Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
August 17, 2000
Date of Patent:
February 21, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
Abstract: The present invention provides materials and methods for predicting the in vivo toxicity of a given compound. For example, the invention comprises conducting at least three distinct assays in parallel to provide information about three distinct parameters of cytotoxicity of a chemical in a given target cell, which information is useful for predicting in vivo cytotoxicity.
Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.
Abstract: An unliganded form of Staphylococcus aureus NAD synthetase (S. aureus NadE) has been crystallized, and the three-dimensional x-ray crystal structure has been solved to 2.3 ? resolution. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing inhibitors of S. aureus NadE activity.
Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.
Type:
Grant
Filed:
January 23, 2002
Date of Patent:
January 17, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson
Abstract: The present invention describes a recombinant rodent model for depression. More particularly, the rodent comprises cells expressing mutations in the WFS1 gene. The rodent is preferably a mouse heterologous for mutations in exon 8 of the WFS1 gene. Preferably, the mutations yield a non-functional wolframin protein that lacks all or some of it transmembrane regions. Methods and compositions for making and using the mouse and cells thereof are disclosed.
Abstract: A method for screening chemical compounds for electrophilic properties comprising the steps of: (a) providing an assay having one or more reaction vessels; (b) adding a predetermined amount of separate chemical compounds for screening to each reaction vessel; (c) adding a predetermined amount of a surrogate chemical marker to each reaction vessel and allowing said separate chemical compounds and surrogate chemical marker to incubate for a period of time; (d) adding a reactive chemical to each reaction vessel which is capable of reacting with residual surrogate chemical marker such that the amount of residual surrogate chemical marker present after step (c) can be quantitatively or qualitatively measured; and (e) quantitatively or qualitatively measuring said residual chemical marker is provided.
Type:
Grant
Filed:
October 5, 2001
Date of Patent:
December 27, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Larry C. Wienkers, Michael J. Hauer, Dennis E. Epps
Abstract: Processes are described for epoxidation reactions. In particular, the process comprises the conversion of a steroid substrate having an olefinic unsaturation in the steroid nucleus to a structure comprising a 9,11-epoxy substituent by reaction of the substrate with a peroxide compound in the presence of a peroxide activator. The epoxidation processes described are conducted at relatively low hydrogen peroxide to steroid substrate ratio. Several optional process modifications are described.
Type:
Application
Filed:
March 22, 2005
Publication date:
December 8, 2005
Applicant:
Pharmacia & Upjohn Company LLC
Inventors:
Joseph Wieczorek, Keith Maisto, Paul David, Marlon Carlos, Chung Kim
Abstract: The present invention provides methods and compositions related to the generation of host cells permissive for virus growth, particularly Porcine Reproductive and Respiratory Syndrome (PRRS) virus.
Type:
Application
Filed:
April 25, 2005
Publication date:
December 8, 2005
Applicant:
Pharmacia and Upjohn Company, LLC
Inventors:
Jay Calvert, Shelly Shields, David Slade, Siao-Kun Welch
Abstract: The present invention relates to the field of cancer treatment and, more particularly, it relates to a method for predicting the sensitivity towards chemotherapy of a patient, by measuring glutathione (GSH) blood levels of the said patient undergoing chemotherapeutic treatment.
Type:
Grant
Filed:
September 26, 2001
Date of Patent:
November 29, 2005
Assignees:
Pharmacia Italia S.p.A., Pharmacia & Upjohn Company LLC
Inventors:
Camilla Fowst, Maria Christina Rosa Geroni, Jennifer Margaret Tursi, Franzanne Vreeland
Abstract: The present invention are macrocycles of the formula (IX): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
June 12, 2002
Date of Patent:
November 29, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Shon R. Pulley, James P. Beck, Ruth E. TenBrink
Abstract: Staphylococcus aureus peptide deformylase has been crystallized, and the three-dimensional x-ray crystal structure has been solved to 1.9 ? resolution. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing modifiers of peptide deformylase activity.
Abstract: A composition comprising: (a) a pharmaceutically effective amount of reboxetine; and selected from the group consisting of clozapine, olanzapine, risperidone and mixtures thereof (b) a pharmaceutically effective amount of one or more neuroleptic agents or a pharmaceutically effective salt thereof is provided.
Type:
Grant
Filed:
December 28, 2001
Date of Patent:
November 15, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Erik Ho Fong Wong, Christopher C. Gallen, Torgny Svensson
Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
January 6, 2003
Date of Patent:
November 8, 2005
Assignees:
Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
Inventors:
Martha A. Warpehoski, Barbara Jagodzinska
Abstract: Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R1, R2 and R20 are defined herein. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
May 22, 2002
Date of Patent:
November 1, 2005
Assignee:
Pharmacia & UpJohn Company
Inventors:
Heinrich Schostarez, Robert Alan Chrusciel, Rebecca S. Centko
Abstract: The present invention provides an emulsion formulation with high oral bioavailability containing lecithin as an emulsifier and solubilizing agent to achieve a high loading of the pyranone compound of formula I
Abstract: The present invention provides a pharmaceutical composition which is substantially free of unpleasant tastes and orally administrable which comprises: (a) an active medicament, (b) an inner coating layer comprising an oil substance having a melting point at a range of from about 50° C. to about 100° C., (c) an outer coating layer comprising at least a polymeric substance.
Abstract: The present invention provides isotopically labeled oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are described herein. These compounds are useful in the diagnostic analysis of diseases wherein modulation of 5-HT activity is desired.
Type:
Grant
Filed:
April 8, 2003
Date of Patent:
August 23, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Ruth Elizabeth TenBrink, Kalpana M. Merchant, Timothy J. McCarthy
Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.
Type:
Grant
Filed:
June 30, 2003
Date of Patent:
August 16, 2005
Assignee:
Pharmacia & UpJohn Company
Inventors:
Barry Craig Finzel, Lee A. Funk, Robert Charles Kelly, Matthew T. Reding, Nancy Anne Wicnienski