Patents Examined by Jason M. Nolan
  • Inhibitors of ion channels
    Patent number: 8063080
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: November 22, 2011
    Assignee: Icagen, Inc.
    Inventors: Alan Fulp, Brian Marron, Mark J. Suto, Xiaodong Wang
  • 3-aminopyrrolidone derivatives
    Patent number: 8063039
    Abstract: A method for treating pain, migraine, inflammation, gastrointestinal tract disorders, disorders of the genito-urinary tract, ophthalmic diseases or obesity in a subject, the method including administering to the subject an effective amount of a compound of a general formula, specific examples of which include 3-(4-Butyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(4-trifluorobutyloxy)-benzylamino]-pyrrolidin-2-one, 3-(4-Pentyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(5-trifluoropentyloxy)-benzylamino]-pyrrolidin-2-one, and 3-(4-Phenylethyl-benzylamino)-pyrrolidin-2-one.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: November 22, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Sara Maestroni, Luca Francesco Raveglia, Patricia Salvati
  • 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1 ,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
    Patent number: 8062665
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: November 22, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis X Muller, Shivakumar G Kapsi
  • Pharmaceutical salts of N-[2-(diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-napthyl)ethoxy]propanamide
    Patent number: 8058294
    Abstract: A pharmaceutically acceptable salt of N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propanamide provided it is not the dihydrobromide or dihydrochloride salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: November 15, 2011
    Assignee: AstraZeneca AB
    Inventors: Robert Whittock, Jane Withnall
  • 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene] hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
    Patent number: 8052994
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: November 8, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis X. Muller, Shivakumar G. Kapsi
  • 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
    Patent number: 8052993
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl) -1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: November 8, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis X Muller, Shivakumar G Kapsi
  • 3-imidazolyl-indoles for the treatment of proliferative diseases
    Patent number: 8053457
    Abstract: The invention relates to 3-heterocyclyl indolyl compounds of formula I capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively: wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: November 8, 2011
    Assignee: Novartis AG
    Inventors: Andreas Boettcher, Nicole Buschmann, Pascal Furet, Jean-Marc Groell, Jorg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Lorenz Mayr, Andrea Vaupel
  • 3'-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene] hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
    Patent number: 8052995
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: November 8, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis X Muller, Shivakumar G Kapsi
  • Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them
    Patent number: 8048893
    Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: November 1, 2011
    Assignee: Aventis Pharma SA
    Inventors: Arielle Genevois-Borella, Jean-Luc Malleron, Jean Bouquerel, Gilles Doerflinger, Andrees Bohme, Gaetan Touyer, Jean-Francois Sabuco, Corrine Terrier, Serge Mignani, Michel Evers, Youssef El-Ahmad
  • Fused pyrrolocarbazoles
    Patent number: 8044064
    Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: October 25, 2011
    Assignee: Cephalon, Inc.
    Inventors: Nadine C. Becknell, Bruce A. Ruggeri, Peter D. Brown, Robert L. Hudkins, Allison L. Zulli
  • Synephrine derivatives useful as anti-inflammatory agents
    Patent number: 8039501
    Abstract: This invention provides compounds having the structural formula: wherein: R1 is an acyl or sulfonyl group, R2 is an acyl group selected from the group consisting of acyl groups derived from cycloaliphatic, aromatic or heterocyclic monocarboxylic acids, imidazolylcarbonyl and triazolylcarbonyl, and R3 is hydrogen or an amino-protecting group, a stereoisomer thereof, a solvate thereof, or a salt thereof, being useful as anti-inflammatory agents and anti-cancer agents.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: October 18, 2011
    Assignee: Universiteit Gent
    Inventors: Wim Vanden Berghe, Karolien De Bosscher, Serge Van Calenbergh, Guy Haegeman, Carl Jeffrey Lacey
  • Process for (3R, 5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt
    Patent number: 8026377
    Abstract: The present invention relates to processes for the manufacture of (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: September 27, 2011
    Assignee: Ranbaxy Laboratories, Limited
    Inventors: Vijay Kaul, Gyan Chand Yadav
  • Modulators of LXR
    Patent number: 8013001
    Abstract: Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: September 6, 2011
    Assignee: Exelixis, Inc.
    Inventors: Christopher D. Bayne, Alan T. Johnson, Shao Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Jr., Haixia Wang, Yinong Xie
  • Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    Patent number: 8003809
    Abstract: Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: August 23, 2011
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Xuedong Dai, Randall A. Scheuerman, Stephen P. Raillard, Suresh K. Manthati, Fenmei Yao, Thu Phan, Maria J. Ludwikow, Ge Peng, Seema Bhat
  • Process for the production of atorvastatin calcium in amorphous form
    Patent number: 7994343
    Abstract: A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided.
    Type: Grant
    Filed: November 19, 2004
    Date of Patent: August 9, 2011
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Yatendra Kumar, Saridi Madhava Dileep Kumar, Swargam Sathyanarayana
  • Process for the purification of thiophenes
    Patent number: 7994345
    Abstract: The invention relates to a process for the purification of thiophenes by means of precipitation. The purified thiophenes are liquid at room temperature, have a purity of at least 99.50 wt. %, and are represented by the following general formula (I), wherein R1 and R2 independently of each other are, for example, a linear or branched C1-C20-alkyl group, or together form a fused C1-C20-dioxyalylene ring. The process involves: (I) precipitating the thiophene by cooling a solution of the thiophene and at least one solvent; or (II) precipitating the thiophene by adding the thiophene to a cooled solution of solvent and optionally the thiophene. The solutions are cooled to a temperature below the melting point of the thiophene.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: August 9, 2011
    Assignee: H. C. Starck GmbH
    Inventors: Lutz Brassat, Stephan Kirchmeyer
  • Binding inhibitor of sphingosine-1-phosphate
    Patent number: 7994204
    Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].
    Type: Grant
    Filed: February 6, 2007
    Date of Patent: August 9, 2011
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
  • Process for continuously preparing N-ethyl-2-pyrrolidone (NEP)
    Patent number: 7994350
    Abstract: Process for the continuous preparation of N-ethyl-2-pyrrolidone (NEP) by reacting gamma-butyrolactone (GBL) with monoethylamine (MEA) in the liquid phase, wherein GBL and MEA are used in a molar ratio in the range from 1:1.08 to 1:2 an the reaction is carried out at a temperature in the range from 320 to 420° C. and an absolute pressure in the range from 70 to 120 bar.
    Type: Grant
    Filed: May 10, 2007
    Date of Patent: August 9, 2011
    Assignee: BASF SE
    Inventors: Helmut Schmidtke, Ralph Versch, Silke Simon, Karl Ott, Ronald Drews, Stephanie Mollner
  • Indane derivatives as modulators of ion channels
    Patent number: 7989481
    Abstract: The present invention relates to indane derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: August 2, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Timothy Neubert, Aarti S. Kawatkar, Esther Martinborough, Andreas Termin
  • Phosphorus derivatives as histone deacetylase inhibitors
    Patent number: 7981874
    Abstract: The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: July 16, 2007
    Date of Patent: July 19, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Jonathan Grimm, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Paul J. Tempest, Kevin J. Wilson, David J. Witter