Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly To Ring Carbon Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/404)
  • Patent number: 11174263
    Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 31, 2019
    Date of Patent: November 16, 2021
    Assignee: BIOMEA FUSION, INC.
    Inventors: Thomas Butler, Jim Palmer, Ravi Upasani, Matthew Welsch, Sridhar Vempati, Brendan Kelly, Edward Painter
  • Patent number: 11135199
    Abstract: A sublingual tablet pharmaceutical composition containing edaravone and (+)-2-borneol, and a preparation method thereof. The sublingual tablet pharmaceutical composition includes edaravone, (+)-2-camphanol, an excipient, a filler, a binder, a disintegrant, and a lubricant. The excipient is selected from one or more of mannitol, lactose, dextran, cysteine, glycine, copovidone, and beta-cyclodextrin.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: October 5, 2021
    Assignees: NEURODAWN PHARMACEUTICAL CO., LTD., SIMCERE PHARMACEUTICAL CO., LTD.
    Inventor: Yijun Wang
  • Patent number: 10894786
    Abstract: The present invention provides substituted pyrazole derivatives of formula (I) which are therapeutically useful as selective CDK12/13 inhibitors. These compounds are useful in the treatment and/or prevention of diseases and/or disorders associated with CDK12/13 in a mammal. The present invention also provides preparation of the compounds and pharmaceutical compositions with at least one of the substituted pyrazole derivatives of formula (I) or a pharmaceutically acceptable salt, an N-oxide or a stereoisomer thereof.
    Type: Grant
    Filed: April 4, 2019
    Date of Patent: January 19, 2021
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Ramulu Poddutoori, Susanta Samajdar, Subhendu Mukherjee
  • Patent number: 10344017
    Abstract: The invention provides compounds of formula (I) or a tautomer, stereoisomer, N-oxide, pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the prophylaxis or treatment of a disease state or condition mediated by ERK5, in particular cancers.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: July 9, 2019
    Inventors: Tristan Reuillon, Duncan Miller, Stephanie Myers, Lauren Molyneux, Celine Cano, Ian Hardcastle, Roger Griffin, Laurent Rigoreau, Bernard Golding, Martin Noble
  • Patent number: 10336706
    Abstract: The present invention relates to crystalline form of Eltrombopag free acid and its process for preparation.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: July 2, 2019
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Jonnala Sambi Reddy, Bandi Vamsi Krishna
  • Patent number: 9974308
    Abstract: The present invention relates to liquid termiticide compositions comprising a pyrethroid and a neonicotinoid selected from the group consisting of imidacloprid, nithiazine, thiamethoxam, dinotefuran, nitenpyram, thiacloprid and clothianadin, these compositions result in an increase in termite mortality at low application rates and a continuous chemical barrier of a termiticide in soil surrounding and beneath a structure in a locus where termites are suspected or known to exist.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: May 22, 2018
    Assignee: FMC Corporation
    Inventors: James B. Ballard, Cristi L. Palmer, Kim Watson
  • Patent number: 9908864
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: May 1, 2017
    Date of Patent: March 6, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9833548
    Abstract: The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a therapeutically effective amount of clonidine or pharmaceutically acceptable salt thereof and a polymer; wherein the depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the depot is capable of releasing (i) about 5% to about 45% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a first period of up to 48 hours and (ii) about 55% to about 95% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a subsequent period of at least 3 days.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: December 5, 2017
    Assignee: Warsaw Orthopedic, Inc.
    Inventors: William F. McKay, Amira Wohabrebbi, Vanja Margareta King, Phillip Edward McDonald, Christopher M. Hobot, Troy Carter
  • Patent number: 9770437
    Abstract: The present invention relates to compositions of eltrombopag olamine. The present invention also relates to process for preparing compositions comprising eltrombopag olamine.
    Type: Grant
    Filed: September 1, 2014
    Date of Patent: September 26, 2017
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Podili Khadgapathi, Nelluri Ramarao
  • Patent number: 9611247
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-·dihydrochloride with acrylonitrile to provide 1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazol-3-amine, by oxidizing to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: April 4, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Xiaoyong Li, Gary Roth, David E. Podhorez
  • Patent number: 9573122
    Abstract: Small crystal LTL framework type zeolites, characterized as polycrystalline aggregates, each of the aggregates comprising a plurality of spherical or cube-like crystallites and wherein each crystallite has an average crystallite size of from 10 to 50 nm, are disclosed. Such zeolites can be prepared by hydrothermal conversion of FAU framework type zeolites at low H2O/SiO2 mole ratios.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: February 21, 2017
    Assignee: Chevron U.S.A. Inc.
    Inventors: Dan Xie, Stacey Ian Zones, Robert James Saxton
  • Patent number: 9422278
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: August 23, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Maurice C. Yap, Ann M. Buysse, Daniel I. Knueppel, Yu Zhang, Negar Garizi, Noormohamed M. Niyaz, Christian T. Lowe, Ricky Hunter, Tony K. Trullinger, David A. Demeter, Dan Pernich, Carl DeAmicis, Ronald Ross, Jr., Timothy C. Johnson
  • Patent number: 9174952
    Abstract: The present invention relates to compounds of the formulae Ia and Ib, wherein 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 formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: November 3, 2015
    Assignee: SANOFI
    Inventors: Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Klaus Wirth
  • Patent number: 9120762
    Abstract: The pharmaceutically acceptable salts of bicycle-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: September 1, 2015
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
  • Publication number: 20150141440
    Abstract: A pharmaceutical composition for headache relief combines a vasoconstricting agent, a pain relief agent, and a disposition altering agent for a three-pronged approach to headache or migraine relief.
    Type: Application
    Filed: March 26, 2014
    Publication date: May 21, 2015
    Inventor: Ford Jennings Mundy
  • Publication number: 20150119375
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
  • Publication number: 20150118179
    Abstract: Biocidally active cationic analogs of N-halamine having two biocidally active groups covalently bonded together in a single molecule and having general Formula (I). Compounds of Formula (I), and precursors thereof, can be in solution form immobilized onto a substrate via physical coating or covalent chemical bonding to functionalize surfaces or added into materials as additives so as to render them biocidal. The biocidal solutions and substrates comprising the compounds or precursors of the present invention can then be used to inactivate pathogenic microorganisms.
    Type: Application
    Filed: May 16, 2013
    Publication date: April 30, 2015
    Applicant: UNIVERSITY OF MANITOBA
    Inventor: Song Liu
  • Patent number: 9005670
    Abstract: The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: April 14, 2015
    Assignee: The Johns Hopkins University
    Inventors: Rhoda Myra Alani, Philip A. Cole, Gai Yan, Erin M. Bowers
  • Patent number: 9006280
    Abstract: Pyrazolone derivative formulations are provided. The formulations include a pyrazolone derivative active agent, e.g., edaravone, and an amphiphilic solubilizing agent. Also provided are methods of making and using the subject formulations.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: April 14, 2015
    Assignees: Teikoku Pharma USA, Inc., Techno Guard Co., Ltd.
    Inventor: Kiichiro Nabeta
  • Publication number: 20150079030
    Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Applicant: GlaxoSmithKline LLC
    Inventor: Stephen Moore
  • Patent number: 8980885
    Abstract: A plant disease controlling composition comprising, as active ingredients, a compound represented by the formula (I), as well as at least one compound A selected from the group consisting of dimoxystrobin, trifloxystrobin, azoxystrobin, pyraclostrobin, a compound represented by the formula (II) and an agrochemically acceptable salt of the compound represented by the formula (II): wherein, R1, Q, X, Y, Z, M and n are as defined in the description.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: March 17, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masato Soma, Masanao Takaishi
  • Patent number: 8957102
    Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: February 17, 2015
    Assignee: Neopharm Co., Ltd.
    Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
  • Publication number: 20150038537
    Abstract: The invention relates to agents for the control of parasites on animals, comprising an active substance from the group of the phenylpyrazoles and vitamin E or a derivative thereof, such as particularly vitamin E acetate, as well as optionally a further active substance from the group of the pyrethroids and/or optionally additionally further active and/or auxiliary substances. In particular, the invention relates to the use of such agents for the control of ectoparasites such as, in particular, fleas, ticks and sand flies in pets such as, in particular, in dogs, cats and ferrets.
    Type: Application
    Filed: June 28, 2012
    Publication date: February 5, 2015
    Applicant: HANSEN-AB GMBH
    Inventors: Jochen Kalbe, Olaf Hansen
  • Publication number: 20150018388
    Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
    Type: Application
    Filed: December 11, 2013
    Publication date: January 15, 2015
    Inventors: Richard B. Silverman, Yinan Zhang
  • Publication number: 20150017267
    Abstract: The present invention relates to the prevention, reduction, inhibition and reversal of pain and inflammation in a non-human mammal by administration of an inhibitor of soluble epoxide hydrolase, as sole active agent or co-administered with other active agents.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 15, 2015
    Applicant: The Regents of the University of California
    Inventors: Alonso G.P. Guedes, Bruce D. Hammock, Christophe Morisseau
  • Patent number: 8933111
    Abstract: The invention provides a crystalline form of (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(1H-[1,2,3]triazole-4-carbonyl)amino]pentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester or its tautomer. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: January 13, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Miroslav Rapta
  • Publication number: 20150004216
    Abstract: A medicant composition is provided. The composition includes a film layer and a powder matrix layer. The powder matrix layer includes a medicant. The powder matrix layer is applied to the film layer by admixing particulate to form a powder matrix and by then applying the powder matrix to the film layer by any desired method. The composition of the powder matrix is varied to alter the dissolution rate of the medicant, the adhesion of the medicant composition, and other physical properties of the powder matrix. The powder matrix layer can be cured.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 1, 2015
    Inventor: Robert Steven Davidson
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Patent number: 8916555
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 23, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20140357687
    Abstract: This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).
    Type: Application
    Filed: October 11, 2012
    Publication date: December 4, 2014
    Applicant: Dana Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Evripidis Gavathiotis
  • Publication number: 20140357686
    Abstract: Methods for treating a variety of diseases that comprises performing auricular anesthesia of the vagus, facial, trigeminal, or glossopharyngeal nerves, or combinations thereof. A pharmaceutical composition is administered to an ear canal of a subject in need of such treatment, the composition including an analgesic and an anesthetic. Compositions useful in the taught methods are also provided.
    Type: Application
    Filed: May 5, 2014
    Publication date: December 4, 2014
    Inventor: THOMAS M. CREWS
  • Publication number: 20140348959
    Abstract: Compositions and methods for treatment of conditions such as ear pain are disclosed.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: Mark A. Mitchnick, Garry Gwozdz
  • Patent number: 8895600
    Abstract: The present invention refers to compounds with inhibitory activity against 14-3-3 proteins and their use in the treatment of tumors, in particular chronic myeloid leukemia. The invention also provides methods for the identification of 14-3-3 protein inhibitors.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: November 25, 2014
    Assignee: Università degli Studi di Siena
    Inventors: Maurizio Botta, Valentina Corradi, Federico Falchi, Manuela Mancini, Maria Alessandra Santucci
  • Publication number: 20140341991
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Shivakumar KAPSI, Francis X. Muller
  • Publication number: 20140336204
    Abstract: Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Changyi Chen, Jian-Ming Lu, Qizhi Yao
  • Publication number: 20140336205
    Abstract: Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Changyi Chen, Jian-Ming Lu, Qizhi Yao
  • Patent number: 8859605
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: October 14, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Pia Kahnberg, Bjorn Klasson, Peter Lind, Lourdes Oden, Kevin Parkes, Daniel Wiktelius
  • Patent number: 8846024
    Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventor: Stephen Moore
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140275074
    Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 24, 2012
    Publication date: September 18, 2014
    Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
  • Publication number: 20140275134
    Abstract: The disclosed subject matter provides certain N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or development of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: October 16, 2012
    Publication date: September 18, 2014
    Inventors: John P. Toscano, Daryl A. Guthrie
  • Publication number: 20140275107
    Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: GlaxoSmithKline LLC
    Inventor: Connie L. ERICKSON-MILLER
  • Publication number: 20140275193
    Abstract: Invented is a method of treating degenerative diseases/injuries, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.
    Type: Application
    Filed: June 2, 2014
    Publication date: September 18, 2014
    Inventors: Connie L. ERICKSON-MILLER, Julian JENKINS
  • Patent number: 8829038
    Abstract: The present invention provides a parasiticidal formulation comprising: Fipronil, or a veterinarily acceptable derivative thereof; at least one C1-C6 alcohol co-solvent, wherein the total amount of C1-C6 alcohol is up to 8% by weight of the formulation; at least one organic solvent which is not the C1-C6 alcohol co-solvent; and at least one crystallization inhibitor, wherein the total amount of crystallization inhibitor is from 2 to 20% by weight of the formulation. The formulations of the invention have higher flash points than known parasiticidal formulations comprising Fipronil and therefore provide safer formulations for use in the home, storage, manufacture and distribution.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: September 9, 2014
    Assignee: Velcera, Inc.
    Inventor: Martin Benedict George Donnelly
  • Patent number: 8828430
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis (monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: September 9, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis X. Muller, Shivakumar G Kapsi
  • Publication number: 20140234322
    Abstract: Disclosed are transgenic non-human mammals, which useful for the screening of thrombopoietin mimetics, thrombopoietin receptor agonists, or thrombopoietin receptor antagonists active on the human thrombopoietin receptor. The transgenic non-human mammal has a genome that comprises a stably integrated transgene construct comprising a polynucleotide sequence encoding a humanized thrombopoietin receptor wherein said transgenic non-human mammal has a baseline blood platelet count corresponding to a physiological blood platelet count of a matched non-transgenic non-human mammal. The chimeric thrombopoietin receptor comprises either the transmembrane domain of a human thrombopoietin receptor or both the extracellular and transmembrane domains of a human thrombopoietin receptor operably coupled to a cytoplasmic domain of a non-human thrombopoietin receptor.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 21, 2014
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Yuhchyau CHEN, J.H. David WU, Jane L. LIESVELD
  • Publication number: 20140235688
    Abstract: Pharmaceutically acceptable compositions of fipronil for oral delivery to mammals and methods for use of the compositions to control external parasites, such as fleas and ticks.
    Type: Application
    Filed: October 4, 2013
    Publication date: August 21, 2014
    Applicant: Piedmont Pharmaceuticals, LLC.
    Inventors: Roland H. Johnson, Douglas I. Hepler, Kathleen G. Palma
  • Patent number: 8809329
    Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: August 19, 2014
    Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.
    Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
  • Publication number: 20140228420
    Abstract: The invention provides a method for treating ALS or suppressing the disease progress thereof, or treating symptoms caused by ALS or suppressing the disease progress thereof by administering an agent containing, as an active ingredient, 3-methyl-1-phenyl-2-pyrazolin-5-one or a physiologically acceptable salt thereof, to a patient that complies with specific criteria.
    Type: Application
    Filed: September 5, 2012
    Publication date: August 14, 2014
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventor: Takatomo Yoneoka
  • Publication number: 20140212486
    Abstract: The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH).
    Type: Application
    Filed: January 17, 2014
    Publication date: July 31, 2014
    Applicant: TONIX PHARMACEUTICALS INC.
    Inventors: SETH LEDERMAN, BRUCE DAUGHERTY, LELAND J. GERSHELL, DARRYL RIDEOUT, ANDREW KAWASAKI