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: The invention related to colchinol derivatives of the formula (I): Wherein: R1; R2 and R3 are each independently hydroxy, phosphoryloxy (—OP3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkly); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when b is O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N-(C1-4alkyl)amino, N,N-di(C1-3alkyl)amino, or of the formula —Y1(CH2)0R11 or —NHCH(R12)COOH; [wh

Abstract: Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.

Abstract: The present invention is directed to novel compounds that function as immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases, to novel adjuvant formulations which include at least one of the adjuvant compounds of the invention, to novel immunostimulatory compositions which comprise an antigen and at least one of the adjuvant compounds of the invention, and to methods for the immunization of an animal by co-administration of a compound of the invention with an antigen against which the animal is to be immunized.

Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is 0 or an integer from 1 to 4 inclusive, (provided that when b is 0, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazo

Abstract: The present invention is directed to novel compounds that function as immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases, to novel adjuvant formulations which include at least one of the adjuvant compounds of the invention, to novel immunostimulatory compositions which comprise an antigen and at least one of the adjuvant compounds of the invention, and to methods for the immunization of an animal by co-administration of a compound of the invention with an antigen against which the animal is to be immunized.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.

Abstract: The present invention provides compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase. The present invention also provides pharmaceutical compositions that contain a compound that inhibits the association of platelet-derived growth factor and phosphatidylinosital 3-kinase, and methods of treating cancer, restenosis, arthritis, dermatitis, atherosclerosis, vein graft intimal hyperplasia, neointimal hyperplasia of vascular smooth muscle and psoriasis using compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase.

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 esters and salts of inorganic or organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: This invention relates to a process for the preparation of the formula I compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, a NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. ##STR1## In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethyl-ethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl ]-2-aminoethylphosphonic acid dialkyl ester (d) in 80% yield Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl ]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl)amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96% yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]prosphonic acid dialkyl ester (c) in 58% yield.

Abstract: A process for producing phosphatidylserine having a long chain unsaturated fatty acid in its side chain. In this process, a natural lecithin containing long chain unsaturated fatty acid side chain is used as the starting material. Using the natural lecithin as a substrate for reaction, phospholipase-D is caused to act on the substrate under the presence of serine, whereby phosphatidylserine having a side chain derived from the long chain unsaturated fatty acid can be easily obtained through a single step reaction.

Abstract: .alpha.-(hydroxyimino)phosphonoacetic acids (also referred to as ".alpha.,.alpha.-disubstituted trifunctional oximes" and "Troika Acids") and their derivatives, and methods to prepare them are disclosed. Also disclosed are the structures and fragmentation pathways of the .alpha.-(hydroxyimino)phosphonoacetic acids. The .alpha.-(hydroxyimino)phosphonoacetic acids and derivatives are useful as pH sensitive chelating agents, enzyme activated drugs, drug delivery agents, phosphorylating reagents and photo-activated reagents.

Abstract: Process for the enzymatic resolution of 2-amino-4-methylphosphinobutyric acid derivatives.L-PTC (L-phosphinothricin, L-2-amino-4-methylphosphinobutyric acid) is the active herbicidal component of D,L-PTC and can be obtained according to the invention when D,L-PTC derivatives which are N-acylated and esterified on the phosphinic acid group as well as optionally esterified or amidated on the carboxylic group, are treated with a hydrolytically active enzyme in an aqueous or aqueous-organic medium, in which process the L-PTC derivatives are selectively hydrolyzed on the N-acyl group or the modified carboxyl group, the resulting product mixture is resolved, and the desired L-PTC derivative is hydrolyzed to give the L-PTC and isolated by customary methods.

Abstract: An improved process for producing ethylenically unsaturated phosphate ester compounds, especially 2-(methacryloyloxyethyl)-2' (trimethylammoniomethyl) phosphate, (HEMA-PC) comprises a two step reaction in the first of which a phospholane reagent is reacted with a hydroxyl containing ethylenically unsaturated starting material, and in the second of which the intermediate formed in the first step is ring opened by reaction with trimethylamine to produce a zwitterionic product. In the process the two steps of the reaction are carried out in the same solvent with substantially no removal or addition of solvent after the first step. The solvent is preferably acetonitrile. The use of pure reagents avoids the production of undesirable by-products. The product is suitable for polymerising, for instance to provide cross-linked hydrogel copolymers used in ophthalmic applications.

Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: Novel .alpha.-aminophosphonates are provided along with processes and intermediates for their preparation. In preferred embodiments, scalemic .alpha.-aminophosphonates are prepared by the stereoselective addition of phosphite salts to chiral imines.

Abstract: Novel naphthyl-substituted .alpha.-amino acid derivatives, pharmaceutical compositions containing the same and a method of using the same, for the blockade of aspartate and glutamate receptors, are described. Novel intermediates of the napthyl-substituted .alpha.-amino acid derivatives are disclosed.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphono- and phosphinocarboxylic acids containing hydroxyl and/or mercapto groups, their use as waterproofing and/or oil-repellency agents, and a method for their preparation.

Abstract: The invention relates to a process for the enantioselective preparation of L-phosphinothricin (L-Ptc) and derivatives of the formula I ##STR1## in which R.sup.1 is H, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.4)-haloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl or (subst.) phenyl-(C.sub.1 -C.sub.4)-alkyl, R.sup.2 is hydrogen, formyl, [(C.sub.1 -C.sub.6)alkyl]carbonyl, [(C.sub.1 -C.sub.6)alkoxy]carbonyl, (subst.) benzyloxycarbonyl, (C.sub.1 -C.sub.6)-alkylsulfonyl or (subst.) (C.sub.6 -C.sub.10)-arylsulfonyl, and R.sup.3 is OH, NH.sub.2 or (C.sub.1 -C.sub.6)-alkoxy, or their salts with acids or bases.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids containing acrylate and/or methacrylate groups, their use as waterproofing or oil-repellency agents, and a method for their preparation.

Abstract: The present invention provides magnetic recording media comprising a magnetizable layer and optionally a backside coating provided on a nonmagnetizable substrate. At least one of the magnetizable layer and the optional backside coating comprises a polymeric binder, wherein the polymeric binder is obtained from reactants comprising a free radical generator and a radiation curable polymer. The radiation curable polymer comprises a plurality of radiation curable, .alpha.

Abstract: A stereospecific method of preparing alpha-aminophosphonic acids and derivatives thereof is provided. A protected amino acid is converted to a acyl aroyl or diacyl peroxide which spontaneously rearranges to form an alpha-amino ester. This rearrangement occurs stereospecifically with retention of configuration. The ester is subsequently converted to an appropriate leaving group and displaced with a phosphite yielding a chiral alpha-aminophosphonic acid or derivative.Alpha-aminophosphonic acids are useful for the synthesis of peptide analogs that possess a phosphonate linkage in the place of an amide linkage. This substitution can impart protease resistance in therapeutic peptides thereby increasing the serum half-life.

Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

Abstract: Substituted phosphorothioate derivatives and pharmaceutical compositions thereof as potential antiradiation agents are disclosed.

Abstract: A urethane reaction product, derived from an alkoxylated diorgano phosphorodithioate and an isocyanate, specifically, toluenediisocyanate and hexamethylene diisocyanate, is a multifunctional antiwear and antioxidant additive for lubricants. The isocyanate groups of the reaction product are substantially converted to urethane and/or urea groups through post reaction with active hydrogen compounds such as dibutylamine, bis(2-hydroxethyl) cocoamine and alcohols such as 2-propanol.

Abstract: A reagent for introducing a nucleic acid into an animal cell.

Abstract: The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect.

Abstract: There is provided longlasting contraceptives against human and animal sperm which contain a synthetic phospholipid spermicide of the formula: ##STR1## wherein: x=1 to 3 or mixtures thereof;x+y=3;z=x;a=0 to 2;B=0.sup.- or OM;A=Anion;M is a cation;R, R.sub.1 and R.sub.2 are the same or different and are alkyl, substituted alkyl, alkyl aryl or alkenyl groups of up to 16 carbon atoms with the proviso that the total carbon atoms in R+R.sub.1 +R.sub.2 is between 10 and 24; or ##STR2## wherein: x is as hereinabove defined;x+y=3;z=x;a=0 to 2;B=O.sup.- or OM;A is on Anion;M is a Cation;R.sub.3 is an amidoamine moiety of the formula: ##STR3## wherein: R.sub.7 is alkyl, alkenyl, alkoxy or hydroxyalkyl of from 5 to 21 carbon atoms each, or aryl or alkaryl of up to 20 carbon atoms;R.sub.6 is hydrogen or alkyl, hydroxyalkyl or alkenyl of up to 6 carbon atoms each or cycloalkyl of up to 6 carbon atoms, polyoxyalkylene of up to 10 carbon atoms;R.sub.4 and R.sub.

Abstract: Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

Abstract: New phosphonic acid derivatives are described which display antibacterial activity.

Abstract: Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.

Abstract: Phosphoric acid esters and their salts corresponding to the formula (I): ##STR1## wherein R represents an aliphatic, cycloaliphatic and/or aromatic moiety having no Zerewitinoff hydrogen, containing at least one ether oxygen atom (--O--) and at least one carboxylic acid ester group (--COO--) and/or urethane group (--NHCOO--), and having an average molecular weight M.sub.n of 200 to 10,000, wherein the hydrogen atoms may be partially replaced by halogen atoms, and wherein the ratio of the number of ether oxygen atoms to the number of the carboxylic acid ester groups and/or urethane groups in the molecule (or in every group R) is in the range from 1:20 to 20:1, and n represents 1 or 2. A method for preparing such phosphoric acid esters and salts and the use of such phosphoric acid esters or salts as dispersants or dispersing aids is also disclosed.

Abstract: The invention relates to an N-sulfomethylglycinate of formula:HO.sub.3 S--CH.sub.2 --NH--CH.sub.2 --COOR.sub.1 (I)COOR.sub.1 being a hydrolysable carboxylic ester group.It also relates to a process for the preparation of the compound of formula (I) consisting in putting in contact sulfur dioxide, formaldehyde, and glycine in the presence of a R.sub.1 OH alcohol, or glycinate.It also relates to the use of the compound of formula (I) for the preparation of herbicides of the glyphosate type of reaction with a phosphite or a phosphonate of formula (R.sub.2 O).sub.2 P(O) H in which (R.sub.2 O).sub.2 P is a hydrolysable phosphonic ester group, then optionally by a subsequent hydrolysis reaction.

Abstract: The invention relates to glycerol derivatives of general formulae Ia, Ib and Ic ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, A and Y stand for various substituents, to a preparation process of said compounds and to therapeutical compositions containing the same.

Abstract: A phosphatidylserine derivative represented by formulae (I), (II), and (III): ##STR1## wherein R represents a protective group which can be removed by an acid; and R' represents a straight chain or branched alkyl group having from 8 to 24 carbon atoms and may contain a substituent group, or may be unsaturated, provided that if an asymmetric carbon is present, the phosphatidylserine derivative is a racemic mixture or an optically active isomer thereof. Preferably, R represents a tertiary butoxycarbonyl group; R' represents a straight chain or branched alkyl group having 14, 16, or 18 carbon atoms; and the substituent is an alkylcarbonyl group, an alkoxycarbonyl group, a halogen atom, or an aryl group.

Abstract: New phosphonic acid derivatives are described which display antibacterial activity.

Abstract: The invention concerns antigens for the production of antibodies to Platelet Activating Factor (PAF). The antigens are PAF analogues of formula (I) ##STR1## wherein X comprises a high molecular weight group, R.sup.1 is a linking group and R.sup.2 to R.sup.5 are selected from C.sub.1 to C.sub.6 alkyl.Other aspects of the invention include PAF-antibodies produced using said antigens, labelled PAF analogues, intermediates for the preparation of PAF analogues and methods and a kit for the immunoassay of PAF.

Abstract: Novel alkoxycarbonylalkylphospholipids, alkylaminocarbonylalkylphospholipids, processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.

Abstract: Ashless hydrogen phosphonate dihydrocarbyl dithiocarbamates have been found to be effective antioxidant/antiwear multifunctional additives for lubricants.

Abstract: Compounds of the fomrula (I): ##STR1## and sterioisomers thereof, wherein X is halogen, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, alkenyl, alkynyl, aryl, amino, arylazo, heteroarylalkyl, heteroaryloxyalkyl, acylamino nitro, nitride, trifluoromethyl, -OR.sup.1, -SR.sup.1, -CO.sub.2 R.sup.2, -CONR.sup.3 R.sup.4, -COR.sup.5, -CR.sup.6 .dbd.NR.sup.7, -N.dbd.CR8R.sup.9, -SOR.sup.10 or -SO.sub.2 R.sup.11 ; W, Y and Z, which may be the same or different, are any of the atoms or groups listed for X above and, in addition, may be hydrogen atoms; or any two of the groups W, X, Y and Z, in adjacent positions on the phenyl ring, optionally join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; R.sup.1 is alkyl, or cycloalkyl optionally containing a heteroatom in the cycloalkyl ring, alkenyl, acyl, aryl, heteroaryl, aralkyl or heteroarylalkyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, R.sup.9, R.sup.10 and R.sup.

Abstract: Water-soluble triphendioxazine compounds having fiber-reactive dye properties conforming to the general formula ##STR1## where: B is --O-- or --S-- or --NH-- or (C.sub.1 -C.sub.6)-alkylamino;R* is hydrogen or optionally substituted alkyl or aryl;W and W.sup.1 are each a bivalent, aliphatic or optionally alkyl-substituted cycloaliphatic or aliphatic-cycloaliphatic radical, which aliphatic radicals can be interrupted by --O--, --S--, sulfonyl, carbonyl, 1,4-piperidino, amino, alkylamino and/or alkanoylamino groups, orthe grouping --B--W.sup.1 --N(R*) and/or --N(R*)--W--B-- each represent the bivalent radical of a five- or six-membered saturated heterocycle which contains two nitrogen atoms, orthe grouping --B--W.sup.1 -- and/or --W--B-- each represent the bivalent radical of a five- or six=-membered saturated heterocycle which contains two nitrogen atoms and which is bonded by one of the two nitrogen atoms via an alkylene group of 2 to 4 carbon atoms to the grouping --N(R*)--CO--G.sup.

Abstract: Described are phosphatidyl compounds of the formula I ##STR1## in which R.sup.1 represents C.sub.3-14 -alkanoyl, benzoyl, the acyl radical of an .alpha.-aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the .alpha.-amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a .beta.-aminocarboxylic acid or an .alpha.- or .beta.-hydroxycarboxylic acid,T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen,Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy,W represents hydrogen, andZ represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphaticC.sub.

Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.

Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.

Abstract: Compounds of the formula ##STR1## wherein the symbols have assigned meanings, and their use for controlling insects and mites.

Abstract: 2-Alkanoyloxy-3-(N-octadecylcarbamoyloxy)propyl trimethylammonioethyl phosphates and a salt thereof exhibit inhibitory activity against multiplication of tumor cells, and are useful as an antitumor agent.

Abstract: The invention relates to new O-acyl-alkanediol-phospholipids of the general formula I ##STR1## processes for their preparation and process for the treatment of certain diseases in humans.

Abstract: O,S-dialkyl S-[carbamyloxyalkyl] dithiophosphates of the general formula (I) ##STR1## where, independently of one another, R.sup.1 and R.sup.2 are each alkyl of not more than 4 carbon atoms and R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or alkyl of not more than 6 carbon atoms, or R.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a saturated or olefinically unsaturated ring which contains not more than 6 carbon atoms and may or may not contain one or more oxygen, sulfur or nitrogen atoms, are used for controlling insects or mites.