C=o In R Patents (Class 514/621)
  • Patent number: 10647779
    Abstract: The present invention provides immunoconjugates composed of antibodies, e.g., monoclonal antibodies, or antibody fragments that bind to mesothelin, that are conjugated to cytotoxic agents, e.g., maytansine, or derivatives thereof, and/or co-administered or formulated with one or more additional anti-cancer agents. The immunoconjugates of the invention can be used in the methods of the invention to treat and/or diagnose and/or monitor cancers, solid tumors, recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for the membrane-anchored, 40 kDa mesothelin polypeptide, which which is overexpressed in several tumors, such as pancreatic and ovarian tumors, mesothelioma and lung cancer cells.
    Type: Grant
    Filed: July 21, 2017
    Date of Patent: May 12, 2020
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Antje Kahnert, Kerstin Unterschemmann, Iring Heisler, Charlotte Kopitz, Joachim Schuhmacher
  • Patent number: 10555525
    Abstract: The present invention relates to a method of controlling abiotic stress on turfgrass using an effective non-phytotoxic amount of acibenzolar-s-methyl.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: February 11, 2020
    Assignee: Syngenta Participations AG
    Inventor: John Robert James
  • Patent number: 9770028
    Abstract: The present invention relates to a method of controlling abiotic stress on turfgrass using an effective non-phytotoxic amount of acibenzolar-s-methyl.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: September 26, 2017
    Assignee: Syngenta Participations AG
    Inventor: John Robert James
  • Patent number: 9133104
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic r
    Type: Grant
    Filed: February 13, 2014
    Date of Patent: September 15, 2015
    Assignee: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
  • Publication number: 20150141465
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Calvin W. YEE, Zhe Li
  • Publication number: 20150073021
    Abstract: The present invention provides a method of inhibiting the binding of anthrax lethal factor with protective antigen comprising contacting the anthrax lethal factor with a compound having the structure:
    Type: Application
    Filed: September 5, 2014
    Publication date: March 12, 2015
    Applicants: The Research Foundation for The State University of New York, Chem-Master International, Inc.
    Inventors: Anthony ANTONELLI, Sanford R. SIMON, Yu ZHANG, Lorne M. GOLUB, Francis JOHNSON
  • Patent number: 8946298
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more guanidine fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: February 3, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20150018355
    Abstract: Compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating leukemia. In particular, compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating acute lymphoblastic leukemia (ALL) in its various forms.
    Type: Application
    Filed: March 13, 2013
    Publication date: January 15, 2015
    Inventors: Mark R. Kelley, Melissa L. Fishel, Angelo A. Cardoso
  • Publication number: 20140371177
    Abstract: A method of treating cancer, inflammatory disease, and autoimmune disease by administering to a subject in need thereof an effective amount of one or more 1,5-dipenylpenta-1,4-dien-3-one compounds. The compounds feature either or both of the phenyl rings being substituted with hydroxyl, diethyl(2-alkoxyethyl)amine, 1-(2-alkoxyethyl)piperidine, sulfonate, phosphinate, or phosphate.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Patent number: 8895552
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: November 25, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Patent number: 8889742
    Abstract: The present invention provides methods of ameliorating or reducing the extent of ischemic injury, reperfusion injury, and myocardial infarction, by administering an inhibitor of histone deacetylase enzyme (HDAC) or an inhibitor of DNA methyltransferase enzyme (DNMT).
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: November 18, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Peter J. Gruber, Jonathan A. Epstein, Ibrahim Abdullah
  • Patent number: 8877815
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: November 4, 2014
    Assignee: Novartis AG
    Inventors: Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Qian Liu, Muneto Mogi, Nikolaus Schiering, Robert Sun
  • Publication number: 20140323457
    Abstract: The present invention relates to beta-O/S/N fatty acids and derivatives thereof, in particular the compounds of formula (I) as described and defined herein, and their pharmaceutical use, including their use in the treatment or prevention of bacterial as well as protozoan infections, in particular the treatment or prevention of infections with Gram-positive and/or Gram-negative bacteria and infectious diseases caused by and/or related to Gram-positive and/or Gram-negative bacteria. The invention further relates to the use of these compounds for preventing or eliminating biofilms.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 30, 2014
    Inventors: Thomas Böttcher, Vadim Korotkov, Katrin Lorenz-Baath, Oliver Baron, Stephan Sieber
  • Patent number: 8853281
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, 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-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Publication number: 20140275271
    Abstract: This invention provides a compound having the structure wherein ?, ?, A, B, and R1-R4 are defined herein. This invention also provides pharmaceutical compositions comprising the above compounds, a method of accelerating the healing of a wound, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: October 16, 2012
    Publication date: September 18, 2014
    Applicants: The Research Foundation for the State University of New York, Chem-Master International, Inc.
    Inventors: Lorne M. Golub, Hsi-ming Lee, Francis Johnson
  • Publication number: 20140243286
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140128463
    Abstract: Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.
    Type: Application
    Filed: June 25, 2012
    Publication date: May 8, 2014
    Applicants: China State Institute of Pharmaceutic Industry, Shanghai Institute of Pharmaceutical Industry
    Inventors: Zhenpeng Yu, Gouping Wang, Zhen Zhang, Minyu Liu, Xiaoling Huang, Ying Liu, Lin Xiao, Li Cai, Xuejun Wu, Yifang Deng, Mianli Pan, Renhai Chen, Shenrong Tang, Quanhai Liu
  • Publication number: 20140128398
    Abstract: Compounds, compositions, and formulations, and accompanying methods useful for treating disorders arising from oxidative DNA damage, including oxidative DNA damage resulting from ionizing radiation or other therapy are described herein.
    Type: Application
    Filed: June 1, 2012
    Publication date: May 8, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Mark R. Kelley, Michael R. Vasko
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Publication number: 20140094464
    Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 3, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Mark R. Kelley, James H. Wikel
  • Patent number: 8653134
    Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: February 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Catherine Vidal, Nathalie Adje, Stéphane Yvon, Jean Jacques Zeiller
  • Patent number: 8618086
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: December 31, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony deLong, John McMillan McIver, Robert Scott Youngquist
  • Publication number: 20130338160
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 19, 2013
    Inventors: Charles SHIH, Qian Shi, Hui-kang Wang
  • Patent number: 8604083
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: December 10, 2013
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. Von Borstel, Kirvin L. Hodge, Michael K. Bamat, Stephen D. Wolpe
  • Patent number: 8592438
    Abstract: A plant disease control composition comprising, as an active ingredient, a compound of formula (I) or a salt thereof, and one or more anilinopyrimidine compounds selected from the group consisting of 4,6-dimethyl-N-phenyl-2-pyrimidinamine, 4-methyl-N-phenyl-6-(1-propynyl)-2-pyrimidinamine and 4-cyclopropyl-6-methyl-N-phenyl-2-pyrimidinamine has an excellent plant disease control effect.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: November 26, 2013
    Assignee: Sumitomo Chemical Intellectual Property Service, Ltd
    Inventors: Masanao Takaishi, Norio Kimura
  • Publication number: 20130274248
    Abstract: [PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.
    Type: Application
    Filed: May 31, 2013
    Publication date: October 17, 2013
    Inventors: Kazuei Igarashi, Hiromitsu Takayama
  • Publication number: 20130261121
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 3, 2013
    Inventors: Charles C.Y. SHIH, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Patent number: 8541466
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 24, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 8519001
    Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: August 27, 2013
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
  • Publication number: 20130217692
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Application
    Filed: September 2, 2011
    Publication date: August 22, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Publication number: 20130178446
    Abstract: The present invention is directed to the topical application of the malonamide ACAT inhibitors described by Formula I. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin.
    Type: Application
    Filed: March 4, 2013
    Publication date: July 11, 2013
    Applicant: Medicis Pharmaceutical Corporation
    Inventors: Catherine R. Kostlan, Raj Neil Raheja, Meera Tugnait, Kimberly Wade
  • Patent number: 8445513
    Abstract: The invention relates to the use of certain alpha-aminoamide derivatives in the treatment of RLS and addictive disorders. The compounds of this invention are able to reduce or even stop the symptoms of RLS and addictive disorders substantially without side effects.
    Type: Grant
    Filed: April 19, 2005
    Date of Patent: May 21, 2013
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Claudia Besana, Elena Barbanti, Emanuela Izzo, Florian Thaler, Ruggero Fariello, Patricia Salvati, Luca Benatti
  • Publication number: 20130096175
    Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.
    Type: Application
    Filed: November 17, 2010
    Publication date: April 18, 2013
    Applicants: SOUTHERN RESEARCH INSTITUTE, UNIVERSITY OF ROCHESTER
    Inventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucile White, Krister Wennerberg
  • Publication number: 20130059853
    Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: April 28, 2011
    Publication date: March 7, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Simon Feldbaek Nielsen, Anne Marie Horneman, Jesper Lau, Jens Christian Hojland Larsen
  • Publication number: 20130034536
    Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Bronislava GEDULIN
  • Patent number: 8367680
    Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: February 5, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen E. Blackwell, Matthew D. Bowman, Joseph R. Stringer
  • Patent number: 8362087
    Abstract: This invention relates to pharmaceutical compositions for veterinary use in form of aqueous injectable suspensions comprising Florfenicol or Florfenicol in form of a substantially water-insoluble complex, co-crystal or salt, sterile and micronised, in a concentration up to 500 mg/ml. The suspensions enable parenteral antimicrobial therapies in animals, with limited numbers of injections and showing good general- and local tolerances. They also possess a limited sedimentation on standing as well as after shipping, are easily resuspendable and have good syringablity.
    Type: Grant
    Filed: July 30, 2004
    Date of Patent: January 29, 2013
    Assignee: Calluna Pharma BVBA
    Inventors: Erwin Embrechts, Jan Embrechts
  • Publication number: 20130005759
    Abstract: MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.
    Type: Application
    Filed: January 21, 2011
    Publication date: January 3, 2013
    Inventors: Alexander Deiters, Douglas D. Young
  • Publication number: 20120322881
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more guanidine fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 20, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20120122934
    Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
    Type: Application
    Filed: May 18, 2011
    Publication date: May 17, 2012
    Inventors: Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
  • Publication number: 20120122696
    Abstract: The invention is directed to the use of oil based suspension concentrates containing a) at least one agrochemical active compound which is solid at room temperature, b) at least one penetration enhancer, c) at least one vegetable or mineral or paraffin oil, d) at least one non-ionic surfactant or dispersing agent and/or at least one anionic surfactant or dispersing agent and e) optionally one or more other additives for the reduction of the drift of a spray liquid containing the oil-based suspension concentrate during spray application.
    Type: Application
    Filed: May 16, 2011
    Publication date: May 17, 2012
    Applicant: Bayer CropScience AG
    Inventors: Ronald Vermeer, Andrew Charles Chapple, Reinhard Frießleben
  • Publication number: 20120095051
    Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: May 14, 2010
    Publication date: April 19, 2012
    Inventors: Francis Johnson, Lorne Golub
  • Publication number: 20120093742
    Abstract: A method of modulating the flavour of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavour-modulating proportion of at least one compound of the formula I in which X is selected from CHOH, C?O, CH2—CO and CH?C(OH), Y is selected from C1-C7 linear and branched alkyl and CH2CH2OH, Z is selected from CH3 and a moiety of the formula II in which the wavy bond represents bond linking Z to X and R1 and R2 are selected from the possibilities (i) both hydrogen; (ii) independently OH and OCH3; and (iii) R1 and R2 together with their bonds to the phenyl ring form a ring of the formula —O—CH2—O—; such that, when Z is CH3, X is C?O and Y is CH2CH2OH.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 19, 2012
    Applicant: Givaudan S.A.
    Inventors: Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
  • Publication number: 20120046247
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Patent number: 8110689
    Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio-C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: February 7, 2012
    Assignee: Bayer Cropsciene AG
    Inventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
  • Patent number: 8093290
    Abstract: A solution consisting essentially of menthyl lactate and menthol carboxamide dissolved in a solvent, such as propylene glycol, which solvent is acceptable for food, oral care or cosmetic products and a method of preparing it.
    Type: Grant
    Filed: October 27, 2003
    Date of Patent: January 10, 2012
    Assignee: Givaudan SA
    Inventors: Christophe Galopin, Eduardo Moraes, Lori Tigani
  • Publication number: 20110306671
    Abstract: The invention provides ethacrynic acid derivatives useful to prevent, inhibit or treat a variety of disorders or diseases including cancer and inflammatory disorders.
    Type: Application
    Filed: December 16, 2009
    Publication date: December 15, 2011
    Applicant: The Regents of the The University of California
    Inventors: Dennis A. Carson, Howard B. Cottam, Guangyi Jin, Desheng Lu
  • Publication number: 20110269776
    Abstract: Methods of treating or suppressing oxidative stress diseases and symptoms related to oxidative stress affecting normal electron flow in the cells or caused by reactive oxygen species with redox-active therapeutics. Use of redox-active therapeutics for the reduction, suppression or treatment of oxidative stress induced by chemical agents such as contrast agents and other nephrotoxic agents, by radiation exposure, and by disruptions in the transport of oxygen to tissues, is disclosed.
    Type: Application
    Filed: October 13, 2009
    Publication date: November 3, 2011
    Applicant: Edison Pharmaceuticals, Inc.
    Inventor: Guy M. Miller
  • Publication number: 20110218214
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Application
    Filed: September 9, 2010
    Publication date: September 8, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
  • Patent number: RE42700
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: September 13, 2011
    Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State University
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs