Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring (e.g., Pyrrole, Etc.) Patents (Class 514/427)
  • Patent number: 9795620
    Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: October 24, 2017
    Assignee: Dr. Reddy's Laboratories, Ltd.
    Inventors: Ankit Baheti, Bijay Kumar Padhi, Supritha Vakada, Rajeev Singh Raghuvanshi
  • Publication number: 20150148362
    Abstract: The present invention relates to a pharmaceutical composition or a functional health food comprising a verbenone derivative and pharmaceutically acceptable salts thereof as active ingredients for treating or preventing a neurodegenerative disease. More specifically, the verbenone derivative according to the present invention reduces neuronal cell death and oxidative stress, and is highly effective in preventing ischemic brain damage and inflammatory cell migration in rats, thereby providing the pharmaceutical composition or the functional health food which is useful in treating neurodegenerative diseases.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 28, 2015
    Inventors: Won Ki Kim, Yongseok Choi, Sumi Song
  • Publication number: 20150133390
    Abstract: Methods for identifying new therapeutic activities for known therapeutic agents, as well as systems for practicing the same, are provided. Aspects of the invention further include are methods and compositions for the treatment of an acute graft rejection (AR).
    Type: Application
    Filed: January 25, 2013
    Publication date: May 14, 2015
    Applicant: National Institutes of Health (NIH), U.S. Dept. of Health and Human Services (DHHS), U.S. Govt.
    Inventors: Purvesh Khatri, Atul J. Butte, Minnie M. Sarwal
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9029402
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: January 2, 2014
    Date of Patent: May 12, 2015
    Assignee: Nivalis Therapeutics, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20150126570
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: January 15, 2015
    Publication date: May 7, 2015
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Patent number: 9023882
    Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: May 5, 2015
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Patent number: 8999358
    Abstract: The present invention relates to aqueous insecticidal preparations in the form of an aqueous dispersion of finely divided polymer particles which comprise at least one insecticidal organic active ingredient with a solubility in water of not more than 5 g/l at 25° C. at 1013 mbar and which have a mean particle size, determined by dynamic light scattering, of not more than 300 nm, where the polymer particles which comprise the at least one insecticidal active ingredient of a cationic surface charge and where the aqueous dispersion of the active-ingredient-comprising polymer particles is obtainable by subjecting a monomer composition of ethylenically unsaturated monomers M, in which the ethylenically unsaturated monomers M comprise the at least one insecticidal active ingredient in dissolved form, to radical aqueous emulsion polymerization.
    Type: Grant
    Filed: March 8, 2006
    Date of Patent: April 7, 2015
    Assignee: BASF Aktiengesellschaft
    Inventors: Patrick Amrhein, Gunnar Kleist, Dirk Haentzschel, Joerg Habicht, Holger Schöpke
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Patent number: 8993574
    Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: March 31, 2015
    Assignee: F2G Ltd
    Inventors: Graham Edward Morris Sibley, Robert Downham, Lloyd James Payne, Derek Law, Jason David Oliver, Mike Birch, Gareth Morse Davies, Patricia Suling Davies
  • Patent number: 8987322
    Abstract: The present invention relates to formulations comprising therapeutically effective amounts of at least one acid-stable, carrier-mediated transport statin, at least one poorly water-soluble, carrier-mediated transport statin, or at least one large molecular weight, carrier-mediated transport statin, such as atorvastatin and rosuvastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to exhibit a controlled-release of a therapeutic amount of the statin in the small intestine, thereby limiting systemic exposure of the statin and maximizing liver-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.
    Type: Grant
    Filed: October 19, 2004
    Date of Patent: March 24, 2015
    Assignee: Circ Pharma Research and Development Limited
    Inventors: Jackie Butler, John Devane, Paul Stark
  • Publication number: 20150080381
    Abstract: Method of treating alopecia and acne with are disclosed.
    Type: Application
    Filed: April 12, 2013
    Publication date: March 19, 2015
    Inventors: Mark G. Currie, Yueh-tyng Chien
  • Patent number: 8975292
    Abstract: The present invention relates to a method for controlling arthropods comprising the application of an aqueous gel which contains an insecticide, an attractant and a thickener, wherein the aqueous gel is applied in the form of spots on fruit trees. The invention further relates to an aqueous gel comprising an insecticide, an attractant, a thickener, a humectant and a feeding stimulant. The invention also relates to a concentrated gel for preparing the aqueous gel.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: March 10, 2015
    Assignee: BASF SE
    Inventors: Claude Taranta, Tatjana Levy, Ouidad Benlahmar, Marc Nolte, Thomas Kröhl, Christoph Randt, Thomas Bork, Wolfgang Meier, Clark D. Klein, Tiffany Hennessey
  • Patent number: 8957105
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: February 17, 2015
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8912227
    Abstract: The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: December 16, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Michael P. Winters
  • Patent number: 8906954
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: December 9, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: Erik Verner, Sriram Balasubramanian, Joseph J. Buggy
  • Patent number: 8906946
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: December 9, 2014
    Assignee: Dompe' S.p.A.
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Publication number: 20140323501
    Abstract: Immune-modulators of formula (I) below are prepared: A pharmaceutical composition contains the immune-modulators. The pharmaceutical composition is used as a drug, especially as an immune-modulating drug. The compound can be used in treatment of immune disorders and for immune suppression. Thus, for example, the compound can be used in treating hypo-immunity, rejection after organ transplantation and auto-immune disease.
    Type: Application
    Filed: July 5, 2012
    Publication date: October 30, 2014
    Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Weijuan Han, Haijing Zhang, Xiaojian Wang, Jing Jin, Gang Li, Yi Zhang, Qiong Xiao, Wanqi Zhou, Xiaoguang Chen, Dali Yin
  • Publication number: 20140315898
    Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
    Type: Application
    Filed: December 12, 2012
    Publication date: October 23, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
  • Publication number: 20140309274
    Abstract: Compounds, methods, and compositions are provided for the treatment of cancer, neurological disorders, and fibrotic disorders. Specifically, the invention includes administering an effective amount of a compound of Formula I, II, or III, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from a cancer, neurological disorder, or fibrotic disorder.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 16, 2014
    Applicant: Avoscience, LLC
    Inventor: Richard Huber
  • Patent number: 8853126
    Abstract: The present invention relates to compositions for controlling plant pests containing the compound of the formula (I) in a mixture with specified fungicidally active compounds.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: October 7, 2014
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christoph Eredelen, Wolfram Andersch, Klaus Stenzel, Astrid Mauler-Machnik, Wolfgang Kraemer
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140275088
    Abstract: In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Timothy J. Cardozo, Jürgen Bosch, Sondra Maureen Nemetski
  • Publication number: 20140274684
    Abstract: The disclosure provides for methods of repelling, directing, altering the behavior, and controlling an insect by utilizing a compound or composition described herein. The disclosure also provides for methods of promoting the health of an insect by repelling a pest that preys on insect and/or by providing an antibiotic or nutritional supplement composition to an insect. The disclosure also provides for a composition including at least one repelling, controlling, or directing compound or composition described herein together with an insecticide, herbicide, fungicide, or miticide. Compounds, compositions, seeds, and plants useful in these methods are also described.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 18, 2014
    Applicant: BAYER CROPSCIENCE LP
    Inventors: Tai-Teh WU, Dick ROGERS, Jian ZHANG, Robert CROFT, Chi Yu Roy CHEN
  • Publication number: 20140275182
    Abstract: The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Michael P. Winters
  • Patent number: 8835480
    Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: September 16, 2014
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Nicholas G. Nickols
  • Patent number: 8778985
    Abstract: Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-? peptide (A?) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of A? in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving A?/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of A? into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.
    Type: Grant
    Filed: January 26, 2007
    Date of Patent: July 15, 2014
    Assignee: The University of Rochester
    Inventors: Berislav V. Zlokovic, Rashid Deane, Benjamin L. Miller
  • Publication number: 20140194425
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8748477
    Abstract: Dihydronepetalactone, a minor natural constituent of the essential oil of catmints (Nepeta spp.) such as Nepeta cataria, has been identified as an effective insect repellent compound. Synthesis of dihydronepetalactone may be achieved by hydrogenation of nepetalactone, the major constituent of catmint essential oils. This compound, and compositions thereof, which also has fragrance properties, may be used commercially for its insect repellent properties.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: June 10, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventor: Mark A. Scialdone
  • Patent number: 8748341
    Abstract: The present invention relates to synergistic mixtures comprising, as active components, chlorfenapyr as insecticidal compound I and a fungicidal compound II selected from the group of azoxystrobin, coumethoxystrobin, coumoxystrobin, dimoxystrobin, enestroburin, fluoxastrobin, kresoxim-methyl, metominostrobin, orysastrobin, pico-xystrobin, pyraclostrobin, pyrametostrobin, pyraoxystrobin, pyribencarb, trifloxysstrobin, 2-(ortho-((2,5-dimethylphenyl-oxymethylen)phenyl)-3-methoxy-acrylic acid methyl ester, 2-(2-(3-(2,6-dichlorophenyl)-1-methyl-allylideneaminooxymethyl)-phenyl)-2-methoxyimino-N-methyl-acetamide.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Egon Haden, Lutz Brahm
  • Publication number: 20140155447
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: February 5, 2014
    Publication date: June 5, 2014
    Applicant: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8741968
    Abstract: The invention relates to aqueous fungicidal active substance compositions and to their use in the control of harmful microorganisms and in particular in the protection of cellulose-comprising materials, particularly wood, from infection by microorganisms, in particular those harmful fungi which can damage wood or cellulose. The active substance composition according to the invention comprises: a) at least one fungicidal organic active substance with a solubility in water of not more than 5 g/l at 25° C./1013 mbar, and b) a finely-divided polymer with an average particle size, determined by dynamic light scattering, of not more than 300 nm, in which the polymer particles comprise the active substance, the polymer being formed from ethylenically unsaturated monomers M comprising: at least 60% by weight, based on the total amount of the monomers M, of at least one neutral monoethylenically unsaturated monomer M1 with a solubility in water of not more than 30 g/l at 25° C.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: June 3, 2014
    Assignee: BASF Aktiengesellschaft
    Inventors: Gunnar Kleist, Joerg Habicht, Holger Schöpke, Patrick Amrhein, Helga Göttsche
  • Publication number: 20140142107
    Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.
    Type: Application
    Filed: September 4, 2013
    Publication date: May 22, 2014
    Applicant: University of Massachusetts
    Inventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
  • Publication number: 20140128408
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 8, 2014
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
  • Publication number: 20140113945
    Abstract: The present invention is directed to novel pyrrole inhibitors of S-nitrosoglutathione reductase, pharmaceutical compositions comprising such inhibitors, and methods of using the same for liver toxicity.
    Type: Application
    Filed: July 3, 2012
    Publication date: April 24, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Gary J. Rosenthal, Charles H. Scoggin, Dorothy Colagiovanni
  • Publication number: 20140113938
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: January 2, 2014
    Publication date: April 24, 2014
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8686010
    Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: April 1, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Atsushi Hasuoka, Terufumi Takagi, Haruyuki Nishida
  • Patent number: 8673961
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: March 18, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140056951
    Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using polyamines is described.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Richard LOSICK, Illana KOLODKIN-GAL, Jon CLARDY, Shugeng CAO, Matt CABEEN, Roberto KOLTER, Liraz CHAI, Thomas BÖTTCHER
  • Publication number: 20140056952
    Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using polyamines is described.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Richard LOSICK, Illana KOLODKIN-GAL, Jon CLARDY, Shugeng CAO, Matt CABEEN, Roberto KOLTER, Liraz CHAI, Thomas BÖTTCHER
  • Patent number: 8648110
    Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: February 11, 2014
    Assignee: Dompe Pha.R.Ma S.p.A.
    Inventors: Alessio Moriconi, Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
  • Patent number: 8642628
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: February 4, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140031398
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Application
    Filed: January 27, 2012
    Publication date: January 30, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Publication number: 20140024679
    Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: December 31, 2012
    Publication date: January 23, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventor: Reviva Pharmaceuticals, Inc.
  • Publication number: 20140004174
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: May 20, 2013
    Publication date: January 2, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
  • Publication number: 20130338209
    Abstract: The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.
    Type: Application
    Filed: January 30, 2012
    Publication date: December 19, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Dhiraj Gambhire, Rajendrakumar Hariprasad Jani, Bipin Pandey, Kaushik Sata, Himanshu Kothari, Pankaj Ramanbhai Patel
  • Patent number: 8609713
    Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: December 17, 2013
    Assignee: AbbVie Inc.
    Inventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
  • Patent number: 8604027
    Abstract: A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: December 10, 2013
    Assignee: Wyeth LLC
    Inventors: Gary Sondermann Grubb, Ginger Dale Constantine