Abstract: There are provided novel thermally stable surfactants for use with fillers in the preparation of polymer composites and nanocomposites. Typically, surfactants of the invention are urethanes, ureas or esters of thiocarbamic acid having a hydrocarbyl group of from 10 to 50 carbons and optionally including an ionizable or charged group (e.g., carboxyl group or quaternary amine). Thus, there are provided surfactants having Formula I: wherein the variables are as defined herein. Further provided are methods of making thermally stable surfactants and compositions, including composites and nanocomposites, using fillers coated with the surfactants.

Abstract: Methods for administering mitomycin C to a multi-drug resistant cell and for reducing the toxicity of the compound are described. In the methods, mitoymic C is provided in the form of a prodrug conjugate, where the drug is linked to a hydrophobic moiety, such as a lipid, through a cleavable dithiobenzyl linkage. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of mitomycin C in its original form. The linkage is stable under nonreducing conditions. The prodrug conjugate can be incorporated into liposomes for administration in vivo and release of mitomycin C in response to endogenous in vivo reducing conditions or in response to administration of an exogenous reducing agent.

Abstract: Conjugates of a hydrophobic moiety, such as a lipid, linked through a cleavable dithiobenzyl linkage to a therapeutic agent are described. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of the therapeutic agent in its original form. The linkage is stable under nonreducing conditions. The conjugate can be incorporated into liposomes for administration in vivo and release of the therapeutic agent in response to endogeneous in vivo reducing conditions or in response to administration of an exogeneous reducing agent.

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: Disclosed are thiol-functionalized phospholipids that have been covalently linked to a gold and/or silver substrate, methods for making them, and intermediates useful for such purposes. The resulting material creates a biomimetic surface that can be included in a conduit containing blood.

Abstract: The invention relates to conjugates of lipids and basic, membrane disturbing peptides, particularly compounds of the formula(R--CONH).sub.n --R.sup.3 (I)and(R--S--S).sub.n --R.sup.3 (II)wherein R is the hydrocarbyl moiety of a straight-chain or branched-chain, saturated or unsaturated aliphatic carboxylic acid, or a phospholipid moiety having a free valence bond; R.sup.3 is a basic membrane disturbing peptide having a free valence bond at one or two carbon atom(s); and n is 1 or 2. These conjugates can be used as a vector for transfecting a cell with a polynucleotide or any other anionic macromolecule.

Abstract: Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S;R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals;provided thatR.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.

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: Novel substrates of phospholipases, lysophospholipases and lipases are disclosed.

Abstract: Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S;R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals;provided thatR.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.

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: The present invention provides [3-(C.sub.16 -C.sub.18)-alkaesulphinyl- and -sulphonyl-2-methoxy-methylpropyl]-(2-trimethylammonioethyl) phosphates having superior anti-tumor activity.

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 modified biologically active protein consisting essentially of a biologically active protein bonded to lecithin via a covalent linking group and a pharmaceutical composition comprising the modified biologically active protein in a pharmaceutically acceptable carrier. The biologically active proteins include antibodies, superoxide dismutase, insulin and callidinogenase. Lecithin derivatives are also disclosed.

Abstract: Novel diacetylenic phospholipids having the diacetylenic moieties chemically decoupled from the rest of the acyl chains by the inclusion of one or more heteroatom, preferably oxygen, spacers on the acyl chains have the chemical formula: ##STR1## where m is 7, 8, 9, 10, 11, 12, or 13, where n is 8, 9, 10, 11, 12, or 13, where W is --O(CO)-- or --OCH.sub.2 --, where X is --CH.sub.2 --, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, or --SiMe.sub.2 CH.sub.2 --, where Y is --CH.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 NH--, or --CH.sub.2 SiMe.sub.2 --, where Z is --N(CH.sub.3).sub.3, saccharide, or --ROH where R is --(CH.sub.2).sub.p -- and p is 0, 1, 2 or 3, and where X and Y are not both --CH.sub.2 --. Novel tubules made from these diacetylenic phospholipids have high flexibility and variable morphology.