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: 2-{[2-(Substituted amino)ethyl]sulfonyl}ethyl N,N-bis(2-chloroethyl)phosphorodiamidates and their salts, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer and autoimmune diseases, alone and in combination with other therapies.

Abstract: Agonist of vascular endothelial sphingosine-1-phosphate receptors are described. Compounds such as FTY720 can be phosphorylated by sphingosine kinase-2 into the phosphorylated forms which serve as sphingosine-1-phosphate receptor agonists. The vascular endothelial sphingosine-1-phosphate receptor agonists are employed in methods of treating a mammal for vascular permeability disorders and unwanted vascular endothelial cell apoptosis, and for the growth of new blood vessels. The sphingosine-1-phosphate receptor agonists can be used for the manufacture of a medicament for treating vascular permeability disorders and unwanted vascular endothelial cell apoptosis, and for the growth of new blood vessels.

Abstract: The invention generally relates to novel fluorescent phospholipid compounds and compositions comprising these compounds.

Abstract: To produce a labeled compound for a selected biological substance not using a radioisotope atom which has a risk of exposure to radioactivity and limitation on handling time but using a stable isotope atom; and that the labeled compound can be measured with good sensitivity separably from naturally occurring compounds of the selected biological substance which are substituted with the stable isotope atom. Choline as a biological substance is labeled by substituting the nitrogen atom of the quaternary ammonium group and all the carbon atoms of the methyl group attached to the nitrogen atom with respective isotopes 15N and 13C and used as a diagnostic agent.

Abstract: A compound of Formula 1 Rf-A-OP(O)(O?M+)(OROH) ??Formula 1 wherein Rf is a C2 to C6 linear or branched perfluoroalkyl optionally interrupted by one, two or three ether oxygen atoms; A is (CH2CF2)m(CH2)n—, (CH2)oSO2N(CH3)(CH2)p—, O(CF2)q(CH2)r—, or OCHFCF2OE-; m is 0 to 4; n, o, p, and r are each independently 2 to 20; q is 2; E is a C2 to C20 linear or branched alkyl group optionally interrupted by oxygen, sulfur, or nitrogen atoms; a cyclic alkyl group, or a C6 to C10 aryl group; M is H or a Group I metal or an ammonium cation (NHxR2y)+ wherein R2 is a C1 to C4 alkyl, x is 0 to 4, y is 0 to 4 and x+y is 4; and R is a C2 to C60 linear or branched alkyl group optionally interrupted by hetero atoms selected from the group consisting of an oxygen, sulfur, or nitrogen atom; a cyclic alkyl; or a C6 to C10 aryl; provided that when R is greater than 8 carbons, the ratio of hetero atoms to carbon atoms is at least 1:2.

Abstract: The present invention relates to a suspension stabilizer for dispersing inorganic nanoparticles into aqueous medium. More particularly, the present invention is directed to a biocompatible suspension stabilizer which comprises phosphoryl domain having an affinity to the surface of an inorganic nanoparticle and poly(ethylene glycol) having an affinity to the aqueous medium, and which is prepared by reacting a biocompatible poly(ethylene glycol)-derivatized polymer with phosphine oxide having a leaving group.

Abstract: A subject-matter of the invention is alkoxyamines resulting from ?-phosphorated nitroxides corresponding to the formula: in which R represents an alkyl radical having a number of carbon atoms ranging from 1 to 3, R1 represents a hydrogen atom or a residue: in which R3 represents an alkyl radical having a number of carbon atoms ranging from 1 to 20, and R2 represents a hydrogen atom, an alkyl radical having a number of carbon atoms ranging from 1 to 8, a phenyl radical, an alkali metal, such as Li, Na or K, H4N+, Bu4N+ or Bu3HN+, exhibiting a kinetic dissociation constant kd, measured at 120° C. by EPR, of greater than 0.05 s?1. These compounds can be used as initiators for the (co)polymerizations of at least one monomer which can be polymerized by the radical route.

Abstract: Aminophosphonic acid derivatives (e.g., 2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentylphosphonate monoester) are represented by the following general formula (1): and act as effective S1P receptor modulators while posing less side effects.

Abstract: The present invention relates to the use of a tri-substituted glycerol compound or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the prevention and/or treatment of radiation injuries. Furthermore, the invention relates to in vitro corresponding methods for preventing or treating of radiation damage or injury in one or more cells comprising contacting said cells with a medicament as defined in the invention.

Abstract: A phosphorylcholine group-containing compound that is a structure having a phosphorylcholine group represented by the following formula 1 and an amino group or a group derived from an amino group in an identical compound. (In the formula, m is 2 or more and 6 or less and p is 1 or 2. Each of X1, X2 and X3 is an alkyl group whose carbon number is 1 or more and 6 or less.

Abstract: Compounds of the formula, A—L—B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.

Abstract: Novel cyclic and acyclic oxazaphospholanes are described, as well as their use in the synthesis of sphingomyelin and sphingomyelin analogous. The production of synthetic sphingomyelins is also described. 2S, 3R stereoisomers of oxazaphospholanes and sphingomyelins, and synthetic methods for their preparation are described.

Abstract: The compound represented by general formula (I) below: wherein R10 represents hydrogen atom or methyl group; X represents —O(C?O)— or the like; and R represents hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or the like, and a polymer obtained by polymerizing a polymeric compound comprising the compound, which are useful for manufacturing hydrophilic polymer materials of high biocompatibility.

Abstract: Novel synthetic oxidized lipids and methods utilizing oxidized lipids for treating and preventing an inflammation associated with an endogenous oxidized lipid are provided.

Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1): in which represents single bond or double bond, R1, R2, R3, R7 and R8 are defined herein, Y represents —O—, —S—, —CH(Z)-, ?C(Z)-, —N(Z)-, ?N—, or —SiH(Z)-, wherein Z represents hydrogen, hydroxy or halogen, or represents C1-C7-alkyl, C1-C5-alkoxy, allyl, hydroxy-C1-C7-alkyl, C1-C7-aminoalkyl or phenyl, Q represents a group having the following formula: wherein X1, and X2 independently of one another represent hydrogen, amino, hydroxy or halogen, or represent C1-C7-alkyl, C1-C5-alkoxy, allyl, hydroxy-C1-C7-alkyl, phenyl or phenoxy each of which is optionally substituted by nitro or C1-C5-alkoxy, or represent C6-C10-arylthio which is optionally substituted by nitro, amino, C1-C6-alkyl or C1-C4-alkoxy, or represent C6-C12-arylamino, C1-C7-alkylamino, di(C1-C7-alkyl)amino, C3-C6-cycloalkylamino or a structure of wherein n denotes an integer of 1 or 2 and Y1 represents O, CH2 or N—

Abstract: One aspect of the present invention relates to a synthetic non-viral vector composition for gene therapy. Another aspect of the invention relates to the use of the composition for in vitro, ex vivo and/or in vivo transfer of genetic material. The invention also encompasses a pharmaceutical composition (useful for delivery of nucleic acids to a cell), containing a non-cationic amphiphilic molecule or macro-molecule; or a cationic amphiphilic molecule or macromolecule that transforms from a cationic entity to an anionic, neutral, or zwitterionic entity upon a chemical, photochemical, or biological reaction. Another aspect of the invention relates to multicationic compounds that are composed of three or more amino acids. The present invention also relates to the use of the pharmaceutical composition for delivery of nucleic acids to a cell. Moreover, the invention encompasses the non-viral vector compositions tethered to a surface.

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 relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.

Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.

Abstract: Two-photon dyes for real-time imaging of lipid rafts are provided. The two-photon dyes emit fluorescence with high intensity in the environments of cell membranes and can be used to clearly discriminate the hydrophobic and hydrophilic domains of the cell membranes. Therefore, the use of the two-photon dyes enables satisfactory imaging of actual lipid raft domains. In addition, since the two-photon dyes show no cytotoxicity, they can be suitably used in bioimaging applications, for example, real-time imaging of lipid rafts over a long period of time.

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 relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, other than N-(phosphonomethyl)-glycine or N,N-bis(phosphonomethyl)-glycine. Also included is a composition including an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, and a cosmetically or pharmaceutically acceptable vehicle for topical or systemic administration to a mammalian subject, as well as a method of administering an effective amount of such a composition for alleviating or improving a condition, disorder, symptom or syndrome associated with at least one of a nervous, vascular, musculoskeletal or cutaneous system.

Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.

Abstract: Aminophosphonic acid derivatives (e.g., 2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentylphosphonate monoester) are represented by the following general formula (1): and act as effective S1P receptor modulators while posing less side effects.

Abstract: The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.

Abstract: Crosslinkers having a covalently bonded phosphorous atom, the phosphorous atom having at least one covalently bonded oxygen atom. Crosslinkers can be used with resins such as epoxy, acrylic, polyurethane, polycarbonate, polysiloxane, polyvinyl, polyether, aminoplast, and polyester resins. A process to produce a crosslinker includes incorporating a pendent group comprising a covalently bonded phosphorous atom.

Abstract: This invention relates to the field of heterogeneous catalysis, and more particularly to catalysts including carbon supports having formed thereon compositions which comprise a transition metal in combination with nitrogen and/or carbon. The invention further relates to the fields of catalytic oxidation, including the preparation of secondary amines by the catalytic oxidation of tertiary amines.

Abstract: A steroid ester compound of a terminally-fluorinated alkyl fatty acid, a steroid compound having bis(trifluoromethyl)phenyl group, a phosphatidylserine compound having a terminally-fluorinated alkyl group, a glyceride compound having bis(trifluoromethyl phenyl group, or a glyceride compound having a terminally-fluorinated alkyl group. A vascular lesion can be selectively imaged by using a contrast medium comprising a liposome containing said compound or a salt thereof.

Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

Abstract: A compound of the invention is a specific compound having a phosphorylcholine group, and a polymer of the invention comprises at least 1 mol % of repeating units with a phosphorylcholine group and has a number-average molecular weight of 1,000 or more, the repeating units with a phosphorylcholine group being represented by the formula (II): wherein A is a bond selected from a single bond, —O—, —COO—, —OOC—, —CONH—, —NH—, —NHCO—, —NR2— and —CH2O— where R2 is an alkyl group having 1 to 6 carbon atoms; and m is an integer of 1 to 12.

Abstract: Provided is a composition comprising a phosphatidyl serine receptor ligand for use in immune therapy. The composition may include an antigen or allergen together with the phosphatidyl serine receptor ligand. The compositions may be used for any type of immune therapy, such as immune modulation to an environmental antigen or allergen, down regulation of immune hypersensitivity reactions, and stimulation of antigen or allergen specific IgA and/or IgG4.

Abstract: The present invention relates to phosphinic acid derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of a disease related to the inhibition of ?-secretase, inter alia for the treatment of Alzheimer's disease.

Abstract: Compounds of formula I wherein m, R, R1 and R3 to R6 are as defined in the specification, m, is 1, 2 or 3 and X is O or a direct bond, and the corresponding unphosporylated compounds have interesting properties, e.g. immunosuppressive properties.

Abstract: An insecticide of formula 1 and the agriculturally acceptable salts thereof, wherein: R1 is selected from the group consisting of: the group OR5 wherein R5 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclic and substituted heterocyclic; the group —NR6OH wherein R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, carbocyclic and substituted carbocyclic; the group NR7R8 wherein R7 and R8 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl and carbocyclic; and the group wherein R1 is linked to R2 to form a diradical bridging group; R2 and R3 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, carbocyclic, substituted carbocyclic, aryl, substituted aryl, acyl and substituted acyl; and A is a diradical linking group which has a molecular weight of preferably

Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.

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 discloses novel phospho-derivatives of branched-chain lipophilic molecules useful for permeabilizing biological barriers and for inhibiting tumor growth. The invention further discloses pharmaceutical compositions comprising said molecules and their uses.

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: 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: An oxidation catalyst is prepared by pyrolyzing a source of iron and a source of nitrogen on a carbon support. Preferably, a noble metal is deposited over the modified support which comprises iron and nitrogen bound to the carbon support. The catalyst is effective for oxidation reactions such as the oxidative cleavage of tertiary amines to produce secondary amines, especially the oxidation of N-(phosphonomethyl)iminodiacetic acid to N-(phosphonomethyl)glycine.

Abstract: The invention relates to compounds which constitute a class of medicaments which have an anti-inflammatory activity and which act by inhibiting leukotriene A4 (LTA4), and enzyme which is responsible for the biosynthesis of leukotriene LTB4, a major proinflammatory mediator. The invention also relates to therapeutic anti-inflammatory, applications of these compounds as well as for methods of preparing these compounds.

Abstract: Intermediates used in the preparation of compounds of formula I, or a stereoisomer thereof, or a pharmaceutically acceptable form of either selected from the group consisting of a salt, a solvate and a combination thereof, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid; and ii) (2R/S,3R)-(3-amino-2-hydroxybutyl)phosphinic acid.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two oxygen or sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes and in assays employing enzyme-labeled specific binding pairs.

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: 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: 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.