Abstract: A description is given of processes for the preparation of mono- and bisacylphosphines and of mono- and bisacylphosphine oxides and mono- and bisacylphosphine sulfides, which comprises first reacting organic P-monohalogenophosphines or P,P-dihalogenophosphines, or mixtures thereof, with an alkali metal or magnesium in combination with lithium, where appropriate in the presence of a catalyst, and then carrying out the reaction with acid halides and, in the case of the process for the preparation of oxides, carrying out an oxidation step and, in the case of the preparation of sulfides, reacting the phosphines so obtained with sulfur. It is characteristic, Inter alia, that the processes are carried out without isolation of the intermediates.

Abstract: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)methylphosphinic acid; ii) (S)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iii) (R)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iv) (3-amino-2-hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2-oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

Abstract: Aminobutylic acid derivatives of the formula (I) wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.

Abstract: The invention relates to the calcium complex of [[(4R)-4-[bis[(carboxy-.kappa.O)methyl]amino-.kappa.N]-6,9-bis[(carboxy-.kappa.O)methyl]-1-[(4,4-diphenylcyclohexyl)oxy]-1-hydroxy-2-oxa-6,9-diaza-1-phosphaundecan-11-ylic-acid-.kappa.N6,.kappa. N9,.kappa.011]1-oxidato(6-)]-, tetrahydrogen(MS-325) and its salts, pharmaceutical agents that contain these complexes, for the production of agents for the reduction of effects that are caused by heavy metals as well as processes for their production.

Abstract: The invention relates to organophosphorus compounds of general formula (I) wherein A corresponds to general formula (II), wherein one or more of the carbon atoms, selected from the group C3, C4, C5 and their respective substituents can be omitted, and at least one substituent of B1 to B10 is a C3-8 cycloalkyl (C0-9) alkyl group, wherein both the C3-8 cycloalkyl group and the C0-9 alkyl group can have one or more double bonds and one or two carbon atoms of the cycloalkyl group can be substituted by nitrogen, oxygen or sulfur atoms, and wherein both the cycloalkyl group and the alkyl group can be substituted by hydrogen, halogen amine, oxo groups with branched or unbranched C1-9 alkyl groups and C2-9 alkenyl groups, wherein the C1-9 alkyl groups and C2-9 alkenyl groups can be substituted by hydrogen, hydroxy, amine, halogen, and oxo groups.

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: A process for oxidizing a hydroxymethylphosphonic acid compound to produce a formylphosphonic acid compound is described. The oxidation reaction is carried out in the presence of an oxidant and a catalyst. For example, hydroxymethylphosphonic acid (HMPA) is oxidized by oxygen or hydrogen peroxide in the presence of a copper-containing catalyst to give formylphosphonic acid (FPA). Formylphosphonic acid can then be reacted with glycine to produce a condensation product which, upon hydrogenation, yields glyphosate. Glyphosate can be incorporated into various formulations for use as a herbicide. In addition to glycine, formylphosphonic acid can also be reacted with ammonia, ethanolamine, or other primary amines to form a precursor compound, which can be converted to glyphosate.

Abstract: Immunoregulatory compounds are disclosed of the formula: as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: The present invention provides improved radioiodinated phospholipid ether analogs which demonstrate significant tumor avidity and longer plasma half-life than shorter-chain analogs. The radioiodinated phospholipid ether analogs of the present invention provide superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.

Abstract: The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders, pain, diabetic neuropathy, and prostate diseases, as well as pharmaceutical compositions comprising the same.

Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: Formylphosphonic acid derivatives are prepared by the catalytic decomposition of a (phosphonomethyl)amine N-oxide compound to form the formylphosphonic acid derivative and a dephosphonomethylated amine.

Abstract: Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided as well as synthetic processes and intermediates used in their preparation. Dioxetanes further substituted with two or more water-solubilizing groups disposed on the dioxetane structure and an additional fluorine atom or lower alkyl group provide superior performance by eliminating the problem of reagent carryover when used in assays performed on capsule chemistry analytical systems. These dioxetanes display substantially improved stability on storage. Compositions comprising these dioxetanes, a non-polymeric cationic surfactant enhancer and optionally a fluorescer, for providing enhanced chemiluminescence are also provided.

Abstract: Processes for preparing compounds of the formula (I) are described: P1OOC—CH(OH)—CHR1—CONH—Z wherein P1 is hydrogen or a protecting group, Z is a group —CHR2COOP2 or —CHR2CONR3R4 wherein P2 is hydrogen or a protecting group and R1-R4 are values known in the TNF-inhibitor art. The compounds of the formula (I) are useful in inhibiting TNF and one or more matrix metalloproteinase enzymes. One intermediate in a process of the invention is formula (II).

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.

Abstract: This invention is directed to an improved process for the preparation of N-(phosphonomethyl)glycine (i.e., “glyphosate”), a salt of N-(phosphonomethyl)glycine, or an ester of N-(phosphonomethyl)glycine. The process comprises combining an N-substituted N-(phosphonomethyl)glycine reactant with oxygen in the presence of a noble metal catalyst. The N-substituted N-(phosphonomethyl)glycine reactant has formula (V): wherein R1 and R2 are independently selected from the group consisting of hydrogen, halogen, —PO3R12R131, —SO3R14, —NO2, hydrocarbyl, and substituted hydrocarbyl other than —CO2R15; and R7, R8, R9, R12, R13, R14, and R15 are independently selected from the group consisting of hydrogen, hydrocarbyl, substituted hydrocarbyl, and an agronomically acceptable cation.

Abstract: Ether-linked phospholipids, derivatized at the polar head group with polyethylene glycol chains having molecular weights greater than 2,000 daltons, are disclosed. Lipid bilayers containing these phospholipids show high oxidative stability. Also disclosed is the use of PEG-derivatized ether-linked lipids in moisturizing and radiation-protective cosmetic compositions.

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: The present invention relate to phosphinic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase activity and to treat glutamate abnormalities and prostate diseases.

Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.

Abstract: A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an alkyl lipid or alkyl lipid derivative.

Abstract: This invention is directed to process for making a composition having the formula (I): ##STR1## wherein R.sup.3, R.sup.4, and R.sup.5 are independently hydrogen, substituted or unsubstituted hydrocarbyl, or an agronomically acceptable cation. The process comprises contacting a solution with a noble metal catalyst and introducing oxygen into the solution. The solution contains an N-substituted glyphosate having the formula (II): ##STR2## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, --PO.sub.3 H.sub.2, --SO.sub.3 H, --NO.sub.2, or substituted or unsubstituted hydrocarbyl other than --CO.sub.2 H. R.sup.3, R.sup.4, and R.sup.5 are as defined for formula (I).This invention also relates to an oxidation catalyst comprising a noble metal having a hydrophobic electroactive molecular species adsorbed thereon.

Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.

Abstract: A process for producing a (meth)acrylate derivative including reacting a compound of formula (1) (wherein R.sup.1 is H or CH.sub.3 ; A is C.sub.1 -C.sub.10 alkylene; and p is 1 to 10) with a chloro-dioxaphosphorus compound of formula (2) (wherein q is 0 or 1) in the presence of a secondary amine of formula (3) (wherein R.sup.2 and R.sub.3 are each C.sub.3 -C.sub.8 alkyl, cycloalkyl, C.sub.6 -C.sub.9 aryl, arylalkyl, etc.) to produce a (meth)acrylate derivative of formula (4) and further reacting the same with a tertiary amine of formula (5) (wherein R.sup.4, R.sup.5 and R.sup.6 are each C.sub.1 -C.sub.4 alkyl etc.) to provide a (meth)acrylate derivative of formula (6).

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: A process for preparing a phosphodiester of the formula: ##STR1## is described that involves (1) reaction of a first alcohol with phosphorous trichloride to form a phosphorodichlorodite, (2) reaction of the phosphorodichlorodite with an amine to form a phosphorodiamidite, (3) reaction with a second alcohol (which may be the same as the first alcohol) to form a phosphoramidite diester, and finally, (4) hydrolysis and oxidation of the phosphoramidite to form the phosphodiester. R and R1 may represent aliphatic, aromatic, heterocyclic, peptidic, peptoid, deoxyribo- or ribonucleotidic or nucleosidic, or organic chelating moieties.

Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.

Abstract: Novel ether-linked phospholipids derivatized with polyethylene glycol at the polar head group are disclosed. Lipid bilayers containing these phospholipids show high oxidative stability. Also disclosed is the use of PEG-derivatized ether-linked lipids in moisturizing and radiation-protective cosmetic compositions.

Abstract: Novel derivatives of lysophingolipids free from sialic acids which are N-acyllysosphingolipids having one of the two formulae: ##STR1## in which -A- stands for the group --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, n.sub.1 is a whole number of between 6 and 18, n.sub.2 is a whole number of between 11 and 15, X is a hydrogen atom or the residue of a monosaccharide or a disaccharide or phosphorylcholine and R represents an alkyl radical derived from a saturated or unsaturated aliphatic carboxylic acid having from 2 to 24 carbon atoms substituted by one or more polar groups. The lysosphingolipid derivatives of the invention exhibit an inhibiting action on protein-kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system.

Abstract: A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an alkyl lipid or alkyl lipid derivative.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

Abstract: The compound of the present invention comprises a substituted lysophospholipid, which includes a C12 to C20 alkyl ether, a C12 to C20 thioether, or a substituted C3 to C6 heterocycle containing at least two ring heteroatoms, selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof; and also includes a choline group or a C4 to C7 heterocycle containing heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof. The compounds of this invention possess antineoplastic and immunomodulatory characteristics.

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: A novel class of cationic phospholipids and a novel method for their synthesis are disclosed. The class of phospholipids comprises phosphotriester derivatives of phosphoglycerides and sphingolipids. It has been unexpectedly found that liposomes comprising one or more of these cationic phospholipids are effective in the lipofection of nucleic lacids. These novel phospholipids are particularly attractive because they are extremely cheap and easy to make.

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: Reactive dyestuffs which, in the form of the free acid, correspond to the following formula ##STR1## wherein D is the radical of an organic dyestuff of the mono-azo, polyazo or metal complex azo series and the other substituents have the meaning given in the description, show improved application properties.

Abstract: Certain phosphocholine derivatives having substantial antifungal therapeutic activity are disclosed. The phosphocholine derivatives may be chemically synthesized, enzymatically prepared or extracted from the plant Irlbachia alata. The phosphocholine derivatives are useful in treating fungal infections including those which are dermatophytic, systemic, ophthalmic and vaginal.

Abstract: A method of inhibiting tumor cell chemotactic and/or chemoinvasion motility comprising contacting the tumor cell with an inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting phagokinetic activity of tumor cells and neutrophils comprising contacting the cells with a phagokinetic inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting tumor cell metastasis comprising administering to a host in need of treatment a metastasis inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives, and pharmaceutically acceptable salts of the agent.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are described. These drugs release a cytotoxic phosphoramide mustard analog following activation by tumor associated proteases and esterases. The general structure for these drugs is: ##STR1## Wherein R1 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; wherein X is a good leaving group such as a halogen; R2 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; or an amino group (NH.sub.2) which may optionally be substituted. Wherein A is a benzyloxy derivative with one or more acyloxy or acylamino groups in para or ortho portions relative to the phosphoester; and wherein the acyloxy or acylamino groups are not (substituted or unsubstituted) p-guanidino-benzoyloxy groups or p-guanidino-benzoylamino groups.

Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains a 10:1 to 1:10 mixture of (1) N-chlorophenyl carbamates and N-chlorophenylthiocarbamates and (2) N-phosphonoglycine derivatives which are systemic herbicides. This composition can also be used to treat viral infections.

Abstract: A novel class of cationic phospholipids and novel method for their synthesis are disclosed. The class of phospholipids comprises phosphotriester derivatives of phosphoglycerides and sphingolipids. It has been unexpectedly found that liposomes comprising one or more of these cationic phospholipids are effective in the lipofection of nucleic acids. These novel phospholipids are particularly attractive because of they are not only effective in lipofection, but are extremely cheap and easy to make.

Abstract: There is provided antimicrobial agents which exhibit broad spectrum antibacterial and antifungal activity of the formula: ##STR1## wherein: x=1 to 3 or, preferably, mixtures thereofx+y=3z=xa=0 to 2B=O.sup.- or OMA=AnionM is a cationR, 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.

Abstract: There is provided antimicrobial agents which exhibit broad spectrum antibacterial and antifungal activity of the formula: ##STR1## wherein: x=1 to 3 or, preferably, mixtures thereofx+y=3z=xa=0 to 2B=O.sup.-- or OMA=AnionM is a cationR, 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.

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: Aminovinylphosphonic esters I ##STR1## where R.sup.1 is cyano, a radical of the formula --CO--OR.sup.6 or a group of the formula ##STR2## R.sup.2, R.sup.3 and R.sup.6 are C.sub.1 -C.sub.20 -alkyl, C.sub.5 -C.sub.8 -cycloalkyl, C.sub.7 -C.sub.18 -aralkyl, phenyl or tolyl,R.sup.4 is an unsubstituted or substituted phenyl or heterocyclic group defined belowR.sup.5 is hydrogen or C.sub.1 -C.sub.12 -alkyl,R.sup.7 is hydrogen, C.sub.1 -C.sub.6 -alkyl, formyl, C.sub.2 -C.sub.6 -alkanoyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.5 - or C.sub.6 -cycloalkoxy, cyanomethyl, 2-hydroxyethyl, benzyl or a radical of the formula --CR.sup.8 .dbd.CH--CO--OR.sup.6,R.sup.8 is hydrogen, C.sub.1 -C.sub.6 -alkyl or a radical of the formula --CO--OR.sup.6, andX is oxygen or NH, are used as light, oxygen and heat stabilizers for organic material.

Abstract: Compounds of formula (I), in which the groups R are hydrogen or C.sub.1-4 alkyl, n is from 2 to 4, X is alkylene, poly(ethoxy) or an aryl-containing group, Y is a valence bond or a divalent functional or heterocyclic group or a trivalent alkylene group, and Z is a sulphur-containing group which contains a thiol or disulphide group are useful to provide biocompatible treatments of metal surfaces, such as silver and gold surfaces. Processes for the preparation of the compounds, intermediates useful in such processes, articles having a metal surface treated with such compounds and processes of rendering metal surfaces biocompatible which comprise treating the metal surfaces with them.