Additional Hetero Ring Which Is Unsaturated Patents (Class 544/333)
  • Compounds for use in treatment of mucositis
    Patent number: 8802683
    Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: August 12, 2014
    Assignee: Cellceutix Corporation
    Inventors: Richard W. Scott, Bozena Korczak
  • NOVEL 1,2- BIS-SULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
    Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Heterocyclic Compounds as Pesticides
    Publication number: 20140221362
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
  • Heteroaryls and uses thereof
    Patent number: 8796271
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Metalloenzyme inhibitor compounds
    Patent number: 8796001
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 5, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
  • Compound for an organic optoelectronic device, organic light emitting diode including the same, and display including the organic light emitting diode
    Patent number: 8796917
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode, and a display device, the compound being represented by the following Chemical Formula 1:
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: August 5, 2014
    Assignee: Cheil Industries, Inc
    Inventors: Dong-Min Kang, Myeong-Soon Kang, Nam-Soo Kim, Chang-Ju Shin, Nam-Heon Lee, Ho-Kuk Jung, Mi-Young Chae
  • Combination of a B-Raf inhibitor: N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1- dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide and the Akt inhibitor: N-{ (1S)-2-amino-1-[(3- fluorophenyl)methyl]ethyl}-5-chIoro-4-(4-chIoro- 1 -methyl- 1 H-pyrazol-5-yl)-2-10 thiophenecarboxamide useful in the treatment of cancer
    Patent number: 8796298
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: August 5, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
  • Pyrrolidine derivatives, pharmaceutical compositions and uses thereof
    Publication number: 20140213568
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 31, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Dihydropyrazoles
    Patent number: 8791114
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • ISOXAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS
    Publication number: 20140206606
    Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 24, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Voriconazole Immunoassays
    Publication number: 20140206020
    Abstract: Methods, compositions and kits are disclosed directed at voriconazole derivatives, immunogens, signal generating moieties, antibodies that bind voriconazole and immunoassays for detection of voriconazole.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Inventors: Johnny Valdez, SOON J. OH, BYUNG SOOK MOON
  • (1-AZINONE)-SUBSTITUTED PYRIDOINDOLES
    Publication number: 20140206696
    Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5 is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Peter GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG, Mark HADDEN, James GRABOWSKI, Alexander USYATINSKY
  • COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC LIGHT EMITTING DIODE INCLUDING THE SAME, AND DISPLAY INCLUDING THE ORGANIC LIGHT EMITTING DIODE
    Publication number: 20140203257
    Abstract: A compound for an organic optoelectronic device represented by Chemical Formula 1: wherein groups X1 to X8, Y1, Y2, L1, L2, Ar1, Ar2, and variables m1, m2, n1, and n2 are described in the specification.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 24, 2014
    Applicants: CHEIL INDUSTRIES INC., SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Kyu Young HWANG, O Hyun KWON, Young Kwon KIM, Hyeon Ho CHOI, Byoung Ki CHOI
  • ORGANIC ELECTROLUMINESCENT ELEMENT, MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENT, AND LIGTH EMITTING DEVICE, DISPLAY DEVICE AND LIGHTING DEVICE EACH USING ORGANIC ELECTROLUMINESCENT ELEMENT
    Publication number: 20140203252
    Abstract: An organic electroluminescent element which has a substrate, a pair of electrodes disposed on this substrate and composed of an anode and a cathode, and at least one organic layer disposed between these electrodes and including a light-emitting layer, and in which a compound expressed by General Formula 1-1 is contained in at least one layer of the aforementioned light-emitting layer(s) exhibits high luminous efficiency, excellent blue color purity, and little change in chromaticity accompanying drive deterioration.
    Type: Application
    Filed: June 5, 2012
    Publication date: July 24, 2014
    Applicant: UDC Ireland Limited
    Inventors: Tetsu Kitamura, Koji Takaku, Wataru Sotoyama, Yasunori Yonekuta, Toshihiro Ise, Saki Takada, Toru Watanabe
  • Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
    Patent number: 8785489
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • N-LINKED QUINOLINEAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20140200222
    Abstract: The present invention is directed to N-linked quinoline amide compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: July 17, 2014
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Zhi-Qiang Yang
  • Pyridinonyl PDK1 inhibitors
    Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Substituted heteroaryl inhibitors of B-RAF
    Patent number: 8778929
    Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
  • SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20140194445
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Pyrazolyl-Based Carboxamides I
    Publication number: 20140194443
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • DUAL-ACTING OXAZOLE ANTIHYPERTENSIVE AGENTS
    Publication number: 20140194426
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: October 24, 2013
    Publication date: July 10, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
  • TETRACYCLIC COMPOUNDS
    Publication number: 20140194414
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 10, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • ALKYNYL SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASES INHIBITORS
    Publication number: 20140194406
    Abstract: The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: July 18, 2012
    Publication date: July 10, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Jay Aaron Bertrand, Paola Gnocchi, Ilaria Motto, Marcella Nesi, Achille Panzeri, Paola Vianello
  • Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
    Patent number: 8772323
    Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
  • Azole Compounds as PIM Inhibitors
    Publication number: 20140187553
    Abstract: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 3, 2014
    Applicant: AMGEM INC.
    Inventors: Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L.M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
  • BENZIMIDAZOLE INHIBITORS OF THE SODIUM CHANNEL
    Publication number: 20140187533
    Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
  • Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer
    Patent number: 8765748
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Positive allosteric modulators of mGluR2
    Patent number: 8765767
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: July 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald J. Mattson, Zhaoxing Meng
  • 1-hydroxyimino-3-phenyl-propanes
    Patent number: 8765730
    Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: July 1, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
  • Carbazole compounds and therapeutic uses of the compounds
    Patent number: 8765738
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Incuron, LLC
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
    Patent number: 8765734
    Abstract: The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: July 1, 2014
    Assignee: Incyte Corporation
    Inventors: Taisheng Huang, Chu-Biao Xue, Hui-Yin Li, Qun Li
  • QUINOLONE COMPOUND
    Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Azabicycloalkane derivatives, preparation thereof and use thereof in therapy
    Patent number: 8759343
    Abstract: The invention relates to compounds of the general formula (I): wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: June 24, 2014
    Assignee: Sanofi
    Inventors: Omar Ben Ayad, Odile LeClerc, Alistair Lochead, Mourad Saady, Franck Slowinski, Julien Vache
  • Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
    Patent number: 8759377
    Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. 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: Grant
    Filed: November 23, 2010
    Date of Patent: June 24, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
  • SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS
    Publication number: 20140171450
    Abstract: The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, X and Y are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Application
    Filed: January 7, 2014
    Publication date: June 19, 2014
    Applicant: CONFLUENCE LIFE SCIENCES INC.
    Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas
  • TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
    Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS
    Publication number: 20140171449
    Abstract: The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, X and Y are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Application
    Filed: January 7, 2014
    Publication date: June 19, 2014
    Applicant: CONFLUENCE LIFE SCIENCES INC.
    Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas
  • INTEGRIN TARGETING AGENTS AND IN-VIVO AND IN-VITRO IMAGING METHODS USING THE SAME
    Publication number: 20140170066
    Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicants: Merck & Co., Inc., Visen Medical, Inc.
    Inventors: Milind Rajopadhye, Guojie Ho, Bohumil Bednar, Le T. Duong, Paul J. Coleman
  • Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones
    Publication number: 20140171451
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Applicant: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • DISUBSTITUTED OCTAHYDROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS
    Publication number: 20140171430
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 19, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
  • PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
    Publication number: 20140162874
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Maurice C. Yap, Ann M. Buysse, Daniel Knueppel, Yu Zhang, Negar Garizi, Noormohamed M. Niyaz, Christian T. Lowe, Ricky Hunter, Tony K. Trullinger, David A. Demeter, Dan Pernich, Carl DeAmicis, Ronald Ross, JR., Timothy C. Johnson
  • Carbazole Compounds For Delayed Fluorescence
    Publication number: 20140158992
    Abstract: Novel carbazole-containing compounds are provided. The novel compounds also contain electron donor groups, aryl linkers, and at least one nitrogen heterocycle. These novel organic compounds are useful in OLED devices and can exhibit delayed fluorescence.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 12, 2014
    Applicant: Universal Display Corporation
    Inventors: Chuanjun Xia, Chun Lin, Raymond Kwong, Scott Joseph, James Esler
  • COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC LIGHT EMITTING DIODE INCLUDING THE SAME, AND DISPLAY INCLUDING THE ORGANIC LIGHT EMITTING DIODE
    Publication number: 20140158999
    Abstract: Disclosed are a compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode. A compound for an organic optoelectronic device represented by Chemical Formula 1 provides an organic optoelectronic device having an excellent life-span and improved luminous efficiency at a low driving voltage due to excellent electrochemical and thermal stability.
    Type: Application
    Filed: July 11, 2013
    Publication date: June 12, 2014
    Inventors: Yong Sik JUNG, Ho Suk KANG, Hyeon Ho CHOI, Sang Mo KIM, Jhun Mo SON, Kyu Young HWANG
  • sGC stimulators
    Patent number: 8748442
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: June 10, 2014
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R Iyengar, Ara Mermerian, Angelika Fretzen
  • Inhibitors of diacylglycerol acyl transferase
    Patent number: 8748426
    Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Grant
    Filed: December 30, 2010
    Date of Patent: June 10, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
  • Metalloenzyme inhibitor compounds
    Patent number: 8748461
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: June 10, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
    Publication number: 20140155415
    Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 4, 2012
    Publication date: June 5, 2014
    Inventors: Michael David Bartberger, Michael D. Croghan, Christopher H. Fotsch, Mark H. Norman, Lewis Dale Pennington, Andreas Reichelt, David J. St. Jean, JR., Christopher M. Tegley
  • [1,2,4]Triazolo[1,5-a]Pyridine and [1,2,4]Triazolo[1,5-c]Pyrimidine Compounds and Their Use
    Publication number: 20140155594
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Application
    Filed: April 24, 2013
    Publication date: June 5, 2014
    Applicant: Cancer Research Technology Limited
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
  • Chemical Compounds - 759
    Publication number: 20140155394
    Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: June 21, 2013
    Publication date: June 5, 2014
    Applicant: Astrazeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20140155413
    Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze