Abstract: The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them.

Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.

Abstract: The invention relates to 2-(2-pyridyl)-5-phenyl-6-aminopyrimidines of formula I, wherein the substitutes and the index have the following meaning: R1 represents halogen, hydroxy, hyano, hxo, nitro, amino, mercapto, alkyl, halogenalkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, halogenalkoxy, carboxyl, alkoxycarbonyl, carbamoyl, alkylaminocarbonyl, dialkylamincarbonyl, morpholinocarbonyl, pyrrolidinocarbonyl, alkylcarbonylamino, alkylamino.

Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Abstract: The invention relates to substituted 2-Phenyl-3(2H)-Pyridazinones, to a method for the production thereof, and to their use as medicaments for the prophylaxis and/or treatment of diseases in humans and/or animals.

Abstract: This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.

Abstract: The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radica

Abstract: The invention relates to substituted pyrido[1,2-a]pyrimidine compounds corresponding to formula (I) wherein: R1, R2 and R3 are as defined in the specification. Related pharmaceutical formulations and methods for inhibiting nitrogen oxide synthesis (NOS) and other treatments are also provided.

Abstract: The invention provides variolin derivatives of formula (I), wherein: R1 and R2 are each independently selected from the group consisting of H, OH, OR, SH, SR, SOR, SO2R, NO2, NH2, NHR, N(R)2, NHCOR, N(COR)2, NHSO2R, CN, halogen, C(?O)H, C(?O)R, CO2H, CO2R, C1-C12 alkyl, C1-C12 haloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; and R3 is selected from the group consisting of H, OH and OMe; wherein the or each group R is independently selected from the group consisting of OH, C1-C12 alkyl, C1-C12 haloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted unsubstituted aralkyl, substituted or unsubstituted arylalkenyl and substituted or unsubstituted heteroaromatic, and wherein the group R1, R2 or R3 is a group of formula N(R)2 or N(COR)2, each of the R groups may be the same or different, or the two R groups, together with the nitrogen atom to which they are attached, m

Abstract: The invention relates to the use of a compound of formula (I): for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-?1.

Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(?O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.

Abstract: A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an aqueous solution containing a stabilized arylcarboxylic acid. According to the stabilization method of the present invention, arylcarboxylic acid and pharmacologically acceptable salts thereof, particularly pranoprofen, can be stabilized at every temperature range, particularly at lower temperatures, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.

Abstract: Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: The present invention provides compounds of the Formula I: wherein R1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH2-alkenyl, X1 is O, NH, N(alkyl), S or —C(?O), Z is N or CH; and R2 and R3 are as defined herein, pharmaceutical compositions comprising same, and methods for their use.

Abstract: This invention relates to methods for lowering lipid levels in mammals using compounds that inhibit advanced glycation endproducts (AGEs), LR-9, LR-74 and LR-90. These compounds, which inhibit non-enzymatic protein glycation, also inhibit the formation of advanced lipoxidation endproducts (ALEs) on target proteins by trapping intermediates in glycoxidation and lopoxidation and inhibiting oxidation reactions important in the formation of AGEs and ALEs.

Abstract: The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.

Abstract: The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of biphenyl-2-ylcarbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5 -yl)ethylamino]nonyl}piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.

Abstract: A number of thalidomide metabolites having superior anti-angiogenic properties have now been isolated and identified. In addition, thalidomide analogs that mimic the effects of the isolated and identified active thalidomide metabolites, and variations of such thalidomide analogs, have been developed. Such thalidomide analog compounds show enhanced potency in the inhibition of undesirable angiogenesis without the undesirable effects of administration of thalidomide.

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Abstract: This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparation and intermediates therefor.

Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl.

Abstract: The present invention relates to methods for treatment or prevention of neoplasia disorders using protein tyrosine kinase inhibitors of the formula I: wherein R1, R2, R3, R4, R5, R6, and R7 are defined herein, in combination with cyclooxygenase inhibitors, in particular cyclooxygenase-2 selective inhibitors.

Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The analog or derivative is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. In some embodiments, the invention may include a pharmaceutical composition including a carotenoid analog or derivative. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include a cyclic ring including at least one substituent. The substituent may be coupled to the cyclic ring with an ester functionality.

Abstract: The present invention provides carbohydrate analogs of the formula: wherein X is CH2, O, or NH, and R1-8 are independently H, a short hydrocarbon, a substituted amine, an alcohol, a substituted ether, a substituted amide, a substituted ketone, a substituted carboxylic acid, a short peptide, or a short oligosaccharide, Y is H, a short hydrocarbon, a short peptide, or a short oligosaccharide, and R9 is H, a short hydrocarbon, a substituted amine, an alcohol, a substituted ether, a substituted amide, a substituted ketone, a carboxylic acid, a short peptide, or a short oligosaccharide.

Abstract: The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.

Abstract: An ophthalmic pharmaceutical composition containing acetylcysteine as the active ingredient having a mucolitic action, suitable for administration in eyedrops, where N-acetyl-cysteine is neutralised with base DEAE-dextrane in order to reach pH levels preferably between 6.0 and 7.5, and having a physiologically acceptable osmolarity less than 320 mOsm/kg. The presence of a neutralising agent for N-acetyl-cysteine that does not negatively affect the composition osmolarity allows the formulation to be isotonic or even hypotonic, thus avoiding the irritative and potentially damaging effects of previous ophthalmic products containing N-acetyl-cysteine.

Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.

Abstract: The invention provides enantiomers of ajoene and derivatives 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 is directed to novel polystyrene foam reduction recycling compositions and methods that solve the volume problem of recycling polystyrene foam materials while simultaneously allowing the easy and inexpensive shipment of the foamed materials after reduction in volume by use of one or more dibasic ester compositions in combination with one or more low heat based mechanical extruders. The methods of the present invention are applicable to all types of expanded or foamed polystyrene materials known to those of skill in the art.

Abstract: A method for curing polymerizable compositions by irradiating the compositions with light that is emitted from an LED. The method of the present invention is especially preferred for curing dental compositions.

Abstract: A method of making an encapsulant composition. The method includes: providing a first quantity of resin material of epoxy or cyanate ester resins; adding to the first quantity of resin material a second quantity of flexibilizing agent; adding to the first quantity of resin material a third quantity of filler material; blending the resin material. After adding the flexibilizing agent, adding the filler material, and blending the resin material, applying the composition to a gap between a substrate and a semiconductor chip. After applying the composition to the gap, pregelling the composition. After pregelling the composition, substantially curing the composition.

Abstract: There are provided an admixture for cement which enhances water reducing property and flowability of a cement composition, and is excellent in slump retaining performance to retain the flowability with time, a polycarboxylic acid-based polymer for an admixture for cement suitable therefor, a producing method thereof, and a cement composition. One admixture for cement of the present invention contains copolymers (A) and (B) as an essential component, weight average molecular weights (AMw and BMw) of copolymers (A) and (B) are AMw>BMw, or peaktop molecular weights (AMp and BMp) of copolymers (A) and (B) are AMp>BMp. Another admixture for cement of the present invention contains a polycarboxylic acid-based polymer having a lower molecular weight side area ratio P of 50 to 87%.

Abstract: The present invention relates to a liquid absorbent thermoplastic composition, which contains particles of a superabsorbent material having angle-lacking shapes. The composition is particularly suitable to be used in absorbent articles for personal hygiene, specifically in disposable absorbent articles, which have one or more transparent regions.

Abstract: Star polymers of soft segment forming monomers are useful in forming surgical devices. The star polymers can be endcapped with diketene acetals, mixed with a filler and/or cross-linked. The polymer compositions are useful, for example, as fiber coatings, surgical adhesives or bone putty, or tissue growth substrate.

Abstract: The invention is concerned with gasket sealing foils having a sealing layer with enhanced properties which is based upon chemically exfoliated vermiculite. The method of producing a sealing foil for gaskets is described. The method comprises the steps of: (a) the application of a wet sealing foil material to a forming sheet to form a layer, (b) partially drying the said wet sealing foil layer on the forming sheet; (c) removing the said layer from the forming sheet to form a core free gasket sealing foil; and (d) forming, preferably cutting, the layer into at least one suitable shape for use in the formation of a gasket The sealing foil comprises a resilient material, which comprises a CEV component in a proportion of at least 25% w/w of the sealing foil, the CEV component being at least partially derived from dry CEV. The sealing foil layer may be combined with a gasket support layer prior to or after the cutting step.

Abstract: A curable formaldehyde-free binding composition for use with fiberglass is provided. Such curable composition comprises a substantially unpolymerized acrylate and/or methacrylate primarily having no more than approximately six recurring moieties. The composition is either unpolymerized at the time of its application to the fiberglass or in the form of an oligomer. The curable composition is coated on fiberglass and thereafter is cured to form a secure binder. In a preferred embodiment the fiberglass is the form of building insulation. In other embodiments the product is a microglass-based substrate useful for as a printed circuit board, battery separator, filter stock, or reinforcement scrim.

Abstract: The invention relates to self-emulsifying copolymers, and to compositions, preferably care and/or treatment and/or make-up compositions for keratin and keratinous materials (including the skin, hair, nails, scalp, and/lips of human beings, keratinous fibers, etc.), containing one or more such self-emulsifying copolymers. Methods of making and using the self-emulsifying copolymers and compositions containing them also make up a part of the invention.

Abstract: A method of manufacturing an intrinsically conductive polymer crosslinking at least a portion of an intrinsically conductive polymer precursor in the solid state, the swollen state, or combinations comprising at least one of the foregoing states, wherein the swollen state is characterized as being one wherein the intrinsically conductive polymer precursor increases in volume upon exposure to a solvent without completely dissolving in the solvent. In another embodiment, a method of manufacturing a pattern comprises casting a film of an intrinsically conductive polymer precursor on a substrate; and crosslinking at least a portion of the film by oxidation, wherein the crosslinking occurs in the solid state, the swollen state or combinations comprising at least one of the foregoing states.

Abstract: Disclosed is a method of making reduced VOC polymers and coating compositions containing such polymers. Provided is a mixture (I) comprising a reactant mixture (a) of polymerizable components and a nonvolatile solvent (bnv) that (i) is not a crystalline solid at 25° C., (ii) is nonvolatile, (iii) comprises at least one functional group (F1) and (iv) is a fluid solid. Reactant mixture (a) is polymerized to provide a polymer (a?). The at least one functional group (F1) of nonvolatile solvent (bnv) is reacted with one or more reactants (e) to obtain a nonvolatile solvent (b?nv) comprising at least two functional groups (F2). Obtained is a mixture (II) comprising polymer (a?) in nonvolatile solvent (b?nv) comprising at least two functional groups (F2). The at least one functional group (F1) is substantially nonreactive: (1) with the components of reactive mixture (a), (2) under the polymerization conditions which polymerize reactant mixture (a), and (3) with polymer (a?).

Abstract: A thermoplastic composition is disclosed, comprising the reaction product of: a polyester polycarbonate comprising a polyester unit and a polycarbonate unit; a polysiloxane polycarbonate copolymer having a haze of 30% or less, comprising a polycarbonate unit and a polysiloxane unit; and a transesterification catalyst. The resulting thermoplastic composition has a haze of 30% or less as measured according to ASTM D1003-00 at a thickness of 3.2 millimeters. A method of forming the composition and articles formed from the composition are also disclosed.

Abstract: Properties of a polymer produced using a dual catalyst on the same support, such as polydispersity and comonomer incorporation, may be controlled by controlling reaction parameters such as temperature, monomer pressure, hydrogen partial pressure and the presence of non-polymerizable hydrocarbon. This provides an easy method to control the bimodality of a polymer as well as comonomer incorporation.

Abstract: Provided is a method of preparing styrene polymers, the method comprising: homogeneously mixing a styrene monomer; a cocatalyst mixture of Group 13 metal-containing organic metal compound cocatalyst and an inert organic solvent; and a catalyst mixture of a metallocene catalyst and the inert organic solvent using a high speed homogenizing mixer to obtain a homogenized mixture; and providing the homogenized mixture to a reactor to initiate polymerization. In this method, catalyst is quickly dispersed among monomers using a high speed homogenizing mixer so that formation of gel, which occurs when a syndiotactic styrene polymer is produced, can be fundamentally prevented. In addition, a styrene polymer prepared using the method has high activity, good stereoregularity, and uniform molecular distribution.

Abstract: The present invention is directed to an amine containing catalyst system for synthesizing rubbery polymers, such as polybutadiene rubber and styrene-butadiene rubber, having a high trans microstructure. The catalyst system, in one embodiment, includes (a) an organolithium compound, (b) a group IIa metal salt, (c) an organoaluminum compound, and (d) an amine compound which can be selected from (1) a heterocyclic aromatic compound which includes a ring structure with one or more nitrogen atoms as part of the ring; (2) a heterocyclic non-aromatic compound which includes a ring structure with two or more nitrogen atoms as part of the ring; (3) an aromatic compound including a ring structure substituted with at least one amine and at least one polar functionality containing group selected from a carboxyl group or a hydroxyl group; (4) a bicyclic chelating diamine compound; or (5) an aliphatic amine which includes a C5-C20 alkyl group.

Abstract: The invention relates to a dilutable, non-aqueous concentrate and an aqueous dilution used for aqueous delivery of fluorinated oligomeric silanes to a substrate, a method of treating a substrate with the aqueous dilution composition to render it oil and water repellent, and articles having coatings made from the aqueous dilution.

Abstract: Aqueous dispersions containing organopolysiloxane/polyurea copolymers prepared by reacting aminoalkyl-functional organopolysiloxanes with a diisocyanate in water in the presence of a protonating acid, and optionally one or more surfactants and/or protective colloids. The organopolysiloxane/polyurea polymers may be prepared without the presence of ionic groups if desired.

Abstract: The invention relates to the polycondensation products produced by reaction of bisphenol residues from bisphenol production with an aldehyde in an acidic medium useful for the production of refractory molded bodies, of unmolded substances used in the refractory industry and, together with coating powder residues, as binding agents or binding agent components for the production of molded nonwoven fabric parts.

Abstract: Impurities are removed from polythiophene by mixing a composition comprising polythiophene, water and an organic liquid at a temperature at which the organic liquid dissolves the polythiophene; allowing an aqueous phase to separate from an organic phase and recovering organic phase; adding water to recovered organic phase and mixing the resulting composition at a temperature at which the organic liquid dissolves the polythiophene; allowing an aqueous phase to separate from an organic phase and recovering organic phase; and allowing polythiophene solid to precipitate from recovered organic phase.

Abstract: Disclosed herein is a method of controlling the stability of multilayer polypeptide films. A method of controlling the stability of a film, comprises exposing the film to an oxidizing agent or a reducing agent, wherein the film comprises a plurality of layers, the layers comprising alternating oppositely charged polypeptides, wherein a first layer comprises a first layer polypeptide and a second layer comprises a second layer polypeptide, and the first layer polypeptide comprises a sulfhydryl-containing amino acid.