Abstract: The invention includes tetrahydroquinoline and related compounds of formula I and pharmaceutical compositions thereof, that exhibit useful antibacterial activity again a wide range of human and veterinary pathogens
Type:
Grant
Filed:
March 7, 2007
Date of Patent:
October 20, 2009
Assignee:
Pharmacia & Upjohn Company LLC
Inventors:
Michael Robert Barbachyn, J. Craig Ruble, Arthur Glenn Romero, Lisa Marie Thomasco, Alexander Ross Hurd, John Raymond Palmer, Peter Laurence Toogood, Dennis Joseph McNamara, Debra Ann Sherry, Paul Joseph Dobrowolski
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. An enzyme that cleaves the ?-secretase site of APP also is provided. 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.
Abstract: The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation.
Type:
Application
Filed:
November 17, 2005
Publication date:
May 28, 2009
Applicants:
Pharmacia and Upjohn Company LLC
Inventors:
Charles Francis Donovan, Vara Prasad Venkata Nagendra Josyula, Manjinder Singh Lall, Adam Robert Renslo
Abstract: The present invention provides for compositions of anti-M-CSF antibodies that are substantially free of endotoxin. Also provided are methods of treating M-CSF-mediated disorders with pharmaceutical formulations of anti-M-CSF antibodies having reduced endotoxin levels, including inflammatory diseases and neoplasia disorders.
Abstract: This present invention relates to prodrug compounds of the formula (Y) and pharmaceutical salts thereof: where RN, R1, R2, R3R4 and RC are defined herein, which are useful in treating Alzheimer's disease and other similar diseases.
Type:
Grant
Filed:
February 27, 2003
Date of Patent:
March 3, 2009
Assignees:
Pharmacia & Upjohn Company LLC, Elan Pharmaceuticals, Inc.
Inventors:
Varghese John, Barbara Jagodzinska, Michel Maillard, James P. Beck, Ruth E. TenBrink, Daniel Getman
Abstract: The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide.
Type:
Application
Filed:
October 13, 2008
Publication date:
February 19, 2009
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Changquan Sun, Todd P Foster, Fusen Han, Michael Hawley, Tom Thamann
Abstract: Gram negative bacterial virulence genes are identified, thereby allowing the identification of novel anti-bacterial agents that target these virulence genes and their products, and the provision of novel gram negative bacterial mutants useful in vaccines.
Type:
Grant
Filed:
May 26, 2004
Date of Patent:
January 13, 2009
Assignee:
Pharmacia & Upjohn Company
Inventors:
David E. Lowery, Troy E. Fuller, Michael J. Kennedy
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. An enzyme that cleaves the ?-secretase site of APP also is provided. 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:
April 5, 2004
Date of Patent:
November 25, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael Jerome Bienkowski
Abstract: The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide.
Type:
Grant
Filed:
February 12, 2004
Date of Patent:
November 18, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Changquan Sun, Todd P. Foster, Fusen Han, Michael Hawley, Tom Thamann
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:
September 2, 2005
Date of Patent:
October 28, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Shon R. Pulley, James P. Beck, Ruth E. TenBrink
Abstract: The present invention provides crystals, and compositions thereof, wherein the crystals include a malic acid salt of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. Methods of preparing such crystals are also disclosed.
Type:
Grant
Filed:
April 26, 2007
Date of Patent:
October 14, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael Hawley, Thomas J. Fleck, Stephen P. Prescott, Mark T. Maloney
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:
Application
Filed:
February 15, 2008
Publication date:
October 2, 2008
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
David E. Lowery, Valdin G. Smith, Teresa M. Kubiak, Martha J. Larsen
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 27, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
Abstract: A method for developing a library of compounds, the compound library, a method for identifying ligands for target molecules, and a method for identifying lead chemical templates, which, for example, can be used in drug discovery and design are provided. Certain embodiments of these methods include the use of NMR spectroscopy.
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 20, 2008
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael J. Bienkowaki, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
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: 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.