Ring Nitrogen In The Additional Hetero Ring Patents (Class 514/235.5)
  • Patent number: 10357477
    Abstract: The invention provides compounds having the general formula I: and salts thereof, wherein the variables RA, RB, RC, L1, L2, L3, A, B, C, X, Y, Z, E, m, n, and p have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: July 23, 2019
    Assignee: Regents of the University of Minnesota
    Inventors: Liqiang Chen, Teng Ai
  • Patent number: 10329314
    Abstract: Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: June 25, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Antoni Krasinski, Venkat Reddy Mali, Shichang Miao, Sreenivas Punna, Yang Song, Valentino J. Stella, Yibin Zeng, Penglie Zhang
  • Patent number: 10266492
    Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.
    Type: Grant
    Filed: July 25, 2017
    Date of Patent: April 23, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Jaroslaw Kalisiak, Antoni Krasinski, Rebecca M. Lui, Jay Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Patent number: 10266505
    Abstract: The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.
    Type: Grant
    Filed: June 19, 2018
    Date of Patent: April 23, 2019
    Assignee: CEDARS-SINAI MEDICAL CENTER
    Inventors: Mouad Edderkaoui, Ramachandran Murali, Stephen Pandol
  • Patent number: 10238661
    Abstract: Disclosed are methods for treating various bacterial infections with (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-[(4S)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,2,4,4a-tetrahydro-2?H,6H-spiro[1,4-oxazino[4,3-a][1,2]oxazolo[4,5-g]quinoline-5,5?-pyrimidine]-2?,4?,6?(1?H,3?H)-trione, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: March 26, 2019
    Assignee: Entasis Therapeutics Limited
    Inventor: Michael Huband
  • Patent number: 10189830
    Abstract: Disclosed herein are alkyl-heteroaryl substituted quinone derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 29, 2019
    Assignee: BIOELECTRON TECHNOLOGY CORPORATION
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Christopher R. Cornell
  • Patent number: 10155725
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: December 18, 2018
    Assignee: MERIAL, INC.
    Inventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
  • Patent number: 10118914
    Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: November 6, 2018
    Assignee: The University of North Carolina at Greensboro
    Inventors: Patricia H. Reggio, Derek M. Shore, Dow P. Hurst
  • Patent number: 10112926
    Abstract: The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: October 30, 2018
    Assignee: Novartis AG
    Inventors: Benjamin Richard Bellenie, Graham Charles Bloomfield, Ian Bruce, Andrew James Culshaw, Edward Charles Hall, Gregory John Hollingworth, James Neef, Matthew Spendiff, Simon James Watson
  • Patent number: 10100019
    Abstract: The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.
    Type: Grant
    Filed: April 6, 2016
    Date of Patent: October 16, 2018
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Pilho Kim, Hyoung Rae Kim, Sung Yun Cho, Jae Du Ha, Hee Jung Jung, Chang Soo Yun, Jong Yeon Hwang, Chi Hoon Park, Chong Ock Lee, Sunjoo Ahn, Chong Hak Chae
  • Patent number: 10080750
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: September 25, 2018
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth C. Deselm, Hui Qiu, Yufang Xiao, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Patent number: 10076529
    Abstract: Compositions, compounds, and methods with significant antiviral effect against RNA viruses and especially orthomyxoviruses are contemplated, and target the viral promoter that is formed by the 5? and 3?-UTR sequences of the viral genome.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: September 18, 2018
    Assignee: NANT HOLDINGS IP, LLC
    Inventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure Le Ny, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
  • Patent number: 10065971
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. wherein Y is n is 1 or 2; q is 1, 2, 3, 4, 5 or 6; X is a bond, —C(O)O—, —C(O)NR8—, —C(O)—, —O— or —C(R4R4?)—; R1 is C(O)R5 or S(O)2R5.
    Type: Grant
    Filed: June 2, 2015
    Date of Patent: September 4, 2018
    Assignee: ESTEVE PHARMACEUTICALS S.A.
    Inventors: Marina Virgili-Bernado, Monica Alonso-Xalma, Carlos Alegret-Molina, Carmen Almansa-Rosales, Ramón Merce-Vidal
  • Patent number: 10035819
    Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: July 31, 2018
    Assignee: The Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Michael Downes
  • Patent number: 10010547
    Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
    Type: Grant
    Filed: February 9, 2015
    Date of Patent: July 3, 2018
    Assignee: Cascadian Therapeutics, Inc.
    Inventors: Robert George Boyle, David Winter Walker, Richard Justin Boyce, Scott Peterson, Francine Farouz, Cong Hung Vo
  • Patent number: 9944597
    Abstract: The present invention provides polysubstituted pyrrole compounds, pharmaceutically effective salts, prodrugs, solvates and hydrates thereof, having antimitotic, antiproliferative and cytotoxic activity, activity against cells expressing the drug efflux protein, P-glycoprotein, or cells expressing the ?-III isotype of tubulin and antitumor activity. Also provided are methods of utilizing these compounds for inhibiting the proliferation of cancer cells as well as their medical use, in particular for treating cancer, including drug resistant cancer.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: April 17, 2018
    Assignees: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, VIRGINIA COMMONWEALTH UNIVERSITY, UNIVERSITY OF RICHMOND
    Inventors: Glen E. Kellogg, Chenxiao Da, Ashutosh Tripathi, John T. Gupton, Nakul Telang, James A. Sikorski, Susan L. Mooberry, Cristina Rohena
  • Patent number: 9938273
    Abstract: Disclosed are compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Z2, Z3, and Z5 are as described herein, compositions thereof, and uses thereof.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: April 10, 2018
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Jeffrey Wu, Katrina Chan, Ken Dong, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Ying Zhang
  • Patent number: 9932330
    Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: April 3, 2018
    Assignees: The University of Nottingham, NewSouth Innovations PTY Limited
    Inventors: David Bates, Jonathan Morris
  • Patent number: 9926319
    Abstract: The invention provides novel substituted pyridyl piperidine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
    Type: Grant
    Filed: March 10, 2015
    Date of Patent: March 27, 2018
    Assignees: MERCK PATENT GMBH, Cancer Research Technology Limited
    Inventors: Kai Schiemann, Frank Stieber, Michel Calderini, Julian Blagg, Aurelie Mallinger, Dennis Waalboer, Christian Rink, Simon Ross Crumpler
  • Patent number: 9889138
    Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: February 13, 2018
    Assignee: Epizyme, Inc.
    Inventor: Heike Keilhack
  • Patent number: 9850207
    Abstract: Provided are methods for treating, reducing, alleviating, and/or inhibiting neuropathic pain by orally, intravenously or intrathecally administering an effective amount of an inhibitor of soluble epoxide hydrolase (“sEH”), to a patient in need thereof. The neuropathic pain treated is selected from the group consisting of post-herpetic neuralgia, trigeminal neuralgia, focal peripheral nerve injury, and anesthesia dolorosa, central pain due to stroke or mass lesion, spinal cord injury, or multiple sclerosis, and peripheral neuropathy due to diabetes, HIV, or chemotherapy.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: December 26, 2017
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Kin Sing Lee, Bora Inceoglu, Karen Wagner
  • Patent number: 9796707
    Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.
    Type: Grant
    Filed: May 31, 2017
    Date of Patent: October 24, 2017
    Assignees: The University of Nottingham, NewSouth Innovations PTY Limited
    Inventors: David Bates, Jonathan Morris
  • Patent number: 9745268
    Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: August 29, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Pingchen Fan, Jaroslaw Kalisiak, Antoni Krasinski, Rebecca Lui, Jay Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Patent number: 9717737
    Abstract: Methods of treating autophagy related diseases, e.g. cancer and malaria, using novel autophagy inhibiting agents are described.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: August 1, 2017
    Assignee: THE UNIVERSITY OF HONG KONG
    Inventors: Jianbo Yue, Yingying Lu
  • Patent number: 9675584
    Abstract: Disclosed herein are substituted pyrazinyl acrylic acids of Formula (II): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: June 13, 2017
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Patent number: 9610249
    Abstract: Methods for determining dosage of HER2-targeted anthracycline-containing immunoliposomes are disclosed, as are methods of treating cancer patients with HER2-positive tumors using dosages so determined. Upon administration, the dosages share the low cardiotoxicity profile of standard dosages of non-immunoliposomal (untargeted), anthracycline-containing liposomes.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: April 4, 2017
    Assignee: Merrimack Pharmaceuticals. Inc.
    Inventors: Joseph G. Reynolds, Kenneth J. Olivier, Jr., Bart S. Hendriks, Thomas Wickham, Stephan Klinz, Elena Geretti
  • Patent number: 9586896
    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: October 9, 2015
    Date of Patent: March 7, 2017
    Assignee: Cardioxyl Pharmaceuticals, Inc.
    Inventors: Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost, John P. Toscano
  • Patent number: 9580387
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: February 28, 2017
    Assignee: Athenex, Inc.
    Inventor: David G. Hangauer, Jr.
  • Patent number: 9573910
    Abstract: The invention relates to novel oxazolidinone compound. More particularly, the invention relates to novel [(S)—N-[[3-[4-fluoro-3-morpholino phenyl]-2-oxooxazolidin-5-yl] methyl] acetamide] compound of Formula-I which was disclosed in Indian Patent Application No. 5063/CHE/2013 and corresponding PCT/IN2014/000018. The compound is a broad spectrum antimicrobial agent effective against Multi-Drug Resistant S. Maltophilia pathogen and a large number of gram positive and gram negative pathogens. The compound has shown excellent biological activities against S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: February 21, 2017
    Assignee: Lee Pharma Limited
    Inventors: Raghu Mitra Alla, Ajay Kumar Dubey, Srinivas Reddy Mallepalli, Ramakrishna Reddy Pongilati
  • Patent number: 9452169
    Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: September 27, 2016
    Assignee: GLAXO GROUP LIMITED
    Inventor: John Liddle
  • Patent number: 9415028
    Abstract: A compound which inhibits the importation of chloride into neurons and a compound which improve the outflow of chloride from neurons for the use in treatment of autism, a pharmaceutical composition for use in the treatment of autism including such compound and a pharmaceutically acceptable carrier are described.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: August 16, 2016
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERSITE D'AIX MARSEILLE, CHU DE BREST
    Inventors: Yehezkel Ben-Ari, Eric Lemonnier
  • Patent number: 9375423
    Abstract: The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: June 28, 2016
    Assignee: Asana Biosciences, LLC
    Inventors: Sandeep Gupta, Tony Priestley, Nicholas James Laping
  • Patent number: 9376407
    Abstract: A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: June 28, 2016
    Assignee: Lee Pharma Limited
    Inventors: Raghu Mitra Alla, Ajay Kumar Dubey, Aruna Kumari Sirigiri, Naga Kama Kumar Mareedu
  • Patent number: 9359297
    Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: June 7, 2016
    Assignee: H. Lundbeck A/S
    Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
  • Patent number: 9359344
    Abstract: The present invention relates to a biaryl heterocycle substituted oxazolidinone antibacterials shown by general formula (I), a pharmaceutically acceptable salt thereof, an isomer or a prodrug thereof, wherein R1, R2, R3, R4, R5, A and B are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound in the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: June 7, 2016
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Aichen Wang
  • Patent number: 9359337
    Abstract: The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R3, X and Y are as defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: June 7, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christine E. Brotherton-Pleiss, Zhi Chen, Shawn David Erickson, Yimin Qian
  • Patent number: 9340505
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: May 17, 2016
    Assignees: University of Massachusetts, President and Fellows of Harvard College
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Patent number: 9328092
    Abstract: The present invention relates to novel acrylamide compounds of formula (I): wherein A, X, R1, and Y are as defined herein, and their pharmaceutically acceptable salts and process of their preparation. The compounds of formula (I) are useful in the treatment of various disorders that related to Histamine H3 receptors.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: May 3, 2016
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Adi Reddy Dwarampudi, Venkateswarlu Jasti
  • Patent number: 9216180
    Abstract: The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating a genetic disease caused by premature termination codons, or other conditions that render messenger ribonucleic acid (mRNA) susceptible to nonsense mediated RNA decay, in a subject. Also disclosed is a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy. The present invention also relates to a method of identifying inhibitors of nonsense mediated RNA decay and/or inducing autophagy. The present invention further relates to a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy in a subject.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: December 22, 2015
    Assignee: New York University
    Inventors: Lawrence B. Gardner, Timothy J. Cardozo, Leenus Martin
  • Patent number: 9168259
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: October 27, 2015
    Assignee: GRÜNENTHAL GMBH
    Inventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Patent number: 9156791
    Abstract: The present invention relates to a pyrazole amide derivative, pharmaceutical compositions containing this compound and to its use in therapy.
    Type: Grant
    Filed: October 19, 2011
    Date of Patent: October 13, 2015
    Assignee: Glaxo Group Limited
    Inventors: Anthony William James Cooper, Paul Martin Gore, David House
  • Patent number: 9108923
    Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: August 18, 2015
    Assignees: Howard Hughes Medical Institute, The Broad Institute, The President and Fellows of Harvard College
    Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
  • Patent number: 9089575
    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: March 5, 2015
    Date of Patent: July 28, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
  • Patent number: 9062027
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: June 23, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Moller, Wilfried Hornberger, Yanbin Lao, Gisela Backfisch, Marjoleen Nijsen
  • Patent number: 9044482
    Abstract: The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: June 2, 2015
    Assignee: Asana Biosciences, LLC
    Inventors: Sandeep Gupta, Tony Priestley, Nicholas James Laping
  • Publication number: 20150139973
    Abstract: The present invention relates to an ophthalmological vehicle system for the permeation and/or for the active substance transport of ophthalmological active substances through the cornea and/or the sclera of the eye of mammals. This vehicle system assists the transport of the active substances through the cornea and/or the sclerotic tissue of the eye. The vehicle system is suitable for the prophylaxis and/or treatment of diseases of the front and/or back portion of the eye. Likewise, the present invention relates to an ophthalmological kit, comprising a special ophthalmological composition and also, as separate formulation, an ophthalmological active substance.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Inventors: Ute Steinfeld, Frank Holzer, Hyeck Hee Lee, Markus Mahler
  • Publication number: 20150141425
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: November 3, 2014
    Publication date: May 21, 2015
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20150133297
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Application
    Filed: April 25, 2013
    Publication date: May 14, 2015
    Inventors: Jacobus Stark, Eva Louise Wilhelmine Sack
  • Publication number: 20150133411
    Abstract: Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of TRPV4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed. Compounds of the invention include N-(3-(trifluoromethyl)phenyl)-2-methyl-1-(3-morpholinopropyl)-5-phenyl-1 H-pyrrole-3-carboxamide, as well as other 2-phenyl-pyrrole carboxamide derivates and indole carboxamide derivatives.
    Type: Application
    Filed: March 15, 2013
    Publication date: May 14, 2015
    Inventors: David Krizaj, Glenn D. Prestwich, Peter Barabas, Yong Xu, Daniel Ryskamp