Abstract: A method for preparing plasmalogens and derivatives thereof represented by Formula B, wherein R1 and R2 are similar or different, derived from fatty acids; R3 is selected from hydrogen and small alkyl groups. The synthetic route involves production of novel cyclic plasmalogen precursors of Formula A and their conversion to plasmalogens and plasmalogen derivatives of Formula B. Also disclosed is the therapeutic use of plasmalogens and derivatives thereof as produced by the synthetic route of the present invention.

Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.

Abstract: The present invention relates to novel derivatives of oxazaphosphorines that are pre-activated, to the methods for preparing same, to the pharmaceutical compositions containing same and to the therapeutic use thereof, in particular for treating cancer.

Abstract: The present disclosure concerns complexes of 4-hydroperoxy ifosfamide. In one embodiment the complexes can be represented by the formula wherein A represents an ammonium species selected from the conjugate acid of a basic amino acid, quaternary ammonium, aliphatic ammonium, heterocyclic ammonium, aromatic ammonium, substituted and unsubstituted pyridinium, guanidinium, and amidinium, and wherein X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

Abstract: The present invention relates to a process for purifying a reaction output which comprises 3-aminopropanol and is obtained in the reaction of ethylene cyanohydrin with hydrogen in the presence of ammonia, which comprises distilling the reaction output comprising 3-aminopropanol in two or more stages, the ammonia content of the reaction output comprising 3-aminopropanol before introduction into the first distillation stage being 1% by weight or less and the temperature in the distillation stages being not more than 135° C. The invention further relates to a process for preparing 3-aminopropanol by reacting ethylene cyanohydrin with hydrogen in the presence of ammonia, which comprises performing the purification of the reaction output comprising 3-aminopropanol in accordance with the invention.

Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: A highly effective Co(II)-based system has been developed for catalytic intramolecular C—H amination with phosphoryl azides without the need of terminal oxidant or other additives, resulting in the high-yielding production of cyclophosphoramidates with nitrogen gas as the by-product; additional features of this new catalytic system include the amination of primary C—H bonds and formation of 7-membered ring structures.

Abstract: The present invention is directed to a phospholipid-based NIR molecular beacon, having a phospholipid moiety; with an NIR fluorophore moiety covalently linked to a phospholipid glycerol backbone and a quencher moiety covalently linked to the phospholipid glycerol backbone. Additionally, provided herein is methods of analyzing a sample for the presence of a phospholipase and methods of identifying the activity of a phospholipase in vivo utilizing phospholipid-based NIR molecular beacon.

Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical control agent of the structural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.

Abstract: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical control agent of the structural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.

Abstract: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical controi agent of the stxuctural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups. heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.

Abstract: Membrane permeable prodrugs of creatine phosphate, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine phosphate or pharmaceutical compositions thereof are disclosed.

Abstract: Phosphinines of formula (I) can be combined with metal salts to prepare hydroformylation catalysts. The phosphinine complexes have two phosphorus centers that may be substituted with a variety of hetero atoms or alkyl substituents to modify the ligand characteristics of the phosphinine. Phosphinine metal complexes are employed under normal hydroformylation reaction conditions. The preparatory routes to the phosphinine ligands of formula (I) allow for their convenient synthesis.

Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.

Abstract: The present invention relates to nitroaryl-substituted phosphoramide prodrug compounds and methods of producing the same for use in targeting and inhibiting undesirable cell growth or proliferation.

Abstract: Novel compounds according to formula I n is 0, 1, 2 or 3; X represents hydroxamic acid (CONHOH), carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R2, R10 and R11 independently represent hydrogen or (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl, all of which may optionally be substituted; R3 and R4 independently represent hydrogen, hydroxy or alkoxy; provided that if A, A′, Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen, and that at least one of R3, R4, R10 and R11 is different from hydrogen; or a salt, hydrate or solvate thereof; pharmaceutical compositions comprising said compound; therapeutical methods comprising administering said compounds; and the use of said compounds in the manufacture of medicaments.

Abstract: An improved phenoxyphosphazene compound is produced by treating a phenoxyphosphazene compound with (a) at least one adsorbent selected from activated carbon, silica gel, activated alumina, activated clay, synthetic zeolite and macromolecular adsorbents, (b) at least one reagent selected from metal hydrides, hydrazine, hypochlorites, thiosulfates, dialkyl sulfuric acids, ortho esters, diazoalkanes, lactones, alkanesultones, epoxy compounds and hydrogen peroxide, or (c) both the adsorbent and reagent, thereby reducing the acid value of said phosphazene compound to lower than 0.025 mgKOH/g.

Abstract: This invention relates to compounds which are N-oxides and derivatives thereof, as well as their use to treat HIF related diseases.

Abstract: The present invention provides a stable, sterile, pharmaceutical product that consists essentially of lyophilized ifosfamide and solutions thereof. The lyophilized ifosfamide of the present invention is suitable for pharmaceutical use, and can be stored in one or more aseptically sealed containers. The present invention further provides a method of producing lyophilized ifosfamide, which method includes freezing a sterile solution of ifosfamide and subjecting it to a primary drying stage. The primary drying stage includes applying a vacuum to remove solvent while raising the temperature to a primary drying temperature, to produce a first intermediate. The first intermediate is subjected to a secondary drying stage, which includes applying a vacuum to further remove solvent while raising the temperature to a secondary drying temperature, to produce the pharmaceutical product.

Abstract: A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme 1

Abstract: A compound of the general formula I wherein Y is O or S; n is 1, 2, 3 or 4; X represents hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R1 is wherein E, when present represents, a bond or optionally substituted methylene or ethylene; s and t are independently 0, 1, 2 or 3; A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical; Z represents a bond, O, S, C(O), C(O)NR7, NR7C(O) or NR7, wherein R7 is hydrogen, hydroxy, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R5 represents a bond, alkane or alkene diradical, one or more ether diradicals (R—O—R′) or amine diradicals (R—N—R′), wherein R and R′ independently represent alkane or alkene diradicals with a C-content from 0 to 3; R6 represents hydrogen, hydroxy, halogen, cyano, nitro,

Abstract: New phosphonamide compounds and methods of forming those compounds are provided. In one embodiment, the inventive methods comprise subjecting an opened-ring phosphonamide template to a ring-closing metathesis reaction in the presence of a ring-closing catalyst (e.g., a Grubbs catalyst) to yield a phosphonamide. In another embodiment, the inventive methods comprise reacting a template structure with a phosphorus (III) compound to yield the phosphonamide. Advantageously, in either embodiment, the template structures can be provided with a wide array of functional groups (e.g., amino acid side chains, peptides) chosen to provide particular properties to the compound.

Abstract: A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme 1

Abstract: This invention relates to novel benzo-2-triazole substituted compounds, pharmaceutical compositions, processes for their preparation, and use thereof in treating IL-8, GRO&agr;, GRO&bgr;, GRO&ggr; and NAP-2 mediated diseases.

Abstract: The invention relates to a synergistic mixture of A from 5 to 99% by weight of a carboxylic acid having more than 4 carbon atoms, an ethercarboxylic acid containing C18-C22-alkyl, C18-C22-alkenyl or C6-C18-alkylaryl substituents, an amidocarboxylic acid, or mixtures thereof, B from 1 to 95% by weight of a phosphoric mono- or diester, or mixtures thereof, which is substituted by C18-C22-alkyl, C18-C22-alkenyl, C6-C18-alkylaryl or alkoxylated groups, where the sum of components A and B is 100% by weight, to crude oils containing such mixtures, and to a process for dispersing asphaltenes in crude oils.

Abstract: A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme in which R1 is H, 2-bromoethyl, 2-chloroethyl, 2-hydroxyethyl, 2-mesyloxyethyl or 1-phenylethyl; R2 is H or 2-chloroethyl; R3 is H, 2-bromoethyl, 2-chloroethyl or 1-phenylethyl; and R4 is H; or R1 and R2, and also R3 and R4, together with the linked N atom, form an aziridide ring, where R1, R2 and R3 are not simultaneously H, and R1 and R3 are not simultaneously 1-phenylethyl; and Y, which is optionally present, is hydrogen chloride or hydrogen bromide. The reaction is carried out in a single vessel with phosphoryl chloride and an auxiliary base as an acid-binding agent with minimization of the effect of water and without isolation of an intermediate compound.

Abstract: A method of lyophilizing an oxazaphosphorin and a preparation produced thereby including dissolving an oxazaphosphorin in water, adding an amino acid to a molar ratio of between 1 to 10 amino acid to 1 oxazaphosphorin to produce a mixture and lyophilizing said mixture to remove said water, is disclosed.

Abstract: Methods and intermediates for the preparation of oligomers containing diastereomerically enriched phosphorothioate linkages are disclosed.

Abstract: A silver halide color photosensitive material is disclosed, which has on a support at least one photosensitive silver halide emulsion layer, wherein at least one nondiffusible compound represented by the following formulas (I), (I-1), or (I-2) is contained to inhibit generation of color stain and color fog and to ensure excellent keeping quality: ##STR1## wherein Y.sup.1 represents atoms completing a phosphorus-containing heterocyclic ring; and ##STR2## wherein R.sup.1 represents an aryl group or a heterocyclic group; R.sup.2 represents an alkyl group, a cycloalkyl group, an aryl group (formula (I-2)), a heterocyclic group (formula CI-2)), an alkoxy group or an aryloxy group; A.sup.1 and A.sup.2 each represent a hydrogen atom or a hydrolyzable group; G represents a carbon atom or a phosphorus atom; X represents an oxygen atom or a sulfur atom; and R.sup.3 represents an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group.

Abstract: Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.

Abstract: New phosphazene derivatives, fully substituted by aromatic groups and perfluoropolyethereal chains, are utilized as stabilizers for oils and greases based on perfluoropolyethers. Such derivatives inhibit the degradation process affecting the perfluoropolyethereal chains when these are subjected to high temperatures in an oxidizing atmosphere and in the presence of metals, such as for example aluminium, titanium, vanadium and their alloys, or steels.

Abstract: Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.

Abstract: Compounds of the general formula I ##STR1## in which n is 1, 2 or 3 and in which X is oxygen or sulfur, T has the meaning of --S--, --S--S--, --S--S--, --S--S--S--S--, --S--S--S--S--S--, ##STR2## and Y has the meaning of ##STR3## in which Z has the meaning of --H, --COR.sup.13, --COOR.sup.13 or --CONHR.sup.13, and Q has the meaning of oxygen or --NR.sup.0 --, and R.sup.1, R.sup.2, R.sup.0, R.sup.4 and R.sup.13 are as defined in claim 1, with the proviso that the compound of the formula C.sub.2 H.sub.5 --S--CH.sub.2 CH(OH)--P(OC.sub.2 H.sub.5).sub.2 is excepted.The invention also relates to compositions containing the compounds of the formula I and organic materials, for example functional liquids and, in particular, lubricants.

Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.

Abstract: Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.

Abstract: Compounds of the present invention are those having the formula: ##STR1## where R.sub.1 and R.sub.3 are the same or different and are a linear or branched chain of 1 to 22 carbon atoms selected from the group consisting of alkyl, alkenyl or alkynyl or said C.sub.1 to C.sub.22 chains substituted with halo, --SR.sub.5, --OR.sub.5, --NHR.sub.5, --NR'.sub.5 R.sub.5 or --C(O)OR.sub.6 where R.sub.6 is hydrogen or C.sub.1 to C.sub.6 alkyl; R.sub.5 and R'.sub.5 are the same or different and are hydrogen, amino-alkyl substituted with phenyl, substituted phenyl, benzoyl, substituted benzoyl, heteroaryl or substituted heteroaryl; R.sub.2 is hydrogen, C.sub.1 to C.sub.6 alkyl, phenyl or substituted phenyl; R.sub.4 is hydrogen, C.sub.1 to C.sub.6 alkyl, phenyl or substituted phenyl; Z is sulfur or oxygen; m is an integer from 1 to 3; and n is an integer from 1 to 23.The compounds provide useful methods of inhibiting protein kinase C.

Abstract: Lubricant additives are disclosed which are produced by reacting an alkanolamine, a carboxylic acid and phosphorous acid. The reaction product may also include a boron compound and/or a monofunctional alcohol. The additives are useful in combination with metalworking oils, particularly in extreme pressure applications, to replace currently used chlorinated paraffin additives.

Abstract: The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.

Abstract: The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.

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: Ifosfamide lyophilizate consisting substantially of ifosfamide and 0.1 to 17 parts by weight of a hexitol.

Abstract: Lubricant additives are produced by reacting an alkoxylated amine with phosphorous acid. The additives preferably also contain a boron moiety which is reacted with the phosphorous acid and amine, preferably in a one step reaction. More preferably, a mono-functional alcohol or a long-chain aliphatic carboxylic acid is added to this mixture. The additives are particularly useful in metal working oils and particularly as extreme pressure additives to replace the currently used chlorinated paraffin additives.

Abstract: Hydrolytically stable phosphite compositions for melt flow and color stabilization of thermoplastics may be prepared from crude tetrahydroabietyl alcohol. The phosphites may be prepared by reacting said alcohol with an organophosphite, such as by transesterification. Other synthesis techniques may also be used.

Abstract: It has now been discovered that oligomers of C.sub.6 - C.sub.20 alpha-olefins, such as 1-decene, with branch ratios below 0.19 and high viscosity indices (HVI) can be functionalized to provide unique phosphite derivatives. Functionalized polyalpha-olefin lubricants compositions are prepared with superior properties by adding functionalized organophosphites to the olefinic bond of HVI-PAO. The invention encompasses a process for the preparation of lubricant range hydrocarbons containing phosphonate functional groups, comprising;reacting olefinic C.sub.20 + polyalpha-olefin oligomers having a branch ratio of less than 0.19 and phosphite ester in a mixture with peroxide catalyst at elevated temperature whereby phosphite ester adduct of said polyalpha-olefin is formed;separating said reaction mixture products and recovering said adduct.

Abstract: Substituted 3H-1,3,2-oxazaphospholidines of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, alkyl, cycloalkyl, phenylalkyl or aryl, n is 1 to 4 and T is an n-valent aliphatic or aromatic hydrocarbon radical are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and/or actinic radiation.

Abstract: Substituted 1,3,2-benzoxazaphospholidines of formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, alkyl, cycloalkyl, phenylalkyl or aryl, n is 1 to 4, and T is an n-valent aliphatic or aromatic hydrocarbon radical are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and actinic radiation.

Abstract: Novel phosphite derivatives of propylene based lube olefins are novel lubricating fluid media with internal synergistic multifunctional extreme pressure, antiwear and antioxidant properties. These compounds exhibit the same multifunctional characteristics when used in minor additive amounts in either mineral or synthetic lubricating oils as well as fuels.

Abstract: New organic phosphorus compounds, comprised of hetero-phosphacycloalkanes whose phosphorus atom forms a complex with a borane. They can be prepared by the action of a borane on a hetero-phosphacycloalkane, within a solvent, at temperatures ranging from -20.degree. to +60.degree. C. Their transformation into other derivatives, phosphinites or phosphines in particular, can be carried out without any modification in the chirality of the initial complex. An especially useful application is their conversion into highly optically active phosphines, used in particular as catalysts in various reactions.