Unsaturated Hetero Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/167)
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Publication number: 20110045101Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is Q2 or R1; X is N, CR2 or CQ3; Y is N or CR3; Z is N or CR4; and Q1, Q2, Q3, R1 R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: May 7, 2009Publication date: February 24, 2011Applicant: E.I. Du Pont De Nemours and CompanyInventors: Thomas Paul Selby, James Francis Bereznak, John Joseph Bisaha, Amy X. Ding, Mary Ann Hanagan, Jeffrey Keith Long, Andrew Edmund Taggi, Vijayagopal Gopalsamuthiram
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Publication number: 20110039864Abstract: Disclosed herein is an alpha-adrenergic compound having a structure. Therapeutic methods, compositions, and medicaments for treating pain are also disclosed herein.Type: ApplicationFiled: August 14, 2008Publication date: February 17, 2011Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
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Publication number: 20110039889Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: April 29, 2009Publication date: February 17, 2011Inventors: Colin David Eldred, Jag Paul Heer, Thomas Daniel Heightman, John Skidmore, Hailong Wang
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Patent number: 7884114Abstract: The present invention relates to a compound which is N-(4-{4-[(6-butyl-8-quinolinyl)oxy]-1-piperidinyl}butyl)ethanesulfonamide and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various diseases, such as allergic rhinitis.Type: GrantFiled: August 13, 2008Date of Patent: February 8, 2011Assignee: Glaxo Group LimitedInventors: Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Panayiotis Alexandrou Procopiou, Sadie Vile
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Publication number: 20110028465Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: January 9, 2009Publication date: February 3, 2011Inventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
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Publication number: 20110028482Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: ApplicationFiled: May 18, 2010Publication date: February 3, 2011Applicant: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Patent number: 7879882Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.Type: GrantFiled: October 6, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
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Publication number: 20110016642Abstract: The present invention relates to the dyeing of keratin materials using two colorless dye precursors, at least one of which contains a disulfide/thiol unit, said precursors reacting together chemically to form the color in situ. The process according to the invention makes it possible in the context of certain variants to solve the problems caused by the color generated during the process, while at the same time not degrading the efficacy of the coloration, and especially of the lightening effect. The colorations obtained are moreover powerful, chromatic, sparingly selective, and fast with respect to external agents such as sunlight, perspiration and especially shampoo.Type: ApplicationFiled: September 23, 2008Publication date: January 27, 2011Inventors: Andrew Greaves, Nicolas Daubresse
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Publication number: 20110021563Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.Type: ApplicationFiled: November 18, 2008Publication date: January 27, 2011Applicants: Howard Florey Institute, St. Vincent's Institute of Medical ResearchInventors: Siew Yeen Chai, Michael William Parker, Anthony Lloyd Albiston, Frederick A.O. Mendelsohn, Keith Geoffrey Watson
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Patent number: 7875618Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.Type: GrantFiled: November 25, 2008Date of Patent: January 25, 2011Assignees: Wyeth, elbion GmbHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Höfgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
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Patent number: 7872010Abstract: Provided herein are compositions of a class of substituted diazabicycloalkane derivative compounds, which are useful as modulators of nicotinic acetylcholine receptors. The compounds are useful in treating conditions and disorders prevented by, or ameliorated by, nicotinic acetylcholine receptors.Type: GrantFiled: June 3, 2008Date of Patent: January 18, 2011Assignee: Abbott LaboratoriesInventors: Jennifer M. Frost, Jianguo Ji, Tao Li, Diana L. Nersesian, Karin R. Tietje
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Publication number: 20110009401Abstract: The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: February 19, 2009Publication date: January 13, 2011Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20110009410Abstract: The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: July 12, 2010Publication date: January 13, 2011Applicant: Gilead Sciences, Inc.Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Publication number: 20110006295Abstract: A compound of the formula R1(CR3?CR4)nAr(CR4?CR3)nR2 wherein: n is 0 or 1; Ar represents aryl or heteroaryl having 1-5 aromatic rings which may be chain or fused or a combination of chain and fused, which may be substituted with alkoxy, fluoro, fluoroalkyl or cyano and which in the case of a 5-membered ring nitrogen heteroatom may be N-substituted with aryl or substituted aryl optionally further substituted with alkoxy, fluoro, fluoroalkyl or cyano; R1 and R2 independently represent aryl or nitrogen, oxygen or sulphur-containing heteroaryl having two to four fused aromatic rings one of which may be 5-membered and optionally substituted by aryl or heteroaryl having 1-5 chain or fused aromatic rings which may be further substituted with alkoxy, fluoro, fluoroalkyl or cyano; and R3 and R4 independently represent hydrogen, methyl, ethyl or benzyl.Type: ApplicationFiled: February 24, 2009Publication date: January 13, 2011Inventors: Poopathy Kathirgamanathan, Sivagnanasundram Surendrakumar
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Patent number: 7868174Abstract: The present disclosure relates to an improved process for the preparation of enantiomerically enriched alcohols of Formula (I), from the corresponding ketone of Formula (II), by asymmetric transfer hydrogenation, using a hydrogen donor, catalyzed by a ruthenium or rhodium complex of an optically active N-sulfamoyl-1,2-diamine. R is as defined herein.Type: GrantFiled: July 21, 2005Date of Patent: January 11, 2011Assignee: Pliva-Istrazivanje I Razvoj d.o.o.Inventors: Amir Avdagic, Barbara Mohar, Damjan Sterk, Michel Stephan
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Publication number: 20110003780Abstract: The present invention relates to the compound of the Formula I: and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form.Type: ApplicationFiled: July 3, 2008Publication date: January 6, 2011Applicant: SCHERING CORPORATIONInventor: Man Zhu
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Publication number: 20100311773Abstract: Disclosed are novel anabaseine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.Type: ApplicationFiled: December 30, 2009Publication date: December 9, 2010Applicant: Cornerstone Therapeutic, Inc.Inventors: Gregory J. Habgood, Daniel Elbaum
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Publication number: 20100311741Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. 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, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.Type: ApplicationFiled: May 16, 2008Publication date: December 9, 2010Applicant: INHIBOX LTD.Inventors: Aigars Jirgensons, Gundars Leitis, Ivars Kalvinsh, Daniel Robinson, Paul Finn, Nagma Khan
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Publication number: 20100311736Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.Type: ApplicationFiled: October 22, 2008Publication date: December 9, 2010Inventors: Nicholas D. Adams, Michael Gerard Darcy, Neil W. Johnson, Jiri Kasparec, Steven David Knight, Kenneth Allen Newlander, Xin Peng, Lance H. Ridgers
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Patent number: 7847101Abstract: Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.Type: GrantFiled: July 23, 2003Date of Patent: December 7, 2010Assignee: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Publication number: 20100292481Abstract: A method for producing a conjugated aromatic compound comprising reacting an aromatic compound (A) wherein one or two leaving groups are bonded to an aromatic ring with an aromatic compound (A) having the same structure as that of the above-mentioned aromatic compound (A) or an aromatic compound (B) being structurally different from the above-mentioned aromatic compound (A) and having one or two leaving groups bonded to an aromatic ring, in the presence of a nickel compound, a ligand, a manganese salt and a metal reducing agent.Type: ApplicationFiled: December 17, 2008Publication date: November 18, 2010Inventors: Seiji Oda, Takashi Kamikawa
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Patent number: 7834030Abstract: The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: March 26, 2008Date of Patent: November 16, 2010Assignee: Sanofi-AventisInventors: Stefanie Keil, Patrick Bernardelli, Matthias Urmann, Hans Matter, Wolfgang Wendler, Maike Glien, Karen Chandross, Lan Lee
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Patent number: 7834029Abstract: A compound according to formula II and the pharmaceutically acceptable salts thereof and the method of treating cancer in a patient in need thereof by administration of said compound.Type: GrantFiled: July 25, 2007Date of Patent: November 16, 2010Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Jason Scott Sawyer, Jonathan Michael Yingling
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Publication number: 20100279868Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.Type: ApplicationFiled: June 26, 2008Publication date: November 4, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Christopher John Mathews, Steve Smith, John Benjamin Taylor, Mangala Govenkar
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Publication number: 20100273774Abstract: A compound of formula (I), wherein R, R1, R2, ring A, which ring contains one or two nitrogen atoms, and ring B are as defined in the Specification, pharmaceutical compositions containing these compounds, and uses for these compounds and compositions, in particular, in transplantation.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100249176Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: October 23, 2008Publication date: September 30, 2010Inventors: James C. Barrow, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20100239496Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: March 23, 2010Publication date: September 23, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharia, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
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Publication number: 20100240620Abstract: The present application relates to novel aryl-substituted 3-cyano-5-thiazolyl- and 3-cyano-5-thiadiazolyl-1,4-dihydropyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: ApplicationFiled: September 8, 2007Publication date: September 23, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lars Barfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche
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Publication number: 20100234344Abstract: The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.Type: ApplicationFiled: March 22, 2008Publication date: September 16, 2010Applicant: JERINI AGInventors: Christoph Gibson, Thomas Tradler, Karsten Schinatbaum, Jochen Pfeifer, Elsa Locardi, Dirk Scharn, Mathias Paschke, Ulf Reimer, Uwe Richter, Gerd Hummel, Ulrich Reineke
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Publication number: 20100234219Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 28, 2006Publication date: September 16, 2010Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Publication number: 20100227331Abstract: The present invention provides methods for determining the presence of immobilized nucleic acid employing unsymmetrical cyanine dyes that are derivatives of thiazole orange, a staining solution and select fluorogenic compounds that are characterized as being essentially non-genotoxic. The methods comprise immobilizing nucleic acid, single or double stranded DNA, RNA or a combination thereof, on a solid or semi solid support, contacting the immobilized nucleic acid with an unsymmetrical cyanine dye compound and then illuminating the immobilized nucleic acid with an appropriate wavelength whereby the presence of the nucleic acid is determined. The cyanine dye compounds are typically present in an aqueous staining solution comprising the dye compound and a tris acetate or tris borate buffer wherein the solution facilitates the contact of the dye compound and the immobilized nucleic acid.Type: ApplicationFiled: May 12, 2010Publication date: September 9, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Matthew Paul BEAUDET, W. Gregory Cox, Stephen Yue
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Patent number: 7781438Abstract: A compound of formula (I) wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.Type: GrantFiled: July 10, 2006Date of Patent: August 24, 2010Assignee: Novartis AGInventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Publication number: 20100210685Abstract: The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Inventors: Timothy Birkinshaw, Roger Bonnert, Tony Cook, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
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Publication number: 20100210577Abstract: Disclosed are methods for the prevention or treatment of tuberculosis in a subject infected with Mycobacterium tuberculosis by administering rhodanine derivatives of formula (I), as well as some novel such compounds. Other embodiments are also disclosed.Type: ApplicationFiled: June 8, 2007Publication date: August 19, 2010Inventors: Jasbir Singh, Carl F. Nathan, Ruslana Bryk, Raghu Samy, Krzysztof Pupek, Mark Gurney
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Patent number: 7777040Abstract: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents.Type: GrantFiled: May 2, 2006Date of Patent: August 17, 2010Assignee: CGI Pharmaceuticals, Inc.Inventors: Scott A. Mitchell, Mihaela Diana Danca, Peter A. Blomgren, David R. Brittelli, Pavel Zhichkin, Matthew E. Voss
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Patent number: 7776883Abstract: Novel quinoline inhibitors of retroviral integrase, particularly HIV-1 integrase. The quinoline inhibitors are oxoquinolines that can be used for preventing or treating AIDS or HIV infection in a subject.Type: GrantFiled: March 9, 2005Date of Patent: August 17, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Roberto Di Santo, Yves Pommier, Christophe Marchand, Marino Artico, Roberta Costi
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Publication number: 20100204219Abstract: The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R1, R2 represent independently from one another hydrogen, a halogen atom, a hydroxyl group, a C1-C3 alkyl group and a C1-C3 alkoxy group, R3 represents, independently from one another if p is not 0, hydrogen, halogen, a C1-C5 linear or branched alkyl, a carboxylyl, a carbomethoxyl, carboethoxyl, a benzyl, an acyl, a hydroxyl, a C1-C4 linear or branched alkoxyl, a trifluoromethyl, a cyano, a morpholino, a 1,3-dioxolyl, an N-acetylamidyl or an amidoyl group, a saturated 5-8 membered ring, a heterocyclic ring, optionally substituted by a C1-C3 alkyl, a hydroxyl or a benzyl group, a C1-C6 alkylsulfonyl, a mono or disubstituted C1-C5 alkyl group, a branched or a cyclic amine, R6 is H or part of a alicyclic, heteroalicyclic ring system, if m is 0 then C represents CF3 or a branched or unbranched C1-C4 alkyl group, if m=1Type: ApplicationFiled: December 11, 2007Publication date: August 12, 2010Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Guy Lemaillet, Leonardo Scapozza
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Publication number: 20100193773Abstract: 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.Type: ApplicationFiled: April 7, 2010Publication date: August 5, 2010Applicant: Idemitsu Kosan Co., Ltd,Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
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Patent number: 7754735Abstract: The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.Type: GrantFiled: May 27, 2003Date of Patent: July 13, 2010Assignee: AstraZeneca ABInventors: Timothy Birkinshaw, Roger Bonnert, Tony Cook, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
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Publication number: 20100168159Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.Type: ApplicationFiled: January 29, 2010Publication date: July 1, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Masataka Morita, Sunao Imada, Yoshito Abe, Hiromichi Itani, Tatsuaki Morokata, Hideo Tsutsumi
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Publication number: 20100152112Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: May 16, 2008Publication date: June 17, 2010Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerard Darcy, Carla A. Donatelli, Steven David Knight
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Publication number: 20100137590Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: ApplicationFiled: February 2, 2010Publication date: June 3, 2010Applicant: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha De La Rosa, Zhi Hong, Stanley Lang
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Publication number: 20100130738Abstract: It is to provide a novel pyrazolone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1,R2: C1-6 alkyl; R3,R4: H, X, C1-6 alkoxy; Z:O, S; A:AA, BB, wherein AA represents wherein BB represents wherein R5: H, C1-6 alkyl; R6,R7: C1-6 alkyl.Type: ApplicationFiled: June 18, 2008Publication date: May 27, 2010Inventors: Yasushi Kohno, Koji Ochiai, Satoshi Takita, Tetsuya Kishi
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Publication number: 20100125091Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: November 12, 2009Publication date: May 20, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
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Publication number: 20100120854Abstract: The present invention provides crystalline 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate.Type: ApplicationFiled: June 29, 2006Publication date: May 13, 2010Applicant: ELI LILLY AND COMPANYInventor: Sreenivasa Reddy Mundla
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Publication number: 20100105726Abstract: The present invention relates to a pharmaceutical composition comprising compound for induction of apoptosis, a method for inducing cancer cell apoptosis, a method to suppress lymphocyte activation, a method to improve intracellular trafficking of misfolded mutants and a screening method to identify additional compounds useful for inducing apoptosis, and more specifically, it relates to pharmaceutical compositions comprising imidazole derivatives as active gradients for induction of apoptosis to treat various diseases including cancers and immune-related diseases, the method of inducing apoptosis by treating cancer cells with the said pharmaceutical composition, the method of inactivating human lymphocytes by treating lymphocytes with the said pharmaceutical composition, the method of improving intracellular trafficking of misfolded mutants by treating cells containing the mutants with the said pharmaceutical composition, and the screening method for identifying additional compound useful for inducing apoptosType: ApplicationFiled: February 26, 2007Publication date: April 29, 2010Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventors: In-Jae Shin, Myung-ryul Lee, Darren Williams
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Publication number: 20100105729Abstract: Disclosed herein are potent and selective aryl-substituted heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.Type: ApplicationFiled: September 20, 2007Publication date: April 29, 2010Applicant: KALYPSYS, INC.Inventors: Steven P. Govek, Guy Oshiro, Stewart A. Noble, James W. Malecha, Andrew K. Shiau