Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract: In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.

Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

Abstract: As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.

Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: The present invention relates to compounds which stimulate soluble guanylate cyclase, to the preparation thereof and to the use thereof as medicaments, in particular as medicaments for the treatment of cardiovascular disorders and/or sexual dysfunction.

Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof, processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as a active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of number of disease states including cancer and rheumatoid arthritis.

Abstract: Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such compounds are useful for treating diseases or medical disorders mediated by protein kinases.

Abstract: This invention comprises the compounds of formula (I): wherein r, s, t, Y1–Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use.

Abstract: Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.

Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

Abstract: The invention concerns 4-aminomethyl-1-aryl-cyclohexylamine compounds, methods for producing same, pharmaceutical formulations containing said compounds and the use of 4-aminomethyyl-1-aryl-cyclohexylamine compounds for producing medicines and in related methods of treatment.

Abstract: The present invention relates to novel CD40:CD154 binding interrupter compounds and use of these compounds and pharmaceutical compositions comprising them, to treat conditions associated with inappropriate CD154 activation in a subject. Specifically, this invention provides compounds which are identified by screening a library of small molecules for those that are capable of specifically binding CD154 and interrupting CD40:CD154 interaction.

Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.

Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.

Abstract: 1) Fungicidal compositions comprising: a) at least one pyridylmethylbenzamide derivative of formula (I): ?in which the various radicals are as defined in the description, and b) at least one compound (II) which is a phosphorous acid derivative, or phosphorous acid itself, and also alkali metal, alkaline-earth metal or metallic salts thereof. 2) Process for curatively or preventively combating the phytopathogenic fungi of crops, characterized in that an effective and non-phytotoxic amount of one of these fungicidal compositions is applied to the aerial parts of the plants.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.

Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.

Abstract: Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R1 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R2 is C1–C3haloalkyl; and R3 is halogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.

Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea,

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.

Abstract: Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.

Abstract: The present invention relates to compounds of formula I, their pharmaceutically acceptable salts as well as their enantiomeric forms, diastereoisomers and racemates; the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds as inhibitors of histone deacetylase (HDAC) and therefore in the control or prevention of illnesses and disorders as mentioned above, or in the manufacture of corresponding pharmaceutical compositions.

Abstract: The invention provides compounds of formula (I) or a salt thereof, radiolabelled versions thereof, and their use in the diagnosis or in vivo imaging of Amyloid-associated diseases such as Alzheimer's disease

Abstract: The present invention relates to a method for the improvement of skin wrinkles using retinal retaliate.

Abstract: Methods for the treatment of a proliferative disorder are provided in which a subject in need of such treatment is administered an effective amount of a compound selected from: compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X1 and X2 are independently H, Cl, F, Br, I, CN, CF3 or NO2, and Ar1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and compounds of formula (II) wherein X3 and X4 are each independently H, Cl, F, Br, I, CN, CF3 or NO2; Y is (C2–C6)alkylene or (C2–C6)heteroalkylene; and Z is Cl, F, Br, I, CN, CF3 or NO2.

Abstract: The present invention discloses compositions and methods useful for treating wasting, especially a loss of muscle mass. The present invention also discloses compositions and methods useful for treating lipodystrophy. The compositions and methods of the present invention are particularly beneficial to HIV-infected individuals.

Abstract: Backside conductive layers with increased conductive efficiency can be provided for thermally developable materials by formulating hydrophilic metal oxide clusters in a hydrophobic environment using low shear mixing conditions. The dry thickness and coating weight of the conductive layer are thereby reduced.

Abstract: A porous ion exchanger includes an open cell structure including interconnected macropores and mesopores whose average diameter is in a range of 1 to 1000 ?m existing on walls of the macropores. Moreover, a total pore volume is in a range of 1 to 50 ml/g, ion exchange groups are uniformly distributed, and an ion exchange capacity is not less than 0.5 mg equivalent/g of dry porous ion exchanger. The porous ion exchanger can be used as an ion exchanger filled into a deionization module of an electrodeionization water purification device, solid acid catalyst, adsorbent, and filler for chromatography.

Abstract: A method is provided for making a crosslinked polymer by direct fluorination of a non-perfluorinated polymer comprising first pendent groups which comprise sulfonyl halide groups or by direct fluorination of a polymer mixture of a first polymer which is a non-perfluorinated polymer and a second polymer which comprises first pendent groups which comprise sulfonyl halide groups. Such crosslinked polymers or polymer mixtures may be used to make polymer electrolyte membranes (PEM's) that may be used in electrolytic cells such as fuel cells and which should demonstrate increased durability in fuel cell use.

Abstract: A thermoplastic foam is provided which contains a thermoplastic resin and a layered silicate and in which foam cells and the layered silicate are evenly and finely dispersed. A volume-expansible gas or heat decomposable blowing agent is incorporated into interlayer spaces of a layered silicate in a composite material containing 100 parts by weight of a thermoplastic resin and 0.1–50 parts by weight of the layered silicate, and the gas or blowing agent is allowed to expand in volume or thermally decompose to form foam cells 6, so that a thermoplastic foam is obtained in which the layered silicate has an average interlayer spacing of over 60 ? when determined by an X-ray diffractometry.

Abstract: A non-crosslinked polyolefin foam comprises a plastics component and a blowing agent. The plastics component comprises a first constituent and a second constituent. The first constituent is a Ziegler-Natta catalyzed linear low density polyolefin and the second constituent is a low density polyolefin in one embodiment. The Ziegler-Natta catalyzed linear low density polyolefin has a polydispersity of less than 10 and a melt flow index less than 10 g/10 minutes. The second constituent may be a polypropylene.

Abstract: The present invention provides a foam cushion, a method of making the foam cushion, and a method of using the foam cushion. The foam cushion is formed from: (a) at least one of rubber and a resin; (b) a blowing agent; (c) a polymeric adhesion modifier; (d) a decomposition accelerating agent, and (e) a cross-linking agent.

Abstract: Photo-curable coating formulations which comprise a durable and/or red-shifted reactable hydroxyphenylbenzotriazole ultraviolet light absorber (UVA) are effectively photocured employing a combination of ?-hydroxy ketone and bisacylphosphine oxide photoinitiators. The reactable UVA's are reacted into the coating upon curing. The combination of the photoinitiators bis(2,4,6-trimethylbenzoyl)phenylphosphine oxide and 1-hydroxycyclohexylphenylketone is especially effective for this purpose.

Abstract: To provide a UV-curable resin composition useful for forming optical parts such as optical lenses. A radiation-curable resin composition for optical parts, comprising (A) 5–70 wt % of urethane (meth)acrylate, (B) 0.1–70 wt % of benzyl (meth)acrylate, and (C) 10–70 wt % of an ethylenically unsaturated group-containing compound other than the components (A) and (B).

Abstract: This invention relates to ophthalmic devices and methods for their production where the ophthalmic device contain a polymer and at least one heterocyclic compound comprising at least one N—Cl and/or N—Br bond.

Abstract: The present invention provides a hardenable (i.e., curable by polymerization, crosslinking, ionic, or other chemical reaction) composition that includes polymerizable urea or thiourea compounds that function as reductants (i.e., reducing agents) in redox polymerization reactions.

Abstract: Sealing and filling compositions for use in filling and/or sealing a root canal. The sealer and filler compositions include a polymerizable material that shrinks when polymerized. The composition also includes a gas releasing component that at least partially offsets the shrinkage caused by polymerization of the polymerizable material. The gas releasing component offsets polymerization shrinkage by creating tiny gas bubbles in the polymeric material, which causes expansion. The gas releasing component can be an acid and a base such as citric acid and sodium bicarbonate, which when mixed give off carbon dioxide. The composition can also include a dispersing agent to disperse the gas bubbles throughout the composition.

Abstract: The present invention includes methods and compositions relating to a hot melt adhesive that includes ethylene methyl methacrylate and a tackifying resin.

Abstract: An aqueous glittering ink composition whose viscosity ranges from about 1,000 to about 10,000 mPa·s, (measured by an ELD-type viscometer: 3° R 14 cone, 0.5 rpm, at the temperature of 20° C.) comprising a. aluminum powder pigments whose median diameter is not less than about 15 ?m compounded with oleic acid and/or stearic acid; b. synthetic resin emulsions selected from acryl based synthetic resin emulsions, styrene-acryl based synthetic resin emulsions and vinyl acetate based synthetic resin emulsions; c. polysaccharide selected from whelan gum, succinoglycan, and rhamsan gum; d. water-soluble organic solvent; and e. colored pigment.

Abstract: A process for preparing a modified pigment having attached at least one organic group is described. This process comprises the step of reacting a dried mixture comprising a pigment having attached at least one reactive group and a modifying agent. The dried mixture is reacted under high intensity mixing conditions for a time and temperature sufficient to form the modified pigment.

Abstract: The casting-mold material designed to manufacture casting molds used in casting high melting-point substances. The casting mold formed from a powder component containing magnesium oxide and aluminum oxide and a liquid component. The powder component additionally contains a calcium aluminate and an alkali fluoride or an earth alkali fluoride and the liquid component contains a polyelectrolyte and a basic component, the latter determining the liquid component pH value between 10 and 14. A fluid slip is prepared by mixing the powder and liquid components and is dried, hardened and sintered to produce a hollow mold.

Abstract: A biodegradable resin composition and an object molded or formed from the composition. The resin composition comprises: 100 parts by weight of a biodegradable polyester resin comprising not smaller than 50% by weight of polylactic acid having a melting point of not lower than 160° C., the biodegradable polyester resin having a melt flow rate of 0.1 to 50 g/10 min as measured under a load of 21.2 N at 190° C.; and 0.1 to 20 parts by weight of a phyllosilicate containing a primary, secondary or tertiary amine salt, a quaternary ammonium salt or a phosphonium salt ionically bonded between layers thereof.