Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 546/121)
  • Publication number: 20140336200
    Abstract: 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: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: ADAMED SP. Z O.O.
    Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
  • Publication number: 20140335019
    Abstract: 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: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
  • Publication number: 20140336190
    Abstract: 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: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: 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
  • Patent number: 8883819
    Abstract: 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: Grant
    Filed: August 30, 2012
    Date of Patent: November 11, 2014
    Assignees: IRM LLC, Novartis AG
    Inventors: 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
  • Publication number: 20140326987
    Abstract: 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: Application
    Filed: November 13, 2012
    Publication date: November 6, 2014
    Inventors: Junghwan Park, Sunhee Lee, Soungyun Mun, Daesung Kim, Hwasoon Jung, Wonsam Kim, Jihun Byun, Bumsung Lee
  • Patent number: 8877743
    Abstract: 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: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Patent number: 8871929
    Abstract: 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: Grant
    Filed: July 28, 2011
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Henry M. Vaccaro
  • Patent number: 8872163
    Abstract: 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: Grant
    Filed: August 20, 2009
    Date of Patent: October 28, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Masatoshi Saito, Yuki Nakano, Hiroaki Nakamura, Hirofumi Kondo
  • Patent number: 8871770
    Abstract: 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: Grant
    Filed: February 3, 2014
    Date of Patent: October 28, 2014
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Patent number: 8871754
    Abstract: 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: Grant
    Filed: November 18, 2013
    Date of Patent: October 28, 2014
    Assignees: IRM LLC, Novartis AG
    Inventors: 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
  • Publication number: 20140316133
    Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed.
    Type: Application
    Filed: March 17, 2014
    Publication date: October 23, 2014
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
  • Publication number: 20140315794
    Abstract: 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: Application
    Filed: November 21, 2013
    Publication date: October 23, 2014
    Applicant: MERIAL LIMITED
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
  • Publication number: 20140315945
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Publication number: 20140315876
    Abstract: ?-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: Application
    Filed: March 12, 2014
    Publication date: October 23, 2014
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8865734
    Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: October 21, 2014
    Assignees: Institut Pasteur Korea, Institut National de la Sante et de la Rech
    Inventors: 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
  • Patent number: 8865711
    Abstract: 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: Grant
    Filed: February 3, 2012
    Date of Patent: October 21, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
  • Publication number: 20140309210
    Abstract: 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: Application
    Filed: February 12, 2014
    Publication date: October 16, 2014
    Applicant: Genentech, Inc.
    Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
  • Patent number: 8859582
    Abstract: 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: Grant
    Filed: October 18, 2011
    Date of Patent: October 14, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Gordon Saxty, Valerio Berdini, Christopher William Murray, Charlotte Mary Griffiths-Jones, Emma Vickerstaffe, Gilbert Ebai Besong
  • Publication number: 20140303171
    Abstract: 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: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Publication number: 20140301999
    Abstract: 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: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20140303158
    Abstract: 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: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: 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
  • Publication number: 20140303140
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: October 9, 2014
    Applicant: GALAPAGOS NV
    Inventors: Nicolas DESROY, Bertrand HECKMANN, Reginald Christophe Xavier BRYS, Agnès Marie JONCOUR, Christophe PEIXOTO, Xavier Marie BOCK
  • Publication number: 20140303143
    Abstract: 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: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: 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
  • Publication number: 20140303150
    Abstract: 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: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Patent number: 8853403
    Abstract: 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: Grant
    Filed: December 7, 2012
    Date of Patent: October 7, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Publication number: 20140296526
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: May 10, 2014
    Publication date: October 2, 2014
    Applicant: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Publication number: 20140296283
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Publication number: 20140291654
    Abstract: 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: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
  • Patent number: 8846928
    Abstract: 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: Grant
    Filed: November 1, 2011
    Date of Patent: September 30, 2014
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Patent number: 8846672
    Abstract: 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: Grant
    Filed: December 16, 2011
    Date of Patent: September 30, 2014
    Assignee: Janssen R&D Ireland
    Inventors: 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
  • Publication number: 20140288064
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicant: WOCKHARDT LIMITED
    Inventors: 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
  • Publication number: 20140288051
    Abstract: 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: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Inventors: Samarendra N. MAlTI, Dai NGUYEN, Jehangir KHAN, Rong LING
  • Publication number: 20140288133
    Abstract: 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: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: JULIA CASTRO PICHEL, RAQUEL FERNANDEZ MENENDEZ, ESTHER PILAR FERNANDEZ VELANDO, SILVIA GONZALEZ DEL VALLE, ARACELI MALLO-RUBIO
  • Publication number: 20140288084
    Abstract: 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: Application
    Filed: October 28, 2012
    Publication date: September 25, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
  • Publication number: 20140288094
    Abstract: 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: Application
    Filed: September 17, 2012
    Publication date: September 25, 2014
    Inventors: 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
  • Publication number: 20140288082
    Abstract: 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: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Inventors: 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
  • Patent number: 8841455
    Abstract: 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: Grant
    Filed: December 20, 2010
    Date of Patent: September 23, 2014
    Assignee: 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
  • Publication number: 20140275065
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
  • Publication number: 20140275018
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: WOCKHARDT LIMITED
    Inventors: Mahesh Vithalbhai PATEL, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Snjeev Joshi
  • Publication number: 20140275527
    Abstract: 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: Application
    Filed: June 27, 2013
    Publication date: September 18, 2014
    Applicant: 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
  • Publication number: 20140275001
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: You Seok Hwang, Jian-Qiao Gu, Akash Jain, Sudhakar Garad, Jacob P. Sizemore
  • Publication number: 20140275152
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Brian W. Metcalf, Zhe Li
  • Patent number: 8835455
    Abstract: 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: Grant
    Filed: May 24, 2013
    Date of Patent: September 16, 2014
    Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
  • Patent number: 8835444
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
  • Publication number: 20140256736
    Abstract: 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: Application
    Filed: October 30, 2012
    Publication date: September 11, 2014
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
  • Publication number: 20140255392
    Abstract: 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: Application
    Filed: March 28, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marcus Koppitz, Ulrich Klar, Antje Margret Wengner, Roland Neuhaus, Gerhard Siemeister
  • Patent number: 8829191
    Abstract: 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: Grant
    Filed: June 15, 2012
    Date of Patent: September 9, 2014
    Inventors: 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
  • Publication number: 20140248646
    Abstract: 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: Application
    Filed: March 4, 2013
    Publication date: September 4, 2014
    Applicant: Indiana University Research and Technology Corporation
    Inventor: Indiana University Research and Technology Corporation
  • Publication number: 20140248240
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: September 4, 2014
    Inventors: 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
  • Publication number: 20140249177
    Abstract: 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: Application
    Filed: February 21, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: 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