Patents Examined by Cecilia M. Jaisle
  • Compositions and methods for modulating c-kit and PDGFR receptors
    Patent number: 8106068
    Abstract: The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: January 31, 2012
    Assignee: IRM LLC
    Inventors: Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka
  • Linear dicationic terphenyls and their aza analogues as antiparasitic agents
    Patent number: 8101636
    Abstract: Novel aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. Also described are processes for synthesizing the compounds.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: January 24, 2012
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: Richard R. Tidwell, David W. Boykin, W. David Wilson, Reto Brun, Karl Werbovetz, Mohamed A. Ismail, Reem K. Arafa
  • Phthalazine compounds and methods of use
    Patent number: 8101612
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of p38 kinase mediated diseases and related inflammatory conditions. The compounds have a general Formula II wherein L1, L2, R1a, R1b, R1c, R2, R3, R3a, R4, R5 and p are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Grant
    Filed: September 4, 2007
    Date of Patent: January 24, 2012
    Assignee: Amgen Inc.
    Inventors: Andrew Tasker, Dawei Zhang, Liping H. Pettus, Rob M. Rzasa, Kelvin K. C. Sham, Shimin Xu, Partha Chakrabarti
  • Pyridopyrimidinone inhibitors of PI3K? and mTOR
    Patent number: 8101622
    Abstract: The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of making and using the compounds.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: January 24, 2012
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Sunghoon Ma, Chris A. Buhr, John M. Nuss
  • Diazaquinolones that inhibit prolyl hydroxylase activity
    Patent number: 8097620
    Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: January 17, 2012
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Kaustav Biswas, Roland Burli, Jennifer E. Golden, Stephanie Mercede, Christopher M. Tegley
  • HIV inhibiting pyrimidines derivatives
    Patent number: 8080551
    Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: December 20, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
  • Pyridazinyl amine derivatives, the use thereof in the preparation of picorna virus inhibitors
    Patent number: 8076339
    Abstract: The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: December 13, 2011
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China of Beijing
    Inventors: Song Li, Chunlai Mi, Zhibing Zheng, Guoming Zhao, Xinbo Zhou, Zehui Gong
  • Substituted pyridazine derivatives
    Patent number: 8076331
    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: July 29, 2010
    Date of Patent: December 13, 2011
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
  • 2-cyanophenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine compounds, compositions and uses thereof
    Patent number: 8076345
    Abstract: Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided 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, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: December 13, 2011
    Assignee: Evotec AG
    Inventors: Zhi-Liang Wei, Donogh John Roger O'Mahony, Matthew Duncton, John Kincaid, Michael G. Kelly, Zhan Wang
  • Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
    Patent number: 8076336
    Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 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: August 5, 2010
    Date of Patent: December 13, 2011
    Assignee: Sanofi-Aventis
    Inventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen, Bodo Scheiper
  • Acetylenyl-pyrazolo-pyrimidine derivatives
    Patent number: 8063048
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Wylie Solang Palmer, Juergen Wichmann, Thomas Johannes Woltering
  • Pyridazine compounds and methods
    Patent number: 8063047
    Abstract: The invention relates to novel chemical compounds of Formula I compositions and methods of using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: November 22, 2011
    Assignees: Centre National de la Recherche Scientifique (CNRS), Northwestern University, Universite de Strasbourg
    Inventors: Martin Watterson, Linda Van El Dik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Veleniza, Wenhui Hu, Magdaena Zasadzki
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 8063064
    Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
  • Heterocyclic antiviral compounds
    Patent number: 8063028
    Abstract: Compounds of formula I, wherein R1, R2, R3, X1, X2 and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Roland Joseph Billedeau, Zachary Kevin Sweeney
  • Pyridine methylene azolidinones and use thereof phosphoinositide inhibitors
    Patent number: 8058289
    Abstract: The present invention is related to pyridine methylene azolidinone derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: November 15, 2011
    Assignee: Merck Serono SA
    Inventors: Thomas Rueckle, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
  • 7H-pyrido[3,4-D]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors
    Patent number: 8058283
    Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: November 15, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Honold, Jane Paul, Carl Roeschlaub, Wolfgang Schaefer, Stefan Scheiblich, Thomas Von Hirschheydt, Alan Whittle
  • Kinase inhibitors and their uses
    Patent number: 8053434
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: November 8, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
    Patent number: 8044062
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Grant
    Filed: October 9, 2006
    Date of Patent: October 25, 2011
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K. S. Yeung
  • Synthesis and purification of pteroic acid and conjugates thereof
    Patent number: 8044200
    Abstract: Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: October 25, 2011
    Assignee: Endocyte, Inc.
    Inventors: Le-Cun Xu, Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Hari Krishna Santhapuram, Chunhong Li
  • Biaryl ether urea compounds
    Patent number: 8044052
    Abstract: The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: October 25, 2011
    Assignee: Pfizer Inc.
    Inventors: Lorraine Kathleen Fay, Douglas S. Johnson, Suzanne Ross Kesten, Scott E. Lazerwith, Mark Anthony Morris, Cory Michael Stiff, Marvin Jay Meyers, Lijuan Jane Wang