Patents Examined by John Mabry
  • Alkaloid aminoester derivatives and medicinal compositions thereof
    Patent number: 8492548
    Abstract: The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for their preparation, compositions comprising them, and therapeutic uses thereof.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: July 23, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Mauro Riccaboni, Stefano Bossolo
  • Phenylpropionamide compounds and the use thereof
    Patent number: 8481743
    Abstract: The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the activation of opioid receptors, particularly ?-opioid receptors. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: July 9, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Xiaoming Zhou
  • Isoxazole derivatives for use as fungicides
    Patent number: 8476446
    Abstract: The present invention relates to isoxazole compounds of formula (I) having fungicidal activity, to agricultural compositions comprising them, and to the use of said compounds and compositions in agriculture for the control of microbial pests, particularly fungal pests, on plants.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: July 2, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Camilla Corsi, Sebastian Volker Wendeborn, Carla Bobbio, Jilali Kessabi, Peter Schneiter, Valeria Grasso, Shy-Fuh Lee, Ulrich Johannes Haas, Micah Gliedt
  • Benzimidazole compound in crystal form and salt thereof
    Patent number: 8471032
    Abstract: The present invention aims to provide a stable form of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, which is free of problems of water adsorption and the like, and shows superior water solubility. The present invention provides a crystal and a salt of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide in a crystal form.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: June 25, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Sumie Sekiguchi, Takayuki Ishige, Masanori Minoguchi, Hideki Horiuchi, Shinichirou Ono, Toshihiko Tanaka
  • Heterocyclic compound and use thereof
    Patent number: 8466282
    Abstract: Compounds represented by the formulas (I) (II) wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: June 18, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara, Yoshiyuki Fukase
  • Thiophene derivatives as factor XIa inhibitors
    Patent number: 8466295
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, L1, R3, and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: December 13, 2006
    Date of Patent: June 18, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Wei Han
  • 2,5-disubstituted morpholine orexin receptor antagonists
    Patent number: 8466281
    Abstract: The present invention is directed to 2,5-disubstituted morpholine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Broc Flores, John D. Schreier
  • 1,5-dideoxy-1,5-imino-D-glucitol compounds
    Patent number: 8466291
    Abstract: 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: June 18, 2013
    Assignee: Academia Sinica
    Inventors: Chun-Hung Lin, Ching-Wen Ho
  • Pyrrolopyridine derivatives and their use as CRTH2 antagonists
    Patent number: 8455645
    Abstract: There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2, R3, R4, R5, R6, Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.
    Type: Grant
    Filed: February 3, 2010
    Date of Patent: June 4, 2013
    Assignee: Novartis AG
    Inventors: Kamlesh Jagdis Bala, Catherine Leblanc, David Andrew Sandham, Katharine Louise Turner, Simon James Watson, Lyndon Nigel Brown, Brian Cox
  • Method for the preparation of montelukast acid and sodium salt thereof in amorphous form
    Patent number: 8450491
    Abstract: A method for the preparation of montelukast acid sodium salt thereof in amorphous form has been described. The method comprises of following steps: (a) generating the dilithium dianion of 1-(mercaptomethyl)cyclopropane acetic acid, by reacting with alkyl lithium, (b) coupling the said dianion with wet mesylate to get montelukast acid in crude form, (c) obtaining DCHA salt in crude form by adding dicyclohexylamine (DCHA) to crude acid obtained in the above step (b), (d) purifying and converting the said DCHA salt in crude form, to montelukast acid in pure form, and (e) reacting the pure montelukast acid in a polar protic solvent with a source of sodium ion followed by evaporating the solvent and triturating of the residue with non-polar water immiscible solvent.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: May 28, 2013
    Assignee: Morepen Laboratories Limited
    Inventors: Sanjay Suri, Jujhar Singh, Gurdeep Singh Sarin, Madan Pal Tanwar, Manu Mahendru
  • Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof
    Patent number: 8436180
    Abstract: The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: May 7, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, Elke Hartmann
  • Pharmaceutically acceptable salts of 2-{4-[(3)-piperidin-3-yl]phenyl}-2-indazole-7-carboxamide
    Patent number: 8436185
    Abstract: The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways and as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy. Further, the compounds of the present invention are useful for reducing cell necrosis (in stroke and myocardial infarction), down regulating inflammation and tissue injury, treating retroviral infections and protecting against the toxicity of chemotherapy.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jennifer R. Foley, Robert Darrin Wilson
  • Thiazolyl piperidine derivatives
    Patent number: 8436186
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: May 7, 2013
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Frank Stieber, Timo Heinrich, Dirk Wienke
  • Kinase inhibitor with improved solubility profile
    Patent number: 8436179
    Abstract: 4-Amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide which inhibits protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved aqueous solubility profile, compositions containing 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide and methods of treating diseases using 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide are disclosed.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: May 7, 2013
    Assignee: AbbVie Inc.
    Inventors: Michael R. Michaelides, Michael L. Curtin, James H. Holms, Douglas H. Steinman
  • Processes for the preparation of piperidinic derivatives and pharmaceutic compositions containing the same
    Patent number: 8436020
    Abstract: Production processes for preparing pharmaceutical compositions containing new molecules capable of inhibiting acetylcholinesterase, thus being useful in the treatment of pathologies associated to cholinergic transmission, such as memory related disorders, neurodegenerative disorders such as Alzheimer's Disease, Miastenia Gravis or in the treatment of intoxications induced by chemical agents of central action.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: May 7, 2013
    Assignees: Universidade Federal do Rio de Janeiro UBRJ, Universidade Estadual Paulists UNESP
    Inventors: Claudio Viegas, Jr., Vanderlan da Silva Bolzani, Eliezer Jesus de Lacerda Barreiro, Newton G. Castro, Maria Claudia Marx Young, Monica Santos Rocha
  • Pyrrolopyridine compounds and their use in treating disease
    Patent number: 8431703
    Abstract: There are provided according to the invention compounds of formula (I) in free ors salt form, wherein R1, R2, R4, R5, R6, A, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: April 30, 2013
    Assignee: Novartis AG
    Inventors: David Andrew Sandham, Catherine Leblanc, Lyndon Nigel Brown
  • Process for preparation of HIV protease inhibitors
    Patent number: 8431745
    Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: April 30, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard P. Polniaszek, Richard Hung Chiu Yu
  • 2-aminopyridine derivatives as glucokinase activators
    Patent number: 8431713
    Abstract: Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: April 30, 2013
    Assignee: Array BioPharma, Inc.
    Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
  • Process for the preparation of ibodutant (MEN15596) and related intermediates
    Patent number: 8431684
    Abstract: This invention relates to a novel process for synthesizing the product ibodutant shown in the figure below, consisting of a small number of high-yield steps involving reagents and solvents with low environmental impact, characterized by the coupling of two portions, compounds (3) and (4), one of which (3) is synthesized by coupling of 6-methyl-2-benzo[b]thiophenecarboxylic acid (1) with 1-amino-alpha-alpha-cyclopentan carboxylic acid and subsequent cyclization with oxazolone, while the other, compound (4), is obtained from suitable highly selective functionalizations of 4-aminomethylpiperidine (2).
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: April 30, 2013
    Assignee: Malesci Istituto Farmacobiologico S.p.A.
    Inventors: Fabrizio Bonaccorsi, Valentina Fedi, Danilo Giannotti
  • 1,2,3,4-tetrahydroqinoline derivative useful for the treatment of diabetes
    Patent number: 8431706
    Abstract: The present invention provides a compound of the formula below or a pharmaceutical salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: April 30, 2013
    Assignee: Eli Lilly and Company
    Inventor: Chafiq Hamdouchi