Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Morpholine Ring Patents (Class 514/237.5)
  • Patent number: 8501812
    Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: August 6, 2013
    Assignee: University of Massachusetts
    Inventors: Roger J. Davis, Anja Jaeschke
  • Publication number: 20130189228
    Abstract: This invention provides compounds of Formula 1, N-oxides and suitable salts thereof wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H; C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, C3-C5 cycloalkyl, or C4-C6 cycloalkylalkyl, each optionally substituted with one substituent selected from the group consisting of halogen, CN, SMe, S(O)Me, S(O)2Me, and OMe; R5 is H or Me; R6 is H, F or Cl; and R7 is H, F or Cl. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula 1, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: E I DU PONT DE NEMOURS AND COMPANY
  • Patent number: 8492365
    Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: July 23, 2013
    Assignees: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
  • Publication number: 20130178457
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Application
    Filed: July 5, 2012
    Publication date: July 11, 2013
    Applicant: LUPIN LIMITED
    Inventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
  • Publication number: 20130172355
    Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.
    Type: Application
    Filed: February 6, 2013
    Publication date: July 4, 2013
    Applicant: NATIONAL SUN YAT-SEN UNIVERSITY
    Inventor: NATIONAL SUN YAT-SEN UNIVERSITY
  • Publication number: 20130165443
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: August 23, 2012
    Publication date: June 27, 2013
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20130158035
    Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.
    Type: Application
    Filed: August 23, 2011
    Publication date: June 20, 2013
    Applicant: Brigham Young University
    Inventor: Marc Hansen
  • Publication number: 20130158022
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Application
    Filed: May 14, 2010
    Publication date: June 20, 2013
    Applicant: CHINESE PLA GENERAL HOSPITAL
    Inventors: Kunlun He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Jie Wang, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Tang
  • Patent number: 8466281
    Abstract: The present invention is directed to 2,5-disubstituted morpholine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Broc Flores, John D. Schreier
  • Patent number: 8450525
    Abstract: Novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I).
    Type: Grant
    Filed: October 21, 2008
    Date of Patent: May 28, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Sridharan Rajagopal, Virendra Kachhadia, Thanasekaran Ponpandian, Abdul Raheem Keeri, Karnambaram Anandhan, Sriram Rajagopal, Rajendran Praveen, Prabhu Daivasigamani
  • Publication number: 20130129839
    Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.
    Type: Application
    Filed: September 1, 2011
    Publication date: May 23, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Vann Gregory, Steven Gutteridge, Andrew Edmund Taggi, James Francis Bereznak
  • Patent number: 8440854
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Melean Visnick
  • Publication number: 20130116256
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Application
    Filed: May 16, 2011
    Publication date: May 9, 2013
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Wu Zhong, Juan Liu, Lili Wang, Kunlun He, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Xin Li, Guoliang Hu
  • Publication number: 20130102609
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.
  • Publication number: 20130096126
    Abstract: A method for enhancing learning or memory of both in a mammal having impaired learning or emory of both from a neuro-degenerative disorder, which entails the step of administering at least one compound or a salt thereof which is a ?1-adrenergic receptor agonist, partial agonist or receptor ligand in an amount effective to improve the learning or memory or both of said mammal.
    Type: Application
    Filed: April 22, 2011
    Publication date: April 18, 2013
    Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Mehrdad Shamloo, Mehrdad Faizi, William Mobley
  • Patent number: 8420644
    Abstract: The present invention relates to the use of at least one compound of formula (I) below: or at least one of the pharmaceutically acceptable salts thereof, for the preparation of a medicament intended for the prevention or for the treatment of cerebral edemas.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: April 16, 2013
    Assignee: Biocodex
    Inventors: Marie-Emmanuelle Le Guern, Philippe Girard, Jean-Marie Gillardin, Laurence Berthon-Cedille, Bernard Hublot
  • Publication number: 20130072491
    Abstract: An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula).
    Type: Application
    Filed: August 31, 2012
    Publication date: March 21, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Reiko YASUDA, Yuzuru Eto, Yoshiro Kitahara
  • Publication number: 20130059853
    Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: April 28, 2011
    Publication date: March 7, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Simon Feldbaek Nielsen, Anne Marie Horneman, Jesper Lau, Jens Christian Hojland Larsen
  • Publication number: 20130035312
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 11, 2012
    Publication date: February 7, 2013
    Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.
    Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
  • Patent number: 8362075
    Abstract: Sulphones of formula (I) are disclosed for use in treatment of cancer.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: January 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Publication number: 20120329799
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more carboxamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. Group (A): a group consisting of thifluzamide, oxadixyl, pencycuron, benalaxyl-M, fenhexamid, furametpyr, isopyrazam, isotianil, mepronil, tecloftalam, boscalid, fluopyram, fluopicolide, carpropamid, diclocymet, mandipropamid, dimethomorph, flumorph, penthiopyrad, and bixafen.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 27, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20120329649
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
  • Publication number: 20120322799
    Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.
    Type: Application
    Filed: November 30, 2010
    Publication date: December 20, 2012
    Applicant: PHARMATROPHIX, INC.
    Inventor: Gopal Damodara
  • Publication number: 20120316138
    Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing obesity or diabetes, optionally in combination with a second treatment therapy such a diet restriction or an increase in duration or exertion in physical activity.
    Type: Application
    Filed: December 15, 2010
    Publication date: December 13, 2012
    Applicant: METABOLIC SOLUTIONS DEVELOPMENT COMPANY, LLC
    Inventors: Gerard R. Colca, Rolf F. Kletzien, Steven P. Tanis, Scott D. Larsen
  • Publication number: 20120308519
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: December 29, 2011
    Publication date: December 6, 2012
    Applicant: Siga Technologies, Inc.
    Inventors: Sean M. Amberg, Dongcheng Dai, Tove C. Bolken, Dennis E. Hruby
  • Publication number: 20120282345
    Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.
    Type: Application
    Filed: June 5, 2012
    Publication date: November 8, 2012
    Applicant: Bayer Intellectual Property GMBH
    Inventors: Koen Van Den Eynde, Wolfgang Thielert, Heike Hungenberg
  • Patent number: 8298992
    Abstract: A composition includes an agricultural component in an amount of at least about 27% by weight and a solvent composition in an amount not greater than about 55% by weight. The solvent composition includes an amide having a structure of Formula I: wherein R1 comprises a C3 to C15 hydrocarbon group, and wherein R2 and R3 comprise a C1 or higher hydrocarbon group.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: October 30, 2012
    Assignee: Huntsman Petrochemical LLC
    Inventors: Alan J. Stern, David Ferguson, Howard Stridde
  • Publication number: 20120270878
    Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: July 2, 2012
    Publication date: October 25, 2012
    Applicant: BAYER HEALTHERCARE LLC
    Inventors: Scott MILLER, Martin OSTERHOUT, Jacques DUMAS, Uday KHIRE, Timothy B. LOWINGER, William J. SCOTT, Roger A. SMITH, Jill E. WOOD, David E. GUNN, Holia HATOUM-MOKDAD, Marell RODRIGUEZ, Robert SIBLEY, Ming WANG, Tiffany TURNER, Catherine BRENNAN
  • Publication number: 20120270877
    Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
    Type: Application
    Filed: November 1, 2010
    Publication date: October 25, 2012
    Applicant: MannKind Corporation
    Inventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
  • Patent number: 8288426
    Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 16, 2012
    Assignee: Bayer CropScience AG
    Inventors: Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
  • Publication number: 20120252776
    Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: March 12, 2012
    Publication date: October 4, 2012
    Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
  • Publication number: 20120245137
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity, are disclosed. Specifically, a series of compounds containing aryl sulphone derivatives, as exemplified by Formula (I).
    Type: Application
    Filed: September 17, 2010
    Publication date: September 27, 2012
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Robert Galemmo, JR., Richard Holland, Yuanxi Zhou, Yongbao Zhu, Eric Simonson, Navjot Chahal, Mike Grimwood
  • Publication number: 20120220577
    Abstract: The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.
    Type: Application
    Filed: June 4, 2010
    Publication date: August 30, 2012
    Inventors: Markus Henrich, Angela Hansen, Jens Nagel, Valerjans Kauss, Jevgenijs Rozhkovs, Ginta Grunsteine, Dina Trifanova
  • Publication number: 20120214814
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 23, 2012
    Inventors: Eric Anderson, Xin Jiang, Melean Visnick
  • Publication number: 20120214782
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Heike NEUBAUER, Bernd NOSSE
  • Publication number: 20120214785
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
  • Publication number: 20120178732
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 6, 2011
    Publication date: July 12, 2012
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Patent number: 8216971
    Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: July 10, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
  • Publication number: 20120171183
    Abstract: This invention provides a composition comprising a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure, and an effective amount of at least one fungicide.
    Type: Application
    Filed: March 6, 2012
    Publication date: July 5, 2012
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 8202999
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 6, 2006
    Date of Patent: June 19, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Publication number: 20120101080
    Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
    Type: Application
    Filed: June 25, 2010
    Publication date: April 26, 2012
    Applicant: BioVersys AG
    Inventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
  • Publication number: 20120095003
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Application
    Filed: October 14, 2011
    Publication date: April 19, 2012
    Applicant: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Publication number: 20120088661
    Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) azolylmethyloxiranes of the general formula I wherein the variables have the meanings described in the application, 2) a fungicidal compound II, and 3) optionally a further fungicidal compound II, where the compounds II of components 2 and 3 independently of one another are selected from the group consisting of the compounds described in the application, with the proviso that components 2 and 3 are not identical, and to the use of the fungicidal mixtures for controlling phytopathogenic fungi and to the compositions comprising them.
    Type: Application
    Filed: June 15, 2010
    Publication date: April 12, 2012
    Applicant: BASF SE
    Inventors: Jochen Dietz, Egon Haden, Jens Renner, Sarah Ulmschneider, Alice Glättli, Marianna Vrettou-Schultes, Silke Stolz
  • Patent number: 8148414
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: April 3, 2012
    Assignee: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Publication number: 20120065206
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 15, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20120052019
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Application
    Filed: August 22, 2011
    Publication date: March 1, 2012
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20120046293
    Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 23, 2012
    Applicant: Merck Frosst Canada Ltd.
    Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Publication number: 20120046292
    Abstract: [Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.
    Type: Application
    Filed: April 19, 2010
    Publication date: February 23, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Tomoaki Kawano, Yasuhiro Yonetoku, Takeshi Hanazawa, Takahiro Nigawara, Hiroki Fukudome, Hiroshi Moritani
  • Publication number: 20120046291
    Abstract: The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).
    Type: Application
    Filed: November 2, 2007
    Publication date: February 23, 2012
    Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
  • Publication number: 20120046272
    Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Applicant: GRUNENTHAL GMBH
    Inventor: Ramesh SESHA