C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/350)
  • Patent number: 10752919
    Abstract: The present invention relates in part to nucleic acids encoding proteins, therapeutics comprising nucleic acids encoding proteins, methods for inducing cells to express proteins using nucleic acids, methods, kits and devices for transfecting, gene editing, and reprogramming cells, and cells, organisms, and therapeutics produced using these methods, kits, and devices. Methods and products for altering the DNA sequence of a cell are described, as are methods and products for inducing cells to express proteins using synthetic RNA molecules. Therapeutics comprising nucleic acids encoding gene-editing proteins are also described.
    Type: Grant
    Filed: October 18, 2019
    Date of Patent: August 25, 2020
    Assignee: Factor Bioscience Inc.
    Inventors: Matthew Angel, Christopher Rohde
  • Patent number: 10653684
    Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: May 19, 2020
    Assignee: Bayer Healthcare LLC
    Inventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
  • Patent number: 10568873
    Abstract: A therapeutic combination of drugs for the treatment of a liver cancer includes safranal or a pharmaceutically acceptable pro-drug thereof, and sorafenib. In representative embodiments, the pro-drug is selected from the group of a safranal salt, hydrate, hemiacetal, acetal, thioacetal, silylether, tautomer, isomer, and combinations thereof. The safranal and the sorafenib may be compounded together in a same unitary pharmaceutical composition including both compounds. Alternatively, the safranal and the sorafenib may be provided in the form of separate pharmaceutical compositions.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: February 25, 2020
    Assignee: United Arab Emirates University
    Inventors: Amr Amin, Ameera AlMansoori, Badriya Baig
  • Patent number: 10500196
    Abstract: Pharmaceutical compositions for simultaneous transdermal delivery of Doxylamine and Pyridoxine comprising Doxylamine or its salts, Pyridoxine or its salts or its active metabolites and a vehicle system wherein pharmaceutical compositions are liquid formulations, semisolid formulations and polymer matrices. Further pharmaceutical compositions can be incorporated into transdermal delivery systems or transdermal patches. The invention provides a method for treatment of nausea and vomiting in general, and for pregnant women in particular by continuous and simultaneous transdermal delivery of Doxylamine and Pyridoxine. This is to be accomplished through topical application of pharmaceutical compositions or by application of a transdermal delivery system or transdermal patch to the surface of the skin wherein the duration of application is once in a day, once every two days, once every three days, once every four days, once every five days, once every six days, or once in a week.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: December 10, 2019
    Assignee: Alpha To Omega Pharmaceutical Consultants, Inc.
    Inventors: Fotios M. Plakogiannis, Donald McAfee, Tamanna Lather, Marina Borovinskaya
  • Patent number: 10130647
    Abstract: The present invention discloses a new use of ginsenoside M1 for treating or preventing silicosis.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: November 20, 2018
    Assignee: SHEAU-LONG LEE
    Inventors: Sheau-Long Lee, Yu-Chieh Lee, Kuo-Feng Hua
  • Patent number: 10081614
    Abstract: The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: September 25, 2018
    Assignee: ACTURUM REAL ESTATE AB
    Inventors: Peter Söderman, Mats A. Svensson, Annika Kers, Liselott Öhberg, Katharina Högdin, Andreas Hettman, Jesper Hallberg, Maria Ek, Johan Bylund, Johan Nord
  • Patent number: 9518020
    Abstract: The present invention provides processes for the preparation of i) Regorafenib (4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, BAY 73-4506, Stivarga®) and its pharmaceutically acceptable salt thereof; ii) a crystalline solid of Regorafenib tosylate; iii) Regorafenib Polymorph I from Regorafenib tosylate, and iv) a pure 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide from 4-amino-3-fluorophenol and 4-chloro-N-methylpicolinamide in the presence of potassium tert-butoxide.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: December 13, 2016
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
  • Patent number: 9446031
    Abstract: The invention is directed to a method of inducing angiogenesis at a site in an individual in need thereof comprising administering locally to the site an effective amount of one or more agents that induce hypoxia induced factor 1? (HIF-1?). In another aspect, the invention is directed to a method of inducing angiogenesis at a site in an individual in need thereof comprising administering locally to the site an effective amount of one or more agents that induce hypoxia induced factor 1? (HIF-1?) and one or more lysophospholipids. In addition, the invention is directed to methods of generating prevascularized tissue, methods of generating a vascular network in a device and compositions thereof.
    Type: Grant
    Filed: January 16, 2013
    Date of Patent: September 20, 2016
    Assignees: National University of Singapore, Massachusetts Institute of Technology
    Inventors: Michael Raghunath, Sei Hien Lim, Roger Dale Kamm
  • Patent number: 9261514
    Abstract: A conformation-switching fluorescent protein probe for detection of alpha synuclein oligomers using an alpha synuclein (?S) variant, PG65 (SEQ ID NO: 4), together with a conformation-sensitive fluorescent molecule to create a molecular probe for rapid, specific, and quantitative detection of ?S oligomers.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: February 16, 2016
    Assignee: New York University
    Inventors: Jin Ryoun Kim, Michael Hernandez
  • Patent number: 9078933
    Abstract: Methods and processes for preparation and production of deuterated ?-diphenylurea are disclosed. Especially, a kind of deuterated ?-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenyl)-N?-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: July 14, 2015
    Assignee: Suzhou Zelgen Biopharmaceutical Co., Ltd.
    Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
  • Publication number: 20150141467
    Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: James Densmore Copp, Ann W. Newman, Anne Luong
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20150132408
    Abstract: The present invention provides sorafenib analogs for use in a method of treating a disease mediated by p21, said method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I. The present invention also provides methods of inhibiting p21 in a cell comprising contacting the cell with an effective amount of a compound of formula I.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 14, 2015
    Inventors: Robert H. Weiss, Bruce D. Hammock, Hiromi Inoue, Sung Hee Hwang
  • Publication number: 20150133464
    Abstract: The present invention generally relates to an novel injectable particle composition essentially consisting of: (a) a population of domains, wherein each domain essentially consists of a drug matrix and a population of subdomains, wherein the subdomains are evenly distributed in the drug matrix, wherein each subdomain essentially consists of an ionizable excipient, and (b) a rate controlling matrix comprising a biocompatible polymer and optionally an excipient. The particle is for the use of cancer therapy.
    Type: Application
    Filed: February 1, 2015
    Publication date: May 14, 2015
    Inventor: David Wong
  • Publication number: 20150118289
    Abstract: A nanoparticle including a hydrophobic active ingredient and a polypeptide, as well as a liposome including the nanoparticle and methods of making and using the nanoparticle.
    Type: Application
    Filed: August 29, 2014
    Publication date: April 30, 2015
    Inventors: Don-wook LEE, Jung-yong Nam, Hyun-ryoung Kim, Eun-sung Park
  • Publication number: 20150111929
    Abstract: The present invention provides an industrially suitable process for the preparation of substantially pure 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide or Sorafenib and its tosylate salt, with a suitable impurity profile and without requirement of any additional purification steps. The present invention also provides Sorafenib base (II) as stable crystalline Form-SSB. The present invention further relates to a process for the preparation of crystalline Sorafenib tosylate Form-I which is free from contamination of any other polymorphic form of Sorafenib tosylate, for e.g. Form II or Form III, and does not involve any seeding requirement for crystallization step.
    Type: Application
    Filed: December 31, 2012
    Publication date: April 23, 2015
    Inventors: Prashant Purohit, Sriram Rampalli, Mohanrao Seshagiri Vijaya Murali, Lavkumar Upalla
  • Publication number: 20150111920
    Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
    Type: Application
    Filed: November 19, 2014
    Publication date: April 23, 2015
    Inventors: Yukinori TAKE, Shinichi KOIZUMI, Takako OKUMURA, Kazuhiko NONOMURA
  • Publication number: 20150099766
    Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
  • Publication number: 20150080435
    Abstract: The present invention relates to an oral solid dosage form, in particular a tablet, comprising sorafenib tosylate polymorphic form III.
    Type: Application
    Filed: January 23, 2013
    Publication date: March 19, 2015
    Applicant: Sandoz AG
    Inventors: Stefan Scheler, Heiko Degendorfer, Johannes Raneburger, Franz Schwarz
  • Publication number: 20150079154
    Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.
    Type: Application
    Filed: July 9, 2012
    Publication date: March 19, 2015
    Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBH
    Inventors: Lars Zender, Ramona Rudalska, Daniel Dauch
  • Publication number: 20150080362
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 19, 2015
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Tamil Arasu, John David Baird, Wu Du, Olya Ginzburg, Yi Jin Kim Gorske, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Anthony Allan Turpoff, Richard Gerald Wilde, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150057298
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Inventors: William BUFFHAM, Hannah CANNING, Richard DAVENPORT, William FARNABY, Stephen MACK, Alka PARMAR, Susanne WRIGHT
  • Patent number: 8962661
    Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: February 24, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Akihiro Nishimura
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Publication number: 20150037372
    Abstract: The present invention relates to a high-density lipoprotein (HDL)-like particle composite which is a drug-encapsulating apoA-I comprising apoA-I and a drug encapsulated in the apoA-I capable of releasing the drug encapsulated in the apoA-I under acidic pH conditions, and a preparation method thereof. Since the HDL-like particle composite of the present invention can release the encapsulated drug under acidic conditions, while remaining stable under non-acidic conditions over a wide temperature range, it can be widely used for the development of target-specific drugs.
    Type: Application
    Filed: July 18, 2014
    Publication date: February 5, 2015
    Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY
    Inventors: Dae Hyuk KWEON, Jae Yoon SHIN
  • Patent number: 8946234
    Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: February 3, 2015
    Assignee: Bayer CropScience AG
    Inventors: Michael Maue, Isabelle Adelt, Wolfgang Giencke, Markus Heil, Peter Jeschke, Bernd-Wieland Krüger, Friedrich August Mühlthau, Alexander Sudau, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Martin Adamczewski, Arnd Voerste, Ulrich Görgens, Tobias Kapferer, Mark Wilhelm Drewes, Angela Becker, Eva-Maria Franken
  • Patent number: 8946438
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
  • Patent number: 8940773
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: January 27, 2015
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Patent number: 8937088
    Abstract: A compound of Formula (I), salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by multiple kinases, such as raf, VEGFR, PDGFR, FLT-3, and c-Kit.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: January 20, 2015
    Assignees: Astar Biotech LLC, Beta Pharma Canada Inc.
    Inventors: Zhaoyin Wang, Chunrong Yu
  • Publication number: 20150018393
    Abstract: The present invention provides compositions and methods for treating cancers which have acquired resistance to a KIT inhibitor by administering effective amounts of DAST.
    Type: Application
    Filed: March 5, 2014
    Publication date: January 15, 2015
    Applicant: BAYER HEALTHCARE LLC
    Inventors: Scott WILHELM, Richard GEDRICH
  • Publication number: 20150005256
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: April 16, 2014
    Publication date: January 1, 2015
    Inventors: Robert Eugene HORMANN, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Publication number: 20150005328
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Patent number: 8921403
    Abstract: The present invention relates to combinations of imazalil, or a salt thereof, and hydroxypyridones which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of imazalil, or a salt thereof, together with one or more hydroxypyridones selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine and rilopirox in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, viruses, and the like.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: December 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Jan Pieter Hendrik Bosselaers, Dany Leopold Jozefien Bylemans, Amber Paula Marcella Thys
  • Publication number: 20140378454
    Abstract: The present invention relates to the field of methods for providing components of pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to methods for providing stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 25, 2014
    Applicant: XSPRAY MICROPARTICLES AB
    Inventors: Magnus Brisander, Mustafa Demirbüker, Gérald Jesson, Martin Malmsten, Helene Dérand
  • Publication number: 20140356443
    Abstract: The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Applicant: XSPRAY MICROPARTICLES AB
    Inventors: Magnus Brisander, Mustafa Demirbüker, Gérald Jesson, Martin Malmsten, Helene Dérand
  • Publication number: 20140357676
    Abstract: A pharmaceutical composition is provided which includes sorafenib and GW5074. This combination therapy inhibits cancer cell growth via c-Raf-PP2A-DAPK signaling transduction pathway in either an in vitro or pre-clinical animal model for orthotopic spontaneous kidney cancer which simulates clinical symptoms. Formation of the bond between c-Raf and GW5074 leads to conformational change which consequently increases the affinity between sorafenib and c-Raf. Binding with the specific drug target facilitates serine 308 dephosphorylation of DAPK by PP2A and induces necrosis in cancer cells. Serine 308 of DAPK protein may also be used as a biomarker for drug screening. A novel pharmaceutical composition is provided which includes sorafenib and GW5074, a protein complex target consisting of c-Raf and DAPK for drug designing, as well as biomarkers including c-Raf protein, DAPK protein and phosphorylation status of DAPK for drug screening.
    Type: Application
    Filed: May 28, 2013
    Publication date: December 4, 2014
    Applicant: National Defense Medical Center
    Inventors: Tai-Lung CHA, Sun-Yran CHANG, Guang-Huan SUN, Chung-Chih LIN, Yi-Ta TSAI
  • Publication number: 20140336210
    Abstract: This invention relates to aryl urea compounds in combination with cytotoxic or cytostatic agents for use in treating raf kinase mediated diseases such as cancer.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Applicant: Bayer HealthCare LLC
    Inventors: CARTER A. Christopher, GIBSON Neil, HIBNER Barbara, HUMPHREY W. Rachel, TRAIL Pamela, VINCENT W. Patrick, ZHAI Yifan
  • Publication number: 20140336236
    Abstract: Novel ALK and NTRK1 fusion molecules and uses are disclosed.
    Type: Application
    Filed: April 21, 2014
    Publication date: November 13, 2014
    Applicant: FOUNDATION MEDICINE, INC.
    Inventors: Maureen T. Cronin, Doron Lipson, Roman Yelensky
  • Publication number: 20140322173
    Abstract: Embodiments of the invention are directed methods that include a thymidine kinase deficient vaccinia virus. The methods include evaluating a tumor for reperfusion after treatment with vaccinia virus and administering an anti-angiogenic agent if reperfusion is detected.
    Type: Application
    Filed: May 8, 2014
    Publication date: October 30, 2014
    Applicant: JENNEREX, INC.
    Inventors: DAVID KIRN, CAROLINE BREITBACH
  • Publication number: 20140323483
    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: Application
    Filed: May 5, 2014
    Publication date: October 30, 2014
    Applicants: University of Massachusetts, President and Fellows of Harvard College
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Publication number: 20140315958
    Abstract: The present invention relates to 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.
    Type: Application
    Filed: May 14, 2014
    Publication date: October 23, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alfons GRUENBERG, Juregen STIEHL, Katharina TENBIEF, Birgit KEIL
  • Patent number: 8865748
    Abstract: Disclosed herein is {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid and the ester and amide prodrugs thereof, that can stabilize hypoxia inducible factor-2 alpha (HIF-2?) and thereby provide a method for treating cancer. Further disclosed are compositions which comprise {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid and/or a prodrug thereof which can be used to treat cancer.
    Type: Grant
    Filed: June 5, 2012
    Date of Patent: October 21, 2014
    Assignee: Akebia Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Patent number: 8865742
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20140309264
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • Publication number: 20140309263
    Abstract: The present invention relates to methods of diagnosing a kidney disorder in a patient, as well as methods of monitoring the progression of a kidney disorder and/or methods of monitoring a treatment protocol of a therapeutic agent or a therapeutic regimen. The invention also relates to assay methods used in connection with the diagnostic methods described herein.
    Type: Application
    Filed: January 31, 2014
    Publication date: October 16, 2014
    Applicant: MESO SCALE TECHNOLOGIES, LLC
    Inventors: Simone Barbero, Eli N. Glezer, Anu Mathew, Mingyue Wang
  • Publication number: 20140296301
    Abstract: The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.
    Type: Application
    Filed: June 26, 2012
    Publication date: October 2, 2014
    Applicants: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Bottger, Georges Von Degenfeld, Julia Freundlieb, Claudia Hirth-Dietrich, Joerg Keldenich, Jurgen Klar, Uwe Muenster, Andreas Ohm, Annett Richter, Bernd Riedl
  • Publication number: 20140296240
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Gary Mark COPPOLA, Yuki IWAKI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI, Robert SUN
  • Patent number: 8846909
    Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: September 30, 2014
    Assignee: University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
  • Patent number: 8841330
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: September 23, 2014
    Assignee: Bayer Healthcare LLC
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood
  • Publication number: 20140275183
    Abstract: The present invention relates to an agent for reducing the side effects of kinase inhibitors, the agent containing at least one branched-chain amino acid selected from among isoleucine, leucine and valine or a salt thereof as an active ingredient, and also relates to an anticancer medicine containing at least one branched-chain amino acid selected from among isoleucine, leucine and valine or a salt thereof, and a kinase inhibitor.
    Type: Application
    Filed: May 29, 2014
    Publication date: September 18, 2014
    Applicants: Ajinomoto Co., Inc., Yamaguchi University
    Inventors: Naoki YAMAMOTO, Isao SAKAIDA