Ring Nitrogen Is Shared By The Cyclos Of The Bicyclo Ring System (e.g., Tetramisole, Etc.) Patents (Class 514/368)
  • Patent number: 10391084
    Abstract: Embodiments provided herein relate to methods and compositions for treating cancer. Some embodiments include treating lung cancers and renal cancers.
    Type: Grant
    Filed: February 21, 2018
    Date of Patent: August 27, 2019
    Assignee: Children's Hospital Medical Center
    Inventors: Jeffrey Whitsett, Yutaka Maeda
  • Patent number: 9333186
    Abstract: The invention relates to a method of treating the coat of an animal. The method includes the steps of applying a composition to the coat of the animal, diffusing the composition by action of a carrier, storing the active ingredients of the composition by the sebaceous glands of the animal, and gradually releasing the active ingredients from the sebaceous glands. The dermo-cosmetic composition includes a diffusion solvent vehicle that enables, by a simple application to one or more points of the cutaneous surface, a diffusion over the entirety thereof and at the level of the sebaceous glands. The active ingredients, primarily including a complex of essential oils and of polyunsaturated fatty acids, stored in these sebaceous glands can be salted out progressively with the sebum product to the surface of the skin.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: May 10, 2016
    Assignee: LABORATOIRE DE DERMO-COSMETIQUE ANIMALE (L.D.C.A) SAS
    Inventor: Lionel Fabries
  • Patent number: 8957066
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 17, 2015
    Assignee: Biomarin Pharmaceutical Inc.
    Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20150018342
    Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 15, 2015
    Applicant: SANOFI
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Patent number: 8895599
    Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: November 25, 2014
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
  • Publication number: 20140343066
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 20, 2014
    Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
  • Patent number: 8889678
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 8853249
    Abstract: The present invention relates to an improved method for the synthesis of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: October 7, 2014
    Assignees: Helmholtz-Zentrum für Infektionsforschungs GmbH, Medizinische Hochschule Hannover, Gottfried Wilhelm Leibniz Universität
    Inventors: Markus Kalesse, Ulrike Eggert
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Publication number: 20140194374
    Abstract: A new method of controlling worm burden in ruminants by using two different injectable anthelmintics at or about the same time to increase the time between treatments and to rely on the animal's immune response. One of the anthelmintics is a long acting formulation capable of providing a sustained release of abamectin or other macrocyclic lactone for 2-14 days, to enable the anthelmintic to remove or kill incoming larvae for a sufficiently long period of time to allow the host to recognise the incoming larvae as foreign, and thus allow the ruminant to mount an immune response against these incoming larvae. The other is a short acting anthelmintic such as levamisole designed to substantially eliminate the initial parasite population of adults, juveniles and larvae. They can be combined into a single injectable formulation with a high percentage of levamisole (preferably over 30% of the formulation w/v) together with about 1% w/v of a macrocyclic lactone such as abamectin, dissolved in glycerol formal.
    Type: Application
    Filed: August 14, 2012
    Publication date: July 10, 2014
    Applicant: VIRBAC
    Inventors: Nicola Jane Cuff, Peter Norman Pulford, Mark Colin Vickers
  • Publication number: 20140179695
    Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.
    Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
  • Publication number: 20140171452
    Abstract: Disclosed is an antidepressant, neuroprotectant, amyloid ? deposition inhibitor, or age retardant composition containing a heterocyclic compound having the general formula (I):
    Type: Application
    Filed: February 12, 2014
    Publication date: June 19, 2014
    Applicant: ZENYAKU KOGYO KABUSHIKI KAISHA
    Inventors: Yoshimasa YAMAGUCHI, Ryogo YUI, Toshiyuki MATSUNO, Kenichi SAITOH, Hitoshi MIYASHITA, Takeshi NAGATA
  • Patent number: 8658425
    Abstract: The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: February 25, 2014
    Assignee: Kyoto University
    Inventors: Norio Nakatsuji, Motonari Uesugi, Kouhei Yamada, Itsunari Minami, Tomomi Otsuji
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20140045885
    Abstract: Apicomplexan parasites that infect horses such as Sarcocystis sp., Sarcocystis neurona and Neospora hughesi may be killed with decoquinate, a 4-hydroxyquinolone and/or a naphthoquinone and enhanced effects for treatment of animal disease are seen with the addition of levamisole, imidazothiazole. Based on such parasite-killing activity, these compounds are used in methods of preventing and treating infections, neurological disease or dysfunction such as protozoal myeloencephalitis, especially equine protozoal myeloencephalitis.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 13, 2014
    Inventor: Siobhan P. Ellison
  • Publication number: 20140031389
    Abstract: The present invention relates to screening methods and pharmaceutical compositions for the treatment of inflammatory bowel disease. More particularly, the present invention relates to a method for screening a plurality of test substances useful for the prevention or treatment of an inflammatory bowel disease comprising the steps consisting of (a) testing each of the test substances for its ability to restore the integrated stress response and (b) and positively selecting the test substances capable of restoring said integrated stress response. A further aspect of the invention relates to an agent capable of restoring the integrated stress response (ISR) for use in the treatment of an inflammatory bowel disease.
    Type: Application
    Filed: April 13, 2012
    Publication date: January 30, 2014
    Applicant: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MDEICALE)
    Inventors: Eric Ogier-Denis, Xavier Treton, Eric Pedruzzi, Fanny Daniel
  • Publication number: 20130317003
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Inventor: Repligen Corporation
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130296342
    Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.
    Type: Application
    Filed: June 28, 2013
    Publication date: November 7, 2013
    Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.
    Inventors: Irina NEAGU, Michael OHLMEYER, Vidyadhar M. PARADKAR, Kurt W. SAIONZ, Koushi IWATA, Takashi OKAMURA, Tadao SHIBUTANI
  • Publication number: 20130274215
    Abstract: The present invention provides methods for the prevention, treatment and/or amelioration of fibrosis or fibrotic conditions. The present invention further provides small molecule inhibitors of Wnt- and TGF-p-mediated ?-catenin signaling to prevent, treat and/or ameliorate fibrosis or fibrotic conditions. Kits comprising small molecule inhibitors of Wnt- and TGF-p-mediated ?-catenin signaling and methods of identifying small molecule inhibitors of Wnt- and TGF-p-mediated ?-catenin signaling are also provided.
    Type: Application
    Filed: April 6, 2011
    Publication date: October 17, 2013
    Applicant: FATE THERAPEUTICS, INC.
    Inventors: R. Scott Thies, Francine S. Farouz, David Jenkins
  • Patent number: 8530504
    Abstract: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: September 10, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Kogyoku Shin, Taro Terauchi, Yoshinori Takahashi, Minako Hashizume, Kunitoshi Takeda, Kodo Shikata, Akira Inomata
  • Publication number: 20130225516
    Abstract: The subject matter disclosed herein is directed to stable, highly-effective topical formulations comprising permethrin, fipronil and a solvent system that is sufficient to solubilize these two active ingredients and limit degradation of fipronil to its sulfone, and their uses in topical applications on animals and the environment. Useful formulations comprise from about 30% to about 55% (w/w) permethrin and about 2 to 15% (w/w) fipronil and a solvent system that comprises N-methylpyrrolidone and a glycol, glycol ether, glycol ester, fatty acid ester or neutral oil, wherein the N-methylpyrrolidone and glycol, glycol ether, glycol ester, fatty acid ester or neutral oil are present in a weight:weight ratio of from about 1:2.0 to about 1:3.5, glycol, glycol ether, glycol ester, fatty acid ester or neutral oil to n-methylpyrrolidone. These two actives when combined in the described amounts have been found to have unexpected enhanced repellent activity against stable fly.
    Type: Application
    Filed: February 22, 2013
    Publication date: August 29, 2013
    Applicant: MERIAL LIMITED
    Inventors: Mark David Soll, James Pate, Lisa A. Baker
  • Publication number: 20130225591
    Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 29, 2013
    Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
  • Publication number: 20130217685
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Application
    Filed: January 8, 2013
    Publication date: August 22, 2013
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventor: University of Massachusetts
  • Publication number: 20130203692
    Abstract: This invention relates to oral veterinary compositions for combating ectoparasites and endoparasites in animals, comprising at least one systemically-acting active agent in combination with a pharmaceutically acceptable carrier. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.
    Type: Application
    Filed: January 31, 2013
    Publication date: August 8, 2013
    Applicant: MERIAL LIMITED
    Inventors: Mark David Soll, Diane Larsen, Susan Mancini Cady, Peter Cheifetz, Izabela Galeska
  • Publication number: 20130171210
    Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating acute wounds, chronic wounds and/or a wound or epithelial tissue surface that contains bacterial biofilm, including unexpected synergy between bismuth-thiol (BT) compounds and certain antibiotics, to provide topical formulations including antiseptic formulations, for management and promotion of wound healing and in particular infected wounds. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating gram-negative bacterial infections.
    Type: Application
    Filed: March 1, 2013
    Publication date: July 4, 2013
    Applicant: MICROBION CORPORATION
    Inventor: MICROBION CORPORATION
  • Publication number: 20130158018
    Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
  • Publication number: 20130156816
    Abstract: The invention features compositions, methods, and kits for the administration of an oxidatively transformed carotenoid, or a fractionated component thereof, for use in aquaculture.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 20, 2013
    Applicant: Chemaphor Inc.
    Inventors: Larry Arthur Stobbs, James Gary Nickerson, Clayton Paul Dick
  • Publication number: 20130129839
    Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.
    Type: Application
    Filed: September 1, 2011
    Publication date: May 23, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Vann Gregory, Steven Gutteridge, Andrew Edmund Taggi, James Francis Bereznak
  • Patent number: 8431603
    Abstract: A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: April 30, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Hisashi Shibata, Kodo Shikata, Akira Inomata, Kogyoku Shin, Taro Terauchi, Yoshinori Takahashi, Minako Hashizume, Kunitoshi Takeda
  • Publication number: 20130090296
    Abstract: The present invention relates to formulations for controlling parasites, comprising a combination of macrocyclic lactone compound and levamisole wherein the levamisole is in particulate form suspended in a non-aqueous solvent
    Type: Application
    Filed: June 23, 2011
    Publication date: April 11, 2013
    Inventors: Hyun Sun Cho, Perterson Fabiano Lopes
  • Publication number: 20130085157
    Abstract: This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Inventors: Emilie D. Smith, Mark E. Fitzgerald, Rong Jiang, Robert N. Atkinson, James M. Veal, Kenneth H. Huang
  • Patent number: 8404729
    Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders for their production. The compounds according to the invention can be represented by general Formula (I) and comprise also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: March 26, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20130071352
    Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Application
    Filed: November 13, 2012
    Publication date: March 21, 2013
    Applicant: IDENIX PHARMACEUTICALS, INC.
    Inventor: Idenix Pharmaceuticals, Inc.
  • Publication number: 20130065846
    Abstract: This invention relates to topical compositions for combating ectoparasites and endoparasites in animals, comprising at least one isoxazoline active agent and a pharmaceutically acceptable carrier, optionally in combination with one or more additional active agents. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 14, 2013
    Inventors: Mark D. Soll, Joseph K. Rosentel, JR., James Pate, Natalya Shub, Monica Motwani-Tejwani, Carol Belansky
  • Publication number: 20120295941
    Abstract: The present invention relates to an improved method for the synthesis of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof.
    Type: Application
    Filed: December 14, 2010
    Publication date: November 22, 2012
    Inventors: Markus Kalesse, Ulrike Eggert
  • Publication number: 20120277175
    Abstract: This invention relates to antihelminthic pharmaceutical combinations comprising iodinated aromatic compounds, such as disophenol or nitroxynil, with other pharmaceutical active ingredients targeting the treatment of animals. More specifically, this invention concerns pharmaceutical compositions comprising disophenol or nitroxynil with at least one other pharmaceutical antihelminthic active ingredient, selected from among benzimidazoles, thiabendazole, levamisole or tetramisole salts, avermectins or milbemycins and, even more preferably, levamisole salts selected from between levamisole chloride or phosphate. This invention also relates to medications and a method for treating animals comprising such antihelminthic medications.
    Type: Application
    Filed: November 5, 2010
    Publication date: November 1, 2012
    Applicant: Ouro Finp Partcipaccoes e Empreedimentos SA
    Inventors: Dolivar Coracci Neto, Nelson Henriques Fernandes Filho, Ricardo da Silva Sercheli
  • Publication number: 20120251629
    Abstract: The present invention relates to a method of treating a patient for a condition where blood flow to a tissue or organ is interrupted. This method involves administering to a patient with a hypoxic condition where blood flow to a tissue or organ is interrupted, or at risk thereof, a compound that reduces the rate of HIF-1? inactivation in cells affected by the condition, thereby treating the patient for the condition. Also disclosed is a method of treating a tumor in a patient. In addition, the present invention relates to methods of identifying compounds as candidate drugs for treatment of hypoxic conditions and for treating tumors in a subject.
    Type: Application
    Filed: October 8, 2010
    Publication date: October 4, 2012
    Applicant: UNIVERSITY OF ROCHESTER
    Inventor: Marc Halterman
  • Publication number: 20120252721
    Abstract: Provided herein are methods for treating or preventing drug-resistant hepatitis C virus infection in a subject, which comprises administering to the subject a 5,5-fused heteroarylene hepatitis C virus inhibitor compound, for example, of Formula I, IA, or IB.
    Type: Application
    Filed: March 29, 2012
    Publication date: October 4, 2012
    Applicant: IDENIX PHARMACEUTICALS, INC.
    Inventors: Cyril B. Dousson, David Dukhan, John P. Billelo, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
  • Publication number: 20120245166
    Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
    Type: Application
    Filed: October 14, 2010
    Publication date: September 27, 2012
    Applicant: Southern Research Institute
    Inventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
  • Publication number: 20120245147
    Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.
    Type: Application
    Filed: April 19, 2012
    Publication date: September 27, 2012
    Inventors: John C. REED, In-Ki Kim
  • Publication number: 20120238516
    Abstract: The present invention relates to anthelmintic compositions comprising two or more anthelmintic active agents selected from one or more of the following groups; imidazothiazoles such as levamisole, benzimidazoles such as oxfendazole, or fenbendazole, macrocylic lactones such as ivermectin or avermectin, salicylanilides, and praziquantel. The composition being in the form of stable granules that are readily dispersible in water so as to provide a homogenous mixture of the anthelmintic agents suitable for administration. Methods of preparing the composition are also described.
    Type: Application
    Filed: March 7, 2012
    Publication date: September 20, 2012
    Inventors: Douglas Robert Cleverly, Debashis Mukhopadhyay
  • Patent number: 8263631
    Abstract: Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I) and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).
    Type: Grant
    Filed: July 30, 2008
    Date of Patent: September 11, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Kosaku Fujiwara, Naomi Shimazaki
  • Patent number: 8252822
    Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: August 28, 2012
    Assignee: Acea Biosciences, Inc.
    Inventors: Haoyun An, Biao Xi, Yama Abassi, Xiaobo Wang, Xiao Xu
  • Publication number: 20120196865
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Application
    Filed: July 19, 2010
    Publication date: August 2, 2012
    Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Patent number: 8227427
    Abstract: Veterinarian composition comprising an organic salt of levamisole in combination with at least one avermectin and/or milbemycin. A veterinarian formulation comprising of organics salts of levamisole, more specifically to the levamisole salt of 2,6-diiodo-4-nitrophenol and the levamisole salt of 4-hydroxy-3-iodo-5-nitrobenzonitrile with avermectins and milbemycins and its use in treatment of helminthiasis in mammals, in particular in bovines, swines, caprines, equines, ovines, canines and felines.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: July 24, 2012
    Assignee: NPA—Nucleo de Pesquisas Aplicadas Ltda.
    Inventors: Dolivar Coracci Neto, Nelson Henriques Fernandes Filho, Ricardo da Silva Sercheli
  • Publication number: 20120114633
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Application
    Filed: April 6, 2010
    Publication date: May 10, 2012
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
  • Publication number: 20120108576
    Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 3, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande