Quinolines (including Hydrogenated) Patents (Class 514/311)
  • Patent number: 10301308
    Abstract: The present invention provides a novel compound of the formula: methods of making this compound, methods of using this compound for tau imaging, and preparations of tau imaging formulations.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: May 28, 2019
    Assignee: Eli Lilly and Company
    Inventors: Giorgio Attardo, Carey Lynn Horchler, Shyamali Ghosh, Hui Xiong
  • Patent number: 10195167
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: February 5, 2019
    Assignee: Glucox Biotech AB
    Inventors: Per Wikström, Erik Walum, Mona Wilcke
  • Patent number: 10149846
    Abstract: Pharmaceuticals which are effective for treatment, prevention, and the like of cancer and have less side effects are disclosed. The antitumor agent of the present invention comprises as an effective ingredient at least one leukotriene inhibitor. Examples of the leukotriene inhibitor includes leukotriene production inhibitors and leukotriene receptor antagonists, and preferred specific examples of the leukotriene inhibitor include montelukast, zafirlukast, pranlukast, and zileuton; pharmaceutically acceptable salts of these compounds; and pharmaceutically acceptable solvates of these compounds and the salts. The leukotriene inhibitor can also be used as a relieving agent for pain accompanying a tumor(s), and as a stromal hyperplasia inhibitor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: December 11, 2018
    Assignee: TOCHIGI INSTITUTE OF CLINICAL PATHOLOGY
    Inventor: Masao Sugamata
  • Patent number: 10117865
    Abstract: Compounds of formula (I) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: November 6, 2018
    Assignee: ChemoCentryx, Inc.
    Inventors: Daniel Dairaghi, Dean R. Dragoli, Jaroslaw Kalisiak, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Rebecca M. Lui, Venkat Reddy Mali, Viengkham Malathong, Jay P. Powers, Hiroko Tanaka, Joanne Tan, Matthew J. Walters, Ju Yang, Penglie Zhang
  • Patent number: 10100029
    Abstract: The present invention relates novel heterocyclic analogs of combretastatin, their synthesis, and their use as anti-cancer compounds. In particular, compounds of Formula (I), Formula (II), and Formula (V) are provided.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 16, 2018
    Assignee: BioVentures, LLC
    Inventors: Narsimha Reddy Penthala, Peter Crooks, Vijayakumar Sonar
  • Patent number: 10058546
    Abstract: A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: August 28, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Rossitza Gueorguieva Alargova, Craig Antony Dunbar, Irina Nikolaevna Kadiyala
  • Patent number: 10039731
    Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: August 7, 2018
    Assignee: Io Therapeutics, Inc.
    Inventor: Roshantha A. Chandraratna
  • Patent number: 9968584
    Abstract: The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: May 15, 2018
    Assignee: Cardioxyl Pharmaceuticals, Inc.
    Inventors: Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost, John P. Toscano
  • Patent number: 9938252
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described; which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Grant
    Filed: September 23, 2014
    Date of Patent: April 10, 2018
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Leticia Toledo-Sherman, Michael Prime, William Mitchell, Naomi Went
  • Patent number: 9931335
    Abstract: Compositions and methods are provided for inhibiting or treating the early and established stages of inflammatory diseases by administration of an effective dose of the desethylhydroxychloroquine (DHCQ). A benefit of the methods is the ability to deliver a dose of agent that is effective in treating inflammation while sparing the individual from retinal toxicity.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: April 3, 2018
    Assignees: The Board of Trustees of the Leland Stanford Junior University, The United States of America as Represented by the Department of Veterans Affairs
    Inventors: William H. Robinson, Jeremy Sokolove, Qian Wang
  • Patent number: 9796736
    Abstract: Provided are a heterocyclic compound which emits blue light and is represented by General Formula (G1) below, and a light-emitting element, a light-emitting device, an electronic device and a lighting device which are formed using the heterocyclic compound represented by General Formula (G1) below. The use of the heterocyclic compound represented by General Formula (G1) makes it possible to provide a light-emitting element which has high emission efficiency, and also a light-emitting device, an electronic device and a lighting device which have reduced power consumption.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: October 24, 2017
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroki Suzuki, Tsunenori Suzuki, Satoshi Seo
  • Patent number: 9775836
    Abstract: Pharmaceuticals which are effective for treatment, prevention, and the like of cancer and have less side effects are disclosed. The antitumor agent of the present invention comprises as an effective ingredient at least one leukotriene inhibitor. Examples of the leukotriene inhibitor includes leukotriene production inhibitors and leukotriene receptor antagonists, and preferred specific examples of the leukotriene inhibitor include montelukast, zafirlukast, pranlukast, and zileuton; pharmaceutically acceptable salts of these compounds; and pharmaceutically acceptable solvates of these compounds and the salts. The leukotriene inhibitor can also be used as a relieving agent for pain accompanying a tumor(s), and as a stromal hyperplasia inhibitor.
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: October 3, 2017
    Assignee: TOCHIGI INSTITUTE OF CLINICAL PATHOLOGY
    Inventor: Masao Sugamata
  • Patent number: 9751885
    Abstract: The present invention provides a compound having a lysine specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, Alzheimer's disease, Parkinson's disease or Huntington's disease, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); B is a benzene ring optionally having further substituent(s); R1, R2 and R3 are each independently a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); A and R1 are optionally bonded to each other to form, together with the adjacent nitrogen atom, a cyclic group optionally having substituent(s); and R2 and R3 are optionally bonded to each other to form, together with the adjacent nitrogen atom, a cyclic group optionally having substituent(s), or a salt thereof.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: September 5, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Naoki Tomita, Daisuke Tomita, Yusuke Tominari, Shinichi Imamura, Shinji Morimoto, Takuto Kojima, Masashi Toyofuku, Yasushi Hattori, Tomohiro Kaku, Mitsuhiro Ito
  • Patent number: 9737523
    Abstract: Presented herein are methods for treatment of diseases or conditions related to fibrosis. Compounds, or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof provide for the treatment of diseases or conditions related to fibrosis.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: August 22, 2017
    Assignee: THE UNIVERSITY OF BRITISH COLUMBIA
    Inventors: Aziz Ghahary, Yunyuan Li, Ruhangiz T. Kilani, Ryan Hartwell
  • Patent number: 9717746
    Abstract: Synthetic ether alkyl-lysophospholipids (APLs) provide an effective treatment for subjects suffering from cholinergic seizures. Among other uses, APLs may be used to treat the effects of epileptic seizures in particular cholinergic seizures caused by exposure to insecticides or chemical warfare nerve agent exposure. Edelfosine, an APL, has been show to be particularly effective in these areas.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: August 1, 2017
    Inventor: Peter Andrew Ferchmin
  • Patent number: 9717702
    Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: August 1, 2017
    Assignee: IO Therapeutics, Inc.
    Inventor: Roshantha A. Chandraratna
  • Patent number: 9714238
    Abstract: This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: July 25, 2017
    Assignee: ALLERGAN, INC.
    Inventor: David W. Old
  • Patent number: 9701627
    Abstract: Compounds, and methods of using the same, are provided as therapies for the treatment leucine-rich repeat kinase-2 (LRRK2)-related disorders including, but not limited to, neurodegenerative and neuroinflammatory disorders, such as Parkinson's Disease.
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: July 11, 2017
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Wanli Smith, Fengtian Xue, Alexander D MacKerell, Jr.
  • Patent number: 9655872
    Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: May 23, 2017
    Assignee: IO Therapeutics, Inc.
    Inventor: Roshantha A. Chandraratna
  • Patent number: 9629835
    Abstract: A method for treating tau-associated disease by administering a pharmaceutical composition comprising a quinoline derivative to a subject in need is disclosed. Particularly, a method for treating Alzheimer's disease by administering a pharmaceutical composition comprising a quinoline derivative to a subject in need is disclosed. The two disclosed quinoline derivatives have the inhibition effect for GSK-3? kinase activity, so as the two disclosed quinoline derivatives have the ability for inhibiting tau hyperphosphorylation or reducing tau aggregation.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: April 25, 2017
    Assignee: National Taiwan Normal University
    Inventors: Guey-Jen Lee-Chen, Hsiu-Mei Hsieh, Guan-Chiun Lee, Ying-Chieh Sun
  • Patent number: 9630918
    Abstract: Cysteine, N-acetylcysteine, and penicillamine related compounds, pharmaceutical compositions comprising the cysteine, N-acetylcysteine, and penicillamine related compounds, and methods of using cysteine, N-acetylcysteine, and penicillamine related compounds and pharmaceutical compositions thereof for treating liver, kidney, lung, neurological, inflammatory, and autoimmune disorders including paracetamol overdose, non-alcoholic steatohepatitis, Wilson's disease, cystinuria, irritable bowel disorder, ulcerative colitis, rheumatoid arthritis, chronic obstructive pulmonary disease, interstitial lung disease, asthma, cystic fibrosis, Parkinson's disease, and Huntington's disease.
    Type: Grant
    Filed: September 19, 2015
    Date of Patent: April 25, 2017
    Inventor: Mark Quang Nguyen
  • Patent number: 9593136
    Abstract: In particular, the compound is effective to inhibit Dxr in Mycobacterium tuberculosis (Mtb). The present invention relates to compounds having general formula (I) or (II) where X is an acidic group, such as carboxylate, phosphonate, sulfate, and tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, preferably 2, 3, or 4. The compounds inhibits 1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr), particularly Dxr in Mycobacterium tuberculosis (Mtb).
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: March 14, 2017
    Assignees: The George Washington University, George Mason University, St. Jude Children's Research Hospital, Inc., The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Helena I. Boshoff, Cynthia S. Dowd, Emily R. Jackson, Kylene Kehn-Hall, Richard E. Lee, Robin Lee, Geraldine San Jose
  • Patent number: 9539303
    Abstract: The present invention provides compositions and methods for the treatment of /??s-expressing tumors using at least one DAC inhibitor (e.g., romidepsin).
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: January 10, 2017
    Assignee: Celgene Corporation
    Inventors: William McCulloch, Mitchell Keegan
  • Patent number: 9540373
    Abstract: This invention relates to a compound of formula I wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: January 10, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Viktor Vintonyak, Matthias Grauert, Marc Grundl, Alexander Pautsch
  • Patent number: 9512065
    Abstract: The invention provides new polymorphs of N—[(R)-1-[(S)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: December 6, 2016
    Assignee: Kalvista Pharmaceuticals Limited
    Inventors: Julian Scott Northen, John Mykytiuk
  • Patent number: 9452985
    Abstract: An object of the present invention is to provide a probe for imaging a ?-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: September 27, 2016
    Assignee: GE Healthcare Limited
    Inventors: Yukitsuka Kudo, Shozo Furumoto, Nobuyuki Okamura
  • Patent number: 9447047
    Abstract: Inhibitors of protein phosphatase-1 (PP-1) and their use in a method for the treatment or prevention of viral infections caused by HIV or ebola virus are disclosed. Inhibitors of protein phosphatase-1 in effective amounts have been shown to slow down viral replication upon contacting ebola virus or cells containing the ebola virus.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: September 20, 2016
    Assignees: Howard University, The Board of Regents of the University of Texas System
    Inventors: Sergei Nekhai, Alexander Bukreyev
  • Patent number: 9358227
    Abstract: Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives are disclosed. Specifically, the 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, are protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.
    Type: Grant
    Filed: December 1, 2014
    Date of Patent: June 7, 2016
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xin Li, Bin Wang
  • Patent number: 9233926
    Abstract: Small molecule compounds and methods for stem cell differentiation are provided herein. An example of a class of compounds that may be used to practice the methods disclosed herein is represented by enantiomerically pure isomers of compounds of Formula I: or a chirally pure stereoisomer, pharmaceutically acceptable salt, or solvate thereof, wherein R1, R2, R3, R4, R5, R5?, R6, R6?, R7, R7? are as described herein.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: January 12, 2016
    Assignees: Sanford-Burnham Medical Research Institute, Human Biomolecular Research Institute, ChemRegen, Inc.
    Inventors: Mark Mercola, John Cashman, Marion Lanier, Erik Willems, Dennis Schade
  • Patent number: 9226901
    Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: January 5, 2016
    Assignee: LOCL Pharma, Inc.
    Inventors: Paul Bosse, John Ameling, Bernard Schachtel, Ray Takigiku
  • Patent number: 9198867
    Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: December 1, 2015
    Assignee: CHARLESTON LABORATORIES, INC.
    Inventors: Paul Bosse, John Ameling, Bernard Schachtel, Ray Takigiku
  • Patent number: 9162983
    Abstract: The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system (CNS) bioavailability and their associated methods of preparation including their use for treatment of exposure to AChE inhibitors such as an organophosphate (OP) insecticides and nerve agents.
    Type: Grant
    Filed: May 22, 2014
    Date of Patent: October 20, 2015
    Assignee: SOUTHWEST RESEARCH INSTITUTE
    Inventors: William E. Bauta, William R. Cantrell, Jr., Michael W. Tidwell
  • Patent number: 9150510
    Abstract: The amino acid derivative of the present invention provides a novel compound that shows excellent analgesic action. The amino acid derivative of the present invention is a novel compound that shows excellent analgesic action to not only a model animal for nociceptive pains but also a model animal for neuropathic pains, so that the amino acid derivative is very useful as a drug for treating various pain diseases.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: October 6, 2015
    Assignee: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Tomohiro Ookubo, Ko Nakamura, Hiroyoshi Nanba, Hiroyuki Yoshida, Yoshitaka Nakazawa
  • Patent number: 9110082
    Abstract: The present invention relates to methods for treating a dalotuzumab responsive cancer, in a patient, comprising determining the expression level of liver kinase B1 (LKB1), in a cancer cell from the patient, and when said expression is determined to be lower than that of a control cell; administering, to said patient, a therapeutically effective amount of dalotuzumab. The invention also relates to methods for assessing neoplastic cells, selecting patients, selecting therapies as well as diagnostic methods.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: August 18, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Sriram Sathyanarayanan, Christopher Winter, Youyuan Xu
  • Patent number: 9102621
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to 5 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): 10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 4, 2011
    Date of Patent: August 11, 2015
    Assignee: Pfizer Limited
    Inventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 9102665
    Abstract: The present invention relates to novel cysteinyl leukotriene (specifically LTD4) antagonists, mainly to quinolin, quinoxaline or benz[c]thiazole derivatives represented by the general formula (I), or the pharmaceutically acceptable salt thereof, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to cysteinyl leukotriene, in mammals, more specially in humans.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: August 11, 2015
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Rajendrasinh Rathod, Tushar Bhatt, Kiritkumar Joshi, Binaka Dole, Kadiyala V. S. N. Murty, Rajamannar Thennati
  • Patent number: 9096500
    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 X, Ar1, 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 4, 2011
    Date of Patent: August 4, 2015
    Assignee: Pfizer Limited
    Inventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150148360
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.
    Type: Application
    Filed: July 19, 2013
    Publication date: May 28, 2015
    Inventors: Jung-Hsin Lin, Jim-Min Fang, Ting-Rong Chen, Jhih-Bin Chen, Ching-Chow Chen, Tzu-Tang Wei
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150148376
    Abstract: The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Michael HAHN, Markus Follmann, Walter Hübsch, Eva-Maria Becker, Johannes-Peter Stasch, Joerg Keldenich, Martina Delbeck, Hanna Tinel, Frank Wunder, Joachim Mittendorf, IIdiko Terebesi, Dieter Lang, René Martin
  • Patent number: 9040553
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9040021
    Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: May 26, 2015
    Assignee: GE Healthcare Limited
    Inventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
  • Publication number: 20150141422
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20150141415
    Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 21, 2015
    Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
  • Patent number: 9034901
    Abstract: The invention provides the process for the preparation of pitavastatin and its pharmaceutically acceptable salts thereof. In particular, the invention provides a process for the preparation of stable pitavastatin calcium in crystalline form having water content less than 5% wt/wt. The present invention also provides stable crystalline form of pitavastatin calcium substantially free from crystal Form-A and use thereof for pharmaceutical compositions.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: May 19, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Dhimant Jasubhai Patel, Alpesh Pravinchandra Shah, Brij Khera
  • Patent number: 9029392
    Abstract: Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 12, 2015
    Assignee: UCB Pharma S.A.
    Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Judi Charlotte Neuss, Joanna Rachel Quincey, Jackalyn Hinkins
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Publication number: 20150126549
    Abstract: The present invention relates to the general field of the treatment and prevention of diseases involving an inflammatory condition, namely sepsis or infectious or viral diseases as well as diseases requiring for the of treatment an immunosuppressive activity namely autoimmune diseases and graft rejection. In particular, the invention relates to an inhibitor of the activity or the formation of the PP1/GADD34 complex for the treatment of a condition requiring an immunosuppressive activity or an anti-inflammatory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 7, 2015
    Applicants: INSERM (Institut National de la Sante et de la Recherche Medicale), Universite d'Aix-Marseille
    Inventor: Philippe Pierre