Abstract: Disclosed are new classes of phenanthridinium derivatives, most notably dihydro-imidazo-phenanthridinium (DIP) compounds. The compounds are prepared by the reaction of the middle b ring of a phenanthridinium core with primary amines to form the DIP compounds. This reaction can also be applied to other classes of starting compounds which comprise a 6-membered ring aromatic heterocycle having a ring nitrogen and at least one alpha hydrogen atom which can be reacted with a primary amine. Also disclosed is a method of using the DIP compounds for treatment of ovarian cancer.
Type:
Grant
Filed:
November 26, 2004
Date of Patent:
May 24, 2011
Assignee:
University Court of the University of Glasgow
Inventors:
Alexis Parenty, Leroy Cronin, Robert Brown
Abstract: Sterically hindered hydroxy substituted alkoxyamine stabilizer compounds are made water compatible via certain backbones with affinity towards water. The sterically hindered amines are for example of the formula (8)-(10) These compounds are particularly effective in stabilizing aqueous polymer systems against the deleterious effects of oxidative, thermal and actinic radiation. The compounds are effective for example in stabilizing water borne coatings, aqueous inks, aqueous ink jet media and photocured aqueous systems.
Type:
Grant
Filed:
April 9, 2009
Date of Patent:
May 24, 2011
Assignee:
BASF SE
Inventors:
Mervin G. Wood, Robert Detlefsen, James Galbo, Wanda Martin, Paul Kondracki, Michael P. DiFazio, Joseph E. Babiarz
Abstract: The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.
Type:
Grant
Filed:
May 12, 2006
Date of Patent:
May 24, 2011
Assignee:
Sanofi-Aventis
Inventors:
Jérôme Cazelles, Frédéric Cosledan, Bernard Meunier, Alain Pellet
Abstract: Solution-processable organic n-type semiconductor materials are provided with processes for preparing the same. Composites and electronic devices including the organic n-type semiconductor materials also are provided.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
May 24, 2011
Assignee:
Polyera Corporation
Inventors:
Tobin J. Marks, Antonio Facchetti, He Yan
Abstract: Anti-malarial alkyloid compounds have the formula: wherein R1-R11 have various disclosed values or their pharmaceutically acceptable salts, and pharmaceutical compositions containing the same.
Type:
Grant
Filed:
October 20, 2006
Date of Patent:
May 17, 2011
Assignees:
Universite Pierre et Marie Curie (Paris VI), Centre National de la Recherche Scientifique, Museum National d'Histoire Naturelle, Institut Malgache de Recherche Appliquee
Abstract: Novel pyridinium salts functionalized with boronic acid and methods of making them are disclosed. When combined with a fluorescent dye, the compounds are useful in the detection of polyhydroxyl-substituted organic molecules.
Abstract: The present invention is directed to a process for reducing the level of ?, ?-unsaturated ketone in an opioid analgesic composition by hydrogenation the opioid analgesic composition with diimide or a diimide progenitor.
Abstract: This invention relates to a new and efficient process for the production of dopamine agonists such as Cabergoline and the intermediates thereof.
Type:
Grant
Filed:
May 4, 2007
Date of Patent:
May 10, 2011
Assignee:
Apotex Pharmachem Inc.
Inventors:
Zhi-Xian Wang, YuanQiang Li, Murali Kondamreddy, Xiongwei Cai
Abstract: The present invention relates to a light emitting transition metal compound represented by the Chemical Formula 1 and Chemical Formula 2 and an organic electroluminescence device including the same. In the above Chemical Formulae 1 and 2, M is Ir, Pt, Rh, Re, Os, or the like, m is 2 or 3 and n is 0 or 1, where the sum of m and n is 3, provided that the sum of m and n is 2 when M is Pt, X and Z are the same or different and may be N or P, and Y is O, S, or Se.
Type:
Grant
Filed:
January 8, 2007
Date of Patent:
May 10, 2011
Assignees:
Samsung Electronics Co., Ltd., Industry-University Cooperation Foundation, Hanyang University
Inventors:
Dong-Hack Suh, Jin-Soo Lim, Ji-Ho Kim, Sun-Hyun Choi
Abstract: The present invention provides a method for the N-demethylation of an N-methylated heterocycle, particularly a morphine or tropane alkaloid or derivative thereof. The method comprises reacting the heterocycle with a metal catalyst and a solvent in the presence of an oxidizing agent.
Type:
Grant
Filed:
June 29, 2007
Date of Patent:
May 3, 2011
Assignee:
Brock University
Inventors:
Robert James Carroll, Hannes Leisch, Tomas Hudlicky
Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
Abstract: A process for the purification of an impure preparation containing naltrexone by means of a reverse phase preparative chromatography process is provided. In an illustrative embodiment a chromatographic column is loaded with a stationary phase, typically a silica particle having an organic ligand bound thereto. With a loading ratio of from about 10 to about 1000 the impure preparation is acidified and passed through the column. The column is eluted with typically an aqueous solution with acetonitrile and the purified naltrexone is obtained in a specified fraction.
Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
Type:
Grant
Filed:
November 4, 2009
Date of Patent:
April 19, 2011
Assignee:
Amgen Inc.
Inventors:
Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
Abstract: Methods of preparing CPT-esters are described. The methods include using at least one acid in the esterification reactions or acylation reactions of camptothecins.
Type:
Grant
Filed:
August 2, 2007
Date of Patent:
April 19, 2011
Assignee:
The Christus Stehlin Foundation for Cancer Research
Abstract: The present invention provides methods for the conversion of thebaine to a morphine derivative, such as hydrocodone. Novel ketal intermediates of the conversion are provided. A one-pot procedure for the conversion comprises treating thebaine with an acid in the presence of a metal catalyst.
Type:
Grant
Filed:
June 29, 2007
Date of Patent:
April 19, 2011
Assignee:
Brock University
Inventors:
Robert James Carroll, Hannes Leisch, Tomas Hudlicky
Abstract: The subject of the present invention is to provide a fluorescent substance excitable under visible light, having higher photostability and a long fluorescence lifetime. Another subject is to provide a fluorescent substance consists of a non-natural amino acid applicable to peptide synthesis systems. Searching fluorescent substances, which are fluorescent amino acids and excitable under visible light, having the lowest possible molecular weight for a high photostability resulted in forming a condensed polycyclic aromatic compound by subjecting a compound having an acridone structure to substitution with an amino acid and further condensation with a benzene ring. Thus, the subject is achieved by the fluorescent substance consisting of amino acid-substituted benzoacridone derivative excitable under visible light.
Type:
Grant
Filed:
June 8, 2006
Date of Patent:
April 19, 2011
Assignee:
National University Corporation Okayama University
Abstract: The present invention provides a compound of formula (I): PtIV(N3)2X1X2Y1Y2, wherein X1 and X2 are the same or different and each one is a group NR1R2R3 wherein R1, R2 and R3 are the same or different and each can be any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or X1 and X2 together represent a group R1R2NR4NR1R2 wherein R1 and R2 have the same meaning as before, and R4 represents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or R4 or two or more of R1, R2, R3 and R4 and the respective N atom(s) to which they are linked, represent an optionally substituted heterocyclyl having at least one ring containing said N atom(s); and Y1 and Y2 are the same or different or when cis together represent a divalent moiety Y3, wherein at least one of Y1 and Y2, or Y3, is a substantially labil
Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and other disorders. The compounds described herein can be water soluble and can act through mechanisms mediated through pathways other than opiate receptors.
Type:
Grant
Filed:
September 8, 2004
Date of Patent:
April 12, 2011
Assignee:
Jenken Biosciences, Inc.
Inventors:
Edwin S. C. Wu, Mao-Hsiung Yen, Chin-Tsai Fan
Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
Type:
Grant
Filed:
July 2, 2008
Date of Patent:
April 5, 2011
Assignee:
Vertex Pharmaceuticals, Inc.
Inventors:
Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
Type:
Grant
Filed:
March 25, 2002
Date of Patent:
March 29, 2011
Assignee:
Novartis AG
Inventors:
Andrew James Culshaw, Peter Gull, Allan Hallett, Hong-Yong Kim, Max Peter Seiler, Kaspar Zimmermann, Yugang Liu, Mahavir Prashad