Abstract: Disclosed are reactive cyclic carbonates and ureas of formula (I) or (II), wherein R and X have the meaning indicated in the description. Said carbonates and ureas allow functional groups to be specifically introduced into biomolecules, polymers, and surfaces in mild conditions.

Abstract: A process for the production of cyclic carbonates comprising contacting an epoxide with carbon dioxide in the presence of a dimeric aluminium(salen) catalyst, and a co-catalyst capable of supplying Y?, where Y is selected from Cl, Br and I, where the dimeric aluminium(salen) catalyst is of formula I:

Abstract: Polycyclic aromatic compounds of formula (I) having at least two conjugated aromatic rings at least one of which has a substituent comprising a cyclic carbonate group can be used as sensitisers for cationic photoinitiators, especially iodonium compounds, and may also function as monomers in cationically initiated radiation curable compositions, especially coating compositions, such as printing inks and varnishes.

Abstract: A process for the preparation of an alkylene carbonate, said process comprising contacting the corresponding alkylene oxide with carbon dioxide in the presence of water and in the presence of a catalytic composition comprising an organic base neutralized with a hydrogen halide, wherein the organic base comprises a carbon-based compound comprising one or more nitrogen atoms with at least one free electron pair and/or one or more phosphorous atoms with at least one free electron pair and wherein the organic base has a pKa greater than 8.

Abstract: Modified stable polyisocyanates are described having at least one isocyanate function modified by a group having cross-linking functionality.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: A secondary battery capable of improving the cycle characteristics is provided. The secondary battery includes a cathode and an anode oppositely arranged with a separator in between, and an electrolytic solution. At least one of the cathode, the anode, the separator, and the electrolytic solution contains a sulfone compound having a carbonate group and a sulfonyl group.

Abstract: The present invention pertains to isocyanate-terminated prepolymers prepared from cyclic alkylene carbonates, the method for preparing the same and the use thereof in preparing polyurethanes, polyureas, polyurethane elastomer, and polyurethane mouldings. The incorporation of cyclic alkylene carbonates into the isocyanate-terminated prepolymers of the present invention improves their liquid stability at low temperatures while maintaining their physical properties.

Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.

Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alk

Abstract: The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.

Abstract: This invention relates to unsubstituted and polymeric leuco colorants for use as consumer product additives to indicate a product function by color change, to make attractive or distinctive visual effects, or to provide latent or delayed color generation. The colorants may be present in a stable, colorless state and may be transformed to an intense colored state upon exposure to certain physical or chemical changes. Alternatively, the colorants may be transformed from one color to another color upon exposure to certain physical or chemical changes. The colored form of the unsubstituted or polymeric leuco colorant may be transient, since the colorant can revert back to its colorless form or its original color after the physical or chemical activation has been removed or changed. Polymeric leuco colorants are typically comprised of at least two components: at least one leuco chromophore component and at least one polymeric component.

Abstract: A process for the preparation of an alkylene carbonate, said process comprising contacting the corresponding alkylene oxide with carbon dioxide in the presence of a metal salt immobilised on a solid support, wherein the metal salt comprises a cation of a metal selected from those in the third period and group 2, the fourth period and groups 2 and 4 to 12, the fifth period and groups 2, 4 to 7, 12 and 14, and the sixth period and groups 2 and 4 to 6 of the periodic table according to IUPAC nomenclature, and an anion selected from anions of inorganic acids and organic acids, and wherein the solid support contains a quaternary ammonium, a quaternary phosphonium, a quaternary arsenonium, a quaternary stibonium, or a ternary sulfonium cation.

Abstract: An alkylene carbonate is produced by the reaction of an alkylene oxide with carbon dioxide in the presence of a phosphonium compound as catalyst in a process in which (a) the alkylene oxide, carbon dioxide and the phosphonium catalyst are continuously introduced into a reaction zone from which a product stream containing alkylene carbonate and catalyst is withdrawn, (b) alkylene carbonate and a mixture of alkylene carbonate and phosphonium catalyst are separated from the product stream, (c) the alkylene carbonate, separated in step (b), is recovered as product, and (d) the mixture of alkylene carbonate and phosphonium catalyst is continuously recycled to the reaction zone. The alkylene carbonate thus produced is suitably reacted with an alkanol to produce an alkane diol and a dialkyl carbonate.

Abstract: The invention relates to a process for the production of glycerol carbonate esters corresponding to formula (I): in which R is hydrogen or an alkyl or alkenyl group containing 1 to 23 carbon atoms, which may be linear or branched, characterized in that a compound corresponding to formula (II): in which Y is a group —O—CO—Z and Z is hydrogen or an alkyl or alkenyl group containing 1 to 3 carbon atoms, which may be linear or branched, is transesterified with dimethyl carbonate or diethyl carbonate and an alkyl ester corresponding to formula (IV): in which R is as defined above and X is an alkyl or alkenyl group containing 1 to 8 carbon atoms, which may be linear or branched, with the proviso that the group R of compound (IV) is different from the group Z of compound (II), in the presence of a transesterification catalyst.

Abstract: The present invention provides an adenine modified solid, ordered, mesoporous, bifunctional, organo-inorganic silica-based catalyst, its method of preparation and also a process for the production of cyclic carbonates of the formula hereinbelow wherein R?H, CH2Cl, CH3, C4H9, C6H11, C6H5.

Abstract: The present invention provides an improved process for the preparation of cyclic carbonates which comprises reacting an olefins or its epoxide with carbon dioxide or a mixture of oxygen-containing compound and carbon dioxide, in the presence of zeolite-based catalyst and a Lewis base co-catalyst, at a minimum pressure of 30 psig and temperature between 40 to 120° C. for 0.5 to 4 hrs., separating the catalyst and recovering the corresponding cyclic carbonate formed by conventional methods.

Abstract: Membrane permeable prodrugs of creatine, pharmaceutical compositions comprising membrane permeable prodrugs of creatine, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine or pharmaceutical compositions thereof are disclosed.

Abstract: Membrane permeable prodrugs of creatine analogs, pharmaceutical compositions comprising membrane permeable prodrugs of creatine analogs, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine analogs or pharmaceutical compositions thereof are disclosed.

Abstract: The present invention provides an adenine modified solid, ordered, mesoporous, bifunctional, organo-inorganic silica-based catalyst, its method of preparation and also a process for the production of cyclic carbonates of the formula hereinbelow wherein R?H, CH2Cl, CH3, C4H9, C6H11, C6H5

Abstract: Disclosed is a process wherein a first olefin selected from certain ?,?-dihydroxyalkenes and 4-(alkenyl)ethylenecarbonates is reacted with a second olefin reactant to produce an olefin metathesis product. When the first olefin reactant is an optically enriched or enantiomerically pure ?,?-dihydroxyalkene, cross metathesis reactions produce products possessing the same optical purity. The ?,?-dihydroxyalkenes and the 4-(alkenyl)ethylene carbonates may be converted to hydrogenated products, and the 4-(alkenyl)ethylenecarbonates may be decarboxylated to provide the corresponding epoxides. The products of the disclosure may be used as monomers for the preparation of specialty polyesters and as intermediates in the manufacture pharmaceuticals and other chemicals.

Abstract: The invention relates to a process for the preparation of compound(s) comprising at least one acrylate or methacrylate group, at least one linear carbonate group and at least one 5-membered cyclic carbonate group. The process comprises (A) a selective ring-opening step and (B) a (meth)acrylation step. The process is environment-friendly and compounds obtained are usable in radiation curable compositions, for example in radiation-curable inks.

Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.

Abstract: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

Abstract: A process for the preparation of 14?-hydroxy-baccatin III-1,14-carbonate useful for the preparation of novel taxane derivatives with antitumor activity.

Abstract: A process for the preparation of 14 beta-hydroxy-1,4-carbonate-deacetylbaccatin III and intermediates useful for the preparation of novel taxan derivatives with antitumor activity are disclosed.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: A method for producing trimethylene carbonate poly(trimethylene carbonate which comprises (a) introducing liquid poly(trimethylene carbonate) and an optional catalyst into a wiped film evaporator reactor under a vacuum about 15 kPa or less, said reactor having walls heated to at least about 230° C. and an internal condenser heated to a temperature above the boiling point of trimethylene carbonate, (b)spreading the poly(trimethylene carbonate) into a thin film and allowing it to flow down the interior surface of the heated walls, (c) depolymerizing the poly(trimethylene carbonate) to form trimethylene carbonate which is driven to the internal condenser and residue poly(trimethylene carbonate) which continues down the reactor, and (d) collecting the trimethylene carbonate in a cooled distillate receiver.

Abstract: Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the ?1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.

Abstract: The present invention provides an alkylene-carbonate synthesis catalyst comprising a compound insoluble to one phase containing alkylene carbonate produced when the alkylene oxide and carbon dioxide are reacted with the catalyst and soluble to the other phase substantially free of alkylene carbonate. The catalyst allows alkylene carbonate to be produced with high yield and selectivity and be readily collected. The catalyst also facilitates repeated or continuous reaction process in a cost-effective manner. The present invention also provides an apparatus for producing alkylene carbonate using the catalyst.

Abstract: A catalytic system comprising of Zinc-substituted polyoxometalate, Na12[WZn3(H2O)2(ZnW9O34)2].48H2O and a Lewis base has been discovered to be efficient for chemical fixation of CO2 with epoxides (I) to form cyclic carbonates of structure II as given below: wherein R is selected from a halogen atom, aliphatic and aromatic group. The reaction was carried out at moderate CO2 pressure of 60 psig and in the temperature range 100-140° C. with very high turn number of more than 40,000, with nearly a quantitative conversion and 95-99% selectivity. The Zinc-substituted polyoxometalate catalyst is easy to separate after the reaction by filtration and reusable for many cycles. The reaction can be carried out without any solvent.

Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.

Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: This invention relates to synthetic excitatory amino acid prodrugs of formula (I) wherein the residues R11, R12 and R13 are as defined in claim 1. The invention further relates to processes for the preparation of the compounds of formula (I), and to pharmaceutical compositions for the treatment of neurological and psychiatric disorders comprising said compounds.

Abstract: A process for the preparation of 14&bgr;-hydroxy-1,4-carbonate-deacetylbaccatin III and intermediates useful for the preparation of novel taxan derivatives with antitumor activity are disclosed.

Abstract: Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2-furyl, 2-thienyl; R1 is t-butoxycarbonyl or benzoyl; R2 is hydroxy; R3 is hydrogen or, together with R2, it forms the residue of a cyclic carbonate of formula: [I] with the proviso that when R3 is hydrogen, R is different from phenyl. Compounds of formula (I) have antitumor activity.

Abstract: A catalytic system comprising of Zinc-substituted polyoxometalate, Na12[WZn3(H2O)2(ZnW9O34)2].

Abstract: An improved aqueous cathodic electrocoating composition having a binder of an epoxy-amine adduct and a blocked polyisocyanate crosslinking agent; wherein the improvement is the use of a hydoxyl-carbonate blocked polyisocyanate crosslinking agent. Electrodeposited finishes are formed that have reduced weight loss when heated to cure.

Abstract: The present invention relates to a process wherein a cyclic carbonate compound bearing an electrophilic group is reacted with a compound containing a nucleophilic group, especially an amine group. Such reactions permit to obtain urethane groups useful in polymer preparation, such as polyurethanes, or other urethane-containing polymers.

Abstract: A fluorosulfonyl group-containing compound having a high polymerization reactivity, a process for its production, a sulfonyl group-containing polymerizable monomer led from the sulfonyl group-containing compound, and a polymer obtainable by polymerizing the sulfonyl group-containing polymerizable monomer, are provided.

Abstract: The invention relates to a process for the preparation of compound(s) comprising at least one acrylate or methacrylate group, at least one linear carbonate group and at least one 5-membered cyclic carbonate group. The process comprises (A) a selective ring-opening step and (B) a (meth)acrylation step. The process is environment-friendly and compounds obtained are usable in radiation curable compositions, for example in radiation-curable inks.

Abstract: Applicant has discovered an in situ method of preparing quaternary ammonium methocarbonate salts and quaternary ammonium alkylcarbonate salts in high yield from tertiary amines, methanol, and at least one of a cyclic carbonate, an aliphatic polyester (such as a polycarbonate), or an ester (such as a carbonate ester), and their subsequent conversion to quaternary ammonium bicarbonates, quaternary ammonium carbonates or both in a one-pot reaction. According to one embodiment of the invention, the method includes reacting an amine and methanol with at least one of a cyclic carbonateand an aliphatic polyester to yield a quaternary ammonium methocarbonate. This method does not produce or require the handling of corrosive quaternary ammonium hydroxides. Another embodiment is a method of preparing quaternary ammonium alkylcarbonate salts by reacting tertiary amines, methanol, and an ester.

Abstract: There is provided a method by which various compounds (1) having a carboxyl group in the molecule have the carboxyl group converted to a (dioxolenon-4-yl)methyl ester at low cost, in a simple way and at high yield.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C2 substituent other than benzoate and/or a C4 substituent other than acetate in which the C2 benzoate substituent and/or the C4 acetate substituent of a derivative of baccatin III or 10-desacetyl baccatin III is/are selectively reduced to the corresponding hydroxy group(s) and converted to R7COO— and/or R8COO—, respectively, wherein R7 and R8 are independently H, C1-C6 alkyl, C2-C6 alkenyl, C2-C8 alkynyl, moncyclic aryl, or monocyclic heteroaryl.

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: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X′, Y′, Z′, n, G′, A′ and B′ are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.