Chalcogen Or Nitrogen Bonded Directly At 1-, 2- Or 3-position Of The Diazole Ring By Nonionic Bonding Patents (Class 514/395)
  • Patent number: 10568869
    Abstract: The invention is directed to a method of inhibiting prostate cancer cell proliferation using a substance that inhibits the activity of a soluble adenylyl cyclase (sAC) protein. The invention also is directed to methods of diagnosing and prognosticating prostate cancer in a subject by evaluating sAC gene or protein expression in the subject.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: February 25, 2020
    Assignee: CORNELL UNIVERSITY
    Inventors: Brian Robinson, Jonathan Zippin
  • Patent number: 10292390
    Abstract: Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: May 21, 2019
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen Blackwell, Reto Frei, Anthony Breitbach, David M. Lynn, Adam H. Broderick
  • Patent number: 10207998
    Abstract: The present invention provides novel inhibitors of TAK1 having formula (I) and methods of using such compounds to treat various diseases.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: February 19, 2019
    Assignee: Duke University
    Inventors: Emily Derbyshire, Timothy A. J. Haystead, Philip F. Hughes
  • Patent number: 9790176
    Abstract: The present invention relates to compounds for the treatment of mTOR (mammalian Target Of Rapamycin) pathway related diseases. Specifically, the present invention relates to the use of aminoactonitrile derivatives (AADs) in the treatment of mTOR pathway related diseases.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: October 17, 2017
    Assignee: Pitney Pharmaceuticals Pty Limited
    Inventors: Mohammad Hossein Pourgholami, David L. Morris, Roger Aston
  • Patent number: 9695129
    Abstract: The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: July 4, 2017
    Assignee: MERIAL INC.
    Inventor: Charles Q Meng
  • Patent number: 9649313
    Abstract: This invention relates generally to the use of ITK (IL-2 inducible T-cell kinase) inhibitors for the treatment of patients who have melanoma or other solid tumors. Applicants demonstrate that ITK lentiviral small hairpin RNA knockdowns and a small molecule inhibitor can each decrease the proliferation and migration of melanoma cell lines and a small molecule inhibitor can be used to inhibit the growth of melanomas in vivo.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: May 16, 2017
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Nancy Thomas, Kathleen Dorsey, Sharon Edmiston, Pamela Groben, Craig Carson
  • Patent number: 9636328
    Abstract: The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: May 2, 2017
    Assignee: Zenith Epigenetics Ltd.
    Inventors: Shuang Liu, John Frederick Quinn, Bryan Cordell Duffy, Ruifang Wang, May Xiaowu Jiang, Gregory Scott Martin, He Zhao, Michael Ellis, Gregory Steven Wagner, Peter Ronald Young
  • Patent number: 9359305
    Abstract: The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: June 7, 2016
    Assignee: MERIAL, INC.
    Inventor: Charles Q Meng
  • Patent number: 9345710
    Abstract: Compounds and combinations of them that inhibit phosphatidic phosphohydrolase (PAP) enzymatic activity are formulated into pharmaceuticals useful in cancer treatment. Inhibitors of PAP can be used for blocking the progression of cancers that depend on the epidermal growth factor receptor (EGFR), its oncogenic variants and other members of its ErbB tyrosine kinase receptor family, through induction of their endocytosis, thus making them inaccessible to the extracellular stimuli that promote maintenance and progression of cancer.
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: May 24, 2016
    Assignee: PONTIFICA UNIVERSIDAD CATOLICA DE CHILE
    Inventors: Alfonso Gonzalez, Andrea Soza, Claudia Metz
  • Patent number: 9061011
    Abstract: Provided herein are pharmaceutical formulations of dry-powder bendamustine suitable for pharmaceutical use. Also provided are methods of producing dry-powder bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: June 23, 2015
    Inventor: Vasilios Voudouris
  • Publication number: 20150147376
    Abstract: Microparticles containing an ultraviolet light absorbing polymer and 3-iodo-2-propynyl butylcarbamate (“IPBC”) resist discoloration by sunlight and other ultraviolet light sources. Methods for preparing the microparticles produce polymer-shielded, formaldehyde-free IPBC formulations which resist discoloration and leaching, and are especially useful in water-based applications. The microparticles include a polymer or a poly(vinyl formal) homopolymer that absorbs light over a range of ultraviolet wavelengths associated with IPBC discoloration. The microparticles may be utilized in paints, stains, stuccoes, adhesives, and plastics, for example.
    Type: Application
    Filed: December 29, 2014
    Publication date: May 28, 2015
    Inventor: Jorg Thomas Wilken
  • Patent number: 9018390
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: April 28, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Patent number: 9012481
    Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: April 21, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-Jin Kim, Ae-Nim Pae, Hye-Jin Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Joo Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunice Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
  • Publication number: 20150086551
    Abstract: The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.
    Type: Application
    Filed: January 31, 2013
    Publication date: March 26, 2015
    Inventors: Yu Chen, Yi Chen
  • Patent number: 8987266
    Abstract: The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and methods of detecting such mutations as well as prognostic methods method for identifying a tumors that are susceptible to anticancer therapy such as chemotherapy and/or kinase inhibitor treatment. The methods involve determining the presence of a mutated EGFR gene or mutated EGFR protein in a tumor sample whereby the presence of a mutated EGFR gene or protein indicates the tumor is susceptible to treatment.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: March 24, 2015
    Assignee: Genentech, Inc.
    Inventor: Somasekar Seshagiri
  • Patent number: 8975247
    Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: March 10, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junion University
    Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
  • Publication number: 20150065495
    Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
  • Publication number: 20150033373
    Abstract: A novel canola variety designated VR 9561 GS and seed, plants and plant parts thereof, produced by crossing Pioneer Hi-Bred International, Inc. proprietary inbred canola varieties. Methods for producing a canola plant that comprises crossing canola variety VR 9561 GS with another canola plant. Methods for producing a canola plant containing in its genetic material one or more traits introgressed into VR 9561 GS through backcross conversion and/or transformation, and to the canola seed, plant and plant part produced thereby. This discovery relates to the canola variety VR 9561 GS, the seed, the plant produced from the seed, and variants, mutants, and minor modifications of canola variety VR 9561 GS. This discovery further relates to methods for producing canola varieties derived from canola variety VR 9561 GS.
    Type: Application
    Filed: July 23, 2013
    Publication date: January 29, 2015
    Applicant: PIONEER HI BRED INTERNATIONAL INC
    Inventors: Jayantilal Devabhai Patel, Igor Falak, Winnifred Marie Mcnabb
  • Publication number: 20150011599
    Abstract: The present invention describes a novel thickening composition that comprises a mixture of esters of an alkoxylated polyol and is used to enhance the viscosity of agrochemical formulations. The composition according to the present invention may present itself in solid for or in liquid form, in this latter case further comprising one or more surfactants, solvents, and optionally water. The thickening composition described in this invention is compatible with a large variety of pesticides and inert components used in agrochemical formulations, and it has evidence that it is capable of improving the stability and the effectiveness of the said formulations.
    Type: Application
    Filed: December 7, 2012
    Publication date: January 8, 2015
    Applicant: Oxiteno S.A. Indústria e Comércio Company
    Inventors: Oscar Osvaldo Hernandez Avila, Priscila Castelani
  • Publication number: 20150011600
    Abstract: The present invention aims to provide a compound capable of inhibiting PCA-1 that can be a target for a novel treatment method of various diseases, and pharmaceutical use of the compound. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 8, 2015
    Inventors: Kazutake Tsujikawa, Akito Tanaka, Shunji Aoki, Hiroaki Mizuno, Miyuki Tokoro, Tatsuhiko Furukawa
  • Patent number: 8921405
    Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: December 30, 2014
    Assignee: Orexo AB
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Klaus Klinder, Raimund Kuelzer, Dimitrijs Lubriks, Juergen Mack, Benjamin Pelcman, Henning Priepke, Robert Roenn, Dirk Stenkamp, Edgars Suna
  • Publication number: 20140336184
    Abstract: The present invention concerns methods and compositions regarding suppression of double stranded RNA-activated protein kinase (PKR) to enhance cognition in an individual. In specific cases, an inhibitor of PKR is provided to the individual such that cognition is enhanced thereby, including by enhancing memory, for example. Kits are encompassed in certain embodiments.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventors: Mauro Costa-Mattioli, Ping Jun Zhu, Jeremy A. May
  • Patent number: 8883837
    Abstract: The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jean-Francois Bonfanti, Koenraad Jozef Lodewijk Andries, Jérôme Michel Claude Fortin, Philippe Muller, Frédéric Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Bern Timmerman
  • Publication number: 20140329873
    Abstract: The meglumine salt of 1-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid (compound (1)) and pharmaceutically acceptable formulations thereof are described. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity.
    Type: Application
    Filed: October 25, 2012
    Publication date: November 6, 2014
    Inventors: Kia Sepassi, Michael C. Rizzolio
  • Publication number: 20140322312
    Abstract: An oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a first population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a first rate; a population of a basic substance; and a second population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a second rate. In another embodiment, the oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a population of a pharmaceutical active; a population of a basic substance; a population of enteric coated pharmaceutical active; and a population of enteric coated basic substance. The composition can provide multiple site specific delivery of a pharmaceutical active in a rapid, delayed and/or sustained release manner into the plasma.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Applicant: INTELLIPHARMACEUTICS CORP
    Inventors: Isa Odidi, Amina Odidi
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Patent number: 8865713
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: October 21, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Publication number: 20140274972
    Abstract: Compositions and Methods are described in which Albendazole sulfone binds to Wolbachia FtsZ providing anti filarial activity.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 18, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Laura Serbus, Fredric Landmann, Catharina Lindley, Pamela White, William Sullivan
  • Patent number: 8835478
    Abstract: The present invention provides methods for the treatment of tumors, comprising administration of an effective amount of at least one taxoid and an effective amount of at least one benzimidazol carbamate compound of formula (I). The invention also provides a method for the treatment of tumors insensitive to one or more anti-mitotic drugs, the method comprising administering a effective amount of at least one benzimidazole carbamate compound of formula (I). Also provide are compositions for carrying out methods of the invention.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: September 16, 2014
    Assignee: Pitney Pharmaceuticals PTY Limited
    Inventors: David L. Morris, Mohammad Hossein Pourgholami
  • Publication number: 20140255498
    Abstract: The present invention in general relates to a pharmaceutical suspension comprising nano-sized cocrystals of at least one active ingredient and at least one dicarboxylic acid. It in particular relates to a pharmaceutical suspension comprising nano-sized cocrystals of at least one anthelmintic drug and at least one dicarboxylic acid. The invention further relates to uses, methods for use and methods for manufacturing the pharmaceutical suspension according to this invention.
    Type: Application
    Filed: October 18, 2012
    Publication date: September 11, 2014
    Inventors: Jean Paul Remon, Chris Vervaet
  • Publication number: 20140256722
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Frances Meredith HOCUTT, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Patent number: 8828928
    Abstract: The inventions provided herein relate to amphiphilic peptides and particles comprising the amphiphilic peptides. Such amphiphilic peptides and particles described herein can be used as a delivery system, e.g., for therapeutic or diagnostic purposes, or as cell penetration vehicles or cell transfection agents.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: September 9, 2014
    Assignee: President and Fellows of Harvard College
    Inventors: Christian Dittrich, Gaudenz Danuser
  • Publication number: 20140249196
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: November 20, 2012
    Publication date: September 4, 2014
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
  • Patent number: 8815864
    Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: August 26, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Elke Langkopf, Holger Wagner
  • Patent number: 8809327
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: August 19, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Publication number: 20140228378
    Abstract: The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: July 7, 2012
    Publication date: August 14, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Patent number: 8796273
    Abstract: The present invention relates to the treatment, alleviation, prevention or reduction in the incidence of symptoms, diseases or conditions resulting from or associated with enteroviruses, more particularly the enteroviral infections they cause.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: August 5, 2014
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Johan Neyts, Armando De Palma, Hendrik Jan Thibaut, Pieter Leyssen, Simon Tucker
  • Patent number: 8791148
    Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: July 29, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wilfried Homberger, Liliane Unger, Juliana Ruiz Caro, Alfred Hahn
  • Publication number: 20140199296
    Abstract: A pharmaceutical composition comprising a cancer therapeutic that is capable of inhibiting and/or reducing the ability of a cancer cell to take up and utilize glucose or other energy source, a lipid or other building block of a cell membrane or organelle, and/or cholesterol. The pharmaceutical composition can comprise one or more cancer therapeutics that can be administered individually or in combination to an individual.
    Type: Application
    Filed: January 14, 2014
    Publication date: July 17, 2014
    Applicant: BIOCOPEA LIMITED
    Inventors: Robin M. Bannister, John Brew, Gregory A. Stoloff
  • Patent number: 8777134
    Abstract: This invention is directed to a pharmaceutical composition for drinking water administration comprising benzimidazole carbamate particles having an effective average particle size of less than 450 mm and a Tween-type surfactant; a method for making the composition; use of the composition to make a medicament for controlling parasites; and use of said composition for the manufacture of a medicament or protecting animal from parasitic infection.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: July 15, 2014
    Assignee: Intervet International B.V.
    Inventors: Carsten Schmidt, Mark Allan, Elizabeth Benedicte Daniele Deschamps
  • Patent number: 8772334
    Abstract: A broad spectrum antimicrobial composition consisting essentially of an iodopropynyl compound in combination with a benzimidazole and a metal borate is disclosed. The composition can be used to protect industrial systems against microbial growth and, more particularly, to protect substrates such as paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, wood-plastic composites, caulking, sealants, textiles, leather, wood, preservatives, metal working fluids, drilling muds, clay slurries, glazes, optical brighteners, carpet backing, and pigments against microbial growth. The composition can be used as a preservative for aqueous products.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: July 8, 2014
    Inventors: Kamlesh Gaglani, Maihua Yang
  • Patent number: 8759345
    Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Publication number: 20140163078
    Abstract: Methods for detecting and treating Mycobacterium-related diseases including reducing Mycobacterial virulence, reducing RV3133c dimerization, and treating a subject with a Mycobacterial infection using identified compounds are disclosed. Examples of compounds useful in the treatment of Mycobacterium-related diseases include N-(4-[(acetylamino)sulfonyl]phenyl)-3-phenylpropanamide; 1-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-(2-imino-3-methyl-2,3-dihydro-1H-benzimidazol-1yl)ethanone hydrochloride; and 1-(1,3-benzoxazol-2-yl)-3-({4-[(2-hydroxyethyl)sulfonyl]phenyl}amino)acrylaldehyde. Further disclosed are methods for identifying agents that interact with a polypeptide in a Mycobacterium cell.
    Type: Application
    Filed: November 21, 2013
    Publication date: June 12, 2014
    Applicant: The UAB Research Foundation
    Inventors: Andries J.C. Steyn, Deborah Mai, Amit Singh
  • Publication number: 20140148462
    Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: November 25, 2013
    Publication date: May 29, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias ECKHARDT, Elke LANGKOPF, Holger WAGNER
  • Publication number: 20140148398
    Abstract: Compounds useful for the treatment of giardiasis are described.
    Type: Application
    Filed: October 12, 2011
    Publication date: May 29, 2014
    Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, UNIVERSITY OF MARYLAND, COLLEGE PARK
    Inventors: Wei Zheng, Catherine Chen, Juan Jose Marugan, Noel Southall, Christopher P. Austin, Andrey Galkin, Liudmila Kulakova, Osnat Herzberg
  • Publication number: 20140142117
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20140127273
    Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
    Type: Application
    Filed: January 8, 2014
    Publication date: May 8, 2014
    Applicant: North Carolina State University
    Inventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
  • Publication number: 20140121103
    Abstract: The present invention relates to synergistic mixtures comprising at least one compound I and at least one active compound II as defined herein and to the use of these mixtures for combating phytopathogenic fungi, and to seeds coated with at least one such mixture. The invention also relates methods for combating harmful fungi using such mixtures.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: BASF SE
    Inventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
  • Patent number: 8710082
    Abstract: The various embodiments relate to a compound comprising: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, alkoxy, aryloxy, heteroaryloxy, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, acyl, acylamino, amino, alkylamino, dialkylamino, arylamino, carboxylate (—CO2H), cyano, nitro, —CONH2, heteroarylamino, oxime, alkyloxime, aryloxime, amino-oxime or halogen when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are carbon, and X is O, NR (where R is hydrogen, alkyl, aryl or acyl), S, SO (sulfoxide), SO2 (sulfone), or C(R)2 (where R=H, alkyl, aryl, alkenyl, alkynyl, or acyl); or wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen or hydroxyl when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are each independently nitrogen, and compositions, combination
    Type: Grant
    Filed: February 4, 2012
    Date of Patent: April 29, 2014
    Assignee: Board of Trustees of Michigan State University
    Inventors: Christopher Waters, Karthik Sambanthamoorthy, Matthew Neiditch, Martin Semmelhack