The Five-membered Hetero Ring Consists Of One Nitrogen And Four Carbons Patents (Class 514/408)
Spiro ring system (Class 514/409)
Polycyclo ring system having the five-membered hetero ring as one of the cyclos (Class 514/410)
Additional hetero ring (Class 514/422)
C=x bonded directly to the five-membered hetero ring by nonionic bonding (x is chalcogen) (Class 514/423)
Chalcogen bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/424)
Nitrogen bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/426)
Two double bonds between ring members of the five-membered hetero ring (e.g., pyrrole, etc.) (Class 514/427)
Chalcogen bonded indirectly to the five-membered hetero ring by acyclic nonionic bonding (Class 514/428)
Carbocyclic ring bonded directly to the five-membered hetero ring (Class 514/429)
  • Nonpeptide HIV-1 protease inhibitors
    Patent number: 8791135
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: July 29, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Agonists of neurotrophin receptors and their use as medicaments
    Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Chemical compounds
    Patent number: 8772293
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: July 8, 2014
    Assignees: Pfizer Limited, Icagen Inc.
    Inventors: Alan Daniel Brown, Marcel John De Groot, Brian Edward Marron, David James Rawson, Thomas Ryckmans, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West
  • BENZOCYCLOHEPTANE AND BENZOXEPINE DERIVATIVES
    Publication number: 20140187557
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 3, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Inhibitors of cognitive decline
    Patent number: 8765816
    Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: July 1, 2014
    Assignee: Cognition Therapeutics, Inc.
    Inventors: Gilbert M. Rishton, Susan Catalano
  • N1-Cyclic Amine-N5-Substituted Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same
    Publication number: 20140179661
    Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: April 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • N1-Cyclic Amine-N5-Substituted Phenyl Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same
    Publication number: 20140179660
    Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: August 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Methods of treating pain
    Patent number: 8747844
    Abstract: The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Saint Louis University
    Inventor: Daniela Salvemini
  • Active compound combinations having insecticidal and acaricidal properties
    Patent number: 8722070
    Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (23) listed in the disclosure.
    Type: Grant
    Filed: May 16, 2013
    Date of Patent: May 13, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • USE OF POLYAMINOISOPRENYL DERIVATIVES IN ANTIBIOTIC OR ANTISEPTIC TREATMENT
    Publication number: 20140128335
    Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.
    Type: Application
    Filed: February 23, 2012
    Publication date: May 8, 2014
    Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE CORSE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Michel Bolla, Jean Michel Brunel, Joseph Pierre Felix Casanova, Vannina Lorenzi, Liliane Berti
  • Methods of treating fatty liver disease
    Patent number: 8716327
    Abstract: The disclosure provides methods for treating fatty liver disease and associated conditions by inhibiting the synthesis of glucosphingolipids, as exemplified by the use of glucosylceramide synthase substrate analogs.
    Type: Grant
    Filed: May 9, 2007
    Date of Patent: May 6, 2014
    Assignee: Genzyme Corporation
    Inventors: Hongmei Zhao, Nelson S. Yew, Seng H. Cheng, Canwen Jiang, Cynthia Marie Arbeeny
  • Compositions, methods and propellant-based systems for respiratory delivery of glycopyrrolate and one or more active agents
    Patent number: 8703806
    Abstract: Compositions, methods and systems are provided for pulmonary or nasal delivery of two or more active agents via a metered dose inhaler. In one embodiment, the compositions include a suspension medium, active agent particles, and suspending particles, in which the active agent particles and suspending particles form a co-suspension within the suspension medium.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: April 22, 2014
    Assignee: Pearl Therapeutics, Inc.
    Inventors: Reinhard Vehring, Michael Steven Hartman, David Lechuga-Ballesteros, Adrian Edward Smith, Vidya B. Joshi, Sarvajna Jumar Dwivedi
  • Estrogen receptor modulators and uses thereof
    Patent number: 8703810
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: April 22, 2014
    Assignee: Seragon Pharmaceuticals, Inc.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
  • Alpha-aminoamide derivatives useful in the treatment of addictive disorders
    Patent number: 8697738
    Abstract: Methods of using certain ?-aminoamide derivatives in the treatment of RLS and addictive disorders, The compounds of this invention are able to reduce or even stop the symptoms of RLS and addictive disorders substantially without side effects.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: April 15, 2014
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Claudia Besana, Elena Barbanti, Emanuela Izzo, Florian Thaler, Ruggero Fariello, Patricia Salvati, Luca Benatti
  • Solid compositions
    Patent number: 8686026
    Abstract: The present invention features solid compositions comprising amorphous Compound I. For instance, Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: April 1, 2014
    Assignee: AbbVie Inc.
    Inventors: Bernd Liepold, Tina Jung, Peter Hölig, Rudolf Schroeder, Nancy E. Sever, Justin S. Lafountaine, Brent D. Sinclair, Yi Gao, Jianwei Wu
  • Chemical compounds
    Patent number: 8685977
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 11, 2011
    Date of Patent: April 1, 2014
    Assignee: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Marcel John De Groot
  • Histone deacetylase inhibitors based simultaneously on trisubstituted 1-pyrroles and aromatic and heteroaromatic spacers
    Patent number: 8685992
    Abstract: The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein: R1 and R2 represent, independently, an optionally substituted C6-C10 aryl radical or an optionally substituted heteroaryl radical; A and M represent, independently, a methylene group or a single bond, in which case the adjacent aromatic ring would be attached directly to the amide group; the Y?Z group represents together and indistinctly an oxygen atom, a sulfur atom, a cis-vinylidene group, an imino group, or a methine group with a sp2-hybridized carbon atom; X represents indistinctly a methine group, a cis-vinylidene group or a nitrogen atom; and W represents a hydroxyl group, an optionally substituted C1-C6 alkyl group, an optionally substituted heteroaryl group or an optionally substituted C6-C10 aryl group; or a salt, solvate or prodrug thereof, as well as to the process for their preparation and the use thereof for the treatment of cancer.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: April 1, 2014
    Assignees: Universidad del País Vasco, Ikerschem, S.L.
    Inventors: Fernando Pedro Cossío Mora, Aizpea Zubia Olascoaga, Yosu Vara Salazar, Eider Ion San Sebastián Larzabal, Dorleta Otaegui Ansa, María del Carmen Masdeu Margalef, Eneko Aldaba Arévalo
  • Use of amisulpride as an anti-emetic
    Patent number: 8686019
    Abstract: Amisulpride is used in the therapy of nausea, vomiting or retches. The therapy may utilize a novel injectable formulation, in unit dosage form, comprising less than 50 mg amisulpride.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: April 1, 2014
    Assignee: Acacia Pharma Limited
    Inventors: Julian Clive Gilbert, Robert William Gristwood, Nicola Cooper, Gabriel Fox
  • Fluorescent probe
    Patent number: 8673957
    Abstract: A compound represented by the formula (I) wherein R1 and R2 represent amino groups that substitute at adjacent positions on the benzene ring, wherein one of the amino groups may have one alkyl group; R3 and R4 represent hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group, R5 and R8 independently represent a C1-6 alkyl group, R6 and R9 represent a carboxy-substituted C1-6 alkyl group, an alkoxycarbonyl-substituted C1-6 alkyl group, a sulfo-substituted C1-6 alkyl group, or an alkyl sulfonate-substituted C1-6 alkyl group, and R7 and R10 represent a C1-6 alkyl group, an aryl group, a C1-6 alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group, and an agent for measurement of nitrogen monoxide containing the compound. Said compound can give a fluorescent substance that is free from change in fluorescence intensity in a wide pH range.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: March 18, 2014
    Assignees: Tetsuo Nagano, Daiichi Pure Chemicals Co., Ltd.
    Inventors: Tetsuo Nagano, Yu Gabe, Yasuteru Urano
  • Injectable formulations containing asenapine and method of treatment using same
    Patent number: 8658687
    Abstract: The present invention provides a formulation comprising asenapine hemipamoate suspended particles, which formulation can be administered via a Depot provided by an IM injection of the formulation, and which depot does not display a particle-size dependent release rate. The present invention provides also methods of treatment using the same.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: February 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Werenfridus Adrianus Faassen, Gerardus Johannes Huissen Kemperman, Johannes Antonius Hendrikus van Laarhoven
  • Use of Aminoindane Compounds in Treating Overactive Bladder and Interstitial Cystitis
    Publication number: 20140051702
    Abstract: The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 20, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Sandeep Gupta, Tony Priestley, Nicholas James Laping
  • Bis-aryl sulfonamides
    Patent number: 8642808
    Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: February 4, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
  • Method of inhibiting apolipoprotein-E expression comprising administering a triarylmethyl amine compound
    Patent number: 8633195
    Abstract: This invention offers an effective method of inhibiting the expression of apolipoprotein E by mammalian cells. Apolipoprotein E is a protein that plays a significant role in the development of Alzheimer's Disease in humans. The method comprises administering an effective amount of a triarylmethyl amine compound having the general formula: wherein the R1 group may comprise acyclic amines and aliphatic amines. The R2 group may comprise one of three aryl varieties: aryl, substituted aryl, or heterocycle. Triarylamine compounds inhibit apolipoprotein E expression in mammalian cells. In one aspect of the invention the mammalian cells may be human cells, and more specifically may be human brain cells.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: January 21, 2014
    Assignees: Fresno California State University, Fullerton California State University
    Inventors: Santanu Maitra, Nilay Patel
  • METHOD OF INHIBITING APOLIPOPROTEIN-E EXPRESSION COMPRISING ADMINISTERING A TRIARYLMETHYL AMINE COMPOUND
    Publication number: 20140005196
    Abstract: This invention offers an effective method of inhibiting the expression of apolipoprotein E by mammalian cells. Apolipoprotein E is a protein that plays a significant role in the development of Alzheimer's Disease in humans. The method comprises administering an effective amount of a triarylmethyl amine compound having the general formula: wherein the R1 group may comprise acyclic amines and aliphatic amines. The R2 group may comprise one of three aryl varieties: aryl, substituted aryl, or heterocycle. Triarylamine compounds inhibit apolipoprotein E expression in mammalian cells. In one aspect of the invention the mammalian cells may be human cells, and more specifically may be human brain cells.
    Type: Application
    Filed: June 28, 2012
    Publication date: January 2, 2014
    Applicants: California State University Fullerton, California State University Fresno
    Inventors: Santanu Maitra, Nilay Patel
  • Heterocyclic amides as modulators of TRPA1
    Patent number: 8614201
    Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: December 24, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Calude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Bryan Branstetter, Wei Xiao, J. Guy Breitenbucher
  • Modulators of ATP-binding cassette transporters
    Patent number: 8609703
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: December 17, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Anna Hazelwood, Peter Grootenhuis, Jinglan Zhou
  • Alkaloid ester and carbamate derivatives and medicinal compositions thereof
    Patent number: 8604015
    Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: December 10, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Mauro Riccaboni, Daniele De Zani
  • Aerosol foams comprising clindamycin phosphate
    Patent number: 8592380
    Abstract: Described herein are emulsions and compositions for the treatment of acne vulgaris. The emulsions may be formulated as aerosol compositions. The aerosol propellant may be a hydrofluoroalkane propellant. The emulsions or compositions may comprise clindamycin phosphate and a buffer salt, and may exhibit decreased rates of clindamycin phosphate hydrolysis. Also described are methods of treating acne vulgaris, comprising the step of applying to an affected area of a subject in need thereof a therapeutically-effective amount of an inventive emulsion or aerosol composition.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: November 26, 2013
    Assignee: Precision Dermatology, Inc.
    Inventors: Mark W. Trumbore, Wendy Schilling, Ravi K. Varanasi
  • Ceramides and apoptosis-signaling ligand
    Patent number: 8592419
    Abstract: The invention provides the compounds of formula (): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: November 26, 2013
    Assignee: MUSC Foundation for Research Development
    Inventors: Alicja Bielawska, Yusuf A. Hannun, James Norris, Zdzislaw M. Szulc, Jian-yun Dong, Jacek Bielawski, David A. Schwartz, David H. Holman, Ahmed M. El-Zawahry, John McKillop
  • Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists
    Patent number: 8592453
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: November 26, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Furanone compounds and lactam analogues thereof
    Patent number: 8586618
    Abstract: The present invention provides a compound of formula I and a compound of formula II, methods of use and formulations thereof.
    Type: Grant
    Filed: October 8, 2007
    Date of Patent: November 19, 2013
    Assignee: Biosignal Limited
    Inventors: Naresh Kumar, George Iskander
  • Azetidine derivatives
    Patent number: 8530461
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
  • Indolopyridines as Eg5 kinesin modulators
    Patent number: 8530493
    Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
    Type: Grant
    Filed: February 21, 2007
    Date of Patent: September 10, 2013
    Assignee: 4SC AG
    Inventors: Matthias Vennemann, Thomas Bãr, Jürgen Braunger, Astrid Zimmermann, Volker Gekeler
  • HCV protease inhibitors and uses thereof
    Patent number: 8524760
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: September 3, 2013
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF RESTLESS LEGS SYNDROME
    Publication number: 20130217747
    Abstract: Methods of using certain a-aminoamide derivatives in the treatment of RLS and addictive disorders, The compounds of this invention are able to reduce or even stop the symptoms of RLS and addictive disorders substantially without side effects.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 22, 2013
    Inventor: Newron Pharmaceuticals S.P.A.
  • Trifluromethoxyphenyl-substituted tetramic acid derivatives pesticides and/or herbicides
    Patent number: 8507537
    Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: October 13, 2007
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
  • Synergistic combination of flumetsulam or diclosulam with zinc pyrithione
    Patent number: 8501725
    Abstract: A synergistic antimicrobial composition containing flumetsulam or diclosulam; and zinc pyrithione.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: August 6, 2013
    Assignee: Dow Global Technologies LLC
    Inventor: Emerentiana Sianawati
  • Therapy of autoimmune colitis using a TIP60 inhibitor
    Patent number: 8497285
    Abstract: This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: July 30, 2013
    Assignees: The Trustees Of The University Of Pennsylvania, The Children's Hospital of Philadelphia
    Inventors: Mark I. Greene, Wayne W. Hancock, Makoto Katsumata, Yan Xiao
  • SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
    Publication number: 20130190338
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Methods of modulating intestinal fluid balance
    Patent number: 8486381
    Abstract: The present invention relates to methods for treating intestinal fluid balance disorders and modulating intestinal fluid secretion and absorption using calcimimetics and calcilytics.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: July 16, 2013
    Assignee: Amgen Inc.
    Inventors: John Peter Geibel, Steven Charles Hebert, David Martin, Deborah A. Russell
  • Inhibitors
    Patent number: 8486940
    Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: July 16, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Biocide composition comprising pyrithione and pyrrole derivatives
    Patent number: 8481523
    Abstract: The present invention is directed to a biocidal composition comprising a blend of one or more pyrithione compounds, and one or more pyrrole compounds of Formula I wherein said biocidal composition is copper free or low copper content.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: July 9, 2013
    Assignee: Arch Chemicals, Inc.
    Inventors: Craig Waldron, Robert Martin, Tina Williams
  • PHENYLAMIDINES HAVING A HIGH FUNGICIDAL ACTIVITY AND USE THEREOF
    Publication number: 20130157851
    Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.
    Type: Application
    Filed: August 18, 2011
    Publication date: June 20, 2013
    Applicant: ISAGRO S.P.A.
    Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
  • Phosphonic acid compounds as inhibitors of serine proteases
    Patent number: 8461195
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: June 11, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • 3-phenoxymethylpyrrolidine compounds
    Patent number: 8455665
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. 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: Grant
    Filed: August 17, 2012
    Date of Patent: June 4, 2013
    Assignee: Theravance, Inc.
    Inventors: Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
  • Method to treat infections using anti-infective agents
    Patent number: 8450318
    Abstract: Molecules having a spacer unit, linker and recognition unit(s) are used for the treatment of various diseases, disorders and conditions. The compounds are useful in treating infectious diseases and diseases, disorders or conditions related thereto. Further, the methods for treating diseases, disorders or conditions involve recognition and binding of carbohydrate structures.
    Type: Grant
    Filed: March 18, 2008
    Date of Patent: May 28, 2013
    Assignees: K.U. Leuven Research and Development
    Inventors: Monika Mazik, Jan Balzarini
  • Iminosugars and methods of treating viral diseases
    Patent number: 8450345
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: May 28, 2013
    Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS
    Publication number: 20130131034
    Abstract: The instant invention relates to derivatives of formula (I) and their application in therapeutics.
    Type: Application
    Filed: March 1, 2011
    Publication date: May 23, 2013
    Applicant: SANOFI
    Inventors: Markus Follmann, Pascale Goberville, Stéphanie Hachtel, Gerhard Hessler, Heinz-Werner Kleemann, Thomas Maier, Gary MC Cort, Carsten Struebing, Bérangère Thiers, Li-Hsing Wang
  • ?-Aminoamide derivatives useful in the treatment of restless legs syndrome
    Patent number: 8445513
    Abstract: The invention relates to the use of certain alpha-aminoamide derivatives in the treatment of RLS and addictive disorders. The compounds of this invention are able to reduce or even stop the symptoms of RLS and addictive disorders substantially without side effects.
    Type: Grant
    Filed: April 19, 2005
    Date of Patent: May 21, 2013
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Claudia Besana, Elena Barbanti, Emanuela Izzo, Florian Thaler, Ruggero Fariello, Patricia Salvati, Luca Benatti
  • Phenethanolamine derivatives for treatment of respiratory diseases
    Patent number: RE44874
    Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: April 29, 2014
    Assignee: Glaxo Group Limited
    Inventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Panayiotis Alexandrou Procopiou