Abstract: A polyalkylene oxide-modified phospholipid represented by formula (1) defined in the specification, has a monoacyl phospholipid content of not more than 3% by weight and a content of a base having a nitrogen atom of not more than 0.02% by weight.

Abstract: The presented invention relates to a medication containing a therapeutically effective amount of phosphatidylcholine as active substrate for treatment of disease where phosphatidylcholine has an advantageous, protective effect on the mucosa of large intestine. The invention also relates to the use and application form of phosphatidylcholine for local treatment of inflammation of the large intestine and prophylaxis against cancer of the colon. Phosphatidylcholine can be administered as a rectal installation for local treatment of inflammation (in rectum or pouch) as well as in orally administered delayed-release form. The orally administered, delayed-release form of phosphatidylcholine prevents absorption in upper intestine and thus provides targeted release in the lower sections of the small intestine or colon.

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 invention relates to adjuvants that contain a lecithin, an oil and an amphiphilic surfactant and that are capable of forming a stable oil-in-water emulsion vaccine so as to minimize local reactions to the vaccine in the injected animal.

Abstract: In order to form liposomes with a longer half-life in blood, use is made of defined compounds with the general formula (A) 1

Abstract: The invention relates to a food product comprising 0.1 to 1.5 wt % of one or more anti-spattering agents comprising no native soy lecithin or native soy lecithin in an amount of from 0 to 0.05 wt % on total product, whereby the anti-spattering agent is preferably selected from the group comprising hydrolyzed lecithin, fractionated lecithin, citric acid esters or combinations thereof; optionally one or more emulsifiers in a total amount of from 0 to 0.5 wt %; optionally one or more browning agents in a total amount of from 0 to 0.07 wt %; one or more salts in an amount of from 0.5 to 3 wt %.

Abstract: The present invention is directed to a method of treating patients with major depression by administering omega-3 fatty acids. These may be administered in a substantially purified form, as part of a pharmaceutical composition, or as part of a larger molecule, e.g., a triacylglycerol, which releases free fatty acid after ingestion by a patient.

Abstract: A polyalkylene oxide-modified phospholipid represented by formula (1) defined in the specification, has a monoacyl phospholipid content of not more than 3% by weight and a content of a base having a nitrogen atom of not more than 0.02% by weight.

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

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

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 mammal related to supranormal intracellular enzyme 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 is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: Novel amides are disclosed, in particular amides of the all-trans-retinoic acid or 13-cis-retinoic acid and arachidonic acid and docosahexaenoic acid and eicosapentaenoic acid or linoleic acid with 2-aminoethanol, alpha-L-serine, alpha-L-threonine, alpha-L-tyrosine containing phosphate groups. Further, the present invention discloses the synthesis and use of these compounds, in particular their pharmaceutical application.

Abstract: The present invention relates to phospho-lipid compounds of formula having solubilizing activity for water-insoluble or poorly water soluble active agents and their use in the delivery of active agents to cells and in the treatment of diseases, i.e., cancer and protozoal diseases. The compounds also exhibit direct therapeutic effects on some diseases. The inventive compounds can be formulated into liposomes containing phospholipids, alkylphospholipids and/or cholesterol. The compounds of the present invention may be prepared by reacting primary and secondary amines with epoxides.

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: Diricinoleylphosphatidylcholine (I) in an optically active form is obtained with good yields and a high purity by means of a process which comprises: a) esterifying the terminal carboxylic group of ricinoleic acid (III) with an alcohol having from 1 to 4 carbon atoms to give the corresponding ester having formula (IV); b) protecting the hydroxylic group of the ester of ricinoleic acid (IV) with a protecting group removable under bland operating conditions and isolating the ester of ricinoleic acid of which the hydroxylic group (V) is protected; c) hydrolyzing the ester of ricinoleic acid of which the hydroxylic group (V) is protected and isolating the ricinoleic acid of which the hydroxylic group (VI) is protected; d) acylating L-&agr;-glycerophosphatidylcholine (II) with an imidazolic or triazolic derivative of the compound having formula (VI) and isolating the diricinoleylphosphatidylcholine of which the hydroxylic group (VII) is protected; e) removing the protecting group from the hydroxylic group of

Abstract: Disclosed is a new structural class of amphiphilic molecules which incorporate a hydrophilic material or polymer attached, at spatially distinct sites, to at least two hydrophobic residues. Certain of the amphiphilic molecules comprise a plurality of hydrophobic moieties. All such amphiphilic molecules have a common structural motif and, in contact with water, display surface activity and self-assemble into multimolecular aggregates and liquid crystalline phases. Also disclosed are enhanced stability liposomes that incorporate such amphiphilic molecules via unique interactions, and methods of using such formulations in a variety of applications including drug delivery, nutrition, bio-diagnostics, cosmetics, blood products and related applications.

Abstract: Novel amides are disclosed, in particular amides of the all-trans-retinoic acid or 13-cis-retinoic acid and arachidonic acid and docosahexaenoic acid and eicosapentaenoic acid or linoleic acid with 2-aminoethanol, alpha-L-serine, alpha-L-threonine, alpha-L-tyrosine containing phosphate groups. Further, the present invention discloses the synthesis and use of these compounds, in particular their pharmaceutical application.

Abstract: Methods of transfecting cells in vivo, including tumor cells in the peritoneal cavity are provided. Related lipid:nucleic acid formulations adapted to transfecting cells in the peritoneal cavity are provided. Assays, including high-throughput assays for screening lipid:nucleic acids are also provided.

Abstract: Nonalcoholic steatohepatitis (NASH) is a disease of the liver characterized by inflammation and damage to the liver cells. Typically, steatohepatitis involves inflammation of the liver related to fat accumulation, and mimics alcoholic hepatitis but is observed in patients who seldom or never consume alcohol. Nonalcoholic steatohepatitis can lead to serious liver damage, and ultimately cirrhosis. The present invention provides methods and compositions useful for the treatment or alleviation of nonalcoholic steatohepatitis and the pharmaceutical formulations for their administration to a human. Specifically, compositions comprised of lecithin, antioxidants and vitamin B complex are administered parenterally, most preferably by oral administration. Specific therapeutic formulations include admixtures of these compounds and specific dosage formulations include daily oral administrations of these compounds in tablet or powder forms.

Abstract: The present invention relates to a series of novel glyceryl phosphobetaine compounds which are exceptional f surface active agents that provide outstanding foam and are very mild to the hair and skin. The compounds, because they contain a pendant ionizable phosphate group and a quaternary amine compound are amphoteric surfactants that is they contain both a positive and negative charge in the same molecule. These combination of properties makes these polymers ideally suited for use in personal care applications.

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 mammal related to supranormal intracellular enzyme 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 is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: Novel ether lipids were obtained from methanogenic (Methanospirillum hungatei, Methanococcus jannaschii, Methanococcus voltae, Methanosarcina mazei, and Methanobrevibacter smithii), and extremely halophilic (Halobacterium cutirubrum) representatives of the archaeobacteria. Several of the ether lipids produced by Methanospirillum and Methanosarcina genera were purified and characterized structurally for the first time. Unilamellar liposomes were prepared from emulsions of the total polar-ether lipid extracts of such bacteria by pressure extrusion through membranes of various pore sizes. Liposome populations were shown by dynamic light scattering and electron microscopy to range in size depending on the pore size of the filter, on the source of the lipids, and on the composition of the suspending buffer medium. In all cases the size ranges indicated highly homogeneous preparations.

Abstract: Described are reversibly N-acylated phosphotidylserine and phosphatidylethanolamine derivatives which are useful as caged aminophospholipids. Also described are pharmaceutical preparations containing pH-sensitive liposomes formed with the caged aminophospholipids, and related methods.

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: Cationic amphiphiles are provided that are alkyl or alkoxyalkyl O-phosphate esters of diacylphosphatidyl zwitterionic compounds such as phosphatidylcholine or phosphatidyl ethanolamine. The amphiphiles can be used as carriers for delivering macromolecules intracellularly.

Abstract: Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active compounds to desired sites in the body, e.g. skeletal muscle or the heart. The pharmaceutically active compound can be a protease inhibitor, a cardioactive drug for combating arrythmia, etc. The linkage is chemical through one or more alcohol, carboxyl or amine groups using reagents such as glutaraldehyde, dicarboxylic acid anhydrides and acid halides and carbodiimides. Carnitine derivatives are also incorporated into liposomes which are then used as carriers of active pharmaceutical agents.

Abstract: The present invention provides a method for introducing nucleic acids into cells. The method involves exposing the cells to a compound having the formula ##STR1## in which: w is a nucleic acidx is a non-amino acid or non-peptide nucleic acid binding groupy is a spacer having a chain length equivalent to 1-30 carbon-carbon single covalent bonds or is absentR.sub.4 is H or halogen or CH.sub.2 O--R.sub.3 ; and R.sub.1, R.sub.2 and R.sub.3 are the same or different and are either hydrogen, methyl, ethyl, alkyl, alkenyl, hydroxylated alkyl, hydroxylated alkenyl groups or ether containing alkyl, alkenyl, hydroxylated alkyl or hydroxylated alkenyl groups optionally being an acyl group having a carbon chain length equivalent to 3-24 carbon atoms saturated or unsaturated, with the proviso that at least one of R.sub.1, R.sub.2 or R.sub.3 includes a group having a carbon chain of 3-24 carbon atoms saturated or unsaturated, or to a compound having the formula:w . . . y--y--NH--CH.sub.2 --CH.sub.2 O--R.sub.

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: ##STR1## or pharmaceutically acceptable salts thereof wherein one of R.sub.1 and R.sub.2 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 ##STR2## and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources;R.sub.3 is hydrogen or lower alkyl andR.sub.

Abstract: Retinoyl substituted glycerophosphoethanolamines are disclosed having the general Formula I: ##STR1## wherein one of A, B or C is a fatty ether substituent, one is a natural or synthetic retinoid ester substituent, and one is a phosphoethanolamine substituent, provided that A, B and C are each a different substituent. The optical and geometric isomers of compounds of Formula I and the pharmaceutically acceptable salts of the compounds, including the isomers, are also disclosed. The compounds (including the isomers thereof) and salts of the invention exhibit anti-tumor, anti-psoriatic and anti-inflammatory activities.

Abstract: The lubricant of this invention is lecithin. The lubricant is applied to the surface to be lubricated by forming a colloidal solution of water and lecithin. This solution may also include a surfactant, Vitamin E or its derivative. In addition, a solution stabilizer and an antimicrobial agent may be used to clarify the solution and to inhibit microbial growth in the solution.

Abstract: Described are reversibly N-acylated phosphotidylserine and phosphatidylethanolamine derivatives which are useful as caged aminophospholipids. Also described are pharmaceutical preparations containing pH-sensitive liposomes formed with the caged aminophospholipids, and related methods.

Abstract: A novel lipomelanin sunscreen complex includes melanin linked to a lipid to form a lipomelanin. One or more ultra-violet-light absorbing compounds can be added to form a lipomelanin sunscreen complex. A method for making the complex includes the oxidization of DOPA in the presence of a lipid and one or more ultra-violet absorbing compounds to form a mixture and precipitating the complex from the mixture by the addition of acid. The lipomelanin sunscreen complex provides protection against harmful ultra-violet radiation. The level of UV protection may be varied according to the presence and properties of the ultra-violet absorbing compounds in the complex.

Abstract: Lipid-containing prodrugs are provided for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids. Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids. The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.

Abstract: Cationic amphiphiles are provided that are alkyl or alkoxyalkyl O-phosphate esters of diacylphosphatidyl zwitterionic compounds such as phosphatidylcholine or phosphatidyl ethanolamine. The amphiphiles can be used as carriers for delivering macromolecules intracellularly.

Abstract: A method for extracting sphingomyelin from a phospho-lipid-containing fat concentrate is described. The method comprises the following steps:A. dissolving the fat concentrate in a solvent mixture of an essentially polar organic solvent and an essentially non-polar organic solvent,B. withdrawing a phase consisting mainly of the non-polar organic solvent and phospholipids dissolved therein,C. adding to the phase withdrawn in step B an organic solvent of intermediate polarity at a temperature of about 13.degree.-25.degree. C., thereby forming a precipitate comprising mainly sphingomyelin, together with a viscous phase and a solvent phase, and thenD. withdrawing the precipitate and the viscous phase, and separating them from one another.

Abstract: The lipids of this invention are derivatives of phosphatidyl choline having the general chemical formula: ##STR1## wherein at least one of R and R' is a polymerizable unsaturated alkyl group, acid or ester, wherein X includes an iminodiacetic acid in the polymerizable metal chelating lipid (2) and wherein z is an integer from 1-20 including 1 and 20. Lipid microstructures are formed by mixing the polymerizable metal chelating lipid monomers (2) with polymerizable non-chelating lipid monomers wherein X includes a non-chelating group, for example, --N.sup.+ (CH.sub.3).sub.3.

Abstract: A novel lipomelanin sunscreen complex includes melanin linked to a lipid to form a lipomelanin. One or more ultra-violet-light absorbing compounds can be added to form a lipomelanin sunscreen complex. A method for making the complex includes the oxidization of DOPA in the presence of a lipid and one or more ultra-violet absorbing compounds to form a mixture and precipitating the complex from the mixture by the addition of acid. The lipomelanin sunscreen complex provides protection against harmful ultra-violet radiation. The level of UV protection may be varied according to the presence and properties of the ultra-violet absorbing compounds in the complex.

Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.

Abstract: The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.

Abstract: A method of inhibiting oxidation of products containing unsaturated fatty acids and their derivatives comprises treating the unsaturated fatty acids and their derivatives with N-acylphosphatidylethanolamines. Preferred N-acylphosphatidylethanolamines are N-acetylphosphatidylethanolamine and N-oleoylphosphatidylethanolamine.

Abstract: A phospholipid comprising two different unsaturated fatty acids, the fatty acids being selected from the twelve n-6 and n-3 essential fatty acids, oleic acid, parinaric acid and combinic acid.

Abstract: Lipid-containing prodrugs are provided for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids. Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids. The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.

Abstract: Provided is a process for removing non-choline phosphatides from a lecithin material to facilitate obtaining a highly purified phosphatidylcholine product which is essentially free of non-choline phosphatides. The product can be obtained efficiently and effectively, even when starting with a raw soybean gum (lecithin).

Abstract: Fumaric acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or a metallic cation, andR.sub.2 is a saturated or unsaturated aliphatic C.sub.6 -C.sub.24 alkyl group, psoralen-9-yl, retinyl, .alpha.-tocopheryl (vitamin E), calciferyl, corticosteroid-21-yl or monosaccharid-.omega.-yl; a group of fumaric acid derivatives based on glycerol, alkane diol or polyol molecules; and fumaric acid derivatives of the formula ##STR2## wherein n is an integer from to 30 to 260,R.sub.3 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group,R.sub.4 is one of the R.sub.3 groups and n is the number of molecule repetitions, processes for their production and compositions containing same are described. These compounds are useful as drugs for the treatment of cryptogenically-caused diseases and have antisporiatic as well as antimicrobial action.

Abstract: A soybean lecithin based topical liniment and method of making the same is disclosed. The liniment utilizes soybean lecithin as a base and major ingredient and as the emulsifier which is mixed with plant oils, natural menthol, calcium stearate, and magnesium stearate. The soybean lecithin, plant oils, natural menthol, calcium stearate, and magnesium stearate are mixed together in predetermined relative proportions with the amount of soybean lecithin being greater than the sum of the amounts of the plant oils, natural menthol, calcium stearate, and magnesium stearate. The soybean lecithin, plant oils, natural menthol, calcium stearate, and magnesium stearate are added to one another and mixed together in a predetermined sequence to prevent precipitation and provide a homogenous mixture having a viscosity suitable for topical application.

Abstract: A phospholipid composition which satisfies the following requirements (i) and (ii):(i) a weight ratio of a nitrogen-containing phospholipid to the sum of a phospholipid, a glycolipid and a sterol derivative of less than 0.5; and(ii) a ratio of an area of a high-polar substance on a silica gel thin-layer chromatogram to the sum of areas of a phospholipid, a glycolipid and a sterol derivative on a silica gel thin-layer chromatogram of less than 500 area/.mu.g. A fat and oil composition containing from 0.001 to 30% by weight of the phospholipid composition is also disclosed. The present invention enables the blending of phospholipids with a frying oil, which has been considered difficult since it causes heat coloration. Thus a fat and oil composition, which is excellent in mold-release characteristics during cooking, has a good smell during heating, suffers from no coloration of oil after heating and shows a good flavor, can be obtained.

Abstract: The present invention provides prodrugs that serve as useful therapeutics for various disease states and conditions mediated by underlying specific hydrolytic enzyme activity. The prodrugs hereof (additionally) impart a physiologically bioactive component thus providing prodrug compounds that are capable of imparting dual effect systemically.

Abstract: An efficient, technically straightforward and inexpensive process for generating conjugates of phospholipids with biologically important molecules is described.

Abstract: A process of producing phosphatidylcholine derivatives by the reaction of glycerophosphatidylcholine with at least one fatty acid anhydride in the presence of a pyridine catalyst is described. The reaction is carried out in a melt of the glycerophosphatidylcholine, the at least one fatty acid anhydride and the catalyst.

Abstract: Disclosed are compositions comprising neutral, negatively and positively charged glycolipids phospholipids derived from lecithin, particularly lecithin fractions, and dilutions of lecithin or lecithin fractions. Also disclosed are methods for the preparation of such compositions, dosage units comprising these compositions, and methods of treatment of warm-blooded animals, preferably humans, with such compositions. These compositions are individually, collectively and selectively useful in the treatment of bacterial, viral, and skin infections and diseases.