Patents Examined by Jeffrey Murray
  • Substituted propenyl piperazine derivatives as novel inhibitors of histone deacetylase
    Patent number: 8426416
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: April 23, 2013
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Sven Franciscus Anna Van Brandt, Kristof Van Emelen, Patrick Rene Angibaud, Laurence Francoise Bernadette Marconnet-Decrane, Janine Arts
  • Quinazoline derivatives
    Patent number: 8426430
    Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: April 23, 2013
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
  • Processes for preparing JAK inhibitors and related intermediate compounds
    Patent number: 8410265
    Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: April 2, 2013
    Assignee: Incyte Corporation
    Inventors: Jiacheng Zhou, Pingli Liu, Qiyan Lin, Brian W. Metcalf, David Meloni, Yongchun Pan, Michael Xia, Mei Li, Tai-Yuen Yue, James D. Rodgers, Haisheng Wang
  • Imidazopyrimidine derivatives
    Patent number: 8410117
    Abstract: The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: April 2, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ruben Alvarez Sanchez, Konrad Bleicher, Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinzen, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Aurora kinase modulators and method of use
    Patent number: 8404694
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: March 26, 2013
    Assignee: Amgen Inc.
    Inventors: Ryan White, Jason Brooks Human
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8399470
    Abstract: Disclosed herein are pyrazolo[3,4-d]pyrimidines that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 19, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Quinazoline inhibitors of BACE 1 and methods of using
    Patent number: 8394807
    Abstract: There is provided a dihydroquinazoline compound of the formula or a pharmaceutically acceptable salt thereof, wherein the values of the radicals are defined herein, as well as a pharmaceutical composition containing the compound, and a method of using the compound for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: March 12, 2013
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
    Patent number: 8389533
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are gem-disubstituted or spirocyclic pyridine, pyrimidine and triazine derivatives.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 5, 2013
    Assignee: Amgen Inc.
    Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang
  • Chemical compounds
    Patent number: 8383635
    Abstract: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: August 12, 2009
    Date of Patent: February 26, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis Louis Atkinson, Jeffrey Michael Axten, Maria Cichy-Knight, Michael Lee Moore, Vipulkumar Kantibhai Patel, Xinrong Tian, Christopher Roland Wellaway, Allison K. Dunn
  • Pyrazolo pyrimidines as casein kinase II (CK2) modulators
    Patent number: 8372851
    Abstract: A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
    Type: Grant
    Filed: October 23, 2006
    Date of Patent: February 12, 2013
    Assignee: Exelixis, Inc.
    Inventors: Kenneth D. Rice, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Angie Inyoung Kim, Jean-Claire Limun Manalo, Csaba J. Peto
  • Pyrrolo[2,3-D]pyrimidine compounds
    Patent number: 8372854
    Abstract: Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: February 12, 2013
    Assignee: Pfizer Inc.
    Inventors: Jin Xie, Michele Ann Promo, Eric Jon Jacobsen, Horng-Chih Huang, Todd M. Maddux
  • Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases
    Patent number: 8372835
    Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said 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: July 30, 2010
    Date of Patent: February 12, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Daniel Robinson, Damien Fraysse, Andrew Miller
  • Pest control agents
    Patent number: 8367707
    Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: February 5, 2013
    Assignees: Meiji Seika Pharma Co., Ltd., The Kitasato Institute
    Inventors: Kimihiko Goto, Ryo Horikoshi, Mariko Tsuchida, Kazuhiko Oyama, Satoshi Omura, Hiroshi Tomoda, Toshiaki Sunazuka
  • Pyrazolopyrimidines and related heterocycles as kinase inhibitors
    Patent number: 8367681
    Abstract: The invention provides compounds of general formula (I) that inhibit selected kinases (Pim and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: February 5, 2013
    Assignee: Cylene Pharmaceuticals, Inc.
    Inventors: Mustapha Haddach, Joe Tran
  • 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
    Patent number: 8367826
    Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: February 5, 2013
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Radoslaw Laufer, An-Hu Li, Mark J. Mulvihill, Arno G. Steinig
  • Substituted amide beta secretase inhibitors
    Patent number: 8367712
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: February 5, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • 4-phenylpiperidine derivatives as renin inhibitors
    Patent number: 8362040
    Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: January 29, 2013
    Assignee: Novartis AG
    Inventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
  • Pyrrolo [2,3-D] pyrimidines as non-nucleoside reverse transcriptase inhibitors for treatment of HIV
    Patent number: 8354532
    Abstract: This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: January 15, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-hyo Koh, Stephanie Shaw, Hong Woo Kim, Zhi Hong
  • Pyrimidine derivatives
    Patent number: 8349859
    Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: January 8, 2013
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Wei-Guo Su, Hong Jia, Weihan Zhang, Yumin Cui, Xiaoqiang Yan, Yongxin Ren, Jifeng Duan, Yang Sai
  • Pyrazolo [3,4-D] pyrimidine derivatives as anti-cancer agents
    Patent number: 8349847
    Abstract: The invention relates to substituted pyrazolo[3,4-d]pyrimidine derivatives of the Formula-(I), or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo[3,4-d]pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man.
    Type: Grant
    Filed: January 12, 2009
    Date of Patent: January 8, 2013
    Inventors: Durga Prasad Konakanchi, Subba Rao Pula, Lakshmi Ananthaneni, Ramakrishna Pilli, Muddasani Pulla Reddy, Bhujanga rao Adibhatla Satya, Nannapaneni Venkaiah Chowdary