance included therein. Specifically disclosed are: a polyethylene glycol derivative represented by the general formula (I); a drug carrier comprising the derivative and 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoyl-glycerol; and a pharmaceutical composition comprising the drug carrier and a pharmacologically active substance (preferably double-stranded RNA, double-stranded DNA or an oligonucleic acid), wherein R represents a saturated or unsaturated aliphatic hydrocarbon group having 10 to 30 carbon atoms or a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms; and n represents an integer of 30 to 150.

Abstract: New targeting or therapeutic compounds which can be incorporated into a composition of gas-filled microvesicles. The invention further relates to gas-filled microvesicles for diagnostic and/or therapeutic use comprising said compounds and to their method of use. The new compounds are compounds of formula M-S-T, wherein: M represents a component capable of associating with an envelope of a gas-filled microvesicle; T represents a component comprising a targeting ligand or a therapeutic agent; and S represents a component comprising at least two bissulfone groups.

Abstract: The present invention is directed to a method for differentially diagnosing dementia or the risk of dementia in a patient. The method comprises obtaining a sample from the patient; analyzing the sample to obtain quantifying data for one or more than one metabolite marker; comparing the quantifying data for the one or more than one metabolite marker to corresponding data obtained from one or more than one reference sample; and using the comparison to differentially diagnose dementia or the risk of dementia. The method may also assis in assessing dementia or the risk of dementia in a patient. The present invention is also directed to metabolite markers and compounds useful in the present method.

Abstract: Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.

Abstract: This disclosure describes structural elements that enhance fusogenicity of lipids and lipid assemblies (e.g. liposomes) with biological membranes, in particular cell membranes, and use of such structures. The elements are pH sensitive in terms of charge and hydrophilicity and undergo a polar—apolar transition when exposed to low pH.

Abstract: The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.

Abstract: The present invention relates to a lipid-based drug delivery system for administration of a lysolipid derivative present in prodrug from, said prodrug furthermore being a substrate for extracellular phospholipase A2 to the extent that an organic radical can be hydrolytically cleaved off, whereas the aliphatic group of the lysolipid derivative remains substantially unaffected, said system having included therein lipopolymers or glycolipids so as to present hydrophilic chains on the surface of the system. Particularly interesting lipid derivatives are ether lipids and ether lipids in which drug substance is covalently attached in the sn-2-position. Pharmaceutical compositions comprising the drug delivery system can be used in the targeted treatment of various disorders, e.g. cancer, infectious, and inflammatory conditions, etc., i.e. disorders and diseases associated with or resulting from increased levels of extracellular PLA2 activity in the diseased tissue.

Abstract: Disclosed is a method for reducing the sterol, for example cholesterol, content of sterol-containing substances such as fats and oils. The method provides an efficient and cost effective process based on the affinity of cholesterol and other sterols for amphipathic molecules that form hydrophobic, fluid bilayers, such as phospholipid bilayers. Aggregates of amphipathic molecules are contacted with, for example, a sterol-containing fat or oil in an aqueous environment and then mixed. Following adequate mixing, the sterol-reduced fat or oil is separated from the aqueous separation mixture. Alternatively, the correspondingly sterol-enriched fraction also may be isolated from the aqueous separation mixture.

Abstract: A process is described for producing ester quats of the formula (I) ##STR1## where X.sup.- is an anion of an inorganic or organic acid, R.sub.a is a C.sub.1 to C.sub.4 alkyl group, R.sub.b and R.sub.c are each, independently of one another, a C.sub.1 to C.sub.3 alkylene group, and R.sub.d is a C.sub.1 to C.sub.22 fragment of a saturated and/or unsaturated aliphatic carboxylic acid, m, n, p, and q are integers, m has a value from 1 to 3, n a value from 0 to 3, p a value from 0 to 1, m+n+p=4, and q has the value 1 or, if m=3, n=0, and p=1, the value 2, in which process a quaternary compound of the formula (II) ##STR2## where X.sup.-, R.sub.a, R.sub.b, R.sub.c, m, n, p, and q have the above meanings, is esterified, in the presence of an oxo acid of phosphorus and/or one of its alkali or alkaline-earth salts as a catalyst, with a saturated and/or unsaturated C.sub.1 to C.sub.22 carboxylic acid, alone or in a mixture, while withdrawing water.

Abstract: A method of manufacturing acyloxysilane compounds having functional groups bonded to a silicon atom via Si--C bonds comprising reacting in a hydrosilation reaction an unsaturated compound (a) selected from the group consisting of (i) styrene or styrene derivative, (ii) vinylsilane compound, (iii) siloxane compound having a vinyl group bonded directly to a silicon atom, (iv) epoxy-functional olefin, (v) diene compound, (vi) allyl compound described by formula CH.sub.2 .dbd.CHCH.sub.2 X, where X is a halogen atom, an alkoxy group, or an acyloxy group, (vii) olefin compound having a terminal vinyl group, and (viii) acetylene-type compound with a silicon compound (b) that contains hydrogen atom bonded to the silicon atom and acyloxy group in the presence of a platinum catalyst.

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: Novel retinoid phosphocholines are disclosed having the general Formula (I): ##STR1## wherein R represents a retinyl or retinoyl moiety. The optical and geometric isomers of compounds of Formula (I) and the pharmaceutically-acceptable salts thereof, are also disclosed. The subject compounds exhibit anti-tumor, anti-psoriatic and anti-inflammatory activities in addition to their inherent Vitamin A-like activities. The invention embraces the novel compounds, pharmaceutical compositions thereof, and methods of using the same.

Abstract: Additives are produced by (i) reacting an O,O-dihydrocarbyl phosphorodithioic acid with a monoepoxide or mixture of monoepoxides having in the range of 20 to about 30 carbon atoms in the molecule or a vegetable oil epoxide such as epoxidized soybean oil or methyl epoxy soyate, (ii) reacting the product with phosphorus pentoxide to produce an acid phosphate intermediate, and (iii) neutralizing the intermediate with at least one amine. At least 50 mole %, and preferably all, of the hydrocarbyl groups of the O,O-dihydrocarbyl phosphorodithioic acid are secondary acyclic hydrocarbyl groups free of acetylenic unsaturation. The additives are multifunctional in that they have limited slip properties, antiwear/extreme pressure properties, and corrosion inhibiting properties.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:X is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --O--, --NR.sup.1 -- or --(S)q;Y and Z are each independently --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O)(OR.sup.2)(OR.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p is 0 or 1; andq is an integer from 1 to 2.

Abstract: The present invention provides a phosphorus-containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group: R.sup.3 and R.sup.4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: ##STR2## (wherein R.sup.5 and R.sup.6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the Formula: --(CH.

Abstract: The invention relates to acyloxymethyl esters of bisphosphonic acids, halo-bisphosphonic acids and hydroxy-bisphosphonic acids which exhibit oral bioavailability and are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.

Abstract: A polypeptide thin film produced by polymerizing a monomolecular film or a built-up film comprising an amphipatic phospholipid compound, wherein the amphipatic phospholipid compound has a hydrophobic portion and a hydrophilic portion having an amino acid ester structure in the molecule, the amino acid ester structure containing a splitting-off group with a pKa value of the conjugated acid thereof being 16 or below.

Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.