1,2-diazoles (including Hydrogenated) Patents (Class 546/275.4)
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Publication number: 20140323486Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: December 21, 2012Publication date: October 30, 2014Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
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Publication number: 20140323470Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: July 14, 2014Publication date: October 30, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
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Patent number: 8871796Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: October 5, 2010Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: William Colby Brown, Jason Brubaker, Christian Fischer, Richard W. Heidebrecht, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
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Publication number: 20140315913Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.Type: ApplicationFiled: March 11, 2014Publication date: October 23, 2014Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
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Publication number: 20140309109Abstract: The present invention relates to N-thio-anthranilamide compounds of the formula (I), the stereoisomers, the salts, the tautomers and the N-oxides thereof, wherein R1 is hydrogen, C1-C6-alkyl or C3-C8-cycloalkyl; R2 is hydrogen, halogen or cyano; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl or the like; R4 is halogen or C1-C6-haloalkyl; R5 is an optionally substituted C1-C10-alkyl, C3-C8-cycloalkyl, C2-C10-alkenyl, C2-C10-alkynyl, phenyl, heterocyclic ring or the like; L is an optionally substituted C1-C8-alkanediyl, C2-C8-alkenediyl, C2-C8-alkynediyl, C3-C8-cycloalkanediyl or the like; G is an optionally substituted C3-C8-cycloalkyl, phenyl, heterocyclic ring or the like; and k is 0 or 1.Type: ApplicationFiled: December 20, 2012Publication date: October 16, 2014Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Prashant Deshmukh, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
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Publication number: 20140309237Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Publication number: 20140290746Abstract: A photoelectric conversion element, having: an electrically-conductive support; a photoconductor layer having a semiconductor fine-particle layer adsorbed a dye; a charge transfer layer containing an electrolyte; and a counter electrode; which are provided on one side of the support in this order, in which the dye has at least one terdentate ligand having at least one acidic group; at least one ligand coordinating to a metal atom M has an sp2 carbon atom; a cyclic group binds to the sp2 carbon atom; a specific substituent R is substituted at an atom of ?- or ?-position to the atom of the cyclic group directly binding to the sp2 carbon atom; and with the metal atom M, an atom G1 of the ?- or ?-position, and an atom G2 of the substituent R, an angle ? (?ZMG1G2) is 150° or less.Type: ApplicationFiled: June 11, 2014Publication date: October 2, 2014Applicant: FUJIFILM CorporationInventors: Yukio TANI, Katsumi KOBAYASHI, Kimiatsu NOMURA
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Publication number: 20140296237Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: June 12, 2014Publication date: October 2, 2014Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
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Publication number: 20140296066Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: October 2, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
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Publication number: 20140288086Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Applicants: PFIZER INC., AGOURON PHARMACEUTICALS, INC.Inventors: Jingrong Jean CUI, Lee Andrew FUNK, Lei JIA, Pei-Pei KUNG, Jerry Jialun MENG, Mitchell David NAMBU, Mason Alan PAIRISH, Hong SHEN, Michelle TRAN-DUBE
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Publication number: 20140288041Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: May 12, 2014Publication date: September 25, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
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Publication number: 20140288129Abstract: Described herein are compounds of Formula (I-a) and (I-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Epizyme, Inc.Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Kevin Wayne Kuntz
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Publication number: 20140288128Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Epizyme, Inc.Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Oscar Miguel Moradei
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Publication number: 20140288084Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 28, 2012Publication date: September 25, 2014Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
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Patent number: 8841327Abstract: An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1, R2, X, Y, ring A, Z, R3 and R4 are as defined in the specification.Type: GrantFiled: September 23, 2011Date of Patent: September 23, 2014Assignee: Eisai R&D Management Co., Ltd.Inventors: Keigo Tanaka, Satoshi Inoue, Norio Murai, Masayuki Matsukura, Kazutaka Nakamoto, Shuji Shirotori, Shinya Abe
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Publication number: 20140275049Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.Type: ApplicationFiled: October 19, 2012Publication date: September 18, 2014Inventors: Thomas John Bleisch, David Andrew Coates, Norman Earle Hughes, Scott Alan Jones, Bryan Hurst Norman
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Publication number: 20140274692Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, a substituted phenol; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 is, for example, A1 is N or C—X, A3 is C—X, and A2, A4 and A5 are C—H, where X, is, for example, halogen; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: September 18, 2014Applicant: Syngenta Participations AGInventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch, Anna Kickova
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Publication number: 20140274961Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: Global Blood Therapeutics, Inc.Inventors: Brian W. Metcalf, Jason R. Harris, Zhe Li, Stephen L. Gwaltney, II
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Publication number: 20140274950Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: March 13, 2013Publication date: September 18, 2014Applicant: Medical University of South CarolinaInventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
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Publication number: 20140275176Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li, Brian W. Metcalf
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Publication number: 20140275152Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Brian W. Metcalf, Zhe Li
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Publication number: 20140275531Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
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Publication number: 20140256745Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: October 19, 2012Publication date: September 11, 2014Applicant: CalciMedica, Inc.Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
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Publication number: 20140256728Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.Type: ApplicationFiled: October 29, 2012Publication date: September 11, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
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Publication number: 20140256771Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: October 19, 2012Publication date: September 11, 2014Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
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Patent number: 8829195Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: GrantFiled: May 13, 2013Date of Patent: September 9, 2014Assignee: Novartis AGInventors: Stephanie Kay Dodd, Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Publication number: 20140243197Abstract: The present invention relates to substituted carbamoylmethoxy and carbamoylmethylthio benzamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the carbamoylmethoxy- and carbamoylmethylthio-benzamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.Type: ApplicationFiled: August 17, 2012Publication date: August 28, 2014Applicant: BASF SEInventors: Prashant Deshmukh, Florian Kaiser, Karsten Körber, Markus Kordes, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
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Publication number: 20140243336Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
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Publication number: 20140243376Abstract: It relates to an anthranilonitrile compound, and to the process for preparing the said anthranilonitrile compound, and to its use. The anthranilonitrile compound has a chemical general formula (I). The compound of the general formula (I) has excellent pesticidal activity, can be used to control pests, and has more than 98% of mortality in 3 days to diamondback moth and pink borer.Type: ApplicationFiled: September 26, 2012Publication date: August 28, 2014Applicant: HANGZHOU UDRAGON CHEMICAL CO., LTD.Inventors: Liangzhong Xu, Hualong Wu, Xianguo Feng, Shukun Gao, Ying Shi, Zongling Han, Xiaowei Liu, Haifeng Fu, Jingjing Liang
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Publication number: 20140243338Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
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Publication number: 20140243337Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Patent number: 8815910Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: January 4, 2013Date of Patent: August 26, 2014Assignee: Ardelyx, Inc.Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
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Patent number: 8815772Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein L is —C(R12a)R12b—C(R13a)R13b—, wherein the carbon atom bonded to R12a and R12b is also bonded to the carboxamide nitrogen atom in Formula 1; or 1,2-phenylene optionally substituted with up to 4 substituents independently selected from halogen and C1-C2 alkyl; and A, Z, R1, R2, n, G and Q 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. Also disclosed are methods for controlling a phytophagous nematode comprising contacting the nematode or its environment with a nematocidally effective amount of a compound of Formula 1 wherein L is —C(R12a)R12b—C(R13a)R13b; and A, Z, R1, R2, n, G and Q are as defined in the disclosure.Type: GrantFiled: June 19, 2013Date of Patent: August 26, 2014Assignee: E I du Pont de Nemours and CompanyInventors: James Francis Bereznak, Steven Gutteridge, Ravisekhara P Reddy, Andrew Edmund Taggi, Matthew James Campbell, Moumita Kar, Johan A. J. Desaeger
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Publication number: 20140235865Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilic acid diamide derivatives of the formula (1) in which R1, R2, R3, R4, Q and Z have the meanings given in the description, by reacting pyrazole acids with anthranilic esters.Type: ApplicationFiled: July 5, 2012Publication date: August 21, 2014Applicant: Bayer Intellectual Property GMBHInventors: Sergii Pazenok, Frank Volz, Norbert Lui, Arnd Neeff, Sylvia Szywalski
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Patent number: 8809378Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: August 19, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20140228358Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 14, 2014Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
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Publication number: 20140221374Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.Type: ApplicationFiled: March 16, 2012Publication date: August 7, 2014Applicant: Ruga CorporationInventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
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Publication number: 20140221362Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Patent number: 8796314Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: January 28, 2010Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
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Publication number: 20140213777Abstract: The present invention relates to organic compounds, usable as ligands in the preparation of lanthanide complexes or of certain water-soluble transition metals, a method for preparation thereof, and the use of said organic compounds as fluorescent probes.Type: ApplicationFiled: September 20, 2012Publication date: July 31, 2014Inventors: Raymond Ziessel, Mathieu Starck, Alexandra Sutter
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Publication number: 20140213568Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 22, 2014Publication date: July 31, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8791144Abstract: The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I) Wherein R1, R2, R3, R4, R5, R6 have the meaning defined in the claims. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: GrantFiled: September 16, 2010Date of Patent: July 29, 2014Assignee: Janssen Pharmaceutica NVInventors: Gregor James Macdonald, Johannes Wilhelmus John F. Thuring, Frans Alfons Maria Van den Keybus, Yves Emiel Maria Van Roosbroeck
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Patent number: 8791091Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.Type: GrantFiled: November 29, 2012Date of Patent: July 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
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Patent number: 8791139Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: GrantFiled: June 14, 2011Date of Patent: July 29, 2014Assignee: Bayer Cropscience AGInventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christian Funke, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Tetsuya Murata
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Patent number: 8791143Abstract: The present invention relates to novel anthranilic diamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: GrantFiled: June 14, 2011Date of Patent: July 29, 2014Assignee: Bayer Cropscience AGInventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
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Publication number: 20140206676Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: January 12, 2013Publication date: July 24, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Patent number: 8785646Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.Type: GrantFiled: January 18, 2013Date of Patent: July 22, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshihiko Nokura, Hiroshi Ikegami, Markus Jachmann
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Patent number: 8785468Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.Type: GrantFiled: February 12, 2010Date of Patent: July 22, 2014Assignee: Amgen Inc.Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, XianYun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
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Patent number: 8785489Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: GrantFiled: October 13, 2009Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Patent number: 8785632Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: GrantFiled: June 29, 2012Date of Patent: July 22, 2014Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube