Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.

Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T, m and R1 have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.

Abstract: The present invention provides compounds useful for prevention, treatment or alleviation of diseases against which activation of the thrombopoietin receptor is effective. A compound represented by the formula (1): wherein A, B, R1, L1, R2, L2, L3, Y, L4, R3 and X are the same as defined in the description, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—COONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical.

Abstract: The present invention relates to the field of polymer chemistry and more particularly to click-functionalized targeting compounds and methods for using the same.

Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The invention relates to drugs and the use thereof, wherein said drugs contain compounds selected from a group comprising general formulas (1), (2), (3) and (4) and/or enantiomers, diastereomers or the pharmaceutically acceptable salts thereof. Said drugs are used for treating autoimmune and tumoral diseases and/or for immunosuppresion.

Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.

Abstract: The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof.

Abstract: Provided are an organic electroluminescent device including an aromatic amine derivative formed of a specific structure having a thiophene structure and an organic thin film layer interposed between a cathode and an anode and formed of one layer or a plurality of layers including at least a light emitting layer, in which at least one layer of the organic thin film contains the aromatic amine derivative alone or as a component of a mixture, the organic electroluminescent device in which molecules hardly crystallize, and which decreases a driving voltage, can be produced with improved yields upon the production of the organic electroluminescent device, and has a long lifetime, and an aromatic amine derivative realizing the organic electroluminescent device.

Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

Abstract: The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.

Abstract: The invention relates to novel compounds with formula I and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.

Abstract: A method of treating in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein the substituents are defined in accordance with the disclosure.

Abstract: Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.

Abstract: This invention refers to substances able to cause selective muscle relaxation, pharmaceutical compositions containing such compounds and their use in the treatment of muscle tissue diseases, with such compounds complying with the general formula (I).

Abstract: Electron acceptor compounds, nonlinear optical chromophores made from the electron acceptor compounds, methods for making the electron acceptor compounds and nonlinear optical chromophores, lattices that include the nonlinear optical chromophores, and devices that include the nonlinear optical chromophores.

Abstract: Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a link, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.

Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.

Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.

Abstract: The present invention relates to a noble 6-alkylamino-2-methyl-2?-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative, a method for preparing the same with high efficiency using a parallel synthetic method, one of combinatorial chemical synthetic techniques, and a use of the novel compound showing a high inhibitory effect to 5-lipoxygenase (5-LO) activity for preventing and treating leukotriene (LTA4, B4, C4, D4) activation-related diseases such as inflammatory diseases, rheumatoid arthritis, colitis, asthma and psoriasis.

Abstract: When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2?-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries.

Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1?, R2, R3, R4, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.

Abstract: Novel compounds of formula (A) or a pharmaceutically acceptable salt thereof: wherein symbols are as defined in claims, which are useful as SGLT inhibitors and for treatment of diabetes and related diseases.

Abstract: The present invention relates to compounds of formula (1), its solvates and pharmaceutically acceptable salts having antifungal activity and its pharmaceutical composition comprising an effective amount of compound of formula (1) wherein R is substituted alkyl, alkenyl, aryl, heteroaryl, 2-thienyl, 3-thienyl, halothienyl, haloalkyl, halophenyl, or pyrrolyl; and R1 and R2, each independent of the other, are hydrogen, halogen, or alkoxy. The invention also relates to a process for the preparation of said compounds by contacting the intermediate alcohol, prepared from 1,2-O-isopropylideneglyceraldehyde and substituted phenylacetates, with acid chlorides under appropriate conditions to obtain some of the preferred compounds of the invention.

Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.

Abstract: The present embodiments relate to a dye for a dye-sensitized solar cell and a dye-sensitized solar cell prepared from the same. The dye includes a fluorenyl-containing compound. The dye according to the present embodiments is applied to a light absorption layer to improve photovoltaic efficiency and increase an open-circuit voltage.

Abstract: Taxanes having a methylcarbonate or ethylcarbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(13) side chain substituents.

Abstract: In the case of the materials according to the invention, the charge carrier mobility in the correspondingly prepared films is achieved if the molecules are composed in such a way that side chains—consisting of conjugated aromatic or heteroaromatic systems—are attached in direct conjugation to a central aromatic or heteroaromatic ring so that the total molecule acquires an octupolar structure. This octupolar structure permits an effective ?-? interaction of the molecules with one another in a manner such that stacking of a plurality of molecules along an imaginary axis (central ring) can take place and various stacks from among these stacks can interact with one another by intermeshing of the side chains. The electronic properties of the materials are determined both by the arrangement of the molecules in a layer and by the molecular design.

Abstract: A metallocene compound of formula (I): wherein M is zirconium, titanium and hafnium; X is a hydrogen atom, a halogen atom or a hydrocarbon radical; R1 is a linear C1-C20-alkyl radical; R2 is a hydrogen atom or hydrocarbon R3, R4, R5, R6, R7, and R8, are hydrogen atoms or hydrocarbon radicals, A is a sulphur (S) atom or an oxygen (O) atom; Q is a radical of formula (II), (III) or (IV) being bonded to the indenyl at the position indicated by the symbol *; (II), (III), (IV) wherein T1 is a sulphur atom, an oxygen (O) atom or a NR; R9, R10 and R11 are hydrogen atoms or hydrocarbon radicals; T2, T3, T4, T5, and T6 are carbon atoms (C) or nitrogen atoms (N); m1, m2, m3, m4 and m5 are 0 or 1; R12, R13, R14, R15 and R16 are hydrogen atoms or hydrocarbon radicals with the provisos that at least one of R12, R13, R14, R15 and R16 is different from hydrogen atoms, and that no more than two of T2, T3, T4, T5 and T6 are nitrogen atoms.

Abstract: Compositions comprising a taxane having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.

Abstract: A red organic light-emitting compound which has a superior heat-resistance and is capable of adjusting the color of the emitted light, and an organic light-emitting device including the same are disclosed.

Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.

Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5a and R5b is C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms.

Abstract: New pyrrolidinium derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.

Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.

Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: A process for the production of 3,4-dioxythiophene compounds represented by the following formula (I), is described. In formula (I) A, B, C and D in each case independently denote a bond, optionally substituted alkylene, optionally substituted cycloalkylene, optionally substituted arylene or (O—(CR1R2)m)x, where R1 and R2 in each case mutually independently denote hydrogen or optionally substituted alkyl, m denotes an integer from 1 to 10 and x denotes an integer from 1 to 10, provided that at least one of the units A, B, C or D does not denote a bond. The process involves reacting a 3,4-dihydroxythiophene or the alkali metal salt thereof with the following compound, TosO-A-B-C-D-OTos, thus forming an intermediate 3,4-dioxythiophene diester. The intermediate 3,4-dioxythiophene diester is saponified, thus forming an intermediate 3,4-dioxythiophene dicarboxylic acid, which is then decarboxylated, thereby forming the 3,4-dioxythiophene compound represented by formula-(I).

Abstract: Compositions comprising a taxane having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2-furyl, 2-thienyl; R1 is t-butoxycarbonyl or benzoyl; R2 is hydroxy; R3 is hydrogen or, together with R2, it forms the residue of a cyclic carbonate of formula: II with the proviso that when R3 is hydrogen, R is different from phenyl.

Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.

Abstract: The invention relates to thiophene carboxamides of formula (I), wherein R1, R2, R3, A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy

Abstract: The invention discloses a compound having the formula (I) wherein R1 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, unsubstituted phenyl, and substituted phenyl; R2 is selected from the group consisting of H, alkene, un-substituted phenol, and substituted phenyl; and pharmaceutically acceptable salts thereof, having digitalis-like properties. The invention further discloses a novel method to synthesize 3,4-methylenedioxybenzoyl-2-thienylhydrazone (LASSBio-294). LASSBio-294 produces positive inotropic effect on cardiac and skeletal muscle. The invention is useful for the treatment of congestive heart failure and muscle fatigue. It lacks toxic effects seen in digitalis glycosides.

Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.

Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.