Abstract: It is disclosed herein that that certain alkylphosphocholine analogs are preferentially taken up by malignant pediatric tumor cells. The alkylphophocholine analogs are compounds having the formula: or salts thereof, wherein n is an integer from 12 to 24; and R2 is —N+(CH3)3. The compounds can be used to treat pediatric solid tumors or to detect pediatric solid tumors. In therapeutic treatment, R1 includes a radioactive iodine isotope that locally delivers therapeutic dosages of radiation to the malignant pediatric tumor cells that preferentially take up the compound. In detection/imaging applications, R1 includes a detection moiety, such as a fluorophore or a radioactive iodine isotope.

Abstract: New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes. The present invention is in the field of molecular biology, and more particularly in the field of transfection, which utilizes new compounds and methods for the introduction of nucleic acids into eukaryotic cells.

Abstract: A method for producing a compound represented by General Formula (1), the method including: reacting a compound represented by General Formula (3) and a compound represented by General Formula (4): where R1 and R2 each represent aliphatic group which may have substituent, or aromatic group which may have substituent (with the proviso that R1 and R2 are different groups), R3 represents aromatic group which may have substituent, and R4 represents aliphatic group which may have substituent, or aromatic group which may have substituent, where R1 and R2 each represent aliphatic group which may have substituent, or aromatic group which may have substituent (with the proviso that R1 and R2 are different groups), and R3 represents aromatic group which may have substituent, where R4 represents aliphatic group which may have substituent, or aromatic group which may have substituent.

Abstract: Organic compounds which contain nitrogen, fluorine, and phosphorus atoms together with carbon atoms and hydrogen atoms and which can be used as a multi-element standard for 1H—, 13C—, 15N—, 19F—, and 31P nuclear magnetic resonance spectroscopy. Also, a nuclear magnetic resonance spectroscopy method, preferably a quantitative nuclear magnetic resonance spectroscopy method, using said compounds and a method for qualitatively and/or quantitatively determining an analyte using such a nuclear magnetic resonance spectroscopy method.

Abstract: The present invention relates to an amino group-containing phosphate ester flame retardant which has both a phosphate group and an amine group to exhibit a good flame retarding effect while overcoming the problems with the conventional phosphor-based flame retardants not having a good flame retarding effect with respect to its added amount, and a method of preparing the same.

Abstract: The present invention relates to a process for the preparation of phosphoric esters, and to selected compounds.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: Disclosed are saccharide and phosphocholine derivatives. The derivatives include azide and alkyne derivatives which form one end of a variable length carbon chain. The opposite end of the variable length carbon chain is covalently linked to the saccharide or phosphocholine. The saccharide may be, for instance, a maltoside. The alkyne and azide derivatives of the saccharides and phosphocholine may be reacted together to form amphiphilic molecules useful in cellular membrane studies and applications. By adjusting the length of the carbon chain, the biochemical and biophysical properties of the resultant 1,4-disubstituted 1,2,3-triazole compounds may be custom tailored for the intended application. Resultant molecules may form micelles, bicelle, lipid bilayers and other like structures useful in the isolation and purification of membrane bound or membrane associated proteins and biochemical components.

Abstract: A storage stable aqueous solution of amifostine at a pH of at least 10.0, in an amifostine concentration of about 50 to about 250 mg/l, which formulation is storage stable under refrigerated conditions.

Abstract: Disclosed are compounds of Formula (I) and/or a salt thereof; wherein R is —OH or —OP(O)(OH)2. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Abstract: Novel compounds and pharmaceutical compositions thereof for the treatment and/or prevention of cancer and precancerous conditions, inflammation-related disorders, pain and fever.

Abstract: Provided are diphenyl sulfide derivatives which have excellent S1P3 antagonistic activity and are useful as drugs. Intensive studies have been made for the purpose of creating a compound having S1P3 antagonistic activity. As a result of the intensive studies, it has been found that diphenyl sulfide derivatives represented by general formula (1) have excellent S1P3 antagonistic activity. In general formula (1), R1 is a hydrogen atom or the like; R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like; X is a methylene group which may be substituted with one or two fluorine atoms, or the like; Y is a hydrogen atom or the like; and Z is a halogen atom.

Abstract: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.

Abstract: The invention relates to pharmaceutical compositions comprising alkylphosphocholines and antimetabolite antitumor substances. The pharmaceutical compositions of the invention are useful for the treatment of benign and malignant oncoses in humans and animals. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.

Abstract: Disclosed are saccharide and phosphocholine derivatives. The derivatives include azide and alkyne derivatives which form one end of a variable length carbon chain. The opposite end of the variable length carbon chain is covalently linked to the saccharide or phosphocholine. The saccharide may be, for instance, a maltoside. The alkyne and azide derivatives of the saccharides and phosphocholine may be reacted together to form amphiphilic molecules useful in cellular membrane studies and applications. By adjusting the length of the carbon chain, the biochemical and biophysical properties of the resultant 1,4-disubstituted 1,2,3-triazole compounds may be custom tailored for the intended application. Resultant molecules may form micelles, bicelle, lipid bilayers and other like structures useful in the isolation and purification of membrane bound or membrane associated proteins and biochemical components.

Abstract: The invention relates to the use of alkylphosphocholines in combination with antimetabolites for the treatment of multiple myeloma, colon cancer or renal cancer. Preferred alkylphosphocholines are described by the Formula II. A particularly effective treatment includes administering a combination of perifosine and capecitabine.

Abstract: Antibodies against PC, PC conjugate or bioactive components and/or fragments thereof for use in combination therapy with one or more biologic agents and/or stem cells are disclosed, as well as compositions comprising the antibodies in combination with one or more biologic agents and/or stem cells. Also disclosed are PC conjugates, PC or bioactive components and/or parts/fragments thereof for use in activation immunotherapy prior to or in combination with treatment with biologic agents and/or stem cells for curing, treating, preventing, and/or reducing the risk of developing auto-immune diseases, chronic inflammatory diseases, and cancer diseases, as well as compositions comprising them in combination with biologic agents and/or stem cells.

Abstract: Provided are compounds, compositions and methods for treating protozoan infections.

Abstract: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.

Abstract: This disclosure provides choline analogs comprising the following structure: where each R1 independently is H or isotopically enriched D, R2 is a protecting group, and N is 14N or isotopically enriched 15N. This disclosure also provides methods of making choline analogs, which include performing a protection step on a betaine aldehyde to form a choline analog, and methods of using choline analogs to form hyperpolarized compounds.

Abstract: The present invention relates to a process for the preparation of phosphoric esters, and to selected compounds.

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: Provided are diphenyl sulfide derivatives which have excellent S1P3 antagonistic activity and are useful as drugs. Intensive studies have been made for the purpose of creating a compound having S1P3 antagonistic activity. As a result of the intensive studies, it has been found that diphenyl sulfide derivatives represented by general formula (1) have excellent S1P3 antagonistic activity. In general formula (1), R1 is a hydrogen atom or the like; R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like; X is a methylene group which may be substituted with one or two fluorine atoms, or the like; Y is a hydrogen atom or the like; and Z is a halogen atom.

Abstract: Disclosed are processes for development and recovery of lipids from biomass. A plant or microorganism-based biomass can be developed to encourage a desired lipid profile. Following development, ecologically friendly normally gaseous fluids such as carbon dioxide can be pressurized to a supercritical state followed by rapid expansion. The fluid is first contacted with a biomass source including oil-containing microorganisms and/or agricultural products. For instance, fungi or algae can be bioconverted from another biomass sources such as canola seed or corn syrup and then contacted with the high pressure fluid. During a contact period, the fluid can diffuse into the biomass, and in particular through the cell walls of the biomass. The fluid undergoes rapid release of pressure and opens the cell structure for improved release of oil. The fluid can optionally be utilized for extraction following the explosion process. For instance, the fluid can be re-pressurized in the same vessel for extraction processes.

Abstract: The invention relates to ophthalmological implants which comprise alkylphosphocholines. Implants of this type may in particular advantageously be used for the prophylaxis of aftercataract.

Abstract: Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.

Abstract: Provided is a method to identify OP-adducted biomarkers of OP exposure as well as compounds containing OPs that can provide OP adducts.

Abstract: The invention relates to a method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) to yield an alkylphosphonic acid, salt or ester (II) thereof in the presence of a catalyst A, b) the thus obtained alkylphosphonic acid, salt or ester (II) thereof is reacted with acetylenic compounds of formula (V) to yield a mono-functionalized dialkylphosphinic acid derivative (VI) in the presence of a catalyst B, and c) the thus obtained mono-functionalized dialkylphosphinic acid derivative (VI) is reacted with a hydrogen cyanide source to yield a mono-functionalized dialkylphosphinic acid derivative (VII) in the presence of a catalyst C, and d) the thus obtained mono-functionalized dialkylphosphinic acid derivative (VII); is reacted to yield a mono-aminofunctionalized dialkylphosphinic acid derivative (III) in the presence of a catalyst D or a reduction agent, wherein R1, R2, R3, R4, R5, R6 are the

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention provides phospholipid in a crystalline form, a method for its preparation, compositions comprising it and its use in the treatment of damaged tissue.

Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.

Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: The object of the present invention is to provide a packing material and a separation method that manifest excellent hydrophilic interactions. The present invention provides a packing material for hydrophilic interaction chromatography consisting of a modified support treated with the surface modifier represented by the following formula (6) or (7). (In this formula, m denotes 2-6 and n denotes 1-4. X1, X2, and X3, independent of each other, denote a methoxy group, ethoxy group, or halogen. Up to two of X1, X2, and X3 can be any of the following groups: a methyl group, ethyl group, propyl group, isopropyl group, butyl group, or isobutyl group.

Abstract: Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.

Abstract: The invention relates to the use of alkylphosphocholines in combination with antimetabolites for the treatment of multiple myeloma, colon cancer or renal cancer. Preferred alkylphosphocholines are described by the Formula II. A particularly effective treatment includes administering a combination of perifosine and capecitabine.

Abstract: A method of manufacturing an affinity particle includes a step of reacting a particle having a reactive functional group on a surface thereof with a ligand having a functional group having a reactivity with the reactive functional group to bond the ligand to the particle, and a step of reacting the particle to which the ligand is bonded with a surface modifying agent having a functional group represented by a general formula of: (wherein each of R1, R2, and R3 is independently an alkyl group whose carbon number is 1 or more and 6 or less, m is an integer of 2 or more and 6 or less, and n is 1 or 2.) and a functional group having a reactivity with the reactive functional group to bond the surface modifying agent to the particle to which the ligand is bonded.

Abstract: Methods and kits for decomposing organophosphorus compounds in non-aqueous media at ambient conditions are described. Insecticides, pesticides, and chemical warfare agents can be quickly decomposed to non-toxic products. The method comprises combining the organophosphorus compound with a non-aqueous solution, preferably an alcohol, comprising metal ions and at least a trace amount of alkoxide ions. In a first preferred embodiment, the metal ion is a lanthanum ion. In a second preferred embodiment, the metal ion is a transition metal.

Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.

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

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.

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 invention relates to the use of oleyl phosphocholine and oleyl-phospho-(N.N.-dimethyl-N-ethyl)-ethyl-ammonium for the long-term and continuous treatment of serious illnesses, such as cancer, leishmaniasis, ehrlichiosis, multiple sclerosis and psoriasis, in addition to other indications mentioned in the application.

Abstract: Novel phospho-derivatives of branched-chain lipophilic molecules useful for permeabilizing biological barriers and for inhibiting tumor growth are disclosed. Pharmaceutical compositions comprising phospho-derivatives of branched-chain lipophilic molecules and their uses are also disclosed.

Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.

Abstract: The present invention is affinity particles that are characterized by having phosphorylcholine groups represented by the following formula (1) covalently bonded onto the surface of inorganic powder and also by having ligands having specific affinity with a certain target substance covalently bonded or adsorbed onto the surface of inorganic powder. The object of the present invention is to provide an affinity separation method that uses affinity particles utilizing inexpensive inorganic particles and is capable of separating the target substance easily and with high accuracy.

Abstract: The present invention relates to lipid-analogous phosphoric acid compounds and in particular phosphoric triesters, phosphoric diester amides and phosphoric diesters. These are preferably cationic phospholipids preferably having at least one free hydroxyl group.

Abstract: An acid gas absorbent comprising a metal sulfonate, phosphonate or carboxylate of a hindered amine and a process for the selective removal Of H2S as well as other acidic components such as carbon disulfide, carbonyl sulfide and oxygen and sulfur derivatives of C1 to C4 hydrocarbons from mixtures containing such acidic components and CO2 using said absorbent.

Abstract: The present invention relates to a novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumors, and to their use in cell ablation, including gene-directed enzyme-prodrug therapy (GPEPT) and antibody-directed enzymeprodrug therapy (ADEPT), in conjunction with nitroreductase enzymes.