1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
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Patent number: 8901127Abstract: The present invention relates to the compounds of general formula I wherein R1 and R2 are defined as described hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the medicaments containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: GrantFiled: August 19, 2011Date of Patent: December 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Raimund Kuelzer
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Patent number: 8901313Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: GrantFiled: March 15, 2012Date of Patent: December 2, 2014Assignee: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
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Patent number: 8901124Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: January 10, 2013Date of Patent: December 2, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Michael Soth
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Publication number: 20140350026Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.Type: ApplicationFiled: November 9, 2012Publication date: November 27, 2014Inventors: Xianjin Luo, Weidong Ye
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Publication number: 20140350244Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: August 7, 2014Publication date: November 27, 2014Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN
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Publication number: 20140349973Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 10, 2012Publication date: November 27, 2014Applicant: Viamet Pharmaceuticals, IncInventors: William J. Hoekstra, Christopher M. Yates
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Publication number: 20140349990Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 20, 2014Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
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Patent number: 8895556Abstract: The invention relates to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.Type: GrantFiled: March 13, 2013Date of Patent: November 25, 2014Assignee: Critical Outcome Technologies Inc.Inventors: Wayne R. Danter, Cheuk Kun Lau
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Publication number: 20140343070Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Patent number: 8889677Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: January 11, 2013Date of Patent: November 18, 2014Assignee: Boehringer Ingellheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Patent number: 8889676Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-oxType: GrantFiled: March 28, 2012Date of Patent: November 18, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Markus Gude, Christian Hubschwerlen, Philippe Panchaud
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Publication number: 20140336165Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.Type: ApplicationFiled: November 14, 2012Publication date: November 13, 2014Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
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Publication number: 20140336381Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Gregor James Macdonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Publication number: 20140336168Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 13, 2014Inventor: AbbVie Inc.
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Publication number: 20140329825Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.Type: ApplicationFiled: November 26, 2012Publication date: November 6, 2014Applicant: NOVARTIS AGInventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
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Publication number: 20140329797Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 16, 2012Publication date: November 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
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Publication number: 20140329795Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, 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 neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 28, 2012Publication date: November 6, 2014Inventors: Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson, Celia Dominguez, Leticia M. Toledo-Sherman, Ignacio Munoz
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Patent number: 8877742Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.Type: GrantFiled: June 8, 2012Date of Patent: November 4, 2014Assignee: GlaxoSmithKline Intellectual Property LimitedInventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
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Patent number: 8877780Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: May 30, 2008Date of Patent: November 4, 2014Assignee: Celgene CorporationInventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman, Hon-Wah Man, Weihong Zhang, Ehab M. Khalil
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Publication number: 20140323492Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: ApplicationFiled: May 23, 2011Publication date: October 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
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Publication number: 20140323300Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R1, R2, R3 and R4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.Type: ApplicationFiled: December 7, 2012Publication date: October 30, 2014Applicant: SYNGENTA LIMITEDInventors: William Guy Whittingham, Nicholas Phillip Mulholland, Russell Viner, Alison Clare Elliott, Katy Louise Bridgwood, John Martin Clough, Kevin Beautement, Glynn Mitchell, Gordon Munns
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Patent number: 8871760Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: GrantFiled: September 15, 2010Date of Patent: October 28, 2014Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
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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: 20140315912Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).Type: ApplicationFiled: July 18, 2011Publication date: October 23, 2014Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
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Patent number: 8865623Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: GrantFiled: January 6, 2010Date of Patent: October 21, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Patent number: 8859553Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.Type: GrantFiled: July 30, 2012Date of Patent: October 14, 2014Assignee: Astar Biotech LLCInventors: Chunrong Yu, Haihong Huang, Dongfeng Zhang, Peng Li
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Patent number: 8859591Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: GrantFiled: July 3, 2013Date of Patent: October 14, 2014Assignee: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20140303158Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: May 9, 2014Publication date: October 9, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Publication number: 20140303174Abstract: Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods of use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.Type: ApplicationFiled: August 2, 2012Publication date: October 9, 2014Applicant: THE BRIGHAM AND WOMEN S HOSPITAL, INC.Inventors: Gregory D. Cuny, Marcie Glicksman, Xeuchao Xing, Chien-Liang Glenn Lin
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Publication number: 20140303142Abstract: 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 28, 2012Publication date: October 9, 2014Inventors: John W. Butcher, David Witter, Christopher Dinsmore, June Kim, John Hendrix, Raksha Acharya, Sean P. Ahearn, Joon Jung, Alexey Rivkin, Philip Jones
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Publication number: 20140303139Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: August 31, 2012Publication date: October 9, 2014Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
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Patent number: 8853211Abstract: Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 10, 2009Date of Patent: October 7, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8853214Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents have the meanings as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: GrantFiled: March 21, 2011Date of Patent: October 7, 2014Assignee: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
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Patent number: 8853390Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.Type: GrantFiled: September 14, 2011Date of Patent: October 7, 2014Assignee: AbbVie Inc.Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
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Publication number: 20140296169Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 18, 2014Publication date: October 2, 2014Inventors: Hauke SZILLAT, Thomas LEEUW, Martin LORENZ
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Publication number: 20140296233Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicants: Sanofi, Celgene Avilomics Research, Inc.Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
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Publication number: 20140296203Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: ApplicationFiled: October 25, 2012Publication date: October 2, 2014Inventors: Jongwon Lim, Elizabeth Helen Kelley, Joey L. Methot, Hua Zhou, Alessia Petrocchi, Faruk Mansoor, Christian Fischer, Brendan O'Boyle, David Joseph Guerin, Corey E. Bienstock, Christopher W. Boyce, Matthew H. Daniels, Danielle Falcone, Ronald D. Ferguson, Salem Fevrier, Xianhai Huang, Kathryn Ann Lipford, David L. Sloman, Kevin Wilson, Wei Zhou, David Witter, Milana M. Maletic, Phieng Siliphaivanh
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Publication number: 20140296246Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicant: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Ruben Martinez, Samuel E. Metobo, Michael R. Mish, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
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Publication number: 20140296067Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has two or more substituents selected, for example, from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, and cyano; 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 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, 2014Applicants: SYNGENTA PARTICIPATIONS AG, University of ExeterInventors: Thomas Pitterna, Olivier Loiseleur, Paul Anthony Worthington, Anthony Cornelius O'Sullivan, Torsten Luksch, Vladimir Bobosik
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Publication number: 20140296245Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: October 2, 2014Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
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Patent number: 8846947Abstract: Provided herein are sirtuin-modulating compounds of formula (II). 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 relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: July 2, 2009Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 8846678Abstract: Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification.Type: GrantFiled: August 2, 2011Date of Patent: September 30, 2014Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Song Li, Hongliang Wang, Junhai Xiao, Xian Zhang, Lili Wang, Zhibing Zheng, Wu Zhong, Yunde Xie, Xingzhou Li, Xinbo Zhou, Guoming Zhao, Xiaokui Wang
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Patent number: 8846677Abstract: Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.Type: GrantFiled: May 15, 2012Date of Patent: September 30, 2014Assignee: High Point Pharmaceuticals, LLCInventors: Rolf Hohlweg, Knud Erik Andersen, Jan Lindy Sorensen, Jane Marie Lundbeck
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Publication number: 20140288070Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Chao Zhang, Ying Zhang
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Publication number: 20140288301Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
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Publication number: 20140288050Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: November 7, 2012Publication date: September 25, 2014Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
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Publication number: 20140288048Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20140288044Abstract: The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.Type: ApplicationFiled: April 12, 2012Publication date: September 25, 2014Applicant: Alzheimer's Institute of America, Inc.Inventors: Ryan Holcomb, Paul R. Sebahar, Kazuyuki Suzuki, Donald A. McLeod, David M. Dastrup, Christophe Hoarau, Robert J. Halter, Matthew Gregory Bursavich, Mark D. Shenderovich, Burt Richards, Paul L. Bartel
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Patent number: 8841310Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.Type: GrantFiled: October 7, 2009Date of Patent: September 23, 2014Assignee: Janssen R & D IrelandInventor: Paul Stoffels
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Patent number: 8841301Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: September 24, 2012Date of Patent: September 23, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, John E. Macor, Richard E. Olson, Christiana I. Iwuagwu, George N. Karageorge