Patents Issued in February 7, 2017
  • Inhibitors of viral replication, their process of preparation and their therapeutical uses
    Patent number: 9562033
    Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: February 7, 2017
    Assignee: LABORATOIRE BIODIM
    Inventors: Richard Benarous, Francis Chevreuil, Benoit Ledoussal, Sophie Chasset, Frédéric Le Strat
  • Endoparasite control agent
    Patent number: 9562034
    Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): (wherein Het represents a 5- or 6-membered heterocyclic group), or a salt thereof as an active ingredient.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: February 7, 2017
    Assignees: The University of Tokyo, Nihon Nohyaku Co., Ltd.
    Inventors: Kiyoshi Kita, Akiyuki Suwa, Masatsugu Oda, Koji Tanaka
  • Benzamide derivative useful as FASN inhibitors for the treatment of cancer
    Patent number: 9562035
    Abstract: The present invention is directed to benzamide derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, liver related disorders and viral infections. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, ?are defined herein.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: February 7, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J Connolly, Tianbao Lu
  • Fluoromethyl-substituted pyrrole carboxamides as CaV2.2 calcium channel blockers
    Patent number: 9562036
    Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: February 7, 2017
    Assignee: GRÜNENTHAL GMBH
    Inventors: Melanie Reich, Stefan Schunk, Florian Jakob, Henning Steinhagen, Nils Damann, Michael Haurand, Marc Rogers, Kathy MacKenzie
  • Synthesis and use of amine-containing flavonoids as potent anti-leishmanial agents
    Patent number: 9562037
    Abstract: The present invention relates to novel series of amine-containing flavonoids and compositions containing the compounds, as well as the synthesis and the use of the same. The invention also relates to methods of treatment and prevention of diseases, in particular, parasitic infections including Leishmaniasis, comprising administration of the compounds.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: February 7, 2017
    Assignee: The Hong Kong Polytechnic University
    Inventors: Larry Ming-Cheung Chow, William Tak Hang Chan, Kin-Fai Chan, Iris Lai King Wong, Wing-Yiu Kan
  • Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus
    Patent number: 9562038
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: February 7, 2017
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Christopher Parker
  • Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both ?2 adrenergic receptor agonist and M3 muscarinic receptor antagonist activities
    Patent number: 9562039
    Abstract: The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a hydroxycarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 7, 2017
    Assignee: Almirall, S.A.
    Inventors: Montserrat Julia Jane, Francesc Carrera Carrera, Maria Prat Quiñones, Carlos Puig Duran, Francesca Pajuelo Lorenzo, Juan Antonio Perez Andres
  • Processes for preparing Rivaroxaban
    Patent number: 9562040
    Abstract: Processes and intermediates for preparing rivaroxaban, and analogs and derivatives thereof, and pharmaceutically acceptable salts of each of the foregoing, are described herein.
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: February 7, 2017
    Assignee: Indiana University Research and Technology Corporation
    Inventor: James R. McCarthy
  • Enhancer of zeste homolog 2 inhibitors
    Patent number: 9562041
    Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: February 7, 2017
    Assignee: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Steven David Knight
  • ?-oxoacyl amino-caprolactam
    Patent number: 9562042
    Abstract: The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an ?-oxoacyl amino-caprolactam that is represented by formula (I) (in formula (I), X represents N or CH, Y represents O or CH2, and Z represents S or CH2); and a bone resorption inhibitor containing the ?-oxoacyl amino-caprolactam.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: February 7, 2017
    Assignee: Seikagaku Corporation
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii, Mizuho Ishikawa, Daisuke Morita
  • Heterocyclic amide derivative and pharmaceutical product containing same
    Patent number: 9562043
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: February 7, 2017
    Assignee: EA PHARMA CO., LTD.
    Inventors: Tamotsu Suzuki, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • 2-acylaminothiazole derivative or salt thereof
    Patent number: 9562044
    Abstract: Thiazole derivatives having pyrazine-2-carbonylamino substituted at the 2-position of the following formula (I): are excellent muscarinic M3 receptor positive allosteric modulators, and are useful for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor. The 2-acylaminothiazole derivatives and salts thereof can be used for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 7, 2017
    Assignee: Astellas Pharma Inc.
    Inventors: Taisuke Takahashi, Jun Maeda, Yusuke Inagaki, Kenji Negoro, Hiroaki Tanaka, Kazuhiro Yokoyama, Hajime Takamatsu, Takanori Koike, Issei Tsukamoto
  • Process for preparation of indolizine based derivatives as potential phosphodiestrase 3 (PDE3) inhibitors
    Patent number: 9562045
    Abstract: The present invention provides compounds of general formula 1 useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: February 7, 2017
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Budde Mahendar, Saidulu Mattapally, Mettu Ravinder, Sanjay Kumar Banerjee, Vaidya Jayathirtha Rao
  • Means and method for treating solid tumors
    Patent number: 9562046
    Abstract: In a cytotoxic compound of the general formula (I) R is H or methyl or methylene substituted by C1-C4 straight or branched alkyl, R1 is selected from the group consisting of H, C1-C4 straight or branched alkyl, methoxy, methoxy substituted by from one to three fluorine, halogen; R2 is H or C1-C4 straight or branched alkyl; X is CH or N; Y is CH or N.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: February 7, 2017
    Assignee: VIVOLUX AB
    Inventor: Stig Linder
  • Pyrazolopyrimidine compounds for the treatment of cancer
    Patent number: 9562047
    Abstract: Compounds of Formula I are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: February 7, 2017
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Xiaodong Wang, Jing Liu, Chao Yang, Weihe Zhang, Stephen Frye, Dmitri Kireev
  • Pyrrolobenzodiazepines and conjugates thereof
    Patent number: 9562049
    Abstract: A compound with the formula I: and salts and solvates thereof.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: February 7, 2017
    Assignee: MEDIMMUNE LIMITED
    Inventor: Philip Wilson Howard
  • Crystalline forms of pemetrexed diacid and processes for the preparation thereof
    Patent number: 9562050
    Abstract: Provided are crystalline forms of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]ben-zoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: February 7, 2017
    Assignee: Sicor, Inc.
    Inventors: Jonathan Busolli, Nicola Diulgheroff, Csilla Nemethne Racz, Moran Pirkes, Alessandro Pontiroli, Marco Villa, Judith Aronhime
  • Methylenedioxybenzo [I] phenanthridine derivatives used to treat cancer
    Patent number: 9562051
    Abstract: The invention provides compounds of formula I: wherein A, B, X, and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds, processes for preparing such compounds, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: February 7, 2017
    Assignee: Rutgers, the State University of New Jersey
    Inventors: Edmond J. LaVoie, Wei Feng, Leroy F. Liu
  • Bicyclicpyridine derivatives
    Patent number: 9562052
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, A1, A2, A3, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: February 7, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Aurelia Conte, Holger Kuehne, Bernd Kuhn, Werner Neidhart, Ulrike Obst Sander, Hans Richter
  • Benzo-fused heterocyclic derivatives useful as agonists of GPR120
    Patent number: 9562053
    Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: February 7, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • Process for preparing isosorbide ethoxylate di(meth)acrylate
    Patent number: 9562054
    Abstract: A process for preparing isosorbide ethoxylate di(meth)acrylate by transesterifying alkyl (meth)acrylate with isosorbide ethoxylate, comprising the steps of: (i) ethoxylating isosorbide to give isosorbide ethoxylate, (ii) reacting alkyl (meth)acrylate with isosorbide ethoxylate in the presence of potassium phosphate as catalyst and a stabilizer and in the presence of an azeotroping agent which forms an azeotrope with the alcohol bound in the alkyl (meth)acrylate, (iii) continuously distilling off the azeotrope of azeotroping agent and alcohol, wherein steps (ii) and (iii) are conducted simultaneously until the isosorbide ethoxylate has been essentially fully converted, (iv) removing the catalyst from the product mixture comprising isosorbide ethoxylate di(meth)acrylate, (v) distilling unconverted alkyl (meth)acrylate and azeotroping agent out of the product mixture.
    Type: Grant
    Filed: February 24, 2016
    Date of Patent: February 7, 2017
    Assignee: BASF SE
    Inventors: Andrea Misske, Friederike Fleischhaker, Christoph Fleckenstein, Martin Kaller, Ulrik Stengel, Mathieu Blanchot, Claudia Stoer, Ritesh Nair
  • Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as TrkA kinase inhibitors
    Patent number: 9562055
    Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: February 7, 2017
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven W. Andrews, James F. Blake, Kevin R. Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Gabrielle R. Kolakowski, Jeongbeob Seo
  • Imidazopyridines Syk inhibitors
    Patent number: 9562056
    Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: February 7, 2017
    Assignee: GILEAD CONNECTICUT, INC.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
  • (Thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HTantagonists
    Patent number: 9562057
    Abstract: A dual H1 inverse agonist/5-HT2A receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: February 7, 2017
    Assignee: Eli Lilly and Company
    Inventor: Peter Thaddeus Gallagher
  • Crystalline forms of an antiviral compound
    Patent number: 9562058
    Abstract: Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: February 7, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Dustin Bringley, Johann Chan, Peter Fung, Katie Keaton, Olga Lapina, Henry Morrison, Dominika Pcion
  • Anticancer maytansinoids with two fused macrocyclic rings
    Patent number: 9562059
    Abstract: This invention provides maytansinoids having improved tumor inhibition activity. In particular, the present invention provides a method of treatment of cancer, in particular colon cancer, using maytansinoid compounds having two fused macrocyclic rings.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: February 7, 2017
    Assignees: Hong Kong Baptist University, The Board of Trustees of the University of Illinois
    Inventors: Hongjie Zhang, Djaja D. Soejarto, Harry H. S. Fong
  • Heterocyclic pyridone compound, and intermediate, preparation method and use thereof
    Patent number: 9562060
    Abstract: The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament.
    Type: Grant
    Filed: May 28, 2012
    Date of Patent: February 7, 2017
    Assignee: SHANGHAI HUILUN LIFE SCIENCE & TECHNOLOGY CO., LTD
    Inventors: Jianjun Cheng, Jihong Qin, Bin Ye
  • Compounds that inhibit MCL-1 protein
    Patent number: 9562061
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: February 7, 2017
    Assignee: Amgen Inc.
    Inventors: Sean P. Brown, Yunxiao Li, Joshua Taygerly, Marc Vimolratana, Xianghong Wang, Manuel Zancanella
  • Ligand compound, organic chromium compound, catalyst system for ethylene oligomerization, and method for ethylene oligomerization using the same
    Patent number: 9562062
    Abstract: The present invention relates to a ligand compound, a catalyst system for ethylene oligomerization, and a method for ethylene oligomerization using the same. The catalyst system for ethylene oligomerization according to the present invention not only has excellent catalytic activity but also shows more improved liquid olefin selectivity, and enables more effective preparation of an alpha-olefin through the oligomerization of ethylene because it is particularly possible to control the selectivity to 1-hexene or 1-octene.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: February 7, 2017
    Assignee: LG Chem, Ltd
    Inventors: Sung Min Lee, Yong Ho Lee, Min Seok Cho, Seok Pil Sa, Ki Soo Lee
  • Process for the preparation of DOPO-derived compounds and compositions thereof
    Patent number: 9562063
    Abstract: This invention relates to a process for producing compounds derived from 9,10-Dihydro-9-Oxa-10-Phosphaphenantrene-10-oxide (DOPO). In particular, the invention relates to producing DOPO-derived compounds by reacting DOPO with diol compounds in the presence of a catalyst. This invention also relates to DOPO derived composition containing a high melting point diastereomer. The DOPO derived compounds may be useful as flame-retardants.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: February 7, 2017
    Assignee: Albemarle Corporation
    Inventors: Qiang Yao, Junuzo Wang, Arthur G. Mack
  • High-purity steviol glycosides
    Patent number: 9562064
    Abstract: Methods of preparing highly purified steviol glycosides, particularly Rebaudioside D, are described. The methods include purification from the extraction stage of the Stevia rebaudiana Bertoni plant, purification of steviol glycoside mixtures, Rebaudioside D and Rebaudioside A from a commercial Stevia extract, and purification of Rebaudioside D from remaining solutions obtained after isolation and purification of Rebaudioside A and a high purity mixture of steviol glycosides. The methods are useful for producing high purity Rebaudioside D, Rebaudioside A, and steviol glycoside mixtures. The high purity steviol glycosides are useful as non-caloric sweeteners in edible and chewable compositions such as any beverages, confectioneries, bakery products, cookies, and chewing gums.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: February 7, 2017
    Assignee: PureCircle Sdn Bhd
    Inventor: Avetik Markosyan
  • Sucrose octasulfates of magnesium, preparation method thereof and pharmaceutical cosmetic uses of same
    Patent number: 9562065
    Abstract: The invention relates to a sucrose octasulfate of magnesium, having general formula I, the preparation method thereof and the use of same in the pharmaceutical and/or cosmetic field, wherein 0?n?4, n is an integer and Y represents OH, Cl, Br, I, NO3, C6H5O7, CH3CO2, CF3CO2 or —OCH3.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: February 7, 2017
    Assignee: PIERRE FABRE DERMO-COSMETIQUE
    Inventors: Séverine Jeulin, Hélène Hernandez-Pigeon, Luc Aguilar
  • Oral therapy of necrotizing enterocolitis
    Patent number: 9562066
    Abstract: The present invention relates to methods of treating or reducing the risk of necrotizing enterocolitis (NEC) in an infant comprising orally administering an effective amount of a CpG-ODN. It is based, at least in part, on the results of experiments in which orally administered CpG-ODNs were observed to reduce the histopathology and markers of inflammation in a murine model for NEC. The present invention further provides for oral formulations of CpG-ODN for administration to infants.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: February 7, 2017
    Assignee: University of Pittsburgh-Of the Commonwealth System of Higher Education
    Inventor: David J. Hackam
  • Process for the production of 19-norpregn-4-en-3,20-dione-17?-ol(gestonorone) and intermediates therefor
    Patent number: 9562067
    Abstract: The present invention relates to a new stereoselective process for the synthesis of 17(?)-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17(?)-17-acetyl-17-hydroxy-estr-4-en-3-one (gestonorone) is an important intermediate in the synthesis of the active ingredients having progestogen activity—such as gestonorone capronate and nomegestroi acetate. Formulas (I), (II) and (III).
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: February 7, 2017
    Assignee: RICHTER GEDEON NYRT.
    Inventors: János Csörgei, Anita Horváth, Csaba Sánta, Sándor Mahó, Zoltán Béni, János Horváth
  • Process for the preparation of 7 ?-(methoxycarbonyl)-3-OXO-17alpha-pregn-4,9(11)-dien-21,17-carbolactone, a useful intermediate for the synthesis of molecules with pharmacological activity
    Patent number: 9562068
    Abstract: An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: February 7, 2017
    Assignee: INDUSTRIALE CHIMICA, S.r.l.
    Inventors: Roberto Lenna, Riccardo Di Brisco, Francesco Barbieri
  • Selective caspase inhibitors and uses thereof
    Patent number: 9562069
    Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: February 7, 2017
    Inventors: Jan-Eric Ahlfors, Khalid Mekouar
  • Induction of tumor immunity by variants of folate binding protein
    Patent number: 9562070
    Abstract: The present invention is directed to variants of antigens comprising folate binding protein epitopes as a composition associated with providing immunity against a tumor in an individual. The variant is effective in inducing cytotoxic T-lymphocytes but preferably not to the extent that they become sensitive to silencing by elimination, such as by apoptosis, or by anergy, as in unresponsiveness.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: February 7, 2017
    Assignees: Board of Regents, The University of Texas System, The Henry M. Jackson Foundation for the Advancement of Military Medicine, Inc.
    Inventors: Constantin G. Ioannides, George E. Peoples
  • Method for preparing eptifibatide
    Patent number: 9562071
    Abstract: Provided is a method for preparing eptifibatide, wherein the method comprises: obtaining an eptifibatide refined peptide solution; and obtaining and freeze-drying an eptifibatide refined peptide concentrate after rotary evaporation of the eptifibatide refined peptide solution, wherein the concentration of the eptifibatide refined peptide concentrate is 15-30 mg/ml and the temperature of rotary evaporation is 251° C.-35° C. The preparation method of the eptifibatide refined peptide solution is as follows: coupling Cys with a resin to obtain a Cys-resin; obtaining a polypeptide having a sequence as represented by SEQ ID NO: 1 by gradually coupling the Cys-resin with Pro, Trp, Asp, Gly, Har and Mpa; and obtaining the eptifibatide refined peptide solution through oxidation, cleavage, purification and transfer to salt.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: February 7, 2017
    Assignee: HYBIO PHARMACEUTICAL CO., LTD.
    Inventors: Xu Kang, Jian Liu, Yaping Ma, Jiancheng Yuan
  • Compositions and methods for regulating glucose metabolism
    Patent number: 9562072
    Abstract: The present disclosure provides compositions for regulating glucose metabolism. The compositions provide for reduced levels of p75NTR and/or reduced binding of p75NTR to a GTPase such as Rab31 or Rab5. The compositions are useful in methods of regulating glucose metabolism, which methods are also provided.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: February 7, 2017
    Assignee: The J. David Gladstone Institutes
    Inventor: Katerina Akassoglou
  • Matriptase and u-plasminogen activator substrates and other cleavable moieties and methods of use thereof
    Patent number: 9562073
    Abstract: The invention relates generally to polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator (uPA), to activatable antibodies and other larger molecules that include the cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator, and to methods of making and using these polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator in a variety of therapeutic, diagnostic and prophylactic indications.
    Type: Grant
    Filed: January 30, 2015
    Date of Patent: February 7, 2017
    Assignee: CYTOMX THERAPEUTICS, INC.
    Inventors: Stephen James Moore, Margaret Thy Luu Nguyen, Daniel R. Hostetter, Olga Vasiljeva
  • Self-assembling peptide cages from coiled-coil peptide modules
    Patent number: 9562074
    Abstract: This invention relates to protein structures, to methods of producing those protein structures, and to peptides used in the formation of the protein structures.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: February 7, 2017
    Assignee: The University of Bristol
    Inventors: Dek Woolfson, Paula Booth, Jordan Fletcher, Richard Sessions, Noah Linden
  • Intradermal HPV peptide vaccination
    Patent number: 9562075
    Abstract: The invention relates to the use of a peptide derived from HPV-E2, E6 and/or E7 protein for the manufacture of a medicament for the treatment or prevention of an HPV related disease, wherein the medicament is for intradermal administration.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: February 7, 2017
    Assignee: Academisch Ziekenhuis Leiden H.O.D.N. LUMC
    Inventors: Sjoerd Henricus Van Der Burg, Gemma G. Kenter, Cornelis Johannes Maria Melief
  • Hydrophobic modified pres-derived peptides of hepatitis B virus (HBV) and their use as HBV and HDV entry inhibitors
    Patent number: 9562076
    Abstract: The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are derived from a HBV preS consensus sequence and are N-terminal preferably acylated and optional C-terminal modified. These hydrophobic modified preS-derived peptides of HBV are very effective HBV entry inhibitors as well as HDV entry inhibitors and are, thus, suitable for the inhibition of HBV and/or HDV infection, prevention of primary HBV and/or HDV infection as well as treatment of (chronic) hepatitis B and/or D. The present invention further relates to pharmaceutical and vaccine compositions comprising these hydrophobic modified preS-derived peptides of HBV.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: February 7, 2017
    Assignee: RUPRECHT-KARLS-UNIVERSITÄT-HEIDELBERG (Rektorat)
    Inventors: Walter Mier, Stephan Urban
  • Protein complex system for increased immunogenicity and functionality, and methods making and use
    Patent number: 9562077
    Abstract: Genes for proteins which spontaneously form dimers and/or oligomers can be recombinantly linked together, which upon expression in E. coli produces stable dimeric fusion proteins that spontaneously self-assemble into enormous, polyvalent complexes having increased immunogenicity and functionality. Linear, network and agglomerate complexes with enormous sizes and polyvalences are constructed using glutathione S-transferase, Norovirus P domains (NoV P? and NoV+), the protruding (P) domain of hepatitis E virus (HEV P), the astrovirus P domain (AstV), a monomeric peptide epitope (M2e of influenza virus), and/or a protein antigen (VP8* of rotavirus) fused in different combinations. The resulting complexes can contain hundreds to thousands NoV P-protein, HEV, AstV, M2e and/or VP8* copies and exhibit higher immunogenicity than the individual proteins alone.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 7, 2017
    Assignee: Children's Hospital Medical Center
    Inventors: Ming Tan, Xi Jiang, Leyi Wang
  • Methods for identifying broadly neutralizing antibodies utilizing recombinant HIV-1 envelope glycoproteins comprising stabilizing mutations
    Patent number: 9562078
    Abstract: The present application relates to novel HIV-1 envelope glycoproteins which may be utilized as an HIV-1 vaccine immunogens, antigens for crystallization and for the identification of broad neutralizing antibodies. The present invention encompasses the preparation and purification of immunogenic compositions which are formulated into the vaccines of the present invention.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: February 7, 2017
    Assignee: INTERNATIONAL AIDS VACCINE INITIATIVE
    Inventors: Simon Hoffenberg, Christopher L. Parks, Alexei Carpov
  • Vaccines and methods to treat lyme disease in dogs
    Patent number: 9562079
    Abstract: The instant invention provides an immunogenic composition comprising an antigenic fragment of OspA protein of Borrelia burgdorferi and a chimeric protein containing antigenic fragments of different phylotypes of OspC protein of Borrelia burgdorferi. Vaccines incorporating the immunogenic composition of the invention, as well as methods of preventing Lyme disease in dogs and/or protecting dogs from Lyme disease using the vaccines are also provided.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: February 7, 2017
    Assignees: Zoetis Services LLC, Virginia Commonwealth University
    Inventors: Robert M. Lohse, Patrick F. M. Meeus, Jason J. Millership, Zhichang Xu, Richard Thomas Marconi, Christopher G. Earnhart
  • Lyme disease vaccine, genetic construct, recombinant protein, method for designing genetic construct, method for producing vaccine, method for producing recombinant proteins, use of recombinant proteins in the production of lyme disease vaccine
    Patent number: 9562080
    Abstract: The present invention relates to a Lyme disease vaccine, a genetic construct, recombinant protein, method for genetic construct design, method for vaccine delivery, method for recombinant proteins delivery, use of recombinant proteins in the production of Lyme disease vaccine. In particular, the method concerns the use of TROSPA and TROSPA-Salp15 recombinant proteins derived from castor bean tick (Ixodes riccinus) as a component of Lyme disease vaccine for animals. The antibodies present in blood of an immunized vertebrate directed against the TROSPA proteins considerably reduce the chance of infecting new ticks by blocking or hindering the interaction of TROSPA protein with OspA protein of Borrelia burgdorferi sensu lato. The interaction is crucial in the process of the spirochete entering a tick.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: February 7, 2017
    Assignee: INSTYTUT CHEMII BIOORGANICZNEJ PAN
    Inventors: Anna Urbanowicz, Marek Figlerowicz, Dominik Lewandowski
  • Sugar transporters
    Patent number: 9562081
    Abstract: A novel class of transporter protein, referred to as SWEET, GLUE or Glü, is disclosed. These transporters provide a novel system for the transportation of sugars across membranes within a cell and between the inside and outside of a cell. Such transporters are useful for understanding and altering the sugar concentration within certain organs of an organism, and within certain organelles within the cell. These transporters are also useful in protecting plants from a pathogen attack.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: February 7, 2017
    Assignee: CARNEGIE INSTITUTION OF WASHINGTON
    Inventors: Wolf B. Frommer, Sylvie Lalonde
  • Production of glycoproteins with low N-glycolylneuraminic acid (Neu5Gc) content
    Patent number: 9562082
    Abstract: The present invention relates to a medium for the cultivation of eukaryotic cells, the medium comprising as (an) additive(s) DMSO, N-acetylmannosamine (NAcMan), N-acetylglucosamine (NAcGlc), or any combination of two or more of these additives, including the combination of NAcMan and NAcGlc.
    Type: Grant
    Filed: May 16, 2014
    Date of Patent: February 7, 2017
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventor: Tanja Ficko Trcek
  • Peptides and methods for inducing cell death
    Patent number: 9562083
    Abstract: The invention provide isolated peptides, protides and conjugates having novel peptide sequences which are able to induce antimicrobial, anti-cancer, anti-inflammatory, anti-proliferative or programmed cell death activity. The invention also provides a method of inducing programmed cell death in a cell by contacting the cell with an isolated peptide, protide or conjugate described herein. In some aspects, the method can be used in the diagnosis, prevention, or treatment of a disease, such as an infection, cancer, autoimmune disease, or inflammatory disease.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: February 7, 2017
    Assignee: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventors: Michael R. Yeaman, Nannette Y. Yount, Eric P. Brass