Abstract: The present invention relates to colchicine derivatives expressed in chemical formula 1, or to pharmaceutically acceptable salts thereof, to a method for preparing said derivatives, and to a pharmaceutical composition comprising said derivatives. The colchicine derivatives according to the present invention exhibit superior immunomodulatory effects as compared with conventional immunomodulators or colchicines, and therefore can be valuably used as an immunomodulator for modulating an acute or chronic immune response in organ transplantation.

Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: Provided are ?-ketosulfide compounds represented by the formula (5): where the structural variables R1, R2, R3 and R4 are as defined herein.

Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumors, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumors, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: The present invention provides a salt represented by the formula (I): wherein R1 and R2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, X1 represents a C1-C17 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO— and which can have one or more fluorine atoms, R3 represents a hydrogen atom or a methyl group, and Z1+ represents an organic counter cation, and a photoresist composition containing the same.

Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.

Abstract: A functional aspartate prepared by A) reacting an aziridine with a Michael-acceptor molecule to form an aziridinyl aspartate, and B) reacting the aziridinyl aspartate with an active hydrogen containing compound to form the functional aspartate. The functional aspartate can be used in adhesive, sealant or coating compositions that also include an isocyanate functional material. The composition can be used in a method of bonding a first substrate to a second substrate that includes applying a coating of the above-identified adhesive composition to at least one surface of the first substrate or the second substrate, and contacting a surface of the first substrate with a surface of the second substrate, where at least on of the contacting surfaces has the coating applied thereto. The composition can also be used to coat substrates.

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

Abstract: A polymerizable optically active compound of formula (1) has high helical twisting power. When added to a liquid crystal (LC) composition it achieves required helical pitch without largely impairing the physical and optical properties of the LC composition. The compound is suited to be compounded with a LC material, particularly a cholesteric LC material for making an optically anisotropic element excellent in heat resistance, solvent resistance, transparency, optical characteristics, and LC alignment fixing ability. The compound is also useful to form a LC alignment layer, a LC alignment controlling agent, a coating material, a protective film, etc. X1 and X2 each represent a (meth)acryloyloxy group; Y1 and Y2 each represent a single bond, an optionally branched C1-8 alkylene group, an ether linkage, a thioether linkage, —COO—, —OCO—, —OCO—O—, —S—CO—, —CO—S—, an optionally substituted 6-membered ring, an optionally substituted naphthalene ring, or a combination thereof.

Abstract: A polymerization accelerator includes a specific thiol compound. A curable composition of excellent thermal stability contains the polymerization accelerator. A cured product is obtained from the curable composition. The polymerization accelerator includes a thiol compound having two or more groups represented by Formula (1) below: wherein R1 is a hydrogen atom or a C1-10 alkyl group, and m is an integer of 0, 1 or 2.

Abstract: The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.

Abstract: A positive photosensitive composition comprises: a polymer compound having an acid-decomposable structure on a terminal of the polymer compound; and a compound capable of generating an acid upon irradiation with actinic ray or radiation.

Abstract: Compounds of the formula (I) as defined herein are useful for stabilizing spandex. Stabilized spandex compositions are obtained by intermixing spandex polymer or prepolymer with stabilizing amounts of one or more compounds of the formula (I). Preferred stabilized spandex polymer or prepolymer compositions exhibit improved color stability.

Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

Abstract: The present invention refers to a process for the synthesis of (1-{1-(R)-(E)-{3-[2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propylsulfanylmethyl}-cyclopropyl)-acetic acid or its salts, comprising the reaction between 7-Chloro-2-vinyl-quinoline and a compound of formula (I) wherein X is a halogen atom or a group of formula —OSO2R, wherein R is selected from the group consisting of CF3, tolyl, methyl and F; in the presence of a palladium based catalyst. The invention is also directed to intermediates compounds of the process.

Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

Abstract: The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetate is prepared in high yield and purity by the reaction of a haloacetate with the reaction product of thiourea and benzhydrol. The reaction employing the haloacetate is conducted in a solvent comprising an organic solvent such as methanol having dissolved therein an organic base or an inorganic basic salt such as sodium bicarbonate. The resulting benzhydrylthioacetate can be amidated and then oxidized to provide the pharmaceutical grade modafinil in high yield and purity.

Abstract: The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetate is prepared in high yield and purity by the reaction of a haloacetate with the reaction product of thiourea and benzhydrol. The reaction employing the haloacetate is conducted in a solvent comprising an organic solvent such as methanol having dissolved therein an organic base or an inorganic basic salt such as sodium bicarbonate. The resulting benzhydrylthioacetate can be amidated and then oxidized to provide the pharmaceutical grade modafinil in high yield and purity.

Abstract: The present invention is directed to labeled compounds of the formulae wherein Q is selected from the group consisting of —S—, —S(?O)—, and —S(?O)2—, Z is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure wherein R1, R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, a C1-C4 lower alkyl, a halogen, and an amino group selected from the group consisting of NH2, NHR and NRR? where R and R? are each independently selected from the group consisting of a C1-C4 lower alkyl, an aryl, and an alkoxy group, and X is selected from the group consisting of hydrogen, a C1-C4 lower alkyl group, and a fully-deuterated C1-C4 lower alkyl group. The present invention is also directed to a process of preparing labeled compounds, e.g.

Abstract: The present invention provides a method for preparing ester or thioester that can conduct catalytic esterification reaction with an equimolar amount of carboxylic acid and alcohol, or catalytic thioesterification reaction with carboxylic acid and an equimolar amount or small amount of thiol, and can be expected as an industrial method that needs an enormous amount of synthesis in the light of green chemistry. By using hafnium chloride (IV), especially tetravalent hafnium compounds represented by hafnium chloride (IV)·(THF)2 or hafnium (IV)t-butoxide as a (poly) condensation catalyst, direct condensation reaction is conducted from carboxylic acid and an equimolar amount of alcohol or a little smaller amount of thiol, in the nonpolar solvent such as toluene and the like, in a deoxidization atmosphere and under heating reflux, and the reaction synthesizes ester monomer or thioester monomer, polyester or polythioester.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

Abstract: Disclosed herein are high refractive index monomers that are curable by ultraviolet light. These monomers may be a component of curable compositions useful in the preparation of optical articles. Also disclosed is a method of synthesizing the monomers.

Abstract: A process for the preparation of 2-[(diphenylmethyl)sulfinyl]acetamide (I) comprising the oxidation of sodium 2-[(diphenylmethyl)sulfenyl]acetate to the corresponding sulfoxide and the derivatization of the latter to amide

Abstract: Compounds of the formula wherein R, R1, COOR2, R3–R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.

Abstract: A polyhydroxyalkanoate that comprises a unit represented by the following chemical formula (1): wherein R1 is a substituent of an aromatic ring selected from the group consisting of H, CH3, C2H5, CH3CH2CH2, (CH3)2CH, (CH3)3C, a halogen atom, CN, NO2, COOR?, and SO2R?, wherein R? is selected from the group consisting of H, Na, K, CH3, and C2H5, and R? is selected from the group consisting of OH, a halogen atom, ONa, OK, OCH3, and OC2H5; and x represents an integer of 1 to 8 being the same or different each other in the polyhydroxyalkanoate. A method for producing the polyhydroxyalkanoate is also provided.

Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2; provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents may

Abstract: A compound having the general formula

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.

Abstract: The present invention provides cystine derivatives, which may be in a free form, a salt form, a solvate form. The cystine derivatives of the present invention may be used to suppress activation of inflammatory factors. Accordingly, the present invention provides: compositions containing the cystine derivatives; a method for suppressing the activation of inflammatory factors by administering the composition; a method for preventing, ameliorating and/or therapeutically treating diseases, skin injuries or disorders involved in the activation of inflammatory factors by administering the composition; a method for preventing, delaying, ameliorating and/or therapeutically treating skin change via aging or aesthetically unfavorable skin change as induced or promoted by inflammatory factors by administering the composition; and pharmaceutical agents containing the cystine derivatives.

Abstract: The invention provides enantiomers of a joene and derivtives of Z(−)-ajoene. The derivative of Z(−)-ajoene are useful for modulating integrin-mediated functions, for treating disorders, diseases or conditions in which integrins play a role, and for treating tissues to improve their condition for a subsequent use, such as transplantation.

Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide 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: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: The invention relates to compound of formula (I): 1

Abstract: A novel process for preparing 3,4-di(carbocyclyl or heterocyclyl)thiophenes comprising reacting a compound of Formula IV with a ring cyclizing reagent to form the compound of Formula V to yield a compound of Formula V wherein R1, R2 and R3 are as defined in the specification.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers are provided.

Abstract: The present invention relates to novel cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Abstract: The present invention relates to novel amino acid esters of arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.

Abstract: The present invention relates to 5-thia-&ohgr;-substituted phenylprostaglandin E derivatives of the formula (I) (wherein, all the symbols are as defined in the specification), process for producing them and pharmaceutical compositions comprising them as active ingredient. The compounds of the formula (I) can bind to PGE2 receptors (especially, subtype EP4) strongly, so they are expected to be useful for prevention and/or treatment of immunological diseases (autoimmune diseases such as amyotrophic lateral sclerosis (ALS), multiple sclerosis, Sjoegren's syndrome, chronic rheumarthrosis and systemic lupus erythematosus etc., and rejection after organ transplantation etc.

Abstract: A fungicidal compound of formula (I) having a fluorovinyloxyphenyl moiety and stereoisomers thereof are useful for protecting crops from fungal diseases: wherein: X is CH or N; Y is O or S; Z is O or NH; R1 is hydrogen or CF3; and R2 is hydrogen, a C1-10 alkyl, naphthyl, thiophenyl or a phenyl group optionally carrying one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, phenoxy, halogen, and methylenedioxy radicals.

Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.

Abstract: aPL analogs that (a) bind specifically to B cells to which an aPL epitope binds and are disclosed. Optimized analogs lack T cell epitope(s) are useful as conjugates for treating aPL antibody-mediated diseases. Conjugates comprising aPL analogs and nonimmunogenic valency platform molecules are provides as are novel nonimmunogenic valency platform molecules and linkers. Methods of preparing and identifying said analogs, methods of treatment using said analogs, methods and compositions for preparing conjugates of said analogs and diagnostic immunoassays for aPL antibodies are disclosed.

Abstract: A mono-, bi- and/or polyfunctional amide of the formulae (Ia) and/or (Ib),

Abstract: Picornaviral 3C protease inhibitors of formula I, obtainable by chemical synthesis, that inhibit or block the biological activity of the picornaviral 3C protease are described. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: An alkyl 3-oxoalkanoate, a process for preparation and use for the synthesis of fatty hydroxylated amino acids, fatty amino alcohols and ceramides.