Abstract: There is provided a prodrug of a pharmaceutically active agent, such prodrug comprising a beta-keto carboxylic acid, a beta-keto carboxylic acid salt or a beta-keto carboxylic acid ester functional group, a pharmaceutical composition comprising the prodrug, and to the use of the prodrug or composition for treatment of a mammalian subject suffering from a condition which can be cured or alleviated by administration of the pharmaceutically active agent. There is further provided a method of inhibiting decarboxylation of a compound comprising a beta-keto carboxylic acid or a salt thereof with a monovalent cation, characterized in that a dry salt of the beta-keto carboxylic acid with a divalent or polyvalent cation is prepared.

Abstract: The invention pertains to novel oligofunctional photoinitiators of the formula (1) or (1A). R1 and R2 are methyl or together are —(CH2)5—; and n is 2 or 3, and the solvent in (1A) is water or an organic solvent; and their use in photopolymerizable compositions, in particular inks.

Abstract: A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.

Abstract: A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.

Abstract: Disclosed are a serious of 2?,5?-dimethoxychalcone derivatives for treating cancer, wherein 2,5-dimethoxyacetophenone and methyl 4-formylbenzoate are condensed to form 4-carboxyl-2?,5?-dimethoxychalcone (compound 1), which is further reacted with alkyl halides or amines to synthesize the chalcone derivatives of compounds 2-17. In addition, 2,5-dimethoxyacetophenone is reacted with 5-formyl-2-thiophenecarboxylic acid to form compound 18 (3-(3-thiophene)carboxyl-1-(2,5-dimethoxyphenyl)prop-2-en-1-one). The synthesized 2?,5?-dimethoxychalcone derivatives can be acted as microtubule-targeted tubulin-polymerizing agents.

Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.

Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.

Abstract: A polymerizable photoinitiator is represented by Formula (I): wherein R1, R2 and R3 are independently selected from the group consisting of a hydrogen, an optionally substituted alkyl group and an optionally substituted aryl group or R1 and R3 represent the necessary atoms to form a five to eight membered ring; p, w, y and z are all integers with y representing a value 1 to 6; p representing the sum of w and z; p representing a value of 1 to 6; w=1 to (p?z) and z=0 to (p?w); L represents an optionally substituted (p+y)-valent linking group comprising 1 to 14 carbon atoms; A represents a radically polymerizable group selected from the group consisting of an acrylate group, a methacrylate group, a styrene group, an acryl amide group, a methacryl amide group, a maleate group, a fumarate group, an itaconate group, a vinyl ether group, an allyl ether group, an allyl ester group and a vinyl ester group; and X represents a photoinitiating moiety including at least one group capable of initiating a free radical p

Abstract: The compound 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobutanoic acid (DPA) is synthesized from 1-[3-(2,6-Dimethylbenzyloxy)-phenyl]-ethanone (DPE) via the intermediate 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobulanoic acid ethyl ester (DPAE).

Abstract: Therapeutic compounds, methods, and compositions are disclosed herein for treating glaucoma and baldness in mammals. The specific compounds are described herein and are modified prostaglandin derivates.

Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.

Abstract: Disclosed are tetrakis(ether-substituted formylphenyl) expressed by General Formula (1), as well as polynuclear polyphenol derived from such tetrakis(ether-substituted formylphenyl): (In the formula, R1 represents an alkyl group with 1 to 8 carbon atoms or alkoxyl group with 1 to 8 carbon atoms, or aromatic hydrocarbon group or saturated hydrocarbon group with 1 to 8 carbon atoms having an aromatic hydrocarbon group, n represents 0 or an integer of 1 to 3, R2 represents a divalent monocyclic or fused-ring aromatic hydrocarbon group with 6 to 15 carbon atoms or divalent aliphatic hydrocarbon group with 1 to 8 carbon atoms that may have a monocyclic or fused-ring aromatic hydrocarbon group with 6 to 15 carbon atoms, R3 represents a hydrogen atom or alkyl group with 1 to 6 carbon atoms, A represents a tetravalent carbon atom group or tetravalent saturated hydrocarbon group with 2 or more carbon atoms, where, if A is a tetravalent saturated hydrocarbon group with 2 or more carbon atoms, the two carbon atoms i

Abstract: Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Abstract: To provide a novel 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative, a method for producing the same, and an agro-horticultural agent and an industrial material protecting agent containing as an active ingredient the abovementioned 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative. To be a 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative represented by Formula (I): wherein X denotes a halogen atom, a C1-C5 alkyl group, a C1-C5 haloalkyl group, a C1-C5 alkoxy group, a C1-C5haloalkoxy group, a phenyl group, a cyano group or a nitro group; n denotes an integer of 0 to 5; when n is not less than 2, Xs may be the same or different; R1, R2, R3, R4 each independently denotes a hydrogen atom, a halogen atom or a C1-C5 alkyl group; and A denotes a nitrogen atom or a methyne group.

Abstract: Fused cyclopentane-4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

Abstract: The invention describes a method for the direct production of molecules with a minimum molecular weight of 78 g/mol by the breakdown of lignin, lignin derivatives, lignin fragments, and/or lignin-containing substances or mixtures in the presence of at least one polyoxometallate and preferably in the presence of a radical scavenger in a liquid medium.

Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.

Abstract: Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-16. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.

Abstract: The invention relates to novel compounds of the formula (I) in which X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates 33 and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.

Abstract: A bis(formylphenyl) compound expressed by general formula (1) is manufactured by, for example, using a corresponding bis(hydroxy-formylphenyl) compound as the direct material and causing it to react with a halogenated alkoxycarbonyl hydrocarbon in the presence of a base according to a known phenylether manufacturing method.

Abstract: Isobenzofuran analogs of sclerophytin A are prepared in a highly concise fashion via an aldol-cycloaldol sequence. The analogs exhibit IC50's as low as 1 ?M in growth inhibitory studies against KB3 cells using an MTT assay. Preferred analogs have one of the following structural formulas, where R is hydrogen or a substituted or unsubstituted lower alkyl group and Ar is a substituted or unsubstituted aryl group.

Abstract: A new tris(formylphenyl) of the following general formula and polynuclear phenol derived therefrom:

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Abstract: The present invention relates to a compound represented by formula (I): wherein ring A, ring B and ring D each independently represents a cyclic group which may have a substituent(s); W is a spacer having 1 to 8 atom(s) in its main chain; X is a spacer having 1 to 2 atom(s) in its main chain; Y is a binding bond or a spacer having 1 to 8 atom(s) in its main chain; and Z is an acidic group, or a salt thereof, a solvate thereof or a prodrug thereof. The compound represented by formula (I) has a PPAR ? agonistic action and is useful as a preventive and/or treating agent for diseases where sugar and lipid metabolisms are abnormal (diabetes, hyperlipemia, arteriosclerosis, cardiovascular diseases, obesity and metabolic syndrome or the like), hypertension, circulatory diseases and skin inflammation diseases.

Abstract: The invention provides a method of functionalizing the sidewalls of a plurality of carbon nanotubes with oxygen moieties, the method comprising: exposing a carbon nanotube dispersion to an ozone/oxygen mixture to form a plurality of ozonized carbon nanotubes; and contacting the plurality of ozonized carbon nanotubes with a cleaving agent to form a plurality of sidewall-functionalized carbon nanotubes.

Abstract: The present invention relates to a process for preparing mumbaistatin derivatives (I), where the anthraquinone skeleton is constructed via a Diels-Alder reaction and the central methylene bridge via a transition metal-catalyzed reaction, and to the intermediates used in this process.

Abstract: A new pharmaceutical compound for treating central nervous disorders, the compound comprising a therapeutically effective amount of valproic acid or pharmaceutically acceptable derivative thereof covalently bonded to myo-inositol. The invention also provides a composition, method for treating a patient and a method for obtaining the compound.

Abstract: A lapping composition is presented, wherein that lapping composition is formed by mixing a solvent, a base, and a phenolic compound having structure I: wherein R1 is selected from the group consisting of —O?Mx+ wherein x is selected from the group consisting of 1, 2, and 3, —O—R3 wherein R3 is selected from the group consisting of alkyl, allyl, and phenyl, —N(R3R4) wherein R4 is selected from the group consisting of —H, alkyl, allyl, and phenyl, and —S—R3; and wherein R2 is selected from the group consisting of —O?Mx+ wherein x is selected from the group consisting of 1, 2, and 3, —O—R3 wherein R3 is selected from the group consisting of alkyl, allyl, and phenyl, —N(R3R4) wherein R4 is selected from the group consisting of —H, alkyl, allyl, and phenyl, and —S—R3.

Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.

Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).

Abstract: A novel tris(formylphenyl) according to the following general formula and polynuclear phenol derived therefrom, which are useful as a material for heat resistant materials, material for photosensitive resist compositions, epoxy resin material or hardener, developer or anti-fade agent for thermosensitive recording materials, or sterilizer, fungicide, antioxidant, etc: In the formula, Y represents a hydrogen atom or —R2COOR3 group, R2 represents a monocyclic or condensed cyclic aromatic hydrocarbon group with a carbon atom number of 6 to 15 or an aliphatic hydrocarbon group with a carbon atom number of 1 to 8 that may have in its main chain a monocyclic or condensed cyclic aromatic hydrocarbon group with a carbon atom number of 6 to 15, and R3 represents a hydrogen atom or alkyl group with a carbon atom number of 1 to 6. R1s may be the same or different and respectively represent a hydrogen atom, alkyl group with a carbon atom number of 1 to 8 or alkoxyl group with a carbon atom number of 1 to 8.

Abstract: The present invention relates to novel derivatives of glycyrrhetinic acid, compositions comprising said derivatives and their use in the treatment of conditions or diseases that benefit from an upregulation of PPAR&ggr; and/or a downregulation of the expression or activity of one or more specificity (Sp) proteins, such as cancer, diabetes and Huntington's disease.

Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8): wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.

Abstract: The present invention has an object to provide a fluorine-containing compound which can be used for applications such as additives making a transparent resin material low in a water absorbing ratio and high in water repellency without deteriorating of various properties such as transparency which the transparent resin material has, a fluorine-containing ester compound which is superior in properties such as heat resistance and low moisture(water) absorption property and can be suitably used in various fields such as a material for electronic information, a material for precision instruments and an optical material, a fluorine-containing aryl ester polymer, methods of producing the same.

Abstract: The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.

Abstract: Archiral (2-hydroxy-3-oxo-cyclopent-1-enyl) acetic acid) alkyl, alkylphenyl and phenyl esters, and a simple and efficient method for the synthesis of both enantiomers of homocitric acid gamma-lactone and the corresponding salts from these esters are described. The method is based on asymmetric oxidation of esters, and the steps of basic and acidic hydrolysis and final acidic lactonization of the homocitric acid into homocitric acid gamma-lactone. The homocitric acid salts are obtained after basic treatment of homocitric acid gamma-lactone. The esters, conditions and reagents used in chemical conversion and separating products are important constituents affording efficient and simple method for production of homocitric acid gamma-lactone and homocitric acid salts.

Abstract: The present invention relates to a process for preparing mumbaistatin derivatives (I), where the anthraquinone skeleton is constructed via a Diels-Alder reaction and the central methylene bridge via a transition metal-catalyzed reaction, and to the intermediates used in this process.

Abstract: The invention provides enzymatic reduction processes for the preparation of 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, particularly, (S)-methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, a key intermediate in the synthesis of Sitagliptin, and the (S)- and (R)-enantiomers of methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate in high enantiomeric purity.

Abstract: The invention provides polyanhydrides that degrade in less than 60 hours following topical administration to deliver biologically active compounds.

Abstract: The present invention provides an industrial method for preparing aminoalcohol derivatives (I) having a biphenyl group, biphenyloxyacetaldehyde derivatives which are used therefore, preparing methods thereof, and intermediates used for the preparing method. The present invention also provides a preparing method including processes for preparing a 3-substituted biphenylcarboxylic acid derivative represented by the following general formula: by allowing a 3-fluorobiphenylcarboxylic acid derivative prepared from a 3-fluorobiphenylcarbonitrile derivative which can be prepared by allowing a 4-halophenol derivative to react with a 2-fluorobenzonitrile derivative which is substituted by a leaving group at 4-position to react with an organometallic reagent.

Abstract: The present invention provides a production intermediate for compound (A-1) and a method for producing the intermediate at high yield and high optical yield. The present invention provides a method for producing compound (3) characterized in that compound (1) is reacted with compound (2) in the presence of a base. (wherein R represents a C1 to C6 alkyl group or a C7 to C8 aralkyl group).

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has ?3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus.

Abstract: Disclosed is a new process and intermediates for preparing benzazepines of Formula (I): wherein R1 and R2 are as defined herein.

Abstract: A process for preparing optically active nitro compounds and cyano compounds using a metal complex, which is obtained by reaction of an optically active nitrogen-containing compound and a periodic table group VIII metal complex, in the asymmetric Michael reaction.