Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
  • Patent number: 10351568
    Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: July 16, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: Daniel J. Finley, Randall W. King, Byung-Hoon Lee, Min Jae Lee, Timothy C. Gahman
  • Patent number: 10351527
    Abstract: This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: July 16, 2019
    Assignees: THE UNIVERSITY OF BRITISH COLUMBIA, SIMON FRASER UNIVERSITY
    Inventors: Paul Rennie, Artem Tcherkassov, Robert N. Young, Christophe M. Andre
  • Patent number: 10323029
    Abstract: The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: June 18, 2019
    Assignee: The Scripps Research Institute
    Inventors: Edward Roberts, Hugh Rosen, Mariangela Urbano, Miguel A. Guerrero
  • Patent number: 10323036
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: June 18, 2019
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Silvana Marcel Leit de Moradei, Craig E. Masse, Thomas H. McLean, Sayan Mondal
  • Patent number: 10300052
    Abstract: The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: May 28, 2019
    Assignee: The UAB Research Foundation
    Inventors: Steven M Rowe, Mark Dransfield
  • Patent number: 10287265
    Abstract: Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: May 14, 2019
    Assignees: AVIDIN Co. Ltd., SONEAS Research Co. Ltd., Synaging SAS
    Inventors: László Puskás, István Kanizsai, Thierry Pillot, Márió Gyuris, András Szabó, Ferenc Takács, László Hackler
  • Patent number: 10267796
    Abstract: Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADR?1 receptors, and determining based on the binding interaction of the test agent with the ADR?1 receptors whether the test agent is an effective ADR?1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADR?1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: April 23, 2019
    Assignee: The Procter & Gamble Company
    Inventors: Leo Timothy Laughlin, II, Tomohiro Hakozaki, Wenzhu Zhao, Jiazhen Wang, John Crist Bierman
  • Patent number: 10251876
    Abstract: The present invention provides 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopro-pylamine used for combating a tumor. Specially, the present invention refers to method for treating tumor, pharmaceutical composition and medicinal kit related to the described compound. Administrating the compound with a suitable dosage regimen can not only make the patient's plasma concentration maintain the level of 100 ng/ml or lower, but also achieve effects of treatments and obtain benefits for various tumours.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: April 9, 2019
    Inventors: Shanchun Wang, Xunqiang Wang, Hongmei Gu, Ping Dong, Hongjiang Xu
  • Patent number: 10246443
    Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
    Type: Grant
    Filed: April 13, 2017
    Date of Patent: April 2, 2019
    Assignee: TIANJIN HEMAY ONCOLOGY PHARMACEUTICAL CO., LTD.
    Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
  • Patent number: 10202367
    Abstract: Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R1, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: February 12, 2019
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of Kansas
    Inventors: Tsanyang Liang, Zongyi Hu, Juan Jose Marugan, Noel Terrence Southall, Shanshan He, Xin Hu, Jingbo Xiao, Marc Ferrer, Wei Zheng, Kevin J. Frankowski, Frank J. Schoenen, Kelin Li
  • Patent number: 10166225
    Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: January 1, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Douglas Clary
  • Patent number: 10166223
    Abstract: The present invention relates to a pharmaceutical composition for the prevention or treatment of diabetes or fatty liver comprising a CYP4A (cytochrome P450A) inhibitor as an active ingredient. The compound of the present invention has activities of promoting glucose uptake into hepatocytes, inhibiting fat accumulation in liver cells, and inhibiting reactive oxygen production in mitochondria, and thus can be very usefully used for the development of a therapeutic agent for diabetes or fatty liver.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: January 1, 2019
    Assignee: KOREA BASIC SCIENCE INSTITUTE
    Inventors: Gun Hwa Kim, Joo Hyun Park, Min Ji Lee
  • Patent number: 10159666
    Abstract: The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: December 25, 2018
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Sriram Naganathan, Wei Xu, Steven Lacy
  • Patent number: 10160726
    Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: December 25, 2018
    Assignee: Novartis AG
    Inventors: Javier de Vicente Fidalgo, Haiying He, Cheng Hu, Zhigan Jiang, Xiaolin Li, Peichao Lu, Wosenu Mergo, Daniel Mutnick, Folkert Reck, Alexey Rivkin, Colin Keith Skepper, Xiaojing Michael Wang, Jianhua Xia, Yongjin Xu
  • Patent number: 10150764
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: December 11, 2018
    Assignee: Epizyme, Inc.
    Inventor: John Emmerson Campbell
  • Patent number: 10150763
    Abstract: A compound of the formula:(I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: December 11, 2018
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. Cecil, Somhairle MacCormick, William J. Nodes, Franck A. Silva
  • Patent number: 10125112
    Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: November 13, 2018
    Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES
    Inventors: Juan Jose Marugan, Jingbo Xiao, Marc Ferrer-Alegre, Catherine Chen, Noel Southall, Wei Zheng, Alexander Agoulnik, Irina Agoulnik
  • Patent number: 10106502
    Abstract: A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: October 23, 2018
    Assignees: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, THE BROAD INSTITUTE, INC.
    Inventors: Longqin Hu, Sadagopan Magesh, Lin Chen, Timothy Lewis, Ben Munoz, Lili Wang
  • Patent number: 10093628
    Abstract: The present invention pertains to a new compound E)-2-(5-((4-methoxy-2-(trifluoromethyl)quinolin-6-yl)methoxy)-2-((4-(trifluoromethyl) benzyl)oxy)-benzylidene) hexanoic acid (MTTB), and its derivatives. The compounds of the invention are useful as selective peroxisome proliferator-activated receptor gamma (PPAR?) antagonists and are indicated for the use in the treatment of immune related diseases such as systemic inflammation, sepsis and septic shock.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: October 9, 2018
    Assignee: FRAUNHOFER-GESELLSCHAFT ZUR FÖDERUNG DER ANGEWANDTEN FORSCHUNG E.V.
    Inventors: Tilo Knape, Andreas Von Knethen, Michael John Parnham, Manfred Schubert-Zsilavecz, Mario Wurglics, Daniel Flesch
  • Patent number: 10093642
    Abstract: The present invention concerns compounds that selectively inhibit the activity of the Hedgehog (Hh) pathway, their preparation and uses thereof. The compounds of the present invention are useful in treating Hh-dependent tumors, such as medulloblastoma (MB).
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: October 9, 2018
    Assignees: UNIVERSITÀ DEGLI STUDI DI ROMA “LA SAPIENZA”, UNIVERSITA DEGLI STUDI DI SIENA
    Inventors: Bruno Botta, Alberto Gulino, Maurizio Botta, Mattia Mori, Lucia Di Marcotullio, Paola Infante, Francesca Ghirga, Sara Toscano, Cinzia Ingallina, Romina Alfonsi
  • Patent number: 10087171
    Abstract: The present invention relates to crystalline forms of cadazolid.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: October 2, 2018
    Inventors: Christian Hubschwerlen, Philippe Panchaud, Timo Rager, Jean-Luc Specklin
  • Patent number: 10077243
    Abstract: Provided herein are compounds of formula (I): and pharmaceutical compositions thereof, useful for the treatment of disorders mediated by metabotropic glutamate receptor 5.
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: September 18, 2018
    Assignee: SUNOVION PHARMACEUTICALS INC.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Patent number: 10039757
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Grant
    Filed: February 7, 2017
    Date of Patent: August 7, 2018
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 10035771
    Abstract: The present invention discloses a class of mercaptonicotinic acid compound and preparation method and use thereof; the general structural formula of the compound is as shown in Formula I. Experiment demonstrates that the mercaptonicotinic acid compound could inhibit activity of botulinum toxin endopeptidase and tetanus toxin endopeptidase in vitro, which has a significant protective effect on botulinum toxin poisoning in mice, and can be used for preparing medicine intended to prevent and/or treat botulism, as well as to prevent botulinum toxin exposure and tetanus.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: July 31, 2018
    Assignee: INSTITUTE OF MICROBIOLOGY AND EPIDEMIOLOGY, ACADEMY OF MILITARY MEDICAL SCIENCES, PR CHINA
    Inventors: Hui Wang, Wannian Zhng, Zhenyuan Miao, Tao Li, Xiong Liu, Yuelin Wu, Sen Luo, Chunquan Sheng, Xiaoxue Lu, Jianzhong Yao
  • Patent number: 10034873
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Grant
    Filed: June 2, 2017
    Date of Patent: July 31, 2018
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 10017488
    Abstract: The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: wherein X is an oxygen atom and the like; Y is —CO—, —SO2— and the like; R1 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkylcarbonyl group and the like; R2 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R3, R4, R5, and R6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: July 10, 2018
    Assignee: Boston Biomedical, Inc.
    Inventors: Toshihiko Sone, Wataru Hirose, Naoaki Shimada, Chiang J. Li, Wei Li, David Leggett
  • Patent number: 10016408
    Abstract: The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing CXCR4 related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: July 10, 2018
    Assignee: EMORY UNIVERSITY
    Inventors: Lawrence J. Wilson, John Wiseman, Dennis C. Liotta, Michael G. Natchus
  • Patent number: 10016409
    Abstract: Provided is a prophylactic and/or therapeutic drug for mild cognitive impairment, which can improve interstitial flow in cerebral blood vessel and the like to achieve sufficient clearance of harmful proteins accumulated in the brain. The prophylactic and/or therapeutic drug includes 6-[4-(1-cyclohexyl-1H-tetrazole-5-yl)butoxy]3,4-dihydrocarbostyril or a salt thereof as an active ingredient. The prophylactic and/or therapeutic drug can improve a flow of interstitial fluid around blood vessels in a drainage pathway to excrete harmful proteins. The prophylactic and/or therapeutic drug for mild cognitive impairment may take the form of a pharmaceutical product for oral administration, a liquid pharmaceutical product for oral administration, or an injectable preparation.
    Type: Grant
    Filed: July 14, 2017
    Date of Patent: July 10, 2018
    Assignee: FOUNDATION FOR BIOMEDICAL RESEARCH AND INNOVATION AT KOBE
    Inventors: Masafumi Ihara, Takakuni Maki, Akihiko Taguchi
  • Patent number: 9956212
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of multiple myeloma.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: May 1, 2018
    Assignee: Active Biotech AB
    Inventors: David Liberg, Anders Olsson, Dmitry Gabrilovich, Yuliya Nefedova
  • Patent number: 9956215
    Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: May 1, 2018
    Assignee: Kura Oncology, Inc.
    Inventors: Antonio Gualberto, Catherine Rose Scholz
  • Patent number: 9957234
    Abstract: The present invention relates to novel polymorphic forms of ivacaftor, process for its preparation and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: May 1, 2018
    Assignee: Laurus Labs Limited
    Inventors: Ram Thaimattam, Venkata Srinivasa Rao Dama, Venkata Sunil Kumar Indukuri, Seeta Rama Anjaneyulu Gorantla, Satyanarayana Chava
  • Patent number: 9949485
    Abstract: Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, wherein the symbols are defined as in claim 1, preferably N-(2-methoxybenzoyl)-4-[(methylaminocarbonyl)-amino]benzenesulfonamide [Compound (A1)].
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: April 24, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Udo Bickers, Stefan Lehr, Klaus Trabold, Mathias Schmidt, Martin Jeffrey Hills, Juan Pedro Ruiz-Santaella Moreno, Erwin Hacker
  • Patent number: 9890406
    Abstract: A method for producing cathine ((1S,2S)-norpseudoephedrine), in which, in a first reaction step, benzaldehyde is reacted with an acetyl donor according to formula (1), where R?H or COOH, by way of an (S)-selective lease to yield an enantiomer mixture according to formulas (2) and (3) and, in a second step, the compound according to formula (3) is reacted with an amine donor by way of an (S)-selective transaminase to yield (1S,2S)-norpseudoephedrine.
    Type: Grant
    Filed: May 17, 2014
    Date of Patent: February 13, 2018
    Assignee: Forschungszentrum Juelich GmbH
    Inventors: Doerte Rother, Martina Pohl, Torsten Sehl, Alvaro Gomez Baraibar
  • Patent number: 9883673
    Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5- to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: February 6, 2018
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
  • Patent number: 9880154
    Abstract: Acetylcholine and its receptors appeared in evolution before development of a nervous system. Cholinergic agonists functions include proliferation, differentiation, and cell-to-cell contact in protozoa] as well as vertebrate cells. Animal models for infection by Apicomplexan parasites require cell-to-cell contact followed by differentiation of parasite and host cells to produce clinical disease. Experimental infections are produced by introducing parasite infected leukocytes into a host. Binding cholinergic receptors on the parasites and leukocytes with levamisole HCl induces non-progressive infections and absence of signs of disease.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: January 30, 2018
    Inventors: William T Killeen, Siobhan Ellison
  • Patent number: 9867816
    Abstract: Methods of treatment of multiple sclerosis (MS) with PPAR? agonists, and in particular with the compound of formula (I) known as INT131:
    Type: Grant
    Filed: January 10, 2017
    Date of Patent: January 16, 2018
    Assignee: InteKrin Therapeutics, Inc.
    Inventor: David Weinstein
  • Patent number: 9861624
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: January 9, 2018
    Assignee: Exelixis, Inc.
    Inventor: Dana T. Aftab
  • Patent number: 9856220
    Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: January 2, 2018
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Jürgen Dinges, Clarissa Jakob
  • Patent number: 9840499
    Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: April 12, 2016
    Date of Patent: December 12, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Patent number: 9833444
    Abstract: The present invention relates preferably to the use of 4-bromo-N-[(E)-(2-methyl-1H-indol-3-yl)methyleneamino]benzenesulphonamide and 4-methyl-3-oxo-2-(3-pyridylmethylene) benzo[3,4-b]furan-6-yl-4-chlorobenzenesulphonate (compounds 5 and 6, respectively), which are compounds that can inhibit the toxic activity of sphingomyelinase D from Loxosceles venom, controlling the development of cutaneous and systemic loxoscelism; reducing haemolysis; inhibiting the formation of skin lesions; inhibiting skin necrosis; inhibiting intracellular signaling pathways and the production of reactive oxygen species. In addition to the therapeutic potential thereof, said inhibitors can be used to study the activity of sphingomyelinases and phospholipases D.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: December 5, 2017
    Assignee: FUNDAÇÃO BUTANTAN
    Inventors: Denise Vilarinho Tambourgi, Priscila Hess Lopes, Mario Tyago Murakami, Fernanda Calheta Vieira Portaro
  • Patent number: 9820997
    Abstract: A method of accelerating remyelination or suppressing demyelination of neurons in a mammal, and a method of treating a disease associated with demyelination of neurons in a mammal.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: November 21, 2017
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Yunil Lee, Kiyoung Chang, Sangchul Park, Sungchun Cho
  • Patent number: 9822078
    Abstract: The present invention relates to quinoline compounds as defined by Formula I below. Such quinoline compounds have been shown to inhibit the formation of amyloid deposits (e.g., amyloid oligomers, fibrils or plaques). Consequently, these compounds are suitable for treating a range of diseases and disorders in which amyloid deposits are implicated, such as type-2 diabetes and Alzheimer's disease.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: November 21, 2017
    Assignee: Oxford University Innovation Limited
    Inventors: David Vaux, Letitia Jean, Stephen Davies, Angela Russell, Graham Wynne, Carole Bataille, Méabh Brennan
  • Patent number: 9815825
    Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: November 14, 2017
    Assignee: DiscoveryBiomed, Inc.
    Inventors: Erik Schwiebert, John Streiff, John Dixon, Hongwu Gao
  • Patent number: 9783501
    Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: October 10, 2017
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Patent number: 9750717
    Abstract: The present invention relates to compounds acting as selective inhibitors of CD40-TRAF6 interaction, their use as medicaments and their use in the treatment of (chronic) inflammatory diseases. The present invention also relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: September 5, 2017
    Assignees: LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, MAASTRICHT UNIVERSITY
    Inventors: Esther Lutgens, Christian Weber, Gerry Nicolaes
  • Patent number: 9732048
    Abstract: The invention relates to N-(isoxazol-3-yl)-aryl-carboxylic acid amides and use thereof as herbicides. In formula (I), A stands for N or C—Y. R, V, X, Y, and Z stand for groups such as hydrogen, halogen, and organic groups such as substituted alkyl.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: August 15, 2017
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Arnim Koehn, Hartmut Ahrens, Ralf Braun, Ines Heinemann, Joerg Tiebes, Christian Waldraff, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Patent number: 9732076
    Abstract: Described herein are solid oral dosage forms containing Compound (1) or a pharmaceutically acceptable salt thereof (Formula 1), wherein Compound (1) is in the amorphous state. Also described are solid oral dosage forms comprising a composition of Compound (1) in the amorphous state and one or more pharmaceutically acceptable excipients. Compound (1) is a specific inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease. Thus, also described herein are methods for using the described solid oral dosage forms in the treatment of HCV infection. Also described are processes for the manufacture of the solid oral dosage forms.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: August 15, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Chitra Telang, Zeren Wang, Li Zhong
  • Patent number: 9717738
    Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.
    Type: Grant
    Filed: April 18, 2016
    Date of Patent: August 1, 2017
    Assignee: Horizon Orphan LLC
    Inventors: David C. Griffith, Michael N. Dudley, Mark W. Surber, Keith A. Bostian, Olga Rodny
  • Patent number: 9708331
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: July 18, 2017
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Patent number: 9701639
    Abstract: The present disclosure relates to co-crystals comprising N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and a co-former and methods for their preparation. The present disclosure further relates to pharmaceutical compositions comprising the co-crystal forms, as well as methods of treatment therewith and kits.
    Type: Grant
    Filed: October 7, 2015
    Date of Patent: July 11, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Strohmeier, John Caesar, Jr., Patrick Raymond Connelly, Majed Fawaz, Eduard Luss-Lusis, Brian McClain, Ales Medek, Hai Miao, Kwame Wiredu Nti-Addae, Ping Yin, Yuegang Zhang