Abstract: The present invention provides the enzyme and enzymatic procedures for cleaving the ? secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associated nucleic acids, peptides, vectors, cells, and cell isolates, and assays that are particularly useful for identifying candidate therapeutics for treatment or prevention of Alzheimer's disease.
Type:
Grant
Filed:
August 29, 2003
Date of Patent:
May 6, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
Abstract: The present invention provides Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells, and methods for its production. The invention also provides methods for the identification of homologs in other species and of DmGPCR agonists/antagonists useful as potential insecticides. The invention further provides methods for binding a DmGPCR, methods for identifying modulators of DmGPCR expression and activity, methods for controlling a population of insects with a DmGPCR antibody, a DmGPCR antisense polynucleotide, a DmGPCR binding partner or modulator, and methods of preventing or treating a disease or condition associated with an ectoparasite. Specifically, this invention discloses the matching of the orphan Drosophila drotachykinin, droleucokinin, and drostatin-C receptors with their cognate peptide ligands.
Type:
Grant
Filed:
August 6, 2002
Date of Patent:
April 29, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
David E. Lowery, Valdin G. Smith, Teresa M. Kubiak, Martha J. Larsen
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:
March 8, 2005
Date of Patent:
April 15, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Heinrich Josef Schostarez, Robert Alan Chrusciel
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:
March 8, 2005
Date of Patent:
April 8, 2008
Assignee:
Pharmacia & Upjohn
Inventors:
Heinrich Josef Schostarez, Robert Alan Chrusciel
Abstract: The present invention provides a Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells and methods for its production. The invention also provides methods for the identification of homologs in other animals, and of DmGPCR agonists/antagonists, useful for the treatment of diseases in animals and for the control of insects that are injurious or harmful to plants or animals.
Type:
Grant
Filed:
December 15, 2003
Date of Patent:
April 8, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
David E. Lowery, Valdin G. Smith, Teresa M. Kubiak, Martha J. Larsen
Abstract: The invention provides 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:
November 26, 2003
Date of Patent:
April 1, 2008
Assignees:
Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
Abstract: Disclosed herein are methods of treating an individual suffering from, chronic fatigue syndrome. The methods generally include administration of a therapeutic amount of racemic reboxetine, or a pharmaceutically acceptable salt thereof, to the individual.
Type:
Grant
Filed:
February 7, 2006
Date of Patent:
March 4, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson
Abstract: The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure: where Z is CR or N, and R1, R2 and R3 are as described in the specification.
Type:
Grant
Filed:
November 19, 2002
Date of Patent:
March 4, 2008
Assignees:
Pharmacia & Upjohn Company, Elan Pharmaceuticals, Inc.
Inventors:
Joseph B. Moon, Shon R. Pulley, Daniel H. Rich, David L. Brown, Barbara Jagodzinska, Varghese John, John Jacobs
Abstract: A method for preventing medical device-associated microorganism infection includes the steps of providing a medical device and incorporating an effective amount of an oxazolidinone compound, such as linezolid, into the medical device.
Type:
Grant
Filed:
January 21, 2003
Date of Patent:
January 29, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
John Kenneth Gibson, Charles W. Ford, Paul J. Pagano
Abstract: Disclosed herein are methods of treating an individual suffering from peripheral neuropathy. The methods generally include administration of a therapeutic amount of optically pure (S,S) reboxetine, or a pharmaceutically acceptable salt thereof. Embodiments of these methods can diminish adverse side effects.
Type:
Grant
Filed:
January 16, 2004
Date of Patent:
January 8, 2008
Assignee:
Pharmacia & Upjohn
Inventors:
Erik H. F. Wong, Saeeduddin Ahmed, Robert Clyde Marshall, Robert McArthur, Duncan P. Taylor
Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds interact with and inhibit the activity of the enzyme beta-secretase. These compounds are therefore useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions and methods of treatment of these diseases are also disclosed.
Type:
Grant
Filed:
December 6, 2002
Date of Patent:
December 25, 2007
Assignees:
Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
Inventors:
Ruth TenBrink, Michel Maillard, Martha Warpehoski
Abstract: The invention provides transgenic animals that are heterozygous or homozygous for a nonfunctional allele of BACE-1. These animals show normal development indicating that BACE-1 is not necessary for development and hence is an appropriate therapeutic target. The transgenic animals are useful in various screening assays including identifying inhibitors of other enzymes involved in processing of APP to A? and determining a toxicity profile of inhibitors of BACE-1.
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
December 18, 2007
Assignees:
Elan Pharmaceuticals, Inc, Pharmacia & Upjohn Company
Abstract: The present invention provides compounds, for example, of formula (I): wherein R1, R2, and R3 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods, and processes and intermediates useful for preparing compounds of formula I.
Abstract: Disclosed herein are methods of treating an individual suffering from, chronic fatigue syndrome. The methods generally include administration of a therapeutic amount of optically pure (S,S) reboxetine, or a pharmaceutically acceptable salt thereof, to the individual. Embodiments of these methods can diminish adverse side effects.
Type:
Grant
Filed:
February 7, 2006
Date of Patent:
October 2, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor
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:
Application
Filed:
November 1, 2004
Publication date:
September 27, 2007
Applicants:
ELAN PHARMACEUTICALS, INC., PHARMACIA & UPJOHN COMPANY LLC
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:
April 30, 2003
Date of Patent:
August 28, 2007
Assignees:
Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
Inventors:
John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Grant
Filed:
August 28, 2006
Date of Patent:
August 14, 2007
Assignees:
Sugen, Inc., Pharmacia & Upjohn Company
Inventors:
Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
Abstract: The invention relates ton novel methods for measuring ion channel transmission and methods and compositions useful in the indentification of ligand gated channel agonists and modulators.
Type:
Grant
Filed:
December 18, 2003
Date of Patent:
July 24, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Vincent E. Groppi, Jr., Mitchell B. Berkenpas
Abstract: The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, such as maleate salts, and to crystalline polymorphs of these salts. The invention further relates to pharmaceutical compositions of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide salts, and methods of treating disorders such as cancer using such compositions.
Type:
Grant
Filed:
September 30, 2004
Date of Patent:
July 24, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Andrei Blasko, Qingwu Jin, Qun Lu, Michael A. Mauragis, Dian Song, Brenda S. Vonderwell
Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 and R2 are independently hydrogen, C1-6 alkyl or R1 and R2 are joined to form pyrrolidiae, piperidine, morpholine or imidazole. X is OCH3, SO2R3, SO2CF3 or CN where R3 is C1-6 alkyl or an Aryl; and Y is hydrogen, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2. These new compounds are suitable for treating anxiolytic disorder, schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure or treating migraine headaches in patients in need of such treatment.