Abstract: Disclosed is a polycyclic ester containing a cyano group and a lactone skeleton, represented by following Formula (1): wherein Ra represents, for example, a hydrogen atom or an alkyl group having one to six carbon atoms which may have a halogen atom; R1s each represent, for example, a halogen atom or an alkyl or haloalkyl group having one to six carbon atoms; “m” is the number of R1s; “n” is the number of cyano groups; and CH2?C(Ra)COO— group may have either of an endo conformation and an exo conformation. Accordingly, there is provided a novel polycyclic ester containing a cyano group and a lactone skeleton which is useful typically as a monomeric component for highly functional polymers. A polymer, for example, derived from this compound is highly soluble in an organic solvent while remaining stable typically to chemicals and exhibits improved hydrolyzability and/or improved solubility in water after hydrolysis.

Abstract: The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.

Abstract: Provided is a method for massive culture of Dinophysis acuminata which is a marine dinoflagellate causing diarrhetic shellfish poisoning, and methods for extracting, isolating and purifying the shellfish toxin pectenotoxin-2 from the cultured Dinophysis acuminata. Particularly, Dinophysis acuminata is cultured massively in massive culture apparatus comprising polycarbonate water bath having the bottom sinking down toward the center of the bottom; acryl tube (E) containing fluorescent lamp laid long in the center of the water bath; air supplying device (B) supplying the air to the sinking center of the bottom of the water bath; and air purifying device containing one or more devices selected from the group consisting of UV lamp (C) and carbon cartridge filter (D) purifying the air supplied by the said air supplying device.

Abstract: Cyclic esters are polymerized in the presence of a catalytic amount of a Group 4 transition metal hydride. The method is capable of producing high molecular weight polyesters with low polydispersities. These high molecular weight polyesters exhibit improved mechanical properties and are useful in a variety of product applications.

Abstract: A process for hydrogenating an organic compound which has at least one carbonyl group, in which the organic compound is brought into contact in the presence of hydrogen with a shaped article which can be produced in a process in which (i) an oxidic material comprising copper oxide, aluminum oxide and at least one of the oxides of lanthanum, tungsten, molybdenum, titanium or zirconium is prepared, (ii) powdered metallic copper, copper flakes, powdered cement, graphite or a mixture thereof is added to the oxidic material, and (iii) the mixture resulting from (ii) is shaped to a shaped article.

Abstract: A method of determining a level of biologically active PON enzyme is provided. The method comprising determining lactonase activity of the PON enzyme, the lactonase activity being indicative of the level of biologically active PON enzyme. Also provided are novel compounds which may be used for measuring a lactonase activity of an enzyme.

Abstract: Heterocycles, e.g., epoxides, are carbonylated at low pressure with high percentage conversion to cyclic, ring expanded products using the catalyst where L is tetrahydrofuran (THF).

Abstract: The present invention relates to a novel process for preparing alkyl polycarboxylates from an aqueous solution of an ammonium salt of the polycarboxylic acid by reactive distillation, and to a process for hydrogenating the alkyl carboxylates prepared in this way.

Abstract: A homogeneous process for the hydrogenation of dicarboxylic acids and/or anhydrides in the presence of a catalyst comprising: (a) ruthenium, rhodium, iron, osmium or palladium; and (b) an organic phosphine; wherein the hydrogenation is carried out in the presence of at least about 1% by weight water and wherein the reaction is carried out at a pressure of from about 500 psig to about 2000 psig and a temperature of from about 200° C. to about 300° C. such that from about 1 mol to about 10 mol of hydrogen are used to strip 1 mole of product from the reactor.

Abstract: Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed.

Abstract: The invention relates to the ether lactone of formula (I) which is characterized by interesting and original odor characteristics, which diffuses extremely well and is suitable for use as a fragrance, for example in cosmetic preparations, technical products or in alcoholic perfumery.

Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract: The invention relates to a process for the recovery of a macrolide in substantial pure form including: a) treating an impure or crude macrolide with water immiscible solvent to form a mixture, b) optionally concentrating the mixture, c) treating with ammonia gas to phase out impurities, d) separating impurities, e) optionally concentrating a phase containing the macrolide, f) loading on silica gel chromatography, optionally reversed phase or pretreated with silver, and eluting the macrolide, g) affording the macrolide in the substantially pure form, h) optional repetition of steps f and g to afford the macrolide in the substantially pure form. The macrolide is preferably tacrolimus, immunomycin or sirolimus.

Abstract: The invention relates to a method for hydrogenation of an organic compound comprising at least one carbonyl group, whereby the organic compound is brought into contact with a moulded body in the presence of hydrogen. Said body may be produced by a method in which (i) an oxidic material is prepared, comprising copper oxide, aluminium oxide, and at least one oxide of lanthanum, tungsten, molybdenum, titanium, or zirconium, followed by (ii) addition of powdered metallic copper, copper platelets, powdered cement, graphite, mixtures or a mixture thereof with graphite to the oxidic material and (iii) moulding the mixture from (ii) to give a moulded body, characterised in that the moulded body is in the form of catalyst tablets or catalyst extrudates with a diameter d and/or height h<2.5 mm, catalyst beads with a diameter d<2.5 mm or catalyst honeycomb with a cell diameter rz<2.5 mm.

Abstract: The present invention is to provide a method by which, in carrying out a liquid-phase oxidation reaction using a catalyst comprising a tungsten species as an essential component, the catalytic activity performance can be improved or maintained and by which the catalyst component tungsten species can be prevented from being leached into liquid reaction mixtures to thereby control decrease in catalytic activity and make it possible to reuse the catalyst. A method of liquid-phase oxidation reaction using a tungsten species, wherein that, in carrying out said method of liquid-phase oxidation reaction using a catalyst comprising a tungsten species as an essential component, said tungsten species is caused to be supported on a porous support and, further, a third element other than the component elements of said porous support and the tungsten element is caused to coexist in said catalyst.

Abstract: Disclosed is a process for purifying a hydroxycarboxylic acid, comprising: a crystallization step of subjecting a hydroxycarboxylic acid aqueous solution to crystallization for purification, a separation step of separating a hydroxycarboxylic acid crystal from a mother liquid, and a washing step of washing the hydroxycarboxylic acid crystal for further purification with a washing liquid, wherein the washing liquid is a hydroxycarboxylic acid aqueous solution. The purified or refined hydroxycarboxylic acid obtained through the above process is suitably used as a starting material for production of a polyhydroxycarboxylic acid. The above process is suitably included in a process for producing a cyclic ester and a process for producing a polyhydroxycarboxylic acid.

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.

Abstract: The present invention relates to dispersants for dispersing a particulate solid for millbases, paints and inks. The present invention provides a composition containing a particulate solid, a polar organic medium and a compound or salts thereof for formula T-(A)m(B)n—X-Z-Q(0-p) wherein T is hydrogen or a polymerisation terminating group; A is the residue of a hydroxy carboxylic acid or lactone thereof; B is the residue of an amino carboxylic acid; X is a direct bond or a divalent group; Z is an acidic or basic group or a moiety which contains an acidic or basic group; Q is an optional residue of an oxide, urea or a dibasic acid or anhydride thereof; m and n are positive integers; and p represents the number of residual amino and/or imino groups in Z.

Abstract: There is provided a cleaning agent comprising a lactone represented by the following formula (1): wherein R1 is an alkylene group having 3 to 6 carbon atoms. The cleaning agent is useful for cleaning an organic electroluminescence material, photosensitive resin, liquid crystal or wax.

Abstract: A flavonoid solubilization agent capable of highly solubilizing flavonoids such as isoflavone, baicalin, rutin and naringin whose solubility is generally low; and a method of effecting the above solubilization. Flavonoids can be solubilized by causing a flavonoid and soybean saponin and/or malonyl isoflavone glycoside to be co-present in an aqueous medium.

Abstract: A dispersant comprising a polyester chain obtainable by polymerising a hydroxy carboxylic acid or lactone thereof such as ?-caprolactone with a cyclic alkylene carbonate such as 5,5-dimethyltrimethylene carbonate. The dispersant may be in the form of a phosphate ester where the polyester chain is reacted with a phosphating agent such as polyphosphoric acid or the polyester chain may be attached to a polyamine or polyimine such as polyethyleneimine.

Abstract: Novel derivatives of prostaglandin compounds of the F-series (PGF), specifically macrocyclic internal 1,15-lactones of fluprostenol and related PGF analogs, such as cloprostenol or latanoprost. The novel analogs can be formulated into ophthalmic solutions and topically applied for the treatment of the increased intraocular pressure caused by glaucoma and the reduction of ocular hypertension.

Abstract: A 5-methylene-1,3-dioxolan-4-one derivative and a monomer and copolymer thereof and a resist composition containing the polymer or copolymer where the 5-methylene-1,3 -dioxolan-4-one derivative is of formula (1): wherein R1 represents a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms, or a linear or branched alkyl group containing 1 to 6 carbon atoms which has a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms as a substituent; R2 represents a hydrogen atom, or a linear or branched alkyl group containing 1 to 6 carbon atoms; or R1 and R2 represent a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms together with the carbon atom to which they are bound, provided that the alkyl group and the bridged cyclic hydrocarbon group may have at least one substituent selected from a group consisting of a linear or branched alkyl group containing 1 to 6 carbon atoms which may be optionally substituted, a hydroxy group, a carboxy group, an acyl group containing 2 to 6 car

Abstract: Alpha-methylenelactone is produced from butyrolactone and valerolactone by the addition of formaldehyde in a supercritical fluid.

Abstract: Provided is a method of purifying a macrolide, especially tacrolimus, that includes loading macrolide onto a bed of sorption resin and elting with a suitable eluent such as a combination of water and tetrahydrofuran.

Abstract: Purification of poly-amino acid-tagged recombinant proteins has been improved by the use of a carboxymethylated aspartate ligand complexed with a third-block transition metal having an oxidation state of 2+ and a coordination number of 6. A method for synthesizing the metal ion-CM-Asp complex is also described. Further, the metal ion-CM-Asp complex can be used for screening protein function.

Abstract: Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length.

Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, Streptomyces, Actinomadura, Micromonospora, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.

Abstract: A method for producing 2-(alkyl)cycloalkenone and a method for producing alkyl(3-oxo-2-alkylcycloalkyl) acetate and 5-alkyl-5-alkanolide which are useful as flavoring materials and physiologically active substances using the same are provided. A method for producing Compound (2) including the steps of: dehydrating Compound (1) using an acid catalyst until the conversion ratio of dehydration reaction reaches 20 to 90% based on Compound (1), thereby obtaining a mixture containing Compound (1) and Compound (3); and isomerizing Compound (3) while dehydrating the remaining Compound (1), and a method for producing Compound (5) or (6) using obtained Compound (2). (wherein n represents 1 or 2, R1 and R2 each represent H, C1-8 alkyl groups and the like and R3 represents C1-3 alkyl groups).

Abstract: The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: in which ring A is a cyclic hydrocarbon or the like; ring B is a heterocyclic ring or the like; each of X and Y is —NR1— (in which R1 is a hydrocarbon or the like); D is a C1-3 alkylene group or the like; E is —NH— or the like; G is a bond or the like; and Ar is an aryl or the like; D may be taken together with a constituent atom of the ring B to form a ring, and R4 may be taken together with a constituent atom of the ring B to form a ring.

Abstract: Catalysts useful for oxidation reactions are disclosed. The catalysts comprise a polymer-encapsulated titanium zeolite. The catalysts are easy to prepare and use, they are easy to recover and reuse, and they provide good conversions in a variety of important oxidation processes. The invention includes a process which comprises oxidizing an organic compound in the presence of hydrogen peroxide and a polymer-encapsulated titanium zeolite. In one example, the organic compound is propylene and the reaction product is propylene oxide.

Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.

Abstract: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?V?3 and/or the ?V?5 integrin.

Abstract: A method for separating a lactone-containing high-molecular weight compound comprising subjecting a mixture of a lactone-containing high-molecular weight compound having, as its side-chain, at least one of a lower alkenyl group and a lower alkoxy group and its analogous compound(s) to either one or both steps in any order of a step (A) for adsorbing the mixture to a nonionic adsorption resin and eluting with an aqueous solvent containing silver ions, and a step (B) for adsorbing the mixture to a basic active alumina and eluting with an organic solvent to separate each of the compounds.

Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.

Abstract: An optically active lactone compound is produced by using a complex in which Pd or Pt is a central metal and a compound having a specified structure is a ligand as a catalyst, and subjecting a cyclic ketone compound to a Baeyer-Villiger oxidation with a specified oxidizer.

Abstract: The present invention relates to a novel compound isolated from Artemisia Sylvatica, expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel compound isolated from Artemisia Sylvatica, a method of isolation, and its use in inhibiting farnesyl transferase activity, which is essential for activating Ras oncogene, and repressing cancer cell growth.

Abstract: (Meth)acrylate compounds having a norbornane, bicyclo[2.2.2]octane, 7-oxanorbornane or cyclohexane ring structure and a &ggr;-butyrolactone ring structure connected together by a suitable linker are novel and useful in forming polymers having high transparency, especially at the exposure wavelength of an excimer laser.

Abstract: The present invention is directed to a process of converting lipstatin to orlistat by catalytic hydrogenation. The present invention further discloses novel crystalline solid orlistat forms, designated form I and form II and methods for their preparation.

Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 o

Abstract: The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or the &agr;v&bgr;5 integrin.

Abstract: (6R)-4,5,6,7-Tetrahydro 3,6-dimethyl-3H-benzo[b]furan-2-one is a compound of use in perfumery and the field of flavorings. The compound can be used to impart a minty, slightly vanilla-scented odor, and its flavor imparts sweetness and roundness to the compositions to which it is added.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I): in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenalkyl, halogeno-alkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenyl-alkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups: in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: A photosensitive monomer including a methylene butyrolactone derivative represented by the following formula: wherein R1 is a hydrogen atom or alkyl group, R2 is an acid-labile group, X is a hydrogen atom, or substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, and Y is a substituted or unsubstitued alkyl group or alicyclic hydrocarbon group having 1 to 20 carbon atoms.

Abstract: Processes are disclosed for the manufacture of lactones, e.g., caprolactone, from hydoxy acids, e.g., 6-hydroxycaproic acid. The reaction is conducted over a suitable catalyst in the presence of water.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups  in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: The invention discloses a method for the production of a macrocyclic lactone represented by a formula (2), which comprises subjecting a hydroxycarboxylic acid ester represented by a formula (1) to intramolecular esterification reaction. In the formulae (1) and (2), m is an integer of from 5 to 10, n is an integer wherein m+n becomes from 11 to 16, X represents —CH2—, —CH═CH—, —O—, —S— or —NH—, and R represents a hydrocarbon group having from (m+n+2) to 40 carbon atoms or a group represented by —(AO)pR1 wherein AO represents an alkyleneoxy group having from 2 to 4 carbon atoms, p is average addition mole number of alkylene oxide and R1 represents a hydrocarbon group having a specified number of carbon atoms so that the total number of carbon atoms of the —(AO)pR1 group becomes from (m+n+2) to 40.