Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
July 1, 2008
Date of Patent:
September 20, 2011
Assignee:
Gilead Sciences, Inc.
Inventors:
Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang
Abstract: An aromatic polyanhydride comprising a repeating unit having the structure is disclosed, wherein Ar and R are selected so that the aromatic polyanhydride hydrolyzes to form a therapeutic salicylate, another non-steroidal anti-inflammatory, an antifibrotic aminobenzoate, or a vasoconstricting phenylethanolamine. Implantable medical devices, such as scaffolding implants for tissue reconstruction, drug delivery systems prepared from the aromatic polyanhydrides, as well as therapeutic dosage forms and treatment methods are also disclosed.
Type:
Grant
Filed:
April 22, 2009
Date of Patent:
September 13, 2011
Assignee:
Rutgers, The State University of New Jersey
Abstract: The present invention relates to a process for the preparation of composites from thermoplastic polymers and (semi)metal oxides, in particular silicon dioxide, wherein at least a part of the (semi)metal oxides is dispersed in the polymers in nanodispersed manner (nanocomposites). The invention relates to the composites obtainable by this process and their processing to give molded articles.
Type:
Grant
Filed:
September 4, 2006
Date of Patent:
September 6, 2011
Assignee:
Deutsches Wollforschungsinstitut an der RWTH Aachen e.V.
Inventors:
Susanne Spiegelberg, Armin Alteheld, Xiaomin Zhu, Karin Peter, Martin Möller
Abstract: The present invention relates to a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6-alkoxy groups and R3 is indolyl or azaindolyl which may carry one or two substituents independently selected from C1-C6-alkyl, C1-C6-alkoxy, phenyl, OH, halogen, NH2, C1-C6-alkylamino, di-C1-C6-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula 1 and of the salts thereof. The compounds of formula (I) are suitable for controlling angiogenesis.
Type:
Grant
Filed:
December 7, 2005
Date of Patent:
August 30, 2011
Assignee:
Johannes Gutenberg-Universitatis
Inventors:
Gerd Dannhardt, Christian Peifer, Stanislav Plutizki, Jan-Peter Kramb
Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
Type:
Grant
Filed:
July 5, 2007
Date of Patent:
August 23, 2011
Assignees:
Array BioPharma Inc., Genertech, Inc.
Inventors:
Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Banka, Jun Liang, Brian Safina, Jun Li, Christine Chabot
Abstract: Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Type:
Grant
Filed:
January 30, 2007
Date of Patent:
August 23, 2011
Assignee:
Array BioPharma, Inc.
Inventors:
James F. Blake, Steven Boyd, Jason De Meese, John J. Gaudino, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian
Abstract: The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
Type:
Grant
Filed:
March 5, 2009
Date of Patent:
August 9, 2011
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Yarlagadda S. Babu, Pooran Chand, Pravin Kotian, Minwan Wu, V. Satish Kumar
Abstract: The invention provides compounds of formula (I) and salts thereof: R1-L-R2—B wherein R1, L, R2, and B have any of the values defined herein, as well as compositions comprising such compounds, and therapeutic methods comprising the administration of such compounds or salts. The compounds block siderophore production in bacteria and are useful as antibacterial agents.
Type:
Grant
Filed:
December 6, 2006
Date of Patent:
August 2, 2011
Assignee:
Regents of the University of Minnesota
Inventors:
Courtney Aldrich, Ravindranadh Venkata Somu
Abstract: Medical devices with at least one surface comprising a polymer or polymers on the surface are provided. The polymer or polymers are capable of breaking down (e.g., including, but not limited to, hydrolyzing) in the physiologic milieu to form an active agent or agents under physiologic conditions, and can contain other active agents dispersed within or appended to the polymer matrix. Methods of delivering an active agent to an interior surface of a vein or artery are also provided.
Type:
Grant
Filed:
November 18, 2003
Date of Patent:
July 26, 2011
Assignee:
Rutgers, The State University of New Jersey
Abstract: A method of promoting or improving the feed efficiency and the muscle to fat ratio in animals by administering to the animals a therapeutically effective amount of a pure or substantially pure RR-isomer of ractopamine is disclosed. Also disclosed are animal feed preparations and compositions and pharmaceutical preparations capable of increasing lean meat deposition in an animal or decreasing body fat, or promoting or improving the growth of an animal or improving the feed efficiency of an animal. Feed preparation, compositions and pharmaceutical preparations including therapeutically effective amounts of a pure or substantially pure RR-isomer of ractopamine are disclosed.
Abstract: A fibronectin type III (Fn3) polypeptide monobody, a nucleic acid molecule encoding said monobody, and a variegated nucleic acid library encoding said monobody, are provided by the invention. Also provided are methods of preparing a Fn3 polypeptide monobody, and kits to perform said methods. Further provided is a method of identifying the amino acid sequence of a polypeptide molecule capable of binding to a specific binding partner (SBP) so as to form a polypeptide:SSP complex, and a method of identifying the amino acid sequence of a polypeptide molecule capable of catalyzing a chemical reaction with a catalyzed rate constant, kcat, and an uncatalyzed rate constant, kuncat, such that the ratio of kcat/kuncat is greater than 10.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
July 19, 2011
Assignee:
Novartis International Pharmaceutical Ltd.
Abstract: The present invention provides novel pseudotyped retroviral vectors that can transduce human and other cells. Vectors are provided that are packaged efficiently in packaging cells and cell lines to generate high titer recombinant virus stocks expressing novel envelope glycoproteins. The present invention further relates to compositions for gene therapy.
Type:
Grant
Filed:
June 11, 2008
Date of Patent:
April 26, 2011
Assignee:
University of Iowa Research Foundation
Inventors:
Paul B. McCray, Jr., Beverly L. Davidson, Colleen Stein
Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
March 30, 2009
Date of Patent:
April 19, 2011
Assignees:
Genentech, Inc., Hoffman-La Roche Inc.
Inventors:
Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.
Type:
Grant
Filed:
February 4, 2008
Date of Patent:
March 8, 2011
Assignees:
University of Iowa Research Foundation, The United States of America, National Institute of Health
Inventors:
David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
Abstract: Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
September 23, 2008
Date of Patent:
February 22, 2011
Assignees:
Genentech, Inc., F. Hoffmann-La Roche AG
Inventors:
Georgette M. Castanedo, Janet L. Gunzner, Kimberly Malesky, Simon Mathieu, Alan G. Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Sally Oxenford, Nan Chi Wan
Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
December 5, 2007
Date of Patent:
February 15, 2011
Assignees:
Piramed Limited, Genentech, Inc.
Inventors:
Tracy Bayliss, Irina Chuckowree, Adrian Folkes, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzner, Tim Heffron, Simon Mathieu, Alan Olivero, Steven Staben, Daniel P. Sutherlin, Bing-Yan Zhu
Abstract: The invention provides a polymer of formula I: wherein A, B, D, E, R1, and R2 have any of the values defined in the specification, as well as electrical devices comprising such polymers.
Abstract: Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
Type:
Grant
Filed:
August 16, 2007
Date of Patent:
January 18, 2011
Assignee:
F. Hoffmann-La Roche AG
Inventors:
Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
Abstract: The invention provides compounds of formula I or formula II: wherein: the bond represented by is a single bond or a double bond, and R1—R5, X, and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.
Type:
Grant
Filed:
April 13, 2009
Date of Patent:
December 28, 2010
Assignee:
Rutgers, The State University of New Jersey
Inventors:
Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu