Patents Examined by Joseph K. McKane
  • Organic compounds
    Patent number: 8343966
    Abstract: Compounds of formula I in free or salt or solvate form, where T1, T2, X, Ra, Rb, R8 and R9 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: January 2, 2009
    Date of Patent: January 1, 2013
    Assignee: Novartis AG
    Inventors: Claire Adcock, Urs Baettig, Peter Hunt, Catherine Leblanc, Maude Nadine Pierrette Pipet, Robert Alexander Pulz, Katrin Spiegel, Nikolaus Johannes Stiefl
  • Method for producing fluorine-containing acylacetic acid derivative, method for producing fluorine-containing pyrazolecarboxylic acid ester derivative, and method for producing fluorine-containing pyrazolecarboxylic acid derivative
    Patent number: 8344156
    Abstract: A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl group or an acyl group, or together represent an atomic group that forms a 5- or 6-membered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl group; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: January 1, 2013
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
  • Carvedilol phosphate sesquihydrate
    Patent number: 8344159
    Abstract: The present invention relates a novel crystalline 1-(Carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol phosphate sesquihydrate (Carvedilol dihydrogenphosphate sesquihydrate), methods of preparing the sesquihydrate by adding phosphoric acid to a suspension of Carvedilol in water, water miscible solvents or a mixture of water and water miscible organic solvent followed by isolating the product directly or by adding solvent.
    Type: Grant
    Filed: June 11, 2007
    Date of Patent: January 1, 2013
    Assignee: Mylan Laboratories Limited
    Inventors: Seeta Ramanjaneyulu Gorantla, Mohan Bandari, Nageshwara Rao Karusala, Sankara Sastry Tummalapalli Uma
  • Derivatives of psammaplin A, a method for their synthesis and their uses for the prevention or treatment of cancer
    Patent number: 8338473
    Abstract: Derivatives of psammaplin A responding to formula (I), a method for their synthesis and their use for the preparation of a medicament for preventing and for treating a tumor or a cancer. Formula (I).
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: December 25, 2012
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg, Institut National de la Sante et de la Recherche Medicale (Inserm), Universidade de Vito, Seconda Universita Degli Studi di Napoli, Radboud University Nijmegen
    Inventors: Hinrich Gronemeyer, Lucia Altucci, Angel De Lera, Hendrik Gerard Stunnenberg
  • Crystal form of cabergoline
    Patent number: 8338445
    Abstract: The present invention relates to a cabergoline crystal form L, its preparation from halogenated aromatic solvents and aliphatic hydrocarbons and to pharmaceutical compositions containing the new form.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: December 25, 2012
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Zoran Ham, Andrej Premrl
  • Tetracyclic compounds
    Patent number: 8338408
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: December 25, 2012
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew A. Protter, Rajendra P. Jain, Sundeep Dugar, Sarvajit Chakravarty, Sergey O. Bachurin, Anatoly K. Ustinov, Bogdan K. Beznosko, Nadezhda Sergeevna Beznosko, legal representative, Elena F. Shevtsova, Vladimir V. Grigoriev
  • Aqueous synthesis of perylene pigments
    Patent number: 8334386
    Abstract: A process for preparing perylene pigments of the general formula (Ia) or (Ib) or mixtures thereof, by reacting perylenetetracarboxylic acids or functional derivatives thereof with aromatic diamines, where R1, R2 may be the same or different and may each independently be phenylene, naphthylene or pyridylene, where R1, R2 may each be mono- or polysubstituted by C1-C22-alkyl, C3-C22-alkenyl, C1-C22-alkoxy, hydroxyl and/or halogen, X1, X2, X3, X4, X5, X6, X7, X8 may be the same or different and may each independently be hydrogen or halogen, wherein the reaction is performed in the presence of a secondary or tertiary amine in an aqueous reaction medium.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: December 18, 2012
    Assignee: BASF SE
    Inventors: Johannes Loebel, Andreas Stohr
  • Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
    Patent number: 8334282
    Abstract: The present invention provides novel substituted amino-azetidines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: December 18, 2012
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Targeted delivery using tissue-specific peptidomimetic ligands
    Patent number: 8333988
    Abstract: Compositions and methods for tissue-specific targeted delivery of therapeutic agents through the use of tissue-specific peptidomimetic ligands are disclosed herein. The ligand comprises a composition of formula A-scaffold-A? and one or more hydrophobic anchors covalently linked to the scaffold. The A and A? compounds linked to the scaffold comprise monovalent peptidomimetic compounds wherein each monovalent peptidomimetic compound is selected from the group consisting of fragments IKs, GKs, IDs, GSs, GTs, VSs, TKs, KTs, ARs, KIs, KEs, AEs, GRs, YSs, IRs, and morpholino.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: December 18, 2012
    Assignee: GRADALIS, Inc.
    Inventor: Nancy Smyth Templeton
  • Metathesis catalyst and process for use thereof
    Patent number: 8329921
    Abstract: This invention relates to a catalyst compound comprising a combination of a cyclic alkyl amino carbene ligand and a benzylidene both attached to a Group 8 metal, preferably ruthenium atom. This invention also relates to a process to make linear alpha-olefins comprising contacting a feed material and an optional alkene (such as ethylene) with the catalyst described above, wherein the feed material is a triacylglyceride, fatty acid, fatty acid alkyl ester, and/or fatty acid ester, typically derived from seed oil (e.g., biodiesel).
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: December 11, 2012
    Assignee: Exxonmobil Chemical Patents Inc.
    Inventors: John R. Hagadorn, Matthew W. Holtcamp, Matthew S. Bedoya
  • Amide compounds and use of the same
    Patent number: 8329691
    Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
    Type: Grant
    Filed: October 14, 2008
    Date of Patent: December 11, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Tawada
  • 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of CCR2
    Patent number: 8324186
    Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: December 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Zhihua Sui
  • Dehydrogenation process
    Patent number: 8324388
    Abstract: Processes comprising: providing a dehydrogenatable compound; and subjecting the dehydrogenatable compound to a dehydrogenation reaction at a temperature of from 150 to 400° C., in the presence of oxygen, and at a temperature profile of the dehydrogenation reaction which does not differ substantially from the temperature profile of the dehydrogenation reaction in the absence of oxygen under otherwise identical conditions.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: December 4, 2012
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Kotrel, Martin Ernst
  • Modulators of ATP-binding cassette transporters
    Patent number: 8324207
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: December 4, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Fredrick van Goor
  • 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors
    Patent number: 8318735
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Lianyun Zhao, Shuyi Tang, Tzu T. Wong, Praveen K. Tadikonda, Luis E. Torres, M. Arshad Siddiqui, Michael P. Dwyer, Kartik M. Keertikar, Timothy J. Guzi
  • 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1 and CX3CR1
    Patent number: 8314099
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: November 20, 2012
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
  • Process for preparing oxazoline-protected aminodiol compounds useful as intermediates to florfenicol
    Patent number: 8314252
    Abstract: Processes for preparing oxazoline compounds are disclosed. These oxazoline compounds are useful intermediates in the preparation of Florfenicol and related compounds.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: November 20, 2012
    Assignees: Intervet Inc., Intervet International B.V.
    Inventors: Leo A. Paquette, James C. Towson
  • Total synthesis of salinosporamide A and analogs thereof
    Patent number: 8314251
    Abstract: The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: November 20, 2012
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Taotao Ling, Samuel Danishefsky
  • 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
    Patent number: 8309593
    Abstract: A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: November 13, 2012
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Thomas H. Jozafiak, Frederic Vinick, Yibin Xiang, John Kane, Junkai Liao
  • Method of forming oseltamivir and derivatives thereof
    Patent number: 8304553
    Abstract: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: November 6, 2012
    Assignee: Nanyang Technological University
    Inventors: Xuewei Liu, Jimei Ma