Abstract: The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 which are useful in treating depression, obesity and other CNS disorders.
Abstract: The present invention provides a gene encoding a heretofore unknown G protein coupled receptor termed CON167; constructs and recombinant host cells incorporating the gene; the CON167 polypeptide encoded by the gene; antibodies to the polypeptide; and methods of making and using all of the foregoing.
Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Type:
Grant
Filed:
October 2, 2003
Date of Patent:
April 5, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail Fedor Gordeev, Adam Renslo, Dinesh Vinoobhai Patel
Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
Type:
Grant
Filed:
December 5, 2003
Date of Patent:
March 22, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
Abstract: The present invention relates to (2S)-enantiomers of 2-aminoindan derivatives of formula I: and a novel process for the preparation of them.
Type:
Grant
Filed:
April 29, 2002
Date of Patent:
March 22, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Arthur Glenn Romero, Thomas Andrew Runge, Bradley D. Hewitt, Kjell Anders Ivan Svensson, Chiu-Hong Lin, Kerry Anne Cleek, Susanne R. Haadsma-Svensson
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:
April 12, 2000
Date of Patent:
March 15, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
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: The present invention provides compounds of Formula I: wherein X, R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula I.
Abstract: The present invention is a process for the preparation of rofleponide of formula (II) where the 22R/22S ratio is 90/10 or greater which comprises contacting an acetonide of formula (I) with CH3—CH2—CH2—CHO (III) in the presence of perchloric acid where the concentration of the acetonide (I) is from about 1 g/20 ml to about 1 g/50 ml in the absence of an inert material.
Abstract: The present invention provides recombinant DNA molecules comprising a sequence encoding a pseudorabies virus (PRV) glycoprotein selected from the group consisting of gI, gp50, and gp63, host cells transformed by the recombinant DNA molecule sequences, the gI, gp50 and gp63 polypeptides. The present invention also provides subunit vaccines for PRV, methods for protecting animals against PRV infection and methods for distinguishing between infected and vaccinated animals.
Type:
Grant
Filed:
December 24, 2002
Date of Patent:
February 22, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Erik Aivars Petrovskis, Leonard Edwin Post, James G. Timmins
Abstract: Highly purified preparations of TFPI or TFPI analogs can be prepared using a method that generally involves the following steps: (1) expression of TFPI or TFPI analog in E. coli, (2) isolation of refractile bodies, (3) dissolution of the refractile bodies and refolding of the expressed TFPI or TFPI analog, (4) SP-Sepharose fast flow (FF) chromatography, (5) a first concentration and diafiltration step, (6) Q-Sepharose high (HP) performance chromatography, (7) butyl hydrophobic interaction chromatography (HIC), (8) SP-Sepharose HP chromatography, and (9) a second concentration/diafiltration step. Less than about 12% of the TFPI or TFPI analog molecules in such preparations are modified TFPI or TFPI analog species (i.e., oxidized, carbamylated, acetylated, deamidated, aggregated, or misfolded species).
Type:
Application
Filed:
January 8, 2004
Publication date:
February 17, 2005
Applicants:
Chiron Corporation, Pharmacia & Upjohn Company
Inventors:
David Reifsnyder, Duane Inlow, Glenn Dorin, Patricio Riquelme, Cynthia Cowgill, Douglas Bolesch, Mark Gustafson
Abstract: The invention provides compounds of the formula and methods of using those compounds for treating a disease or condition in a mammal wherein a 5-HT receptor, such as a 5-HT6 receptor, is implicated and modulation of a 5-HT function is desired, wherein A, G and W1-W3 are defined as herein.
Abstract: The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.
Type:
Grant
Filed:
August 6, 2002
Date of Patent:
February 1, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael D. Ennis, Kristine E. Frank, Robert L. Hoffman, Jian-Min Fu
Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.
Abstract: The present invention is disubstituted amines of formula (I) and disubstituted amines of formula (II) useful in treating Alzheimer's disease and other similar diseases.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
January 25, 2005
Assignees:
Pharmacia & Upjohn Company, Elan Pharmaceuticals, Inc.
Inventors:
James P. Beck, Andrea Gailunas, Roy Hom, Barbara Jagodzinska, Varghese John, Michel Maillard
Abstract: The present invention provides for a polypeptide aggregation screening assay for the purpose of detecting modulators of polypeptide aggregation, which can provide for new therapies in pathologic states associated with polypeptide aggregation, especially considered is Alzheimer's Disease.
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.