Abstract: The present invention relates to compounds having general formula (I), i.e. poly-alkyl-bis-maltolic molecules and in particular to derivates of [(3-hydroxy-4-pyron-2-yl)methyl]-amine and pharmaceutically acceptable salts thereof, and to the use thereof as anti-neoplastic drugs, in particular, for the preparation of a medicament for the treatment of neoplastic diseases.

Abstract: A method of selecting or determining a candidate compound suitable for use as a phosphate binder is disclosed. The candidate compound includes ferric compounds, ferric compound complexes, and their derivatives, salts, analogs, and metabolites. The effectiveness of the candidate compound as a phosphate binder is evaluated by a method, comprising measuring and correlating reduction of phosphate concentration in solution and reduction of phosphate absorption in cells.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract: Provided herein, inter alia, are novel compounds for the inhibition of HIV integrase. The compounds disclosed herein are useful for methods of treating HIV infection in a subject in need thereof.

Abstract: Novel processes and intermediates are provided according to the general reaction scheme: Formula I, II, III, IV (I), (II), (III), (IV) utilizing a ruthenium catalyst in an oxidative cleavage of the triene 4 whereby an aldehyde may be produced and optionally taken on to a carboxylic acid 5: Formula V (V)

Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.

Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract: The present invention provides compounds of the formula Formula I or a salt thereof: and the uses of such compounds for the treatment of a disease or disorder involving oxidative damage, for preventing UV damage to the skin of a mammal and for preventing or reversing the effects of ageing, or for treating or preventing dry skin.

Abstract: [Object] An object of the present invention is to provide a human sweet taste receptor-acting sweet taste regulating substance to a sweet taste substance by which the advantageous effects such as improvement in a taste, saving of a sweetener, reduction in calorie, low caries etc. can be obtained by applying to various foods and beverages. [Solution] The sweet taste receptor-acting sweet taste regulating substance of the present invention is identified by measurement of a physiological response by a sweet taste substance, using a cultured cell strain which is allowed to express hT1R2 and hT1R3, and a G protein ? subunit, by transferring an expression construct obtained by inserting respective cDNAs encoding the hT1R2 and the hT1R3, and the G protein ? subunit into the same plasmid, into a 293 cell in which an FRT (Flippase Recognition Target) site has been incorporated into one place in a genome DNA.

Abstract: The invention is directed to compounds of Formula (I) or salts thereof. The invention is also directed to use of the compounds of formula (I) in the in vitro preservation of living animal cells. The living cells can be isolated cells, such as stem cells, or groups of cells such as tissue or an organ.

Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.

Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Described herein are novel HDAC modulators, formulations containing them and methods of using them. In some embodiments, the HDAC modulators possess specific stereo chemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.

Abstract: Methods for producing amrubicin and structural analogs thereof. The present invention encompasses synthetic pathways for the production of amrubicin (Formula I) and structural analogs thereof. The synthetic pathways of the present invention preferably employ as a starting material an anthracycline compound having the generic Formula II: Compounds of Formula II may have any combination of the following identities for the indicated moieties: R1, R2, R3, R4, and R8 may be H, OH, or alkoxy; R5 may be H, alkyl, or alkoxycarbonyl; R6 may be H or alkyl; R7 may be OH or alkyl. In certain embodiments, ?-rhodomycinone or daunomycinone may be used as starting materials according to Formula II. The present invention employs a compound of Formula II as part of a semi-synthetic method that combines traditional chemical synthetic steps with biosynthetic steps to produce amrubicin, derivatives thereof, and structural analogs thereof.

Abstract: Disclosed is 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate, which has strong antibacterial activity. The compound is highly safe and useful as an original drug for pharmaceutical preparations. Also disclosed is a method which is useful for producing 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate.

Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.

Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.

Abstract: This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.

Abstract: A method of selecting or determining a candidate compound suitable for use as a phosphate binder is disclosed. The candidate compound includes ferric compounds, ferric compound complexes, and their derivatives, salts, analogs, and metabolites. The effectiveness of the candidate compound as a phosphate binder is evaluated by a method, comprising measuring and correlating reduction of phosphate concentration in solution and reduction of phosphate absorption in cells.

Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.

Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.

Abstract: Analogs of 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-napthalenyl)-1-propenyl]benzoic acid and methods of manufacture and use thereof, such as for use in cancer prevention and treatment.

Abstract: Skin brightening compositions based on esters of 5-hydroxy-2-methyl-4H-pyran-4-one. Also disclosed are methods of making the compositions as well as methods of using the compositions.

Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.

Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.

Abstract: D-pyranosyl-substituted phenyls of general formula I wherein the groups R1 to R5, X, Z and R7a, R7b, R7c are defined as in claim 1, have an inhibiting effect on the sodium-dependent glucose cotransporter SGLT. The present invention also relates to pharmaceutical compositions for the treatment of metabolic disorders.

Abstract: A method of inhibiting or effecting the activity of an integral receptor which comprises contacting an integrin with a compound of formula I, or a pharmaceutically acceptable salt thereof; General Formula I Wherein the ring may be of any configuration; Z is sulphur, oxygen, CH2, NH, NRA or hydrogen, in the case where Z is hydrogen then R1 is not present, RA is selected from the set defined for R1 to R5, X is oxygen or NRA providing that at least one X of General Formula I is NRA, X may also combine independently with one of R1 to R5 to form an azide, R1 to R5 are independently selected from the group comprising H, —(CO)R6 or an alkyl, acyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl substituent of 1 to 20 atoms, which is optionally substituted, and can be branched or linear wherein substituents may optionally be further substituted, wherein R6 is selected from the group comprising an alkyl, acyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl s

Abstract: Therapeutic compositions are provided. The compositions include a single molecule that can display both antioxidant and carbonyl trapping properties. This can effectively reduce inflammation, oxidative stress and carbonyl stress, such as to prevent and/or treat cardiovascular disease and inflammatory diseases in kidney disease patients.

Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.

Abstract: The present invention relates to antifungal compounds having the structural formula: and pharmaceutically acceptable salts, solvates and prodrugs thereof. The present invention further relates to pharmaceutical compositions containing said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof, for use in the treatment of a fungal infection in an animal host.

Abstract: A process has been developed for production of a food flavoring compound maltol which comprises (a) extracting the dried and pulverized leaves of the plants belonging to the genus Abies with an alcohol at 20-40° C. and concentrating the solvent to obtain an alcoholic extract, (b) adsorbing the alcoholic extract with an adsorbent and drying the adsorbed material at a temperature ranging between 20-50° C., (d) partitioning of the adsorbed material between selected solvents consisting of aliphatic hydrocarbon and chlorinated solvent successively, (d) concentrating the chlorinated solvent to a residue and crystallizing it from a suitable organic solvent or mixtures of such solvents to get pure maltol.

Abstract: A process of making arbutin and its derivatives comprises solvolyzing an acylated precursor of arbutin or its derivative in a solution comprising an organic solvent and a base, neutralizing the solution with an acid, and crystillizing the product arbutin or its derivative. The process may be employed on an industrial scale and avoids the use of ion exchange columns. The process has the advantages of not requiring ion exchange columns and peripheral devices, which leads to cost and time savings, due to the elimination of column regeneration steps. Waste water from column regeneration is also eliminated.

Abstract: A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.

Abstract: A method and compound for the treatment of disease involving hyperproliferation of dermis cells is provided. In particular, compounds isolated from the species of plants known as calendula have been found to be beneficial in the treatment of psoriasis. An extract of plant material obtained from calendula officinalis has been found to be advantageous as an active compound in medicaments for use in the treatment of psoriasis.

Abstract: The present invention relates to cyclic ketones represented by the following formula and to drugs in which an effective component is such a cyclic ketone or a pharmacologically acceptable salt thereof. The cyclic ketones of the present invention encourage the production of blood platelets, leukocytes and erythrocytes, and can be employed in the prevention or treatment of cytopaenia brought about by cancer chemotherapy, radiotherapy or drug therapy, or by immunological abnormality, anaemia and the like.

Abstract: PURPOSE: To produce a novel antibiotic substance zofimarin having antimicrobial activity against fungi and obtain an antimicrobial agent containing the antibiotic substance zofimarin as an active constituent, by cultivating a microorganism, belonging to the genus Zopfiella and capable of producing the zofimarin.CONSTITUTION: An ascomycete belonging to the genus Zopfiella, e.g. Zopfiella marina; is cultivated. The cultivation is carried out according to general fungi, but artifical seawater is used in place of tap water in a liquid culture medium. A carbon source, nitrogen source, inorganic salt, etc., are added, and a defoaming agent is suitably used to carry out the cultivation at 20-30.degree. C. by the spinner culture method with aeration. After completing the cultivation, microbial cells are removed, and the resultant product in the supernatant liquid or filtrate is extracted and purified to afford the aimed zofimarin.

Abstract: Compounds of the formula (I) ##STR1## and pharmaceutically acceptable salts or metabolically labile derivatives thereof, processes for their preparation, their use as antifungal agents and intermediates for use in their preparation.

Abstract: Sordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and a blocking group, characterized by the presence of a covalent bond which is cleaved at pH values below 7.0. The prodrug may be used in a technique for treating a condition or disease in a mammal related to elevated hydrogen ion concentrations, whereby on administering it to a mammal having such a condition or disease, the pharmacologically active compound is activated selectively within tissues having such elevated hydrogen ion concentrations.

Abstract: 4-Cyano-4-deformylsordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Abstract: A process for recovering .gamma.-pyrones such as maltol and/or ethyl maltol from solutions containing other substances involves an elution chromatographic treatment using a stationary phase that separates the .gamma.-pyrones from the other substances by means of ion exclusion, size exclusion, hydrophobic partitioning, and/or chelation. In one embodiment, a cation exchange resin such as sulfonated divinyl benzene-cross-linked polystyrene is employed, and the .gamma.-pyrones obtained can be further purified by crystallization from water and/or other means.

Abstract: Maltol and ethyl maltol can be produced from a haloenone intermediate by reacting the intermediate with acid in a reaction medium comprising an aprotic solvent.

Abstract: A process for the preparation of compounds having the formula ##STR1## wherein: R is a methoxy or thiomethyl group;R.sub.1 is a .beta.-D-glycopyranosyloxy or6-deoxygalactopyranosyloxy residue; andR.sub.2 is a C.sub.1 -C.sub.7 alkyl groupwhich process comprises reacting a protected material selected from the group consisting of derivatives of 1-fluoroglucose and 1-fluorofucose with a compound having the formula ##STR2## wherein R and R.sub.2 are as defined above to form a crude reaction product containing at least one compound of formula (I).

Abstract: A propiophenone derivative the formula ?I!: ##STR1## wherein R' is a lower alkanoyl group and R" is a hydrogen atom, or R' is a hydrogen atom and R" is a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Pure maltol is recovered from a mixture containing maltol by extraction into an aqueous solution, optionally in the presence of a substantially water-immiscible solvent in which the maltol in the mixture is substantially insoluble.

Abstract: Disclosed herein is a process where maltol is extracted from a source material containing maltol by employing an aqueous extraction process wherein reverse osmosis is utilized to concentrate an aqueous extract of maltol. The maltol in the concentrated aqueous extract is adsorbed on a bed containing an adsorbent material and then desorbed using a hydrophilic solvent and separated.

Abstract: There is provided a lubricant which is produced by dissolving a sorbitan ester compound in a solvent such as hexane or toluene. In the sorbitan ester compound, at least one of hydroxyl groups of 1,5-sorbitan is linked by ester linkage to a perfluoro polyether having a terminal carboxyl group and at least an other hydroxyl group is linked by ester linkage to a hydrocarbon having a terminal carboxyl group. There is also provided a thin magnetic metal film type magnetic recording medium or a coated magnetic recording medium in which the above lubricant is held on the surface of a magnetic layer. The lubricant exhibits superior lubricating effects under all conditions and is capable of maintaining the lubricating effects for prolonged time. Consequently, the magnetic recording medium which has the lubricant held on the magnetic layer exhibits superior running durability and resistance against abrasion.