The Additional Polycyclo Ring System Contains A 1,3-diazole [e.g., Bis (benzimidazol-2-yl) Stilene, Etc.] Patents (Class 548/305.4)
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Publication number: 20100222331Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Bodo Betzemeier, Guido Boehmelt, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Daniel Kuhn, Jens Juergen Quant, Ulrich Reiser, Otmar Schaaf, Flavio Solca, Heinz Stadtmueller, Ulrike Tontsch-Grunt, Matthias Treu, Stephan Karl Zahn
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Publication number: 20100222402Abstract: A carboxylic acid of the general formula R1COOH, wherein R1 is the hydrogen atom or a C1-C4 alkyl, is added to a solution of the potassium salt of telmisartan in an alcohol of the formula R2OH with the water content lower than 2%, wherein R2 is ethyl or methyl.Type: ApplicationFiled: July 8, 2008Publication date: September 2, 2010Inventors: Jan Stach, Stanislav Radl, Josef Cinibulk, Ivo Strelec, Kamal Jarrah
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Publication number: 20100197871Abstract: Ligands useful for promoting copper-catalyzed azide-alkyne cycloaddition reactions comprise a compound represented by structural Formula (I) as described in the specification, wherein in Formula (I) Z1 is a nitrogen-containing heterocyclic group or a group represented by the formula: Y1—(CH2)c—Y2—(CH2)d—Y3—CH2—N(CH2Z4)(CH2Z5), where Y1 is -E1-C(O)O—, -E1-C(O)NH—, -E1-, or a covalent bond; Y2 is a covalent bond, —CH?CH—, or a 1,4-(1,2,3-triazolyl) group; Y3 is —OC(O)-E2-, —NHC(O)-E2-, -E2-, or a covalent bond; each of E1 and E2 is a benzimidazolyl group attached at the 1 and 2 positions; each of c and d is independently 1, 2, 3, 4, or 5; each of Z2, Z3, Z4 and Z5 is a nitrogen-containing heterocyclic group including a substituent X1 and optionally including a substituent (CH2)n—R1, and Y1, Y2, Y3, X1, R1, c, d and n are each as defined in the specification.Type: ApplicationFiled: September 15, 2008Publication date: August 5, 2010Inventors: M.G. Finn, Valentin O. Rodionov
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Publication number: 20100187520Abstract: Disclosed is a light emitting device material characterized by containing a specific fluorine compound. This light emitting device material enables to obtain a light emitting device having high luminous efficiency, excellent color purity and excellent durability. Also disclosed is a light emitting device using such a light emitting device material.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: Toray Industries, Inc.Inventors: Kazunori Sugimoto, Tsuyoshi Tominaga
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Publication number: 20100152259Abstract: A compound having the structure (Formula I), wherein R an angiotensin receptor antagonist active group, Y is Y1—Y2—Y3—Y4—Y5. Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 11, 2007Publication date: June 17, 2010Applicants: Merck & Co Inc., NICox S.A.Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali, Chris Franklin, Nicoletta Almirante, Laura Storoni, Silvia Stefanini
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Publication number: 20100144810Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 2, 2009Publication date: June 10, 2010Inventors: Michael Man-Chu Lo, Amjad Ali, Ravi P. Nargund
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Patent number: 7723321Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R1, R2, R3, R4, R5, R6, R7 and R8 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.Type: GrantFiled: December 19, 2006Date of Patent: May 25, 2010Assignee: RaQualia Pharma Inc.Inventors: Takeshi Hanazawa, Hiroki Koike
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Publication number: 20100109514Abstract: The present invention relates to compounds of the formula (I), a process for their preparation and their use in organic light emitting diodes (OLEDs), especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or special characteristics of electroluminescent devices.Type: ApplicationFiled: March 19, 2008Publication date: May 6, 2010Inventors: Thomas Schäfer, Peter Murer, Frédérique Wendeborn, Beat Schmidhalter, Kristina Bardon, Andrea Ricci, Joern Pommerehne
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Patent number: 7692027Abstract: A process for the preparation of telmisartan (I) and novel intermediates useful for its synthesis.Type: GrantFiled: May 2, 2006Date of Patent: April 6, 2010Assignee: Dipharma S.p.A.Inventors: Pietro Allegrini, Marcello Rasparini, Gabriele Razzetti, Alberto Bologna, Giuseppe Barreca
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Patent number: 7608722Abstract: A process for preparing 1,7?-dimethyl-2?-propyl-2,5?-bi-1H-benzimidazole of formula (I) reacting N-methyl-o-phenylenediamine of formula (II) or the salts thereof with 2-propyl-4-methyl-1H-benzimidazole-6-carboxylic acid of formula (III) or the salts thereof wherein the coupling and cyclization is achieved using 1,3,5-triazine and tertiary amine.Type: GrantFiled: July 12, 2006Date of Patent: October 27, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Helmut Heitger, Juan M. Rodriguez-Dehli, Rolf Dach
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Publication number: 20090227802Abstract: The present invention relates to a bilayer pharmaceutical tablet comprising a first layer formulated for immediate release of the angiotensin II receptor antagonist telmisartan from a dissolving tablet matrix which contains telmisartan in substantially amorphous form, and a second layer formulated for immediate release of a diuretic like hydrochlorothiazide from a fast disintegrating tablet matrix. A method of producing the bilayer tablet is also disclosed.Type: ApplicationFiled: May 13, 2009Publication date: September 10, 2009Inventors: Thomas FRIEDL, Gottfried Schepky
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Publication number: 20090211038Abstract: The present disclosure relates to a novel dye composition for the dyeing and/or lightening of keratin materials, such dye comprising a hemicyanin styryl chromophore thiol or disulfide dye of formula (I) or (II): the organic or mineral acid salts thereof, optical isomers and geometric isomers thereof, and the solvates thereof such as hydrates. The present disclosure further relates to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, including human keratin fibers such as the hair, using said composition. This composition makes it possible to obtain a coloring with a lightening effect which is particularly resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: August 27, 2009Inventors: Andrew GREAVES, Nicolas DAUBRESSE
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Patent number: 7569688Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: June 20, 2005Date of Patent: August 4, 2009Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Patent number: 7563815Abstract: The present invention relates to substituted benzimidazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: GrantFiled: May 5, 2004Date of Patent: July 21, 2009Assignee: Merck & Co., Inc.Inventors: Emma R. Parmee, Ronald M. Kim, Rui Liang, Jiang Chang, Elizabeth Ashley Rouse, Kevin T. Chapman
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Publication number: 20090176849Abstract: The invention relates to a new process for the preparation of sartans 2-butyl-3-[[2?-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1?-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one is disclosed, which proceeds via novel intermediate, 4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]phenylboronic acid (Formula (II)) or its analogs. Compound (II) reacts with 5-(2-bromophenyl)-1-(triphenylmethyl)-1H-tetrazole (III) in the presence of catalyst, using conditions of Suzuki reaction, to give trityl irbesartan (I), whereas analogs to compound (II) may give candesartan, valsartan, telmisartan, losartan and olmesartan.Type: ApplicationFiled: May 22, 2006Publication date: July 9, 2009Applicant: LEK PHARMACEUTICALS, D.D.Inventor: Lovro Selic
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Publication number: 20090156585Abstract: A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.Type: ApplicationFiled: November 8, 2006Publication date: June 18, 2009Inventors: Lili Feng, Sven Erik Godtfredsen, Bin Hu, Yugang Liu, Piotr Karpinski, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Thomas J. Blacklock
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Publication number: 20090149649Abstract: The present invention provides an aromatic heterocyclic compound represented by Formula 1 below, an organic light-emitting diode including an organic layer comprising the aromatic heterocyclic compound, and a method of manufacturing the organic light-emitting diode: wherein A, Ar1, Ar2, n, m, and k are as described in the detailed description of the present invention.Type: ApplicationFiled: April 30, 2008Publication date: June 11, 2009Inventors: Dong-woo Shin, Myeong-suk Kim, Tae-woo Lee, Yu-jin Kim, Eun-sil Han, Woon-jung Paek, Yu-ri Choi, Byoung-ki Choi, Tae-yong Noh, O-hyun Kwon, Haa-jin Yang, Young-mok Son
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Publication number: 20090143376Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: March 3, 2006Publication date: June 4, 2009Applicant: Sitris Pharmaceuticals, Inc.Inventors: Michael Milburn, Jill Milne, Jean Bemis, Joseph J. Nunes, Roger Xie, Karl D. Nomington, Chi B. Vu
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Publication number: 20090124814Abstract: Provided are processes for preparing telmisartan-alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel.Type: ApplicationFiled: January 12, 2009Publication date: May 14, 2009Inventors: Nurit Perlman, Eyal Gilboa
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Patent number: 7514569Abstract: A benzimidazolone compound represented by a general formula (1), (in the formula, each of R1, R2, R3 and R4 represents independently a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, or an alkoxy group having 1 to 5 carbon atoms).Type: GrantFiled: December 7, 2004Date of Patent: April 7, 2009Assignee: Dainippon Ink and Chemicals, Inc.Inventor: Masaki Hosaka
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Publication number: 20090088570Abstract: An organic electroluminescent device, which has, between a pair of electrodes, at least one organic layer including a light-emitting layer, in which the organic layer contains a specific tetraphenylene compound, and in which the light-emitting layer contains a phosphorescent material; and a specific tetraphenylene compound that can be used in the device.Type: ApplicationFiled: November 20, 2008Publication date: April 2, 2009Applicant: FUJIFILM CORPORATIONInventors: Jun OGASAWARA, Tatsuya Igarashi, Satoshi Sano
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Patent number: 7503973Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale-sized pigment particles.Type: GrantFiled: March 7, 2008Date of Patent: March 17, 2009Assignee: Xerox CorporationInventor: Rina Carlini
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Patent number: 7501448Abstract: Provided are processes for preparing telmisartan alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel.Type: GrantFiled: October 13, 2005Date of Patent: March 10, 2009Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Nurit Perlman, Eyal Gilboa
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Patent number: 7485658Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.Type: GrantFiled: August 16, 2004Date of Patent: February 3, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Joshua Bolger, Arlindo L. Castelhano, Andrew Phillip Crew, Radoslaw Laufer, An-Hu Li, Colin Peter Sambrook Smith, Yingchuan Sun
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Publication number: 20090030057Abstract: The present invention provides a pharmaceutical composition of telmisartan comprising a) a telmisartan compound, b) a surfactant, c) a basic agent, and d) at least one diluent wherein the composition comprises less than 25% of water soluble diluents. The telmisartan compound is preferably present from about 12.5% to about 15.5%. At least one water insoluble diluent is preferred for use in the pharmaceutical composition in an amount from about 40% to about 70% of the total weight of the pharmaceutical composition. A preferred water insoluble diluent is microcrystalline cellulose. Also described are a pharmaceutical composition comprising telmisartan having a powder X-ray diffraction pattern, methods of preparing such pharmaceutical composition, and a crystalline form of Telmisartan.Type: ApplicationFiled: May 8, 2008Publication date: January 29, 2009Inventors: Shlomit Wizel, Gershon Kolatkar, Erela Zisman
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Patent number: 7482373Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: September 29, 2006Date of Patent: January 27, 2009Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Alan Bradley Fulp, Albert Michiel van Rhee, Kerry Leigh Spear
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Publication number: 20090023931Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.Type: ApplicationFiled: February 8, 2008Publication date: January 22, 2009Applicant: Ewha University - Industry Collaboration FoundationInventors: Kim Kwan Mook, Tang Lijun
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Publication number: 20090023932Abstract: The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-1H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole ii) Treating 4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4?-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent and isolating the ester as acid addition salt iii) Converting ester acid addition salt to Telmisartan dihydrochloride and iv) Converting Telmisartan dihydrochloride to Telmisartan.Type: ApplicationFiled: July 19, 2006Publication date: January 22, 2009Applicant: MATRIX LABORATORIES LTDInventors: Satyanarayana Chava, Seeta Ramanjaneyulu Gorantla, Sai Prasanna Ginjupalli
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Publication number: 20090011929Abstract: To provide a multinuclear complex including at least one ligand L satisfying the following requirements (i) r (ii) and (iii), and a plurality of metal atoms in a molecule: (i) having a group having polymerizable reactive multiple bonds, and/or a ring-opening polymerizable ring, (ii) having five or more coordination atoms bonding to the metal atoms, and (iii) being soluble in a solvent.Type: ApplicationFiled: February 7, 2007Publication date: January 8, 2009Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Takeshi Ishiyama, Hideyuki Higashimura
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Publication number: 20080284322Abstract: A novel nitrogen-containing heterocyclic compound having a specific structure and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer which comprises a single layer or a plurality of layers comprising at least a light emitting layer and is disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the above nitrogen-containing heterocyclic derivative singly or as a component of a mixture. The organic electroluminescence device exhibits a great luminance of emitted light and a great efficiency of light emission even under application of a low voltage.Type: ApplicationFiled: July 7, 2006Publication date: November 20, 2008Applicant: Idemitsu Kosan Co., Ltd.Inventors: Chishio Hosokawa, Hiroshi Yamamoto, Takashi Arakane
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Publication number: 20080221146Abstract: Nucleophosmin inhibitors are disclosed which inhibit the multimerization of nucleophosmin and the biological activity of nucleophosmin, such as the ability of nucleophosmin to inhibit apoptosis and inhibit cellular differentiation. These small molecule inhibitors are useful for treating diseases and disorders, such as cancer associated with dysregulated nucleophosmin expression. Methods for identifying small molecule inhibitors of nucleophosmin involving multimerization sites for nucleophosmin are also disclosed.Type: ApplicationFiled: February 28, 2008Publication date: September 11, 2008Applicant: ARIZONA BOARD OF REG. ON BEHALF ON THE UNIV. OF AZInventors: Daruka Mahadevan, Wenquing Qi, Bogdan Olenyuk
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Patent number: 7388099Abstract: Provided are hydroxycucurbituril derivatives, their preparation methods and uses. The hydroxycucurbituril derivative is easy to further functionalize with enhanced solubility in common solvents, thereby providing wider applications.Type: GrantFiled: November 26, 2002Date of Patent: June 17, 2008Assignee: POSTECH FoundationInventors: Ki-Moon Kim, Sang Yong Jon, Narayanan Selvapalam, Dong Hyun Oh
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Patent number: 7371870Abstract: There are provided benzimidazolone compounds that provide a plurality of hues from a single structural formula, and are useful as pigments that offer superior dispersibility in binder resins, as well as benzimidazolone compounds that are useful as pigments, and show minimal flocculation when pigments of two or more different hues are blended together to produced a desired hue. A benzimidazolone compound represented by a general formula (1) shown below. (wherein, R1, R2, R3 and R4 each represent, independently, a hydrogen atom, an alkyl group of 1 to 5 carbon atoms, or an alkoxy group of 1 to 5 carbon atoms, and R5 and R6 each represent, independently, an alkyl group of 1 to 5 carbon atoms).Type: GrantFiled: June 23, 2004Date of Patent: May 13, 2008Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Masaki Hosaka, Toshio Takei
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Patent number: 7345090Abstract: The invention relates to compounds of the formula I where R1, R2, R3, R4 and R5 have the meanings given in claim 1. The compound is suitable in particular for use in skin care compositions. They protect, firstly, against harmful oxidation reactions and, secondly, also act as UV filters.Type: GrantFiled: April 28, 2004Date of Patent: March 18, 2008Assignee: Merck Patent Gesellschaft mit Beschraenkter HaftungInventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
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Publication number: 20070259937Abstract: The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.Type: ApplicationFiled: May 2, 2007Publication date: November 8, 2007Inventors: Vincent L. Giranda, Thomas D. Penning, Virajkamar B. Gandhi, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong
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Publication number: 20070219240Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: March 14, 2007Publication date: September 20, 2007Applicant: WyethInventors: Derek Cecil Cole, Magda Asselin, Joseph Raymond Stock, Albert Jean Robichaud, Ji-In Kim, William Ronald Solvibile, Jonathan Laird Gross
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Publication number: 20070202357Abstract: An organic electroluminescent element comprises: a pair of electrodes; and one or more organic compound layers at least one of which is a light-emitting layer, the one or more organic compound layers being provided between the pair of electrodes, wherein at least one of the one or more organic compound layers comprises a compound represented by general formula (Z): wherein R31 and R32 each represents a hydrogen atom or a substituent, R3A represents a substituent other than an aromatic hetero ring connected through a nitrogen atom, or a hydrogen atom, X31 to X38 each represents a substituted or unsubstituted carbon atom or a nitrogen atom, and Y31 to Y33 each represents a nitrogen atom or C—R3B (wherein R3B represents a substituent other than an aromatic hetero ring connected through a nitrogen atom, or a hydrogen atom).Type: ApplicationFiled: February 23, 2007Publication date: August 30, 2007Applicant: FUJIFILM CorporationInventors: Itaru Osaka, Tatsuya Igarashi, Toshihiko Ise, Eiji Fukuzaki, Satoshi Sano
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Patent number: 7244847Abstract: The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods for using the same.Type: GrantFiled: February 6, 2002Date of Patent: July 17, 2007Assignee: Isis Pharmaceuticals, Inc.Inventors: Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
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Patent number: 7232912Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: April 22, 2005Date of Patent: June 19, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, III, Michael Brennan Wallace
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Patent number: 7193089Abstract: A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1?-methylbenzimidazol-2?-yl)benzimidazole with a compound of formula (IV) wherein Z is a leaving group, to obtain the compound 2-cyano-4?-[2?-n-propyl-4?-methyl-6?-(1??-methylbenzimidazol-2??-yl)benzimidazol-1?-ylmethyl]biphenyl, and subsequently hydrolyzing the nitrile function to obtain the acid function.Type: GrantFiled: March 17, 2004Date of Patent: March 20, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Rolf Dach, Helmut Heitger, Oliver Meyer
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Patent number: 7183279Abstract: The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities.Type: GrantFiled: May 25, 2006Date of Patent: February 27, 2007Assignee: University of OttawaInventors: Simon Lemaire, Irma Bernatchez-Lemaire, Hoang-Thanh Le
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Patent number: 7132439Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: May 13, 2003Date of Patent: November 7, 2006Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Alan B. Fulp, Albert M. van Rhee, Kerry L. Spear
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Patent number: 7118760Abstract: The present invention provides novel aryl benzimidazole sulfonic acid esters and cosmetic compositions that employ the novel aryl benzimidazole sulfonic acid esters as sunscreens. The cosmetic compositions can be water, organic solvent or emulsion based. Also provided are methods of using the compositions to protect skin from exposure to the sun, and optionally, repel insects.Type: GrantFiled: December 23, 2003Date of Patent: October 10, 2006Assignee: Avon Products, Inc.Inventors: Anthony D. Gonzalez, Andrew H. Pechko, Glen T. Anderson, Robert E. Kalafsky, Michael V. Lowenborg
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Patent number: 7074786Abstract: The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities.Type: GrantFiled: March 14, 2005Date of Patent: July 11, 2006Assignee: University of OttawaInventors: Simon Lemaire, Irma Bernatchez-Lemaire, Hoang-Thanh Le
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Patent number: 7002021Abstract: Diketopyrrolopyrroles of the formula (I): wherein R1, R2, R3 and R4 independently of one another are a C1–C4 alkyl radical or a substituted or unsubstituted phenyl radical, wherein the phenyl radical can be substituted by 1, 2, 3 or 4 substituents from the group C1–C4 alkyl, C1–C4 alkoxy, CN, F, Cl, Br, NO2, CF3, S—C1–C4 alkyl, phenyl or (C1–C2)alkylenephenyl, with the proviso that at least one of the radicals, R1, R2, R3, or R4, is one of the stated substituted or unsubstituted phenyl radicals.Type: GrantFiled: June 6, 2003Date of Patent: February 21, 2006Assignee: Clariant GmbHInventors: Felix W. Grimm, Hans Joachim Metz, Joachim Weber, Andreas Wacker
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Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6960591Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: July 4, 2001Date of Patent: November 1, 2005Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Patent number: 6849742Abstract: The present invention provides a binaphthol compound represented by formula [1]: and a salt thereof. The binaphthol compound of the present invention is useful for manufacturing antiseptic compounds or chiral catalysts. According to the method of the present invention, binaphthol compounds can be prepared in high yield with low cost.Type: GrantFiled: April 18, 2002Date of Patent: February 1, 2005Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
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Publication number: 20040236113Abstract: A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1′-methylbenzimidazol-2′-yl)benzimidazole with a compound of formula (IV) 1Type: ApplicationFiled: March 17, 2004Publication date: November 25, 2004Applicant: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Rolf Dach, Helmut Heitger, Oliver Meyer
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Publication number: 20040197697Abstract: Infrared absorbing compounds that absorb at 800 nm±50 nm and at 1050 nm±50 nm, the two different regions of the infrared spectrum typically used for imaging, are disclosed. Thermally imageable elements that comprise these infrared absorbing compounds can be imaged with radiation in either of these two regions of the infrared spectrum. The elements are especially useful as lithographic printing plate precursors.Type: ApplicationFiled: April 7, 2003Publication date: October 7, 2004Inventors: Lee Korionoff, Ting Tao, Kevin B. Ray