Abstract: The present invention relates to a process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans.

Abstract: The present invention relates to a process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans by reacting 3-methylbut-3-en-1-ol (isoprenol) with the corresponding alkenealdehydes in the presence of a strongly acidic ion exchanger with subsequent hydrogenation. Specifically, the present invention relates to a corresponding process for the preparation of 2-isobutyl-4-hydroxy-4-methyltetrahydropyran by reacting isoprenol with prenal, with subsequent hydrogenation.

Abstract: The present invention relates to a process for the integrated preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans and of 2-substituted 4-methyltetrahydropyrans.

Abstract: A compound of formula I, wherein the groups R1, R2, R3, X, m, and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Abstract: Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.

Abstract: A fluorinated monomer of cyclic acetal structure has formula (1) wherein R is a C1-C20 alkyl group which may be substituted with halogen or separated by oxygen or carbonyl, and Z is a divalent organic group which forms a ring with alkylenoxy and contains a polymerizable unsaturated group. A polymer derived from the fluorinated monomer may be endowed with appropriate water repellency, water sliding property, lipophilicity, acid lability and hydrolyzability and is useful in formulating a protective coating composition and a resist composition.

Abstract: The present invention relates to a process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans by reacting 3-methylbut-3-en-1-ol (isoprenol) with the corresponding alkenealdehydes in the presence of a strongly acidic ion exchanger with subsequent hydrogenation. Specifically, the present invention relates to a corresponding process for the preparation of 2-isobutyl-4-hydroxy-4-methyltetrahydropyran by reacting isoprenol with prenal, with subsequent hydrogenation.

Abstract: Process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans of the formula (I) where the radical R1 is a straight-chain or branched alkyl or alkenyl radical having 1 to 12 carbon atoms, an optionally alkyl-substituted cycloalkyl radical having in total 3 to 12 carbon atoms or an optionally alkyl- and/or alkoxy-substituted aryl radical having in total 6 to 12 carbon atoms, comprising the reaction of 3-methylbut-3-en-1-ol of the formula (II) with an aldehyde of the formula (III) R1—CHO??(III), where the radical R1 has the same meaning as in formula (I) and where the reaction is carried out in the presence of water and in the presence of a strongly acidic cation exchanger, and then the isolation and/or the distillative separation is carried out in a dividing wall column or in an interconnection of (at least) two distillation columns in the form of a thermal coupling and one or more side take-off points at an absolute operating pressure of up to 500 mbar.

Abstract: The present invention relates to a process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans by reacting 3-methylbut-3-en-1-ol(isoprenol) with the corresponding alkenealdehydes in the presence of a strongly acidic ion exchanger with subsequent hydrogenation. Specifically, the present invention relates to a corresponding process for the preparation of 2-isobutyl-4-hydroxy-4-methyltetrahydropyran by reacting isoprenol with prenal, with subsequent hydrogenation.

Abstract: The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.

Abstract: The present invention relates to a process for the preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyranols by reacting 3-methylbut-3-en-1-ol (isoprenol) with the corresponding aldehydes in the presence of a strongly acidic cation exchanger. Specifically, the present invention relates to a corresponding process for the preparation of 2-isobutyl-4-hydroxy-4-methyltetrahydropyran by reacting isoprenol with isovaleraldehyde.

Abstract: Provided herein are pure and isolated natural products and analogs thereof of Formula (I), (II), (III), and (IV), pharmaceutical compositions thereof, and methods of use, for example, for treating a bacterial infection. Further provided are methods useful in identifying an inhibitor of bacterial sugar fermentation in a bacterial strain, such as a compound (inhibitor) of Formula (I), (II), (III), or (IV): or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are processes for preparing 1,6-hexanediol and synthetic intermediates useful in the production of 1,6-hexanediol from renewable biosources. In one embodiment, a process comprises contacting levoglucosenone with hydrogen in the presence of a first hydrogenation catalyst at a first temperature to form product mixture (I); and heating product mixture (I) in the presence of hydrogen and a second hydrogenation catalyst at a second temperature to form product mixture (II) which comprises 1,6-hexanediol.

Abstract: The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.

Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: The present invention relates to alkyl-substituted tetrahydropyrans, mixtures containing these alkyl-substituted tetrahydropyrans, their respective use and corresponding flavored products.

Abstract: The present invention is directed to a novel method for preparing a synthetic intermediate for treprostinil via a stereoselective alkyne addition reaction. Also described are methods of preparing treprostinil comprising the alkyne addition reaction described herein as well as novel intermediates useful for synthesis prostacyclin derivatives, such as treprostinil.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: Pyranone, thiopyranone and cyclohexenedione compounds of formula (I), which are suitable for use as herbicides.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with tetradentate ligands having at least one amino or imino coordinating group and at least one phosphino coordinating group in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.

Abstract: The present invention related to a determination of a stereochemistry, a synthesis and dauer effect of 6R-(3,6-dideoxy-L-arabino-hexopyranosyloxy) heptanoic acid as a pheromone isolated from the Caenorhabditis elegance related to suppression of aging and stress. It becomes possible to develop medical substances using the pheromone relating to aging, stress, metabolism, signal transfer system in vivo, and anticancer, obesity and a suppressing agent for aging and stress.

Abstract: Aspects of the present invention are directed to novel methods for making discrete polyethylene compounds selectively and specifically to a predetermined number of ethylene oxide units. Methods which can be used to build up larger dPEG compounds (a) containing a wider range of utility to make useful homo- and heterofunctional and branched species, and (b) under reaction configurations and conditions that are milder, more efficient, more diverse in terms of incorporating useful functionality, more controllable, and more versatile then any conventional method reported in the art to date. In addition, the embodiments of the invention allow for processes that allow for significantly improving the ability to purify the intermediates or final product mixtures, making these methods useful for commerial manufacturing dPEGs. Protecting groups and functional groups can be designed to make purification at large scale a practical reality.

Abstract: A process of preparing a compound of formula (I) wherein R represents a linear or branched C5 alkyl group, as well as the use of such compounds in a fragrant and/or flavouring composition.

Abstract: Pyran derivatives of general formula (I) wherein Y is a 5-, 6- or 7-membered ring, preferably a 5-membered ring, methyl or ethyl mono- or polysubstituted, and optionally unsaturated, and R1, R2, R3, R4 are, each independently, a hydrogen atom or a linear or branched C1-5 alkyl or C2-5 alkenyl group, and X is present or absent; when X is present, R5, R6, R7, R8, R9 are all present, and X is a hydrogen atom or an OZ group, wherein Z is a hydrogen atom or a R10 group or a C(O)R10 group; when X is absent, a double bond involving the carbon atom at the 4 position is present and R7, R8 and R9 are present, and one of R5 or R6 is present and the other one is absent, or R5, R6, and R7 are present, and one of R8 or R9 is present and the other one is absent, or R7 is a ?C(R11)(R12) group and R5, R6, R8, R9 are present; and when they are present, each of R5-R12 group is, independently, a hydrogen atom or a linear or branched C1-5 alkyl or C2-5 alkenyl group; and use of at least one pyran derivative of formula (I)

Abstract: The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with tetradentate ligands having at least one amino or imino coordinating group and at least one phosphino coordinating group in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.

Abstract: Silicon compounds having fluorinated hemiacetal structure are provided. Silicone resins having the same structure have an appropriate acidity to enable formation of a finer pattern by minimizing the pattern collapse by swelling, exhibit improved resistance to the etching used in the pattern transfer to an organic film, and are thus suited for use in resist compositions for the bilayer process.

Abstract: Enantiopure substituted 4-deoxypentenosides (4-DPs) and related dihydropyrans (DHPs) are prepared from common carbohydrates via a novel process. The 4-DPs and related DHPs are amenable to a broad range of stereoselective transformations and are used as synthetic intermediates to prepare a variety of enantiopure tetrahydropyrans (THPs), including rare or exotic sugars and other complex THPs of commercial or medicinal value. In one embodiment of the instant invention, 4-DPs are converted to L-sugars in a novel process that offers distinct advantages over known synthetic methods.

Abstract: The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae and pharmaceutically acceptable salts, amides, esters, and ethers thereof, wherein: Ar1, Ralk, —ORO, and -Q are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds. The compounds inhibit osteoclast survival, formation, and/or activity, and inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, and are useful in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, aseptic loosening of prosthetic implants, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.

Abstract: The present invention relates to 2-(4-sulphonylphenyl)pyran-4-one derivatives of general formula processes for their preparation, pharmaceutical compositions containing them, and their medical uses.

Abstract: The invention relates to a new synthetic process for the production of key intermediates useful in the synthesis of epothilones or epothilone derivatives, to certain compounds used to produce these key intermediates and to a process to produce said compounds.

Abstract: The present invention relates to a process for preparing tetrahydropyran-4-ol which comprises the steps of (A) a cyclization step of preparing tetrahydropyranyl-4-formate represented by the formula (1): by reacting 3-buten-1-ol, a formaldehyde compound and formic acid, and (B) then, a solvolysis step of subjecting the tetrahydropyranyl-4-formate to solvolysis to obtain tetrahydropyran-4-ol represented by the formula (2): and an intermediate and a process for preparing the same.

Abstract: Disclosed herein is an acrylic compound that can be polymerized by itself or with at least one other ethylenically unsaturated monomer to provide a polymer. The polymer may be used, for example, within a sub-200 nm photoresist composition. Also disclosed is a method to make the acrylic compound of the present invention from the raw material trifluoroacetone.

Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.

Abstract: A method for producing pyrone derivatives of the general formula (I), wherein X1 is halomethyl, whereby an acetoacetic acid derivative of the general formula (II), wherein X1 has the aforementioned meaning and X2 is chlorine or bromine, is treated with a Lewis acid and is subsequently converted into the desired product by means of water.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether 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: Novel cyclic ether vitamin D3 compounds having a cyclic ether side chain are disclosed. These compounds were first identified as metabolites of 3-epi vitamin D3 produced via a tissue-specific metabolic pathway which catalyzes the formation of a cyclic ether structure. Also disclosed are 1&agr;(OH) 3-epi vitamin D3 compounds, which are produced via the epimerization of a 3-&bgr;-hydroxyl group of 1&agr;(OH) vitamin D3 precursor in vivo. The vitamin D3 compounds of the present invention can be used as substitutes for natural and synthetic vitamin D3 compounds.

Abstract: Compounds of formula (I) or their salts or esters: [wherein R1 is alkyl or haloalkyl; R2 and R3 each represents hydrogen or aliphatic acyl; X is hydroxy, halogen, alkoxy, or a group of formula RaO—, where Ra is aliphatic acyl; Y is a group of formula RbRcN— or RbRcN—O—, where Rb and Rc each is hydrogen or alkyl; and Z is oxygen or sulfur] have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.

Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.

Abstract: This invention relates to novel processes for making (2S, 3S, 5S) oxetanone derivative lipase inhibitor compounds and intermediates therefor, which processes for producing such derivatives that are useful as lipase inhibitors are capable of being scaled to commercial quantities. Further the invention relates to processes for producing salts and for producing pharmaceutical compositions compounds comprising at least one such oxetanone derivative or salt, as well as methods for using such compounds and compositions for inhibiting lipases.

Abstract: A method of producing (S)-3-[2-{(methylsulfonyl)oxy}ethoxy]-4-(triphenylmethoxy)-1-butanol methane sulfonate using 1,3-butadiene and a ketoethanal to form an intermediate racemic mixture. The racemic mixture is resolved to remove one isomer from the reaction product mixture. Following resolution, the following steps are performed: reduce the isomer to an alcohol, react the alcohol with triphenylmethyl chloride, ozonalyze the resulting reaction product, reduce the ozonalyzed product to yield a diol and react the diol with a methane sulfonyl compound to form (S)-3-[2-{(methylsulfonyl)oxy}ethoxy]-4-(triphenylmethoxy)-1-butanol methane sulfonate. Alternatively, the racemic mixture may first be reduced and the resulting racemic alcohol mixture is resolved to isolate one isomer of the alcohol and the remaining process steps are followed.

Abstract: A compound of formula (II), wherein R1 is chloro, fluoro or trifluoromethyl; R2 is hydrogen, chloro, fluoro or trifluoromethyl; and R is hydrogen or a protective group for the hydroxy moiety useful as an intermediate for the synthesis of antimycotic azole compounnds.

Abstract: The invention relates to a process for preparing substituted chroman derivatives of the general formula VII, ##STR1## where X is the group --CN, --COOR.sup.3, --CHO, --CH.sub.2 OR.sup.7 or --CH(OR.sup.8).sub.2,R.sup.2 is a C.sub.1 -C.sub.23 -alkyl, C.sub.2 -C.sub.23 -alkenyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aralkyl radical,R.sup.3 is hydrogen or an optionally substituted C.sub.1 -C.sub.4 -alkyl radical,R.sup.4, R.sup.5, R.sup.6 are, independently of one another, hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.7 is hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.8 is a C.sub.1 -C.sub.4 -alkyl radical, or the two radicals are a C.sub.2 -C.sub.6 -alkylene radical which links the two oxygen atoms to form a cyclic acetal and is optionally branched or may carry one or two carboxyl groups, cyclohexyl or phenyl radicals,and to the novel intermediates of the process.

Abstract: Novel .alpha.-pyrones are described. The .alpha.-pyrones are useful in a method for controlling .alpha.-pyrone responsive states in a mammal. The method includes administering to a mammal a therapeutically effective amount of an .alpha.-pyrone such that control of .alpha.-pyrone responsive states in a mammal occurs. .alpha.-Pyrone responsive states can be associated with undesirable cell proliferation such as bacteria or cancer. Packaged pharmaceuticals and pharmaceutical compositions including the novel .alpha.-pyrones are also described.

Abstract: Triene-containing compounds which mimic the chemical and/or biological activity of the spongistatins are provided, as are methods and intermediates useful in their preparation.

Abstract: The present invention relates to the use of cytokine restraining agents to treat inflammatory bowel disease.

Abstract: Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolinProcess for the manufacture of 6.beta.

Abstract: Compounds of the formula I ##STR1## in which R.sup.1, A and B have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases.