Patents Examined by Cecilia M. Jaisle
  • Patent number: 8927540
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4?, have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: January 6, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Patent number: 8921372
    Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: December 30, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Robert Murray McKinnell, Daniel D. Long, Lori Jean Van Orden, Lan Jiang, Mandy Loo, Daisuke Roland Saito, Sheila Zipfel, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa, Xiaojun Huang, Weijiang Zhang
  • Patent number: 8916566
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: December 23, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
  • Patent number: 8912183
    Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: December 16, 2014
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
  • Patent number: 8895739
    Abstract: Functionalized bis-peptides as well as other amide-containing compounds are obtained by acylation of hindered amines. The functionalized bis-peptides are useful as shape-programmable nanostructures that are immune to denaturation and that contain arrays of functional groups having designed catalytic, protein-binding and/or sensor capabilities.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: November 25, 2014
    Assignees: Temple University of the Commonwealth System of Higher Education, University of Pittsburgh of the Commonwealth System of Higher Education
    Inventors: Christian E. Schafmeister, Zachary Z. Brown
  • Patent number: 8877756
    Abstract: The invention relates to new pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system and cancers. This invention also relates to pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: January 19, 2010
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Horst Dollinger, Domnic Martyres, Juergen Mack, Rolf Goeggel, Birgit Jung, Peter Nickolaus
  • Patent number: 8871764
    Abstract: Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: October 28, 2014
    Assignee: University of Virginia Patent Foundation
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Patent number: 8859545
    Abstract: Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, respiratory conditions, and others.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: October 14, 2014
    Assignee: Evotec AG
    Inventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
  • Patent number: 8853206
    Abstract: The invention relates to novel compounds of formula I where X, A?, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: October 7, 2014
    Assignee: Sanofi
    Inventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen
  • Patent number: 8853214
    Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents have the meanings as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: October 7, 2014
    Assignee: BASF SE
    Inventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
  • Patent number: 8853211
    Abstract: Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: October 7, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Patent number: 8841305
    Abstract: Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: September 23, 2014
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
  • Patent number: 8802703
    Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: August 12, 2014
    Assignee: Merck Serono S.A.
    Inventors: Andreas Goutopoulos, Benny C. Askew, Jr., Nhut Kiet Diep, Srinivasa R. Karra, Matthias Schwarz, Henry Yu
  • Patent number: 8791120
    Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: July 29, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
  • Patent number: 8785445
    Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: July 22, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
  • Patent number: 8759362
    Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: June 24, 2014
    Assignee: Purdue Pharma L.P.
    Inventor: Laykea Tafesse
  • Patent number: 8735581
    Abstract: Provided is a novel organometallic complex which can be synthesized easily and emits phosphorescence, or a compound which emits red phosphorescence. The inventors focused on easy synthesis of an m-aminophenyl pyrazine derivative represented by the following general formula (G0), synthesized an organometallic complex having a structure in which the derivative is coordinated to a Group 9 or Group 10 metal ion, and further synthesized a useful substance which emits red phosphorescence.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: May 27, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Tomoka Nakagawa, Satoshi Seo
  • Patent number: 8729105
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: May 20, 2014
    Assignee: Hoffmann La-Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Patent number: 8729089
    Abstract: Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I): wherein: R4 is hydrogen, and R1, R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: May 20, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Chien-hung Chou, William John Watkins, Lee S. Chong, Jennifer R. Zhang, Ruchika Mishra
  • Patent number: 8729083
    Abstract: The present invention relates to pyrazole compounds of formulae I or II and the salts and N-oxides thereof, wherein A is a pyrazole radical of formulae A1, A2 or A3, wherein # denotes the binding site; R41, R42, R43, R51 are H, halogen, CN, NO2, C1-C10-alkyl and the like; R52, R53 are H, halogen, CN, NO2, C1-C10-alkyl, and the like; R61, R62, R63 are H, CN, NO2, C1-C10-alkyl, and the like; T is C(Rt) or N; U is C(Ru) or N; V is C(Rv) or N; W is C(Rw) or N; with the proviso that at least one of the groups T, U, V and W is N; Rt, Ru, Rv, Rw are H, halogen, C1-C4-alkyl and the like; X1 is S, O or NR1a, wherein R1a is selected H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alk
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: May 20, 2014
    Assignee: BASF SE
    Inventors: Steffen Groβ, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Prashant Deshmukh, Joachim Dickhaut, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Douglas D. Anspaugh, Deborah L. Culbertson, Faraneh Oloumi