Abstract: The present invention provides novel compounds and pharmaceutical compositions for the prevention and/or treatment of cancer and precancerous conditions thereof, for the treatment of pain and fever, for the treatment of skin disorders, and for treating and/or preventing inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention also have analgesic properties and anti-platelet properties. The compounds of the invention may be provided to animals, including mammals and humans, by administering a suitable pharmaceutical dose in a suitable pharmaceutical dosage form. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. The compounds of the invention comprise a biologically active moiety or portion (A) that has, or is modified to have at least one carboxyl group.

Abstract: Novel compounds and pharmaceutical compositions thereof administered by the respiratory route for prevention and/or treatment of lung and brain cancer and precancerous conditions thereof.

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: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.

Abstract: This invention concerns isotopically coded or non-isotopically coded affinity-tags for analysis of certain target molecules in complex samples, in particular for mass spectrometric analysis of proteomic samples. The affinity-tags have the following general formula X-SPACER-OPO3H2, wherein X is a functional group or moiety capable of reacting with a functional group of a protein, peptide, DNA, lipid, sugar and/or steroid. These phosphate affinity tags (‘PTAG’) are capable of high but reversible binding to metal-oxides like TiO2. Due to this property, tagged sample fractions can be isolated from non-tagged sample fraction by affinity chromatography. The binding of organophosphate to metal-oxides remains intact during multiple washings of preferably acidic solutions to remove non-specifically bound components. PTAG's are also envisaged wherein X is selected such that it is capable of binding proteins, peptides, nucleic acid molecules, lipids, carbohydrates, steroids and the like.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

Abstract: The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.

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: Embodiments of the invention include linking agents including photo groups and vinyl groups and coatings and devices that incorporate such linking agents, along with related methods. Exemplary methods herein include methods of priming substrates and methods of coating substrates using compounds having the formula R1—X—R2, wherein R1 is a radical comprising a vinyl group, X is a radical comprising from about one to about twenty carbon atoms, and R2 is a radical comprising a photoreactive group. Embodiments herein also include linking agents having the formula R1—X—R2, wherein R1 is a radical comprising a vinyl group, X is a radical comprising from about one to about twenty carbon atoms, and R2 is a radical comprising a photoreactive group. Other embodiments are also included herein.

Abstract: The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants. In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.

Abstract: Compounds of formula wherein the variables are defined in the specification, are used in compositions which stimulate T cell responses.

Abstract: The present invention discloses processes for the preparation of 3-[(1R,2R)-3-(dimethyl-amino)-1-ethyl-2-methyl-propyl]phenol (Tapentadol), salts thereof and related compounds of formula (A), including stereoisomers and pharmaceutically acceptable salts thereof, and to certain intermediates used in such process.

Abstract: Use of long carbon chain quaternary ammonium salt phosphoric acid ester of formula (I) as conditioner for hair.

Abstract: The present invention provides compositions and methods for protecting cells and tissues from damage associated with therapeutic treatments of cancers and other diseases and conditions where reactive oxygen species are produced. The present invention also provides compositions useful as research reagents.

Abstract: The invention relates to a dental restorative material which comprises (a) at least one antimicrobially active compound of Formula (I) [AG]m-R1—Z—SP—Y—R2—[WG]p??(I), or a filler that is surface-modified with at least one compound of Formula (I), (b) at least one radically polymerizable monomer and (c) at least one initiator for the radical polymerization. The invention also relates to a use of such dental restorative material for the preparation of an adhesive, primer, cement, coating material or filling material. The invention also relates to a dental material which comprises at least one compound of Formula (I), as well as a use of a compound of Formula (I) for modifying the surface of a substrate selected from ceramic materials, noble and non-noble metals, hard tooth structure, tooth enamel, dentine, collagen, soft tissue, mucous membrane and leather.

Abstract: Compounds of formula wherein the variable are defined in the specification, are used in compositions which stimulate T cell responses.

Abstract: There are disclosed compound of formula I, in which R1 represents a hydrophobic moiety adapted to occupy the C? channel of human CDId, R2 represents a hydrophobic moiety adapted to occupy the A? channel of human CDId, such that R1 fills at least at least 30% of the occupied volume of the C? channel compared to the volume occupied by the terminal nC14H29 of the sphingosine chain of ?-galactosylceramide when bound to human CDId and R2 fills at least 30% of the occupied volume of the A? channel compared to the volume occupied by the terminal nC25H51 of the acyl chain of ?-galactosylceramide when bound to human CDId R3 represents hydrogen or OH, Ra and Rb each represent hydrogen and in addition, when R3 represents hydrogen, Ra and Rb together may form a single bond, X represents or —CHA(CHOH)nY or —P(=0)(0?)0CH2(CH0H)mY, in which Y represents CHB1B2, n represents an integer from 1 to 4, m represents 0 or 1, A årepresents hydrogen, one of B1 and B2 represents H, OH or phenyl, and the other represents hydrogen or o

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: Disclosed are: a sense-improving agent which comprises, as an active ingredient, a phospholipid or a sphingosine-containing phospholipid and/or a derivative thereof, particularly a sphingomyelin, and which has an effect of improving the dulling of senses at a periphery when ingested orally or directly applied to the skin; and a sense-improving food, beverage, feed or cosmetic comprising the sense-improving agent. The phospholipid to be used may be a chemically synthesized phospholipid or a naturally occurring phospholipid, preferably a phospholipid derived from an edible material such as soybean and egg yolk, particularly preferably a phospholipid derived from milk.

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: 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: A polysiloxane includes a structural unit in which a functional group represented by a general formula of (in the formula, each of R1, R2, and R3 is independently an alkyl group with a carbon number of 1 or more and 6 or less and m is an integer of 2 or more and 6 or less), an ester bond or an amide bond, a spacer, and a silicon atom are bonded sequentially.

Abstract: Use of long carbon chain quaternary ammonium salt phosphoric acid ester of formula (I) as conditioner for hair.

Abstract: The invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1?n?20, R1 is an unbranched or branched alkyl group having 1 to 20 carbon atoms, and R2 is hydrogen or —CH2—O—R3 group, wherein R3 has the same meaning as R1. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.

Abstract: Perfluoropolyether amide-linked phosphonates and derivatives thereof are provided. Compositions containing perfluoropolyether amide-linked phosphonates or derivatives thereof, perfluoropolyether amide-linked phosphates or derivatives thereof, or combinations thereof are also provided. Additionally, articles, methods of making articles, and methods of reducing contaminant adhesion to a substrate are described.

Abstract: Polymerizable dental material, characterized in that it contains at least one (meth)acrylamide phosphate of the following general formula (I): in which R1 is H or CH3; R2 is H or a C1-C4 alkyl radical or forms together with the nitrogen atom to which it is bonded and one or more atoms which belong to R3 or R3? a heterocyclic ring; R3, R3? independently of each other are a linear or branched aliphatic C1-C50 radical with a valency of m+n or p+n, an aromatic C6-C18 radical with a valency of m+n or p+n, or a cycloaliphatic, araliphatic or heterocyclic C3-C18 radical with a valency of m+n or p+n, wherein the carbon chains of the radical or radicals can be interrupted by O, S, CONR4, OCONH, or form together with one or more atoms which belong to R2 and the nitrogen atom, to which the R2 is bonded a heterocyclic ring, R3? being H if p=0, and R4 being H, C1-C10 alkyl, C6-C12 aryl, C6-C10 aralkyl or a bicyclic C4-C12 radical; n is 1, 2, 3 or 4 if p=0, and is 1 or 2 if p?0; m is 1, 2, 3 or 4; p is 0, 1, 2, 3 or 4;

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 invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1?n?20, R1 is an unbranched or branched alkyl group having 1 to 20 carbon atoms, and R2 is hydrogen or —CH2—O—R3 group, wherein R3 has the same meaning as R1. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.

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

Abstract: The 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 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 compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.

Abstract: The present invention relates to a production method of a compound represented by the formula (3), which includes reacting a compound represented by the formula (2) with a diphenylmethyl halide compound represented by the formula (1) in the presence of alkali metal alkoxide. According to the method of the present invention, compound (3) can be produced at a high purity and in a high yield. wherein each symbol is as defined in the specification, *1 and *2 each show an asymmetric carbon atom, and the configuration of the asymmetric carbon atom of *1 and *2 is (S,S) or (R,R).

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: A material contains at least a polymerizable N,O-functionalized acrylic acid hydroxyamide of the Formula (I) in which A is an n+m-valent linear or branched aliphatic C1 to C50 radical, in which the carbon chain can be interrupted by O, S, —CO—O—, CO—NH, O—CO—NH or NH—CO—NH, an n+m-valent aromatic C6 to C18 radical or an n+m-valent cycloaliphatic or heterocyclic C3 to C18 radical, wherein the radicals can carry one or more substituents, Y is not present, or is O, S, an ester, amide or urethane group, R1 is hydrogen, an aliphatic C1 to C20 alkyl or C3 to C8 cycloalkyl radical which can carry one or more substituents, R2 is H or a C1 to C10 alkyl radical, R3 is not present or is a C1 to C16 alkylene radical which can be interrupted by O, HG is not present, is —COOH, —P?O(OH)2; —P?O(OH)(OR4); —O—P?O(OH)2, —SO2OH or —O—P?O(OH)(OR4), R4 is a C1 to C15 alkyl radical, phenyl or benzyl radical and n is a number from 1 to 5 and m a number from 0 to 3.

Abstract: The present invention relates to an glucose uptake modulator, a pharmaceutical composition comprising the glucose uptake modulator, and a method of treating a diabetes or diabetic complications in a mammal in need thereof, which comprises administering to said mammal an effecting amount of a glucose uptake modulator.

Abstract: Aspects of the present invention include methods of synthesizing phosphocholine analogues and the phosphocholine conjugates formed therefrom and their use in preventing infections caused by microorganisms.

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: 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 phosphate esters of florfenicol (prodrugs) and florfenicol analogs having superior water solubility that are hydrolyzed to florfenicol or the respective florfenicol analog in vivo, upon administration to an animal.

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: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thixophosphpnate of formula (I). Out of the phosphonates of formula (I), some are known and others are new. The novel compounds constitute another aspect of the invention.

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 invention is directed to compounds of formula (I) wherein R1 alkyl, alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; and the physiologically safe salts, esters, optically active forms, racemates and derivatives thereof which can be metabolized in vivo to yield compounds of general formula (I), methods of preparing same, and drugs containing said compounds, for treating bone metabolic disorders.

Abstract: The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, and treating a wound.

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

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

Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-Dmyo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor 5 agents which effectively inhibit the growth of mammalian cells.

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