Patents Issued in July 10, 2014
  • Publication number: 20140194427
    Abstract: Provided is a compound of formula (I): or a pharmaceutically acceptable salt thereof. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a compound of formula (I) described herein. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 10, 2014
    Applicant: Biogen IDEC MA Inc.
    Inventor: Jianhua CHAO
  • Publication number: 20140194428
    Abstract: The invention relates generally to novel compositions and methods comprising a scyllo-inositol compound and one or both of valproic acid compound and lamotrigine. The compositions and methods provide beneficial effects in the treatment of bipolar disorders.
    Type: Application
    Filed: September 28, 2012
    Publication date: July 10, 2014
    Applicant: Elan Pharmaceuticals. Inc.
    Inventor: Elan Pharmaceuticals. Inc.
  • Publication number: 20140194429
    Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 10, 2014
    Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
  • Publication number: 20140194430
    Abstract: The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 30, 2012
    Publication date: July 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut Eis, Florian Pühler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther, Jörg Fanghänel, Daniel Korr
  • Publication number: 20140194431
    Abstract: The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: January 7, 2014
    Publication date: July 10, 2014
    Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri, Zhuming Zhang
  • Publication number: 20140194432
    Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: January 7, 2014
    Publication date: July 10, 2014
    Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri
  • Publication number: 20140194433
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Publication number: 20140194434
    Abstract: Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: MAP Pharmaceuticals, Inc.
    Inventors: Robert O. Cook, THOMAS A. ARMER, Sergey Alexandrovich KOSAREV, Dejian Xie, Jian Zhang
  • Publication number: 20140194435
    Abstract: Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: MAP Pharmaceuticals, Inc.
    Inventors: Robert O. COOK, Thomas A. ARMER, Sergey Alexandrovich KOSAREV, Dejian XIE, Jian ZHANG
  • Publication number: 20140194436
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: February 24, 2014
    Publication date: July 10, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Publication number: 20140194437
    Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
    Type: Application
    Filed: October 11, 2013
    Publication date: July 10, 2014
    Inventor: Andreas Haupt
  • Publication number: 20140194438
    Abstract: Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.
    Type: Application
    Filed: November 1, 2013
    Publication date: July 10, 2014
    Applicant: Helsinn Healthcare S.A.
    Inventors: Fabio TRENTO, Sergio CANTOREGGI, Giorgia ROSSI, Roberta CANNELLA, Daniele BONADEO
  • Publication number: 20140194439
    Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
    Type: Application
    Filed: December 4, 2013
    Publication date: July 10, 2014
    Inventor: Joseph P. Errico
  • Publication number: 20140194440
    Abstract: The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.
    Type: Application
    Filed: September 27, 2013
    Publication date: July 10, 2014
    Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
  • Publication number: 20140194441
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: January 8, 2014
    Publication date: July 10, 2014
    Applicant: Samumed, LLC
    Inventors: Sunil Kumar KC, John Hood
  • Publication number: 20140194442
    Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 10, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
  • Publication number: 20140194443
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • Publication number: 20140194444
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 10, 2014
    Inventors: Juan-Miguel Jimenez, Andrew Miller, Jeremy Green, Huai Gao, Gregory Henkel, Michael Liu, Timothy Neuberger
  • Publication number: 20140194445
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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: March 10, 2014
    Publication date: July 10, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Publication number: 20140194446
    Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
    Type: Application
    Filed: November 26, 2013
    Publication date: July 10, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Jospeh J. BUGGY, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
  • Publication number: 20140194447
    Abstract: Compounds and their pharmaceutically acceptable salts for treatment of ?-amyloid diseases, such as observed in Alzheimer's disease and synucleinopathies, such as Parkinson's disease.
    Type: Application
    Filed: October 10, 2012
    Publication date: July 10, 2014
    Inventors: Luke Esposito, Kelsey Hanson, Marisa C. Yadon, Thomas Lake, Alan D. Snow, Joel Cummings, Anil Kumar
  • Publication number: 20140194448
    Abstract: The present invention relates to a new application of phosphodiesterase inhibitors for couple infertility treatment which forms an effective alternative to the invasive assisted reproductive techniques such as conjugal artificial insemination and which consists of the transvaginal administration of a phosphodiesterase inhibitor immediately before and/or after coitus. It also relates to dosage forms suitable for the intravaginal administration of phosphodiesterase inhibitors.
    Type: Application
    Filed: June 20, 2012
    Publication date: July 10, 2014
    Inventors: Maria Carmen Pardina Palleja, Miguel Angel Vaz-Romero Uña
  • Publication number: 20140194449
    Abstract: Provided herein is an optically active pyrozolylaminoquinazaline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: Ambit Biosciences Corp.
    Inventors: Mark W. HOLLADAY, Eduardo SETTI
  • Publication number: 20140194450
    Abstract: The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment.
    Type: Application
    Filed: January 10, 2013
    Publication date: July 10, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Gurpreet Ahluwalia, Frederick C. Beddingfield, Sydney G. Edwards, Scott M. Whitcup
  • Publication number: 20140194451
    Abstract: Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.
    Type: Application
    Filed: November 22, 2013
    Publication date: July 10, 2014
    Inventors: Qun Lu, Huchen Zhou, Yanhua Chen, Amy Friesland
  • Publication number: 20140194452
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • Publication number: 20140194453
    Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.
    Type: Application
    Filed: January 31, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Andreas HAFNER, Fritz BLATTER, Martin SZELAGIEWICZ, Bernd SIEBENHAAR
  • Publication number: 20140194454
    Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: TheraVida, Inc.
    Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
  • Publication number: 20140194455
    Abstract: A thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising a pharmacologically active ingredient (A), a free physiologically acceptable acid (B) in an amount of from 0.001 wt.-% to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and a polyalkylene oxide (C) having a weight average molecular weight Mw of at least 200,000 g/mol.
    Type: Application
    Filed: February 28, 2014
    Publication date: July 10, 2014
    Applicant: GRUNENTHAL GMBH
    Inventors: Lutz BARNSCHEID, Eric GALIA, Sebastian SCHWIER, Ulrike BERTRAM, Anja GEISSLER, Kornelia GRIESSMANN, Johannes BARTHOLOMÄUS
  • Publication number: 20140194456
    Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: Purdue Pharma
    Inventors: Frank S. CARUSO, Huai-Hung KAO
  • Publication number: 20140194457
    Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20140194458
    Abstract: Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, aryl substituted C1-6 alkyl, phosphate substituted C1-6 alkyl, amino-substituted C1-6 alkyl, carboxyl substituted C1-6 alkyl, hydroxyl substituted C1-6 alkyl, and amide- substituted C1-6 alkyl; R1 is selected from hydrogen and t-butoxycarbonyl substituted amino. Also provided in the present invention are the preparation method of the derivate and the use thereof in anti-tumor drug preparation.
    Type: Application
    Filed: June 15, 2012
    Publication date: July 10, 2014
    Applicant: Northeast Forestry University
    Inventors: Yang Wang, Xiufeng Yan, Lijia Jing, Weimin Ding, Jian Zheng, Qiuying Pang, Tao Yu
  • Publication number: 20140194459
    Abstract: Methods and compositions for the treatment of alpha-adrenoceptor mediated conditions.
    Type: Application
    Filed: March 5, 2014
    Publication date: July 10, 2014
    Applicant: Vanda Pharmaceuticals, Inc.
    Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt D. Wolfgang
  • Publication number: 20140194460
    Abstract: A pharmaceutical composition comprising quinagolide for the treatment and/or prevention of endometriosis.
    Type: Application
    Filed: August 7, 2013
    Publication date: July 10, 2014
    Applicant: Ferring B.V.
    Inventors: Antonio Pellicer-Martinez, Carlos Simon-Valles, Edurne Novella-Maestre, Joan Carles Arce Saez
  • Publication number: 20140194461
    Abstract: Described herein are liquid rapamycin formulations. Described herein are methods of treating or preventing diseases or conditions, such as choroidal neovascularization, wet AMD and dry AMD, and preventing transition of dry AMD to wet AMD, using the liquid rapamycin formulations described herein.
    Type: Application
    Filed: January 9, 2014
    Publication date: July 10, 2014
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Sreenivasu MUDUMBA, Philippe JM DOR, Thierry NIVAGGIOLI, David A. WEBER, Sidiq FAROOQ
  • Publication number: 20140194462
    Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on ?7nAChR in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: October 8, 2013
    Publication date: July 10, 2014
    Applicant: Anvyl LLC
    Inventor: Richard Kanner
  • Publication number: 20140194463
    Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 10, 2014
    Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
  • Publication number: 20140194464
    Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:
    Type: Application
    Filed: October 14, 2013
    Publication date: July 10, 2014
    Inventor: Vinay K. Jain
  • Publication number: 20140194465
    Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 10, 2014
    Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
  • Publication number: 20140194466
    Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt or enantiomer thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt or enantiomer thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.
    Type: Application
    Filed: February 21, 2014
    Publication date: July 10, 2014
    Applicant: The University of Birmingham
    Inventors: Houman ASHRAFIAN, Michael Paul FRENNEAUX
  • Publication number: 20140194467
    Abstract: The invention relates to novel biological markers for plasma cell disorders, such as multiple myeloma, and in particular to the use of microRNAs as diagnostic and prognostic markers in assays for detecting such disorders. The invention also relates to methods of determining the efficacy of treating a plasma cell disorder with a therapeutic agent, and kits for carrying 5 out the assays and methods. The assays are qualitative and/or quantitative, and are adaptable to large-scale screening and clinical trials.
    Type: Application
    Filed: December 13, 2011
    Publication date: July 10, 2014
    Applicant: THE UNIVERSITY OF SUSSEX
    Inventors: Sarah Faith Newbury, Timothy James Telfer Chevassut, Christopher Iain Jones, Maria Vasilyevna Zabolotskaya, Helen Jayne Susan Stewart
  • Publication number: 20140194468
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Application
    Filed: November 10, 2013
    Publication date: July 10, 2014
    Applicants: The Governing Council of the University of Toronto, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20140194469
    Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 5, 2013
    Publication date: July 10, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • Publication number: 20140194470
    Abstract: The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R?)—, —NH(R?)— or a heteroatom chosen from O and S, it being understood that R? represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; or
    Type: Application
    Filed: March 7, 2014
    Publication date: July 10, 2014
    Applicant: SANOFI
    Inventors: Jean-Michel Altenburger, Valerie Fossey, Stephane Illiano, Geraldine Manette
  • Publication number: 20140194471
    Abstract: In one aspect, the invention relates to substituted 1-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 6, 2013
    Publication date: July 10, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindlsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney
  • Publication number: 20140194472
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.
    Type: Application
    Filed: August 26, 2012
    Publication date: July 10, 2014
    Applicants: WOMEN AND INFANTS' HOSPITAL OF RHODE ISLAND, UWM RESEARCH FOUNDATION, INC.
    Inventors: Alexander E. Arnold, Preetpal Singh Sidhu, Premchendar Nandhikonda, Rakesh K. Singh
  • Publication number: 20140194473
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 10, 2013
    Publication date: July 10, 2014
    Applicant: E I Du Pont De Nemours And Company
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Publication number: 20140194474
    Abstract: Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4?-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPAR? inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPAR? ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1? (IL-1?) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL).
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: Kaohsiung Medical University
    Inventors: Yang-Chang WU, Fang-Rong Chang, Tusty-Jiuan Hsieh, Suh-Hang Juo, An-Shen Lin, Ying-Chi Du
  • Publication number: 20140194475
    Abstract: Methods and formulations for treating animal ectoparasites, effective against parasites such as fleas and ticks are provided. The methods comprise topically co-administering a non-mobile insect growth regulator and a mobile insect growth regulator to the animal. Parasiticidal formulations for treating animal ectoparasites are also provided, which can be safe to use and avoid the many common deleterious side effects of conventional topical formulations. The topical formulations comprise a combination of two insect growth regulators, a non-mobile insect growth regulator and a mobile insect growth regulator. The topical formulation can be packaged with the two insect growth regulators together or packaged to prevent mixing of the two insect growth regulators prior to administering the topical insecticide formulation to the animal.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: The Hartz Mountain Corporation
    Inventors: William Ecker, Lance Hemsarth
  • Publication number: 20140194476
    Abstract: The present invention relates to a compound having the general formula (II), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: January 7, 2014
    Publication date: July 10, 2014
    Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley