Patents Examined by Jason M. Nolan
  • Dendrimer conjugates
    Patent number: 8252834
    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: August 28, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: James R. Baker, Jr., Xue-min Cheng, Thommey P. Thomas, Baohua Mark Huang
  • Urea derivatives methods for their manufacture and uses thereof
    Patent number: 8247412
    Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: August 21, 2012
    Assignee: Galapagos Sasu
    Inventors: Pierre Deprez, Hélène Jary, Taoues Temal
  • Process for production of aralkyloxypyrrolidine derivative
    Patent number: 8247578
    Abstract: The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: August 21, 2012
    Assignee: Kaneka Corporation
    Inventors: Toshihiro Takeda, Masatoshi Ohnuki
  • Organic sulfur compound and its use for controlling harmful arthropod
    Patent number: 8247612
    Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods represented by the formula (I): wherein, R1 represents a C1-C5 haloalkyl group having at least one fluorine atom, R2 represents a C1-C4 alkyl group optionally substituted with at least one halogen atom or the like, R3 represents a hydrogen atom or the like, R4 represents a cyano group or the like, R5 represents a hydrogen atom or the like, m represents an integer of 1 to 4, and n represents 0, 1 or 2.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: August 21, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hiroyuki Miyazaki
  • Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
    Patent number: 8242270
    Abstract: The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: August 14, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jean Lajeunesse, John D. DiMarco, Michael Galella, Ramakrishnan Chidambaram
  • Mitotic kinesin inhibitors and methods of use thereof
    Patent number: 8236825
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: August 7, 2012
    Assignee: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R Laird, John Robinson, Shelley Allen
  • Thiazoles and oxazoles useful as modulators of ATP-binding cassette transporters
    Patent number: 8232302
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: July 31, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Thomas Miller, Sara S. Hadida Ruah, Peter Diederik Jan Grootenhuis, Matthew Hamilton
  • Lactam-substituted dicarboxylic acids and use thereof
    Patent number: 8217063
    Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 15, 2008
    Date of Patent: July 10, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
  • Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
    Patent number: 8217048
    Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: July 10, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert B. Perni, John J. Court, Shawn D. Britt, Janos Pitlik, John H. van Drie
  • Hepatitis C virus inhibitors
    Patent number: 8211928
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: July 3, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rico Lavoie, Clint A. James, Edward H. Ruediger
  • Heterocyclic derivatives for modulation of calcium channels
    Patent number: 8211935
    Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 3, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Andreas P. Termin, Esther Ann Martinborough, Nicole Hilgraf, Charles J. Cohen, Corey Anderson
  • Nitric oxide releasing derivatives of paracetamol
    Patent number: 8207222
    Abstract: The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the corresponding nitrate ester derivatives. The nitrate esters of paracetamol are useful as analgesic, anti-inflammatory agents.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: June 26, 2012
    Assignee: Council of Scientific and Industrial Research
    Inventors: Tilak Raj Bhardwaj, Manoj Kumar, Necraj Mehta, Neelima Dhingra
  • Benzofuran-3-yl(indol-3-yl) maleimides as potent GSK3 inhibitors
    Patent number: 8207216
    Abstract: Compounds of formula: and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: June 26, 2012
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Alan P. Kozikowski, Irina Gaysina
  • Sub-type selective azabicycloalkane derivatives
    Patent number: 8198296
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, such as those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: June 12, 2012
    Assignee: Targacept, Inc.
    Inventors: Philip S. Hammond, Anatoly Mazurov, Yun-De Xiao, Srinivasa V. Murthy, Srinivisa Rao Akireddy
  • Thiophene-carboxamides useful as inhibitors of protein kinases
    Patent number: 8188134
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: May 29, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Brenchley, Steven Durrant, Jean-Damien Charrier, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
  • Stereoselective reduction of a morphinone
    Patent number: 8183376
    Abstract: A synthetic method is provided, wherein the method comprises stereoselectively reducing a ketone of a morphinone to form a reduced morphinone and optionally covalently attaching a water soluble polymer to the reduced morphinone.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: May 22, 2012
    Assignee: Nektar Therapeutics
    Inventors: Lin Cheng, Michael D. Bentley
  • Tetra-substituted NDGA derivatives via ether bonds and carbamate bonds and their synthesis and pharmaceutical use
    Patent number: 8178527
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: May 15, 2012
    Assignee: Erimos Pharmaceuticals LLC
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • Compounds having CRTH2 antagonist activity
    Patent number: 8168673
    Abstract: Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: May 1, 2012
    Assignee: Oxagen Limited
    Inventors: Richard Edward Armer, Carole Eliane Andree Maillol, Colin Richard Dorgan, Graham Michael Wynne, Julia Vile
  • Imidazolium-type ionic oligomers
    Patent number: 8168801
    Abstract: The present disclosure relates to structurally defined imidazolium-type ionic oligomers of the formula: wherein n is an integer ranging from 1 to 20; A is N or m is an integer ranging from 1 to 5; X is selected from the group consisting of Br, OTf, CF3CO2, CH3CO2, BF4, PF6, NTf2, F, Cl and I; and R is selected from the group consisting of hydrogen and C1-10 alkyl. The imidazolium-type ionic oligomers lend themselves as soluble/solid supports for biopolymer synthesis.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: May 1, 2012
    Assignees: The Royal Institution for the Advancement of Learning/McGill University, The Hong Kong Polytechnic University
    Inventors: Tak-Hang Chan, Xun He
  • 3-(4-fluorophenyl)-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic activity
    Patent number: 8168631
    Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: February 3, 2009
    Date of Patent: May 1, 2012
    Assignee: Allergan, Inc.
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac