Patents Examined by Jeffrey Murray
  • Processes for the preparation of paliperidone
    Patent number: 8481729
    Abstract: The present invention relates to a novel process for the preparation of paliperidone and its intermediates and also relates to an improved process for the preparation of paliperidone compound of formula (I).
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: July 9, 2013
    Assignee: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Revu Satyanarayana
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 8476284
    Abstract: Disclosed herein are compounds, including compounds having the Formula (A) where A, R1, R2, R3, and R4 are as defined in the specification, 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: December 16, 2011
    Date of Patent: July 2, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • [6,5]—bicyclic GPR119 G protein-coupled receptor agonists
    Patent number: 8476283
    Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: July 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John M. Fevig, Dean A. Wacker
  • Folate mimetics and folate-receptor binding conjugates thereof
    Patent number: 8470822
    Abstract: This present disclosure relates to folate mimetics and their use in therapeutic and diagnostic applications. More particularly, the disclosure relates to using des-glutamyl folic acid analogs recognized by and selectively bound by folate receptors and other folate binding proteins and the use of such analogs for targeted delivery of diagnostic or therapeutic agents to folate-receptor bearing cell populations.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: June 25, 2013
    Assignees: Purdue Research Foundation, Endocyte, Inc.
    Inventors: Mark A Green, Chun-Yen Ke, Christopher P Leamon
  • 4-substituted derivatives of pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine and uses thereof
    Patent number: 8466164
    Abstract: The present invention relates to a compound 4-substituted derivative of pyrazolo[3,4-d]pyrimidine or of pyrrolo[2,3-d]pyrimidine having the formula (I) and uses thereof, in particular for the treatment of bone related diseases and tumors.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: June 18, 2013
    Assignee: Universita degli Studi di Siena
    Inventors: Silvia Schenone, Francesco Bondavalli, Olga Bruno, Maurizio Botta, Fabrizio Manetti, Marco Radi, Alessandra Santucci, Giovanni Maga, Mauro Bologna, Adriano Angelucci, Annalisa Santucci, Adriano Spreafico, Fabio Carraro, Jurgen Borlak
  • Pyrazolo[1,5-a]pyrimidine derivatives
    Patent number: 8461162
    Abstract: Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew G. Stanton, Njamkou Noucti, David L. Sloman, Jongwon Lim, Benito Munoz
  • Salts of prodrugs of piperazine and substituted piperidine antiviral agents
    Patent number: 8461333
    Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: June 11, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
  • Pyrrolopyrimidinedione and its therapeutic use
    Patent number: 8455505
    Abstract: The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: June 4, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Christine Edwards, Janus Kulagowski, Harry Finch
  • Triazolo[4,5-D]pyramidine derivatives and their use as purine receptor antagonists
    Patent number: 8450328
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: May 28, 2013
    Assignee: Vernalis (R&D) Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • LIMK2 inhibitors, compositions comprising them, and methods of their use
    Patent number: 8450332
    Abstract: Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: May 28, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Hugh Alfred Burgoon, Nicole Cathleen Goodwin, Bryce Alden Harrison, Jason Patrick Healy, Ying Liu, Ross Mabon, Brett Marinelli, David Brent Rawlins, Dennis Stewart Rice, Norris Andrew Whitlock
  • Gamma secretase modulators
    Patent number: 8450343
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: May 28, 2013
    Inventors: Xianhai Huang, Anandan Palani, Jun Qin, Robert G. Aslanian, Zhaoning Zhu, William Greenlee, Hubert Josien, Wei Zhou, Xiaohong Zhu, Chad E. Bennett, Dmitri Pissarnitski, Mihirbaran Mandal, Pawan Dhondi, Troy McCracken, Thomas Bara, Zhiqiang Zhao, Duane Burnett, John Clader
  • Inhibitors of polo-like kinase
    Patent number: 8445503
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: May 21, 2013
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
  • Bicycloaniline derivative
    Patent number: 8436004
    Abstract: The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ?NH or ?O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: May 7, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Hidetomo Furuyama, Kenji Niiyama, Toshihiro Sakamoto, Satoshi Sunami, Keiji Takahashi, Fuyuki Yamamoto, Takashi Yoshizumi
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 8436015
    Abstract: Glucagon receptor antagonist compounds of formula I are disclosed: The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Christian P. Stevenson, Emma R. Parmee, Libo Xu, Xibin Liao, Edward Metzger, Rui Liang, Fengqi Zhang, John E. Stelmach
  • Substituted imidazo- and triazolopyrimidines, imidazo- and pyrazolopyrazines and imidazotriazines
    Patent number: 8436003
    Abstract: The invention relates to substituted triazolopyrimidines of the formula processes for their preparation, and their use for the treatment of hematological disorders.
    Type: Grant
    Filed: May 2, 2009
    Date of Patent: May 7, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephan Siegel, Andreas Wilmen, Niels Svenstrup, Mark Jean Gnoth, Adrian Tersteegen, Ulrich Rester
  • [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds and their use
    Patent number: 8431596
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: April 30, 2013
    Assignee: Cancer Research Technology Limited
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Wynne
  • Imidazopyrimidines and uses thereof
    Patent number: 8431581
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: April 30, 2013
    Assignee: Avexa Limited
    Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Van de Graff, Lisa Jane Winfield
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 8426409
    Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: April 23, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Rama K. Kondru, Yan Lou, Eric Brian Sjogren, Michael Soth
  • Certain substituted amides, method of making, and method of use thereof
    Patent number: 8426424
    Abstract: The invention relates to compounds of the following Formula I wherein R1, R2, Z, W, and D are defined herein, that inhibit Btk and therefore are useful in the treatment of diseases responsive to inhibition of Btk activity such as cancer. The invention also relates to pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, as well as methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described, and methods for determining the presence of Btk in a sample.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: April 23, 2013
    Assignees: CGI Pharmaceuticals, Inc., Genentech, Inc.
    Inventors: Peter A. Blomgren, David R. Brittelli, Kevin S. Currie, Seung H. Lee, Jeffrey E. Kropf, Scott A. Mitchell, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Zhongdong Zhao, Pavel E. Zhichkin
  • Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties
    Patent number: 8426432
    Abstract: The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: April 23, 2013
    Assignee: University of Connecticut
    Inventors: Amy C. Anderson, Dennis L. Wright, Phillip M. Pelphrey, Tammy M. Joska, Erin S. D. Bolstad, David B. Bolstad, Veljko Popov