Abstract: Disclosed herein are novel compositions for delivery of biologically active agents into cells comprising a cationic amphiphile and a complementary lipid composition. Also disclosed are methods of making and using such novel compositions.

Abstract: The present invention relates to an glucose uptake modulator, a pharmaceutical composition comprising the glucose uptake modulator, and a method of treating a diabetes or diabetic complications in a mammal in need thereof, which comprises administering to said mammal an effecting amount of a glucose uptake modulator.

Abstract: The present invention relates to novel therapeutical use of agonist ligands specific to G2A receptor. More particularly, the present invention relates to methods for treating a disease or disorder associated with neutrophil accumulation and hyperactivity and/or excessive release of IL-8, or with microbial infection, in a subject, comprising administering LPC (lysophosphatidylcholine), SPC(sphingophosphorylcholine) or derivatives thereof to the subject. The agonist ligands for G2A receptor according to the present invention and pharmaceutical- or therapeutical composition comprising said ligands can be used effectively in treatment of a disease or disorder associated with neutrophil accumulation and hyperactivity and/or excessive release of IL-8, specifically inflammatory diseases and diseases associated with ischemia-reperfusion injury as well as microbial infection.

Abstract: The disclosure relates to a method for in vivo differentiation of monocytes in mature dendritic cells, wherein a) monocytes are provided in an appropriate culture medium, b) the monocycles are differentiated in dendritic cells in the presence of a differentiation factor, c) L-?-lysophosphatidylcholine is added to the medium and mature dendritic cells are obtained. The disclosure also relates to the use of at least one inhibitor of L-?-lysophosphatidylcholine in the production of a medicament for the prevention of an inflammation and/or in order to combat an inflammatory disease and/or autoimmune disease.

Abstract: A method for the treatment or prevention of tissue damage in a subject having an inflammatory and/or tissue damaging condition, which comprises administering to the subject an effective amount of a compound capable of inhibiting the binding of C-reactive protein (CRP) to an autologous or extrinsic ligand.

Abstract: The invention relates to novel medicament formulations containing, as active ingredients, alkylphosphocholines and the like, alkyl-alkanediol-phosphocholines and the like, and (ether)lysolecithines and the like, in different forms of embodiment. Said active ingredients are integral constituents of liposomes, also containing cholesterol and the like and a negative charge carrier. The medicament formulations are especially suitable for the treatment and/or prophylaxis of cancer, protozoan diseases such as leishmaniasis and amoebic diseases, acariasis and diseases caused by arthropods, and bacterial diseases, such as ehrlichiosis. Ocular diseases accompanied by uncontrolled cellular processes can also be advantageously influenced.

Abstract: The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.

Abstract: The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.

Abstract: The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.

Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpes virus, is disclosed. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative.

Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpes virus, is disclosed. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative.

Abstract: Methods, compositions, and kits for separating heteroduplex and homoduplex DNA molecules in a test mixture by temperature-compression denaturing high performance liquid chromatography (tcDHPLC). The method includes use of nitrogen-containing additives in the mobile phase that allow detection of diverse heteroduplex molecules to be performed at the same pre-selected temperature. An example of a preferred additive is betaine. Standard mixtures of DNA fragments, such as mutation standards containing known heteroduplex and homoduplex molecules, can be used to select the concentration of additive and temperature. Compositions and kits including the mobile phase, mutation standards, PCR primers, separation media, and DNA polymerase are also provided.

Abstract: The present invention relates to peptide-like compounds, e.g. aminocarboxylic acid amide derivatives, and to methods of using same in the field of general health care, for example, to improve resistance to stress, improve production of desired characteristics or useful products in animals, to increase weight gain, prevent diseases caused by pathogens, and to decrease feed efficiency. The invention has applications in the field of animal husbandry, and in treating or preventing weight loss associated with a disease in humans. It also relates to administering carbobenzoxy beta-alanyl taurine to improve feed efficiency in an animal, comprising administering to the animal an amount of carbobenzoxy beta-alanyl taurine sufficient to reduce the amount of food required to increase a unit of weight in the animal.

Abstract: The present invention is directed to methods of antimicrobial therapy for a patient infected with, or suspected of being infected with a microorganism that has mycolic acid structures in its outer membrane, said method comprising coadministering a betaine-like detergent and an antibiotic to said patient in an amount and for a length of time sufficient to kill said microorganism.

Abstract: A method of administering an antifolate to a mammal in need thereof, comprising administering an effective amount of said antifolate in combination with a methylmalonic acid lowering agent.

Abstract: A novel use of platelet-activating factor antagonists that bind to intracellular PAF binding sites such as BN-50730 (tetrahedra-4,7,8,10 methyl-1 (chloro-1 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9 pyrido [4?,3?-4,5] thieno [3,2-f] triazolo-1,2,4 [4,3-a] diazepine-1,4) has been discovered. These intracellular-binding platelet-activating factor antagonists were found to inhibit both in vivo and in vitro tumor growth and angiogenesis where the angiogenesis is stimulated by basic fibroblast growth factor.

Abstract: Pharmaceutical uses of glycine betaine, such as for the treatment of thromboses not induced by hyperhomocystenemia or homocystinuria, of blood disorders, such as blood coagulation, thrombi formation.

Abstract: The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.

Abstract: The present invention relates to novel compositions and, more particularly, to a class of compounds having specific quaternized amine based upon a guerbet amido amine linked to specific phosphate esters. Guerbet acids are a specific group of branched acids that have no unsaturation present in the group, but nonetheless are liquid, and are outstanding skin care emollients, providing great spreadability on the skin. In addition this material is not toxic to human skin and is well tolerated by human tissue making it suitable for use in the preparation products for personal care applications.

Abstract: This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: or pharmaceutically acceptable salts thereof wherein one of R1 and R2 is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources; R3 is hydrogen or lower alkyl and R4 is hydrogen, hydrocarbyl containing from 1-18 carbon atoms in a principal chain and up to a total of 23 carbon atoms, said principal chain may contain 1-5 double bonds or 1-2 triple bonds; phenyl which may be unsubstituted or substituted with lower alkyl; naphthyl which may be unsubstituted or substituted with low

Abstract: The present invention relates to the use of a series of etherlysophospholipids (ELPs) for the preparation of a medicament for the treatment of an inflammatory disease without causing adverse gastrointestinal side effects and/or without inhibition of phospholipase A2 and prostaglandin E2, as well as preventing or treating ulcerative conditions of the gastrointestinal tract.

Abstract: A method of controlling protozoa trophozoite and cysts is disclosed, comprising administering a phosphonium salt of the formula: (R1)3P−R2.X−, wherein R1 is an alkyl group having from 1-8 carbons and R2 is a chain substituent having 6-20 carbons, to aqueous systems harboring protozoa trophozoites and cysts. Addition of such phosphonium salts to aqueous systems was found to be effective at killing both the protozoa trophozoites and cysts. By effectively killing both the protozoa trophozoites and cysts, organism such as Legionella cells harbored in both the trophozoites and cysts are killed.

Abstract: The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.

Abstract: Increasing methylation of DNA in an unborn offspring of a pregnant mammal results in changing the epigenetically determined phenotype of the unborn offspring, inhibiting parasitic DNA sequences in the unborn offspring, and/or reducing susceptibility to tumor formation in the unborn offspring. Increased methylation is achieved by administering to the pregnant mammal a pharmaceutical composition which includes at least three of the following: Choline, Betaine, Folic acid, Vitamin B12, L-Methionine, and Zinc. The effective amount for each of these ingredients is: about 5-15 g/kg diet/day of Choline, about 5-15 g/kg diet/day of Betaine, about 5-15 mg/kg diet/day of Folic acid, about 0.5-1.5 mg/kg diet/day of Vitamin B12, about 0 to 7.5 g/kg diet/day of L-Methionine, and about 0 to 150 mg/kg diet/day of Zinc.

Abstract: A composition formulated from a primary anionic surfactant; optionally a secondary surfactant and/or a resin; and a nitrogen-containing compound of the structural formula: wherein R is a saturated, linear, branched or cyclic alkyl or aryl group containing 12 to 22 carbon atoms, with the proviso that R contains at least 80% of a single chain length and R is not lanolin, wheat germ or other natural broad-based chain distribution oil, R1 is a saturated or unsaturated, linear, branched or cyclic alkyl or aryl group containing 1 to 6 carbon atoms and may contain one or more hydroxyl groups, R2 is selected from the group consisting of hydrogen, methyl, ethyl and benzyl; and A− is a monovalent anion.

Abstract: A pharmaceutical combination comprising an accelerated lymphocyte homing agent in free form or in pharmaceutically acceptable salt form, and one or more compounds selected from the group consisting of an antibody to the IL-2 receptor, an immunosuppressive macrocyclic lactone and a soluble human complement inhibitor is used to treat or prevent insulin-producing cell graft rejection.

Abstract: A method to inhibit inflammation in a mammal is disclosed. The method includes administering to the mammal a composition comprising a phospholipid, which can be lysophosphatidic acid. The administration of a phospholipid is believed to down regulate expression of adhesion molecules on the surface of vascular endothelial cells and circulating leukocytes of the mammal.

Abstract: A pharmaceutical formulation comprising a pharmaceutically active agent, which is insoluble or sparingly soluble in water and a sterol phosphocholine surfactant.

Abstract: The object of the invention is to provide a medicament which is suitable for the treatment of tumors, such as via topical administration.

Abstract: Novel compositions comprising a potassium channel opener, such as minoxidil, and a protein kinase C inhibitor, such as procyanidin B2 are presented, as are kits containing a first composition comprising a potassium channel opener and a second composition comprising a protein kinase C inhibitor. Also presented are methods for using the novel compositions for treating and preventing hair loss in a region of a patient.

Abstract: The present invention relates to novel compounds and, more particularly, to a class of compounds having specific quatenized amine based upon a castor amido amine linked to specific phosphate esters. Castor oil contains predominantly ricinoleic moiefies. This phospholipid is an excellent emulsifier, conditioner and provides foam in formulations. It is also substantitive to human skin and is well tolerated by human tissue making it suitable for use in personal care applications.

Abstract: This invention provides a composition and method for increasing fat absorption from the intestine by increasing the amount of lysophosphatidylcholine in the intestine. The composition comprises phospholipase A2 and lipid molecules.

Abstract: The present invention is related to methods and compositions for susceptibility testing of bacteria containing mycolic acid structures using betaine-like detergents, and inducing the susceptibility of such bacteria using the same.

Abstract: A novel composition for treating nervous system disorders. The composition is formed by preparing a mixture comprising an effective amount of vitamin B-6, folic acid, vitamin C, magnesium, vitamin B-3, copper, probiotics, fructo-oligosaccharide (FOS), betaine, pancreatin, papain, pepsin, vitamin B-1, vitamin B-2, vitamin B-12, biotin, pantothenic acid, chromium polynicotinate and a digestive support ingredient selected from the group consisting of dandelion root, juniper, aloe vera, burdock, ginger root, artichoke, and kelp. Other ingredients may include: beta carotene, vitamin E, selenium, zinc, sea vegetation, alfalfa, trace minerals and molybdenum.

Abstract: Phospholipid-HETE derivatives, compositions and methods of use are disclosed. The compounds are particularly useful for treating dry eye.

Abstract: The present invention relates to compounds and, more particularly, to a class of compounds having specific quaternized amine based upon a dimer acid amido amine linked to specific phosphate esters. Dimer acid is a C-36 diacid having a cyclic structure and two amine groups that allow for the synthesis of a high molecular weight material phospholipid composition which is extremely substantitive to human skin and are well tolerated by human tissue making them suitable for use preparation of barrier products for personal care applications.

Abstract: A composition formulated from a primary anionic surfactant; optionally a secondary surfactant and/or a resin; and a nitrogen-containing compound of the structural formula: wherein R is a saturated, linear, branched or cyclic alkyl or aryl group containing 12 to 22 carbon atoms, with the proviso that R contains at least 80% of a single chain length and R is not lanolin, wheat germ or other natural broad-based chain distribution oil, R1 is a saturated or unsaturated, linear, branched or cyclic alkyl or aryl group containing 1 to 6 carbon atoms and may contain one or more hydroxyl groups, R2 is selected from the group consisting of hydrogen, methyl, ethyl and benzyl; and A− is a monovalent anion.

Abstract: Application of synthetic or naturally occurring lung surfactant to the posterior pharyngeal region prior to a period of sleep significantly reduces episodes of sleep disturbance resulting in apnea or hypopnea. The present invention provides lung surfactant in a convenient applicator container for easy use and storage. Incidents of oxygen desaturation are reduced, thereby lowering the risks of apnea-associated pathologies.

Abstract: A composition for preventing and treating milk fever in freshening cows, and a method of administering the composition. The basic composition is a mixture of water, calcium chloride, propylene glycol, B vitamins and minerals. The calcium content is lower than conventional calcium treatments used for this purpose. The propylene glycol gives the cow an energy boost and sweetens the taste so the cow does not object to it as it does to conventional gels and liquids. The B vitamins stimulate the cow's appetite. The minerals replace minerals lost in the milk and also help the cow absorb calcium. The composition of the present invention is in a liquid form and is preferably administered using a 200-300 cc drench gun. The end of the dispensing tube of the drench gun is placed between the teeth and cheek of the cow near the receptors that stimulate the esophageal groove reflex.

Abstract: An assay for emetic activity among inhibitors of type 4 phosphodiesterase (PDE 4) is disclosed. The assay comprises: (A) administering to a test mammal an anesthetic compound in an amount sufficient to cause an anesthetic effect; (B) administering to the test mammal a test compound that has PDE 4 inhibitory activity; (C) observing the test mammal for changes in the anesthetic effect, and (D) correlating any change in the anesthetic effect observed in the anesthetized test mammal to a standard.

Abstract: The present invention relates to compounds, which are phospholipid derivatives of valproic acid, to compositions comprising said compounds and their use for treating epilepsy, migraine, bipolar disorders and pain.

Abstract: Provided is a cosmetic composition, which comprises (A) at least one moisture retaining component selected from the group consisting of amino acids and salts thereof, pyrrolidonecarboxylic acid and salts thereof, lactic acid and salts thereof, urea and betaines; and (B) at least one sesquiterpene alcohol. This cosmetic composition exhibits high effects for alleviating the rough or moisture-lost skin and improving the skin condition such as dry skin or sensitive skin.

Abstract: A pharmaceutical compositions comprising L-carnitine or alkanoyl L-carnitine and hydroxycitric or pantothenic acid or derivatives thereof for the prevention and treatment of diseases brought about by lipid metabolism disorders, is disclosed.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a human related to supranormal intracellular enzyme (.e.g. phospholipase and/or esterase) activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3-glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.

Abstract: Disclosed herein are methods for increasing the bioavailability of pharmaceutical agents by conjugation to phospholipids. Also disclosed are phospholipid-derivatized steroids, peptides, antibiotics and other biologically active agents and pharmaceutical formulations comprising these compounds.

Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.

Abstract: The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

Abstract: The present invention provides an improved mode of operation of an apparatus for angioplasty or cardiac catheterization, apparatus for angioplasty and cardiac catheterization, and method of angioplasty or cardiac catheterization. The improvement and improved mode of operation includes the step of administering a therapeutically effective amount of a lipid acceptor during angioplasty or cardiac catheterization of a subject with the apparatus or component thereof. The lipid acceptor is selected from the group consisting of a large liposome comprised of phospholipids substantially free of sterol and small acceptors. The effective period of time is in the range of about less than 1 minute to about two years from the time of the angioplasty or cardiac catheterization. The improved angioplasty or cardiac catheterization apparatus includes means for administering a therapeutically effective amount of a lipid acceptor, and optional co-administration means for administering the lipid acceptor and a diagnostic agent.