4370 results about "Benzimidazole" patented technology

The present invention relates to an anthracene derivative and an organic electroluminescent device using the same. More specifically, the present invention relates to: a novel compound which has a core (for example, an indenoanthracene core) where both an anthracene moiety with excellent device characteristics and a fluorene moiety with excellent fluorescent properties are fused, wherein substituents (for example, a heterocyclic group such as a benzimidazole group, a benzothiazole group, a benzoxazole group, a pyridinyl group or a bipyridinyl group) with an electron transfer capacity are substituted to the core; and an organic electroluminescence element which has improved luminous efficiency, brightness, thermal stability, driving voltage, and lifetime, by comprising an organic layer which is positioned between a positive electrode and negative electrode and contains the novel compound.

Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described

A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.

Organic compounds having the structure I are provided where the variables have the values described herein. A method of inhibiting c-ABL in a patient includes administering an effective amount of a compound of structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable salt of the tautomer to the patient.

The present invention is directed to, inter alia, pharmaceutical compositions comprising at least one proton pump inhibitor and at least one buffering agent. Compositions of the invention are useful in treating, inter alia, gastric acid related disorders.

Organic compounds having the structure I are provided where the variables have the values described herein.Pharmaceutical formulations and medicaments include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compound or a pharmaceutically acceptable salt of the organic compound with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation or medicament according to the invention to a patient in need thereof.

The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I):and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of serine-threonine protein kinases and tyrosine protein kinases and interactions thereof.

Disclosed herein are compositions and methods for treating gastric acid disorders employing pharmaceutical compositions comprising a proton pump inhibitor (PPI) in a pharmaceutically acceptable carrier.

The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula I:

Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The invention relates to compounds of structural formula (I) or (III): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein ring A, X1, X2, X3, X5, R1, R4, Y, Z, L, m and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer.

Object of the present invention is to search a novel pharmaceutical use of 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione being a condensed heterocyclic compound, or a salt thereof. 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione or a salt thereof can exert an excellent effect to promote healing in a dry eye model, and is useful as a therapeutic agent for keratoconjunctival disorders such as dry eyes, corneal ulcer, keratitis, conjunctivitis, superficial punctate keratopathy, corneal epithelial defects, conjunctival epithelial defects, keratoconjunctivitis sicca, superior limbic keratoconjunctivitis and filamentary keratitis.

This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C17alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the a-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

A compound of the formula:or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M-, (C3-C7)cycloalkyl-M-, (C2-C6)alkenyl-M-, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M-, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M-, aryl-M-, aromatic or non-aromatic heterocyclic-M-, aryl-(C1-C5)alkyl-M- or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M-, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

The present invention relates to novel hetero-substituted benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses hetero-substituted benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of hetero-substituted benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making hetero-substituted benzimidazole compounds, methods of using the hetero-substituted benzimidazole compounds and compositions comprising the hetero-substituted benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.

The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II:

The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II:

The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and / or Factor VIIa (FVIIa), and have utility as anti cancer agents and / or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

The present invention provides a stable pharmaceutical composition of an acid labile drug such as a pharmaceutically active substituted benzimidazole compound, comprising: a) an inner core coated with the acid labile drug; b) a first intermediate coating devoid of an alkaline stabilizing agent and the benzimidazole compound; c) a second intermediate coating comprising an alkaline stabilizing agent; and, d) an outer enteric layer. The present invention also provides a method of preparing the same.

A method for obtaining an aromatic polyamide crumb from an aromatic diamine and an aromatic diacid chloride, which aromatic polyamide comprises 5(6)-amino-2-(p-aminophenyl)benzimidazole terephthalamide units and has a relative viscosity ηrel of at least 3, by: (1) adding at least monomers (i)-(iii) in N-methyl pyrrolidone as solvent wherein (i) is 0-30 mole % para-phenylenediamine (PPD), (ii) is 20-50 mole % 5(6)-amino-2-(p-aminophenyl)benzimidazole (DABPI), (iii) is 49.05-50.05 mole % terephthaloyl dichloride (TDC), and optionally calcium chloride to obtain a CaCl2 / aromatic diamine molar ratio less than 0.5, and an aromatic diamine / aromatic diacid chloride ratio between 0.99 and 1.01; (2) mixing the monomers and the optional calcium chloride to a homogenous mixture having a monomer concentration of 5 to 12 wt %; followed by (3) adding calcium chloride to the homogeneous mixture to obtain a CaCl2 / aromatic diamine molar ratio 0.6-1.0; and (4) polymerizing the mixture.

Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.

The invention relates to compounds of formula (XVI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein Y2, Z, L1, R9, R10, m and u are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, immune disorders, and allergic disorders.

The invention relates to the fields of analytical chemistry and food safety, in particular to a method for detecting the residual quantity of multiple alkaline drugs in animal derived food. Based on the vortex mixed extracting of acetonitrile, isopropanol and citric acid buffer solutions, the purification of a hydrophilic polystyrene-divinylbenzene solid phase extraction column and a cation exchange solid phase extraction column and the liquid phase chromatography-mass spectra determination, the method can detect the residual quantity of multiple alkaline drugs in pork, pork liver, eggs, shrimps and milk, such as beta-receptor agonists,sulfonamides, benzodiazepines, nitroimidazoles, benzimidazoles and triphenylmethanes. The method has the advantages of simple operation, fast and accurate detection and high efficiency.