Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 546/121)
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Publication number: 20140336200Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Applicant: ADAMED SP. Z O.O.Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
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Publication number: 20140335019Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.Type: ApplicationFiled: November 30, 2012Publication date: November 13, 2014Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
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Publication number: 20140336190Abstract: 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, R2, R2b, R3, R4a, R4b, and R5 are described herein.Type: ApplicationFiled: May 8, 2014Publication date: November 13, 2014Applicant: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
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Patent number: 8883819Abstract: Bicyclic heterocyclic derivatives of formula I useful in inhibiting PDGF receptor mediated biological activity. wherein A is and R1, R1a, R2, R3, R4, R5, R6 and X are as defined herein.Type: GrantFiled: August 30, 2012Date of Patent: November 11, 2014Assignees: IRM LLC, Novartis AGInventors: Ian Bruce, Sylvie Chamoin, Stephen Paul Collingwood, Pascal Furet, Vikki Furminger, Diana Janus, Sarah Lewis, Jon Christopher Loren, Valentia Molteni, Alex Michael Saunders, Duncan Shaw, Lilya Sviridenko, Christopher Thomson, Ryan West, Vince Yeh
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Publication number: 20140326987Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode. The organic material layer includes the compound represented by Formula 1. When the organic electric element includes the compound in the organic material layer, luminous efficiency, stability, and life span can be improved.Type: ApplicationFiled: November 13, 2012Publication date: November 6, 2014Inventors: Junghwan Park, Sunhee Lee, Soungyun Mun, Daesung Kim, Hwasoon Jung, Wonsam Kim, Jihun Byun, Bumsung Lee
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Patent number: 8877743Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: June 14, 2013Date of Patent: November 4, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8871929Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.Type: GrantFiled: July 28, 2011Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Tin-Yau Chan, Henry M. Vaccaro
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Patent number: 8872163Abstract: A compound for an organic thin film transistor having a structure represented by the following formula (1): wherein R1 and R2, and R3 and R4 are respectively combined with each other to form an aromatic hydrocarbon ring having 6 to 60 carbon atoms or an aromatic heterocyclic ring having 3 to 60 carbon atoms; the ring being fused to the ring to which the groups are bonded, whereby the structure of the formula (1) has 5 or more aromatic rings that are fused; and the fused rings formed by R1 and R2, and R3 and R4 each may have a substituent.Type: GrantFiled: August 20, 2009Date of Patent: October 28, 2014Assignee: Idemitsu Kosan Co., Ltd.Inventors: Masatoshi Saito, Yuki Nakano, Hiroaki Nakamura, Hirofumi Kondo
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Patent number: 8871770Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: February 3, 2014Date of Patent: October 28, 2014Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 8871754Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.Type: GrantFiled: November 18, 2013Date of Patent: October 28, 2014Assignees: IRM LLC, Novartis AGInventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan K S Yeung, Bin Zou, Venkatataiah Bollu
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Publication number: 20140316133Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed.Type: ApplicationFiled: March 17, 2014Publication date: October 23, 2014Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
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Publication number: 20140315794Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: ApplicationFiled: November 21, 2013Publication date: October 23, 2014Applicant: MERIAL LIMITEDInventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
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Publication number: 20140315945Abstract: The present invention relates to azole 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: March 14, 2014Publication date: October 23, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Publication number: 20140315876Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: ApplicationFiled: March 12, 2014Publication date: October 23, 2014Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Patent number: 8865734Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: GrantFiled: March 18, 2011Date of Patent: October 21, 2014Assignees: Institut Pasteur Korea, Institut National de la Sante et de la RechInventors: Zaesung No, Jaeseung Kim, Priscille Brodin, Min Jung Seo, Young Mi Kim, Jonathan Cechetto, Heekyoung Jeon, Auguste Genovesio, Saeyeon Lee, Sunhee Kang, Fanny Anne Ewann, Ji Youn Nam, Thierry Christophe, Denis Philippe Cedric Fenistein, Jamung Heo, Jang Jiyeon
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Patent number: 8865711Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: February 3, 2012Date of Patent: October 21, 2014Assignee: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Publication number: 20140309210Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.Type: ApplicationFiled: February 12, 2014Publication date: October 16, 2014Applicant: Genentech, Inc.Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
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Patent number: 8859582Abstract: The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, q, A, B, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: October 18, 2011Date of Patent: October 14, 2014Assignee: Astex Therapeutics LimitedInventors: Gordon Saxty, Valerio Berdini, Christopher William Murray, Charlotte Mary Griffiths-Jones, Emma Vickerstaffe, Gilbert Ebai Besong
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Publication number: 20140303171Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
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Publication number: 20140301999Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: June 23, 2014Publication date: October 9, 2014Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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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: 20140303140Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.Type: ApplicationFiled: March 12, 2014Publication date: October 9, 2014Applicant: GALAPAGOS NVInventors: Nicolas DESROY, Bertrand HECKMANN, Reginald Christophe Xavier BRYS, Agnès Marie JONCOUR, Christophe PEIXOTO, Xavier Marie BOCK
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Publication number: 20140303143Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
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Publication number: 20140303150Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.Type: ApplicationFiled: December 22, 2011Publication date: October 9, 2014Applicant: LEO Laboratories LimitedInventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
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Patent number: 8853403Abstract: To provide a novel heterocyclic compound having a bipolar property. To improve element characteristics of a light-emitting element by application of the novel heterocyclic compound to the light-emitting element. A heterocyclic compound represented by a general formula (G1) and a light-emitting element formed using the heterocyclic compound represented by the general formula (G1) are provided. When the heterocyclic compound represented by the general formula (G1) is used for the light-emitting element, the characteristics of the light-emitting element can be improved.Type: GrantFiled: December 7, 2012Date of Patent: October 7, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20140296526Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: May 10, 2014Publication date: October 2, 2014Applicant: WOCKHARDT LIMITEDInventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
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Publication number: 20140296283Abstract: The present invention relates to azole bicyclic heteroaryl 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: March 14, 2014Publication date: October 2, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Publication number: 20140291654Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 to R12 are defined as in the specification.Type: ApplicationFiled: June 12, 2014Publication date: October 2, 2014Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
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Patent number: 8846928Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: GrantFiled: November 1, 2011Date of Patent: September 30, 2014Assignee: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Patent number: 8846672Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: September 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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Publication number: 20140288064Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Applicant: WOCKHARDT LIMITEDInventors: Sachin BHAGWAT, Prasad Keshav DESHPANDE, Satish BHAWSAR, Vijaykumar Jagdishwar PATIL, Ravikumar TADIPARTHI, Shivaji Sampatrao PAWAR, Sunil Bhaginath JADHAV, Sanjay Kisan DABHADE, Vikas Vitthalrao DESHMUKH, Bharat DHOND, Satish BIRAJDAR, Mohammad Usman SHAIKH, Deepak DEKHANE, Piyush Ambalal PATEL
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Publication number: 20140288051Abstract: New bicyclic compounds, their preparation, and their use as antibacterial agents, either alone or in combination with an antibiotic for the treatment of infections caused by ?-lactamase-producing pathogenic bacteria, are described.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Inventors: Samarendra N. MAlTI, Dai NGUYEN, Jehangir KHAN, Rong LING
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Publication number: 20140288133Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3 alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Applicant: GLAXO GROUP LIMITEDInventors: JULIA CASTRO PICHEL, RAQUEL FERNANDEZ MENENDEZ, ESTHER PILAR FERNANDEZ VELANDO, SILVIA GONZALEZ DEL VALLE, ARACELI MALLO-RUBIO
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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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Publication number: 20140288094Abstract: This invention relates to pyrazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.Type: ApplicationFiled: September 17, 2012Publication date: September 25, 2014Inventors: D. Jonathan Bennett, Jaiqiang Cai, Emma Carswell, Andrew Cooke, Scott B. Hoyt, Clare London, John MacLean, Min K. Park, Paul Ratcliffe, Yusheng Xiong, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
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Publication number: 20140288082Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8841455Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.Type: GrantFiled: December 20, 2010Date of Patent: September 23, 2014Assignee: Array BioPharma Inc.Inventors: Mark Laurence Boys, Michael F. Bradley, Robert Kirk DeLisle, D. David Hennings, April L. Kennedy, Fredrik P. Marmsater, Matthew David Medina, Mark C. Munson, Bryson Rast, James P. Rizzi, Martha E. Rodriguez, George T. Topalov, Qian Zhao
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Publication number: 20140275065Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
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Publication number: 20140275018Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: WOCKHARDT LIMITEDInventors: Mahesh Vithalbhai PATEL, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Snjeev Joshi
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Publication number: 20140275527Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: ApplicationFiled: June 27, 2013Publication date: September 18, 2014Applicant: Exelixis, Inc.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20140275001Abstract: This disclosure provides compositions containing solid forms of sodium (2S,5R)-2-(1,3,4-oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl sulfate, and methods of manufacturing and using these compositions.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: You Seok Hwang, Jian-Qiao Gu, Akash Jain, Sudhakar Garad, Jacob P. Sizemore
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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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Patent number: 8835455Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.Type: GrantFiled: May 24, 2013Date of Patent: September 16, 2014Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
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Patent number: 8835444Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: GrantFiled: January 31, 2011Date of Patent: September 16, 2014Assignee: Novartis AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Publication number: 20140256736Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Applicant: XENON PHARMACEUTICALS INC.Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
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Publication number: 20140255392Abstract: The present invention relates to substituted imidazopyridine compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: March 28, 2012Publication date: September 11, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Antje Margret Wengner, Roland Neuhaus, Gerhard Siemeister
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Patent number: 8829191Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).Type: GrantFiled: June 15, 2012Date of Patent: September 9, 2014Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew John Phillips, Mahendra G. Dedhiya
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Publication number: 20140248646Abstract: A fluorophore and methods of detecting cations and hydrophobic environments using the fluorophore are disclosed. The fluorophore includes an imidazo[1,5-a]pyridinium ion core and has the formula where R1, R2, R3 and X? are as defined in the specification, and n is an integer from 1 to 4.Type: ApplicationFiled: March 4, 2013Publication date: September 4, 2014Applicant: Indiana University Research and Technology CorporationInventor: Indiana University Research and Technology Corporation
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Publication number: 20140248240Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: September 4, 2014Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Judith D. Kuntz, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
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Publication number: 20140249177Abstract: The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: February 21, 2014Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Ian BRUCE, Sylvie CHAMOIN, Stephen Paul COLLINGWOOD, Pascal FURET, Vikki FURMINGER, Sarah LEWIS, Jon Christopher LOREN, Lin LV, Valentina MOLTEN, Alex Michael SAUNDERS, Duncan SHAW, Roy Maxwell TURNER, Vince YEH