Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
  • Patent number: 8722695
    Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: May 13, 2014
    Assignee: Autifony Therapeutics Limited
    Inventors: Giuseppe Alvaro, Anne Décor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • Publication number: 20140128374
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.
    Type: Application
    Filed: November 5, 2013
    Publication date: May 8, 2014
    Applicant: PFIZER INC
    Inventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
  • Publication number: 20140128345
    Abstract: Described are drug delivery systems incorporating electrospun fibers that comprise and deliver physicochemically diverse drug compounds. Such fibers provide significant advantages in drug agent release, such as adaptability for solid dosage delivery to mucosal tissues. This is in addition to allowing for controlled drug release. Systems and methods for large-scale electrospinning productivity are described, including novel microarchitectures allowing for variable pharmacokinetics in drug release.
    Type: Application
    Filed: November 6, 2013
    Publication date: May 8, 2014
    Applicant: UNIVERSITY OF WASHINGTON
    Inventors: Kim A. Woodrow, Cameron Ball, Anna Blakney, Emily Krogstad, Huarong Nie
  • Publication number: 20140128352
    Abstract: Compounds that modulate mitochondrial reactive oxygen species (ROS) production are provided. The compounds may modulate ROS production at defined sites without also altering energy production. Methods of using and identifying such compounds are also provided.
    Type: Application
    Filed: September 20, 2013
    Publication date: May 8, 2014
    Applicant: Buck Institute for Research on Aging
    Inventors: Martin D. Brand, Adam Orr
  • Publication number: 20140127272
    Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 8, 2014
    Applicant: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20140128373
    Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: February 1, 2012
    Publication date: May 8, 2014
    Inventors: Prabha N. Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
  • Publication number: 20140128367
    Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: June 14, 2012
    Publication date: May 8, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
  • Patent number: 8716346
    Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: May 6, 2014
    Assignee: Case Western Reserve University
    Inventors: Stanton Gerson, Lili Liu
  • Patent number: 8716184
    Abstract: A herbicide combination comprising a) at least one herbicide (A) selected from the group consisting of glyphosate (A1) and its agrochemically compatible salts, and glufosinate (A2) and its agrochemically compatible salts, and b) a herbicide (B) which is a hydrate of the compound 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyrimidinyl]-4-fluoro-N-[[methyl-(1-methylethyl)amino]sulfonyl]benzamide, and the use thereof for controlling harmful plants.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: May 6, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Alfred Angermann, Stefan Lehr, Hubert Menne, Lothar Willms, Erwin Hacker, Britta Olenik
  • Publication number: 20140121206
    Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: GlaxoSmithKliine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Publication number: 20140120182
    Abstract: The invention is based on the surprising finding that treatment with a chemotherapeutic agent such as 5-fluorouracil (5-FU) and an autophagy inducer effectively inhibit the continued growth of, and prevent the recovery following drug withdrawal, of cancer cells. In vivo, drug resistance from a failure to adequately engage in apoptotic programmed cell death leads to a recurrence of cancer and tumours can remain dormant for periods of time before re-emerging as drug resistant metastases. It has been hypothesised that autophagy (Type II cell death) may help cancer cells survive in response to growth limiting conditions, such as nutrient depletion, hypoxia, absence of growth factor, or presence of cytotoxic drug. LiCl is a known autophagy inducer and accelerates cell survival to autophagic programmed cell death.
    Type: Application
    Filed: March 5, 2013
    Publication date: May 1, 2014
    Applicant: UNIVERSITY COLLEGE CORK, NATIONAL UNIVERSITY OF IRELAND, CORK
    Inventor: UNIVERSITY COLLEGE CORK, NATIONAL UNIVERSITY OF IRELAND, CORK
  • Publication number: 20140113922
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 24, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: Yun JIN, Zehong Wan, Qing Zhang
  • Publication number: 20140113908
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY, Beatrix WAGNER
  • Publication number: 20140113921
    Abstract: The present disclosure relates to pharmaceutical compositions of pyrimidinedione derivative compounds and methods of preparing and uses thereof. The disclosure also relates to methods of enhancing bioavailability of pyrimidinedione derivative compounds in pharmaceutical compositions administered to a subject and methods of reducing the amount of a pyrimidinedione derivative compound in a pharmaceutical composition while achieving the same bioavailability in a subject.
    Type: Application
    Filed: October 18, 2013
    Publication date: April 24, 2014
    Inventors: Yanxia Li, Ping Gao, Yi Shi, Yi Gao, Jianwei Wu
  • Publication number: 20140112918
    Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.
    Type: Application
    Filed: May 30, 2012
    Publication date: April 24, 2014
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy
  • Publication number: 20140113892
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 24, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
  • Patent number: 8703725
    Abstract: The present disclosure is directed to compositions for the promotion of muscle protein synthesis and control of tumor-induced weight loss in patients that are, for example, suffering from cancer cachexia. The present disclosure is also directed to methods of administering such compositions.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: April 22, 2014
    Assignee: Nestec S.A.
    Inventors: John P. Troup, Robert R. Wolfe
  • Patent number: 8703759
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: April 22, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
  • Publication number: 20140107139
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: June 7, 2012
    Publication date: April 17, 2014
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
  • Publication number: 20140107140
    Abstract: Pharmaceutical compositions and methods for the treatment of Gulf War Illness in human patients comprising administering a central nervous system (CNS) stimulant in a daily low-dosage amount, and micronutrients acetyl L-carnitine, L-tyrosine, N-acetyl cysteine, and alpha-lipoic acid. The CNS stimulant and micronutrient components may be in admixture for convenient daily oral administration of a low dosage CNS stimulant and micronutrients in the range of about 60-250 mg acetyl L-carnitine, 50-200 mg L-tyrosine, 60-250 mg N-acetyl cysteine, and 25-100 mg alpha-lipoic acid per day.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: K-PAX Pharmaceuticals, Inc.
    Inventor: Jon D. Kaiser
  • Publication number: 20140107068
    Abstract: A marker can determine whether or not a patient has a therapeutic response to an anti-cancer agent. A novel cancer therapy employs the marker. The marker can be N-acetylglucosamine, an amino-acid-metabolism-related substance, a nucleic-acid-metabolism-related substance, a substance in the pentose phosphate pathway, a substance in the glycolytic pathway, a substance in the TCA cycle, a polyamine-metabolism-related substance, lauric acid, 6-phosphogluconic acid, butyric acid, 4-methylpyrazole, isobutylamine, glycolic acid, NADH, NAD+, or a substance involved in the metabolism of any of these substances.
    Type: Application
    Filed: February 24, 2012
    Publication date: April 17, 2014
    Applicants: KABUSHIKI KAISHA YAKULT HONSHA, KEIO UNIVERSITY
    Inventors: Yusuke Tanigawara, Akito Nishimuta, Yuki Otani, Mitsuhisa Matsuo
  • Publication number: 20140107062
    Abstract: The present invention provides compositions and methods for treating or preventing diseases associated with vascular and non-vascular body passageways, the method comprising the step of delivering to a body passageway a therapeutic agent delivered locally through a polymer matrix from an implanted stent or other structure.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: ARAVASC INC.
    Inventor: Narmada Shenoy
  • Patent number: 8697064
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: April 15, 2014
    Assignee: Pierre Fabre Medicament
    Inventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
  • Patent number: 8697125
    Abstract: The present invention provides a tablet without causing a tableting trouble, which is superior in the tablet formability, dissolution property of pharmaceutically active ingredient, and the like.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: April 15, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Akihiko Ono, Shigeyuki Marunaka, Makoto Fukuta
  • Patent number: 8697715
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: April 15, 2014
    Assignees: Array BioPharma, Inc., Genentech, Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • Patent number: 8697883
    Abstract: The invention relates to cyclopenta[c]pyrrole-2-carboxylate derivatives, to their preparation and to their therapeutic use.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: April 15, 2014
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yaiche
  • Patent number: 8697681
    Abstract: The present invention provides an antitumor agent comprising cisplatin and a combination drug of tegafur/gimeracil/oteracil potassium that ensures an excellent life-prolongation effect in advanced gastric cancer patients that is superior to that of the standard therapy in Europe and the U.S. using an agent that contains 5-FU and does not contain a dihydropyrimidine dehydrogenase inhibitor, by way of selecting the patients based on dihydropyrimidine dehydrogenase.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: April 15, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Toshinori Oka
  • Publication number: 20140100108
    Abstract: 3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.
    Type: Application
    Filed: March 26, 2012
    Publication date: April 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht, Jeffrey Martin Hills, Philippe Rinolfi, Heinz KEHNE
  • Publication number: 20140100214
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: April 10, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Patent number: 8691878
    Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: April 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Jeorg Rosenberg, Ulrich Reinhold, Bernd Liepold, Gunther Berndl, Joerg Breitenbach, Laman Alani, Soumojeet Ghosh
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140094475
    Abstract: Disclosed are solid forms of antiretroviral compounds and anti-oxidative acids, and processes for their preparation. Pharmaceutical compositions using the solid forms are also disclosed.
    Type: Application
    Filed: April 9, 2012
    Publication date: April 3, 2014
    Applicant: LAURUS LABS PRIVATE LIMITED
    Inventors: Venkata S. Indukuri, Vamsee K. Muppidi, Sree R. Joga, Seeta R. Gorantla, Satyanarayana Chava
  • Publication number: 20140094457
    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: Application
    Filed: October 2, 2013
    Publication date: April 3, 2014
    Applicant: NEW YORK UNIVERSITY
    Inventors: Lawrence B. Gardner, Timothy J. Cardozo, Leenus Martin
  • Publication number: 20140094479
    Abstract: A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (A), (ii) at least one mixing section (B), and (iii) a discharging section (E), wherein the processing element(s) defining the mixing section (B) comprise(s) a mixing element (11, 12, 13) that is derived from a screw type element (FIG. 2).
    Type: Application
    Filed: December 2, 2013
    Publication date: April 3, 2014
    Applicant: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thomas Kessler, Jörg Breitenbach, Christoph Schmidt, Matthias Degenhardt, Jörg Rosenberg, Harald Krull
  • Patent number: 8685974
    Abstract: Thienylpyri(mi)dinylazole of the formula (I) in which R1 to R8 and X1 have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: April 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Alexander Sudau, Mazen Es-Sayed, Julia Neumann, Catherine Sirven, Jürgen Benting, Christoph Andreas Braun, Ruth Meissner, Anne-Sophie Rebstock, Samir Bennabi, Philippe Desbordes, Arounarith Tuch, Philippe Rinolfi, Stephane Brunet, Hiroyuki Hadano, Marie-Claire Grosjean-Cournoyer
  • Patent number: 8686007
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 1, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8685991
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: April 1, 2014
    Assignee: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140088125
    Abstract: Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease.
    Type: Application
    Filed: April 27, 2012
    Publication date: March 27, 2014
    Applicant: JSC Grindeks
    Inventors: Ivars Kalvins, Edgars Liepins, Einars Loza, Maija Dambrova, Limars Stonans, Daina Lola, Janis Kuka, Osvalds Pugovics, Reinis Vilskersts, Solveiga Grinberga
  • Publication number: 20140088059
    Abstract: The invention provides compositions and methods for the prevention, diagnosis, or treatment of conditions affecting breast tissue. The compositions can include one or more therapeutic agents or diagnostic agents, and an effective carrier. The composition can be specifically adapted for transdermal permeation through the mammary papilla, areola, or a combination thereof, and into underlying breast tissue.
    Type: Application
    Filed: July 15, 2013
    Publication date: March 27, 2014
    Inventors: Omathanu P Perumal, Kaushalkumar Dave, Chandradhar Dwivedi, Sreevidy Santha
  • Publication number: 20140088082
    Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: The U.S.A., as represented by the Secretary, Department of Health and Human Services.
    Inventors: Sanjay A. Desai, Ajay D. Pillai
  • Publication number: 20140079693
    Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: November 15, 2013
    Publication date: March 20, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
  • Publication number: 20140080782
    Abstract: A method of diagnosing pancreatic cancer in a subject is provided. The method comprising determining a level and/or activity of at least one saliva secreted marker in a saliva sample of the subject wherein an alteration in said marker with respect to an unaffected saliva sample is indicative of the pancreatic cancer.
    Type: Application
    Filed: December 13, 2011
    Publication date: March 20, 2014
    Applicant: Hadasit Medical Research Services and Development Ltd.
    Inventors: Aaron Palmon, Omer Deutsch, Doron Aframian, Oren Lahav
  • Publication number: 20140079636
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 8673926
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: March 18, 2014
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8673910
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in formula II: or a pharmaceutically acceptable salt or hydrate thereof.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: March 18, 2014
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Publication number: 20140073651
    Abstract: The invention relates to benzamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: February 21, 2012
    Publication date: March 13, 2014
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Kurt Hilpert, Francis Hubler, Mark Murphy, Dorte Renneberg
  • Publication number: 20140073636
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 13, 2014
    Applicant: TAKEDA GMBH
    Inventor: Ulrich KAUTZ
  • Publication number: 20140073658
    Abstract: Disclosed herein are compounds, or pharmacologically acceptable salts thereof, having glucokinase activating activity.
    Type: Application
    Filed: September 9, 2013
    Publication date: March 13, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Satoru Kaneko, Hiroyuki Tsuruoka, Masatoshi Honzumi, Manabu Abe, Taishi Yoshida
  • Patent number: 8669246
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: March 11, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto
  • Patent number: 8669273
    Abstract: A combination of a 4-anilino-3-cyanoquinoline compound (e.g. HKI-272, SKI-606, EKB-569) and a capecitabine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: March 11, 2014
    Assignee: Wyeth LLC
    Inventors: Charles Michael Zacharchuk, Susan Elizabeth Quinn, Kenneth Kuan-Yuen Wang, Florence Marie Helene Binlich