Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1? and/or TNF-?. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.

Abstract: The present invention provides an antiproliferative compound having a structural formula where X and Y independently are oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers or nitriles; R2 and R3 are hydrogen or R4; R4 is methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide or amine; and R5 is alkenyl; where when Y is nitrogen, said nitrogen is substituted with R6, wherein R6 is hydrogen or methyl. Also provided are methods for treating a cell proliferative disease and for inducing apoptosis in a cell comprising administering this compound is also provided.

Abstract: The present invention provides methods and compositions for treating lung cancer by cyclohexenone compounds.

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: [Problem] The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.

Abstract: The invention relates to the use of compounds as new chiral selectors for separating the optical or enantiomeric isomers of a compound, wherein the chiral selector comprises at least one compound of formula (I): and at least one metal ion, for example Cu2+, Ni2+, Zn2+, Cd2+ or Co2+.

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 invention provides a liquid crystal compound that has a large negative dielectric anisotropy (??) and also has at least one of characteristics such as the stability to heat, light or the like, a high clearing point, a suitable refractive index anisotropy (?n), a large negative dielectric anisotropy (??) and an excellent compatibility with other liquid crystal compounds. An excellent effect in which especially the value of the dielectric anisotropy (??) is increased negatively is achieved by use of the compound having two moieties of 1) a tetrahydropyran ring and and thus the effect is utilized.

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 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 present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).

Abstract: The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4?-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4?-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4?-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4?-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.

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: The present invention relates to phenyloxyaniline derivatives, to methods of their production and to uses thereof.

Abstract: A liquid crystal compound is provided that has excellent characteristics, such as a negatively large dielectric anisotropy. A liquid crystal composition containing the compound, and a liquid crystal display device containing the composition are also provided. A compound having the three factors, i.e., (1) a tetrahydropyran ring, (2) —CH2O— or —OCH2— and (3) exhibits excellent characteristics including a negatively large dielectric anisotropy. The use of the compound having the characteristics provides an excellent liquid crystal composition and an excellent liquid crystal display device.

Abstract: Compounds including at least one mesogenic substructure and at least one long flexible segment and methods of synthesizing the same are disclosed. Formulations which include various embodiments of the mesogen containing compounds and their use in articles of manufacture and ophthalmic devices are also disclosed.

Abstract: Liquid crystal compositions comprising compounds including at least one mesogenic substructure and at least one long flexible segment and a compound selected from a photochromic compound, a dichroic compound and a photochromic-dichroic compound and methods of synthesizing the same and their use in articles of manufacture and ophthalmic devices are disclosed.

Abstract: The invention provides a liquid crystal compound having stability to heat, light and so forth, a wide temperature range of a nematic phase, a small viscosity, a suitable optical anisotropy, a suitable elastic constant K33, a suitable and negative dielectric anisotropy, and an excellent compatibility with other liquid crystal compounds. The invention provides a liquid crystal composition containing the compound described above and having stability to heat, light and so forth, a small viscosity, a suitable optical anisotropy, a suitable and negative dielectric anisotropy, a suitable elastic constant K33, a low threshold voltage, a high maximum temperature of a nematic phase, and a low minimum temperature of the nematic phase. The invention also provides a liquid crystal display device having a short response time, a small power consumption, a low driving voltage, and a large contrast, and containing the composition described above which can be used in a large temperature range.

Abstract: The invention provides a liquid crystal compound having stability to heat, light and so forth, a wide temperature range of a nematic phase, a small viscosity, a suitable optical anisotropy, and a suitable elastic constant K33, and further having a suitable and negative dielectric anisotropy and an excellent compatibility with other liquid crystal compounds, and a liquid crystal composition having stability to heat, light and so forth, a low viscosity, a large optical anisotropy, a suitable and negative dielectric anisotropy, and a suitable elastic constant K33, a low threshold voltage, a high maximum temperature (phase-transition temperature on a nematic phase-isotropic phase) of a nematic phase, and a low minimum temperature of the nematic phase. The liquid crystal compound which has a specific structure having fluorine at a lateral position and also having phenylene in which hydrogen on the benzene ring is replaced by fluorine, and a liquid crystal composition containing the compound are prepared.

Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.

Abstract: The compounds of formula I in which R1, R2 and R3 have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.

Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: Methods of performing cycloadditions are described that include (a) combining a first reactant and a second reactant in a hydrogen bonding solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form a cycloadduct. Methods of performing asymmetric catalytic reactions are also described that include (a) combining a first reactant, a second reactant, and a catalytic amount of a chiral hydrogen-bond donor in a solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form an enantiomeric excess of a reaction product. Reaction mixtures corresponding to these methods are also described.

Abstract: The present invention relates to a process for preparing tetrahydropyran-4-one represented by the formula (1): which comprises reacting at least one kind of dihydropyran-4-one and pyran-4-one represented by the formula (2): wherein represents a single bond or a double bond, and hydrogen (a) in the presence of a metal catalyst, in a mixed solvent of an aprotic solvent and an alcohol solvent, or (b) in the presence of an anhydrous metal catalyst in which a hydrated metal catalyst is subjected to dehydration treatment, in a hydrophobic organic solvent.

Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.

Abstract: The present invention provides ?-hydroxy benzeneacetic acid derivatives of the formula as defined in the specification which is a precursor indispensable for synthesis of compounds having two 5-membered lactone rings fused to central cyclohexa-1,4-diene nucleus, and a process of easily preparing the same. According to the preparation process of the present invention, the ?-hydroxy benzeneacetic acid derivative can be readily prepared at high purity and yield without using toxic materials or producing toxic by-products. Some novel compounds, synthesized by using such a ?-hydroxy benzeneacetic acid derivative, have excellent fastness properties, dye fixing rate and leveling property to general synthetic fiber materials such as polyester fibers and their blends with other fibers, especially to micro fibers, and also can be used as a coloring agent for plastic resins, color tonors, color filters, etc.

Abstract: The present invention comprises small molecule inhibitors of cell proliferative conditions, in particular cancer and conditions associated with cancer. For example, associated malignancies include ovarian cancer, cervical cancer, breast cancer, colorectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. Thus, the present invention also comprises pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit cancer and treat, prevent, or inhibit the foregoing diseases.

Abstract: The invention relates to the use of compounds as new chiral selectors for separating the optical or enantiomeric isomers of a compound, wherein the chiral selector comprises at least one compound of formula (I): and at least one metal ion, for example Cu2+, Ni2+, Zn2+, Cd2+ or Co2+.

Abstract: The present invention provides an antiproliferative compound having a structural formula where X and Y independently are oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers or nitriles; R2 and R3 are hydrogen or R4; R4 is methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide or amine; and R1 is alkenyl; where when Y is nitrogen, said nitrogen is substituted with R6, wherein R6 is hydrogen or methyl. Also provided are methods for treating a cell proliferative disease and for inducing apoptosis in a cell comprising administering this compound is also provided.

Abstract: A process for the preparation of glycerol formal, from a paraformaldehyde and crude glycerin in a condensation reaction without the use of a secondary distilling agent for the removal of the water.

Abstract: Compounds including at least one mesogenic substructure and at least one long flexible segment and methods of synthesizing the same are disclosed. Formulations which include various embodiments of the mesogen containing compounds and their use in articles of manufacture and ophthalmic devices are also disclosed.

Abstract: An efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative, is provided, which includes the synthesis of the intermediate compound, a hydroxymethyl-substituted enone. In addition, a method is provided for synthesizing inhibitors, which includes PI?-modified analogues. These analogues selectively bind to a major immunoproteasome catalytic subunit LMP2 and inactivate its proteolytic activity in a method of treating diseases, including myeloma and other cancers, Huntington's disease and Alzheimer's disease.

Abstract: The present invention provides compounds having formula (I) (and pharmaceutically acceptable derivatives thereof): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R14 and n are as defined herein.

Abstract: Compounds including at least one mesogenic substructure and at least one long flexible segment and methods of synthesizing the same are disclosed. Formulations which include various embodiments of the mesogen containing compounds and their use in articles of manufacture and ophthalmic devices are also disclosed.

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: A liquid crystal compound is provided that has excellent characteristics, such as a negatively large dielectric anisotropy. A liquid crystal composition containing the compound, and a liquid crystal display device containing the composition are also provided. A compound having the three factors, i.e., (1) a tetrahydropyran ring, (2) —CH2O— or —OCH2— and (3) exhibits excellent characteristics including a negatively large dielectric anisotropy. The use of the compound having the characteristics provides an excellent liquid crystal composition and an excellent liquid crystal display device.

Abstract: A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.

Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.

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: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

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

Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract: Cyclic structure-bearing fluorinated monomers having formula (1) wherein Z is a divalent organic group containing a polymerizable unsaturated group are useful to produce polymers for the manufacture of radiation-sensitive resist compositions which are fully transparent to radiation having a wavelength of up to 300 nm and have improved development properties.

Abstract: The invention provides a production process of a tetrahydropyran compound, characterized by allowing 3,4-dihydro-2-alkoxy-2H-pyran compound or tetrahydro-2-alkoxy-2H-pyran compound which can be easily prepared through reaction between acrolein and alkylvinylether, with hydrogen in the presence of a catalyst containing an element of Groups VIII to X under acidic condition. The production process of the invention is useful for production of Grignard reaction solvent or polymer solvent and intermediate of organic compound.

Abstract: The present invention provides a process for producing a compound having a group represented by general formula (II): (wherein R1, R2, and R3 may be the same or different, and each represent a substituted or unsubstituted alkyl, a substituted or unsubstituted aryl, or a substituted or unsubstituted aralkyl, or R1 and R2 may bind to each other to form an alicyclic hydrocarbon ring together with the adjacent carbon atoms, or R2 and R3 may bind to each other to form a alicyclic heterocyclic ring together with the adjacent O—C—C that may have a substituent), which comprises allowing a compound having a hydroxyl group to react with halogenated alkyl ether represented by general formula (I): (wherein R1, R2, and R3 are the same as those defined above, respectively and X represents a halogen atom).

Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.

Abstract: The invention provides a production, process of a tetrahydropyran compound, characterized by allowing 3,4-dihydro-2-alkoxy-2H-pyran compound or tetrahydro-2-alkoxy-2H-pyran compound which can be easily prepared through reaction between acrolein and alkylvinylether, with hydrogen in the presence of a catalyst containing an element of Groups VIII to X under acidic condition. The production process of the invention is useful for production of Grignard reaction solvent or polymer solvent and intermediate of organic compound.