Abstract: This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in figure BG.sub.4-1, below. ##STR1## where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8) alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3) alkoxy, halogen, trifluoromethyl;where R.sup.2 is --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.
Type:
Grant
Filed:
July 24, 1997
Date of Patent:
October 5, 1999
Assignee:
Pharmacia & Upjohn Company
Inventors:
Thomas J. Fleck, Bruce A. Pearlman, William W. McWhorter, Jr.
Abstract: This invention describes the isolation and identification of a new protein, p56, useful for the identification of drugs that will selectively open or close K channels. The protein p56 has a molecular weight of about 56,000 daltons and the N-terminal peptide sequence is: Glu-Pro-Arg-Ala-Pro-Pro-Glu-Lys-Ile-Ala-Ile-Val-Gly-Ala-Gly-Ile.
Type:
Grant
Filed:
August 26, 1997
Date of Patent:
July 20, 1999
Assignee:
Pharmacia & Upjohn Company
Inventors:
Vincent E. Groppi, Jr., Martin R. Deibel, Jr., Mark L. Wolfe, Anthony W. Yem
Abstract: The present invention comprises human DNA compositions encoding proteins that confer potassium channel activity to membranes or recipient cell lines. The DNA compositions include structural genes coding for the potassium channel proteins, expression and replication plasmids or vectors containing the structural genes and host cells expressing those genes. Methods of screening compounds for potassium channel modulating activity are also described.
Type:
Grant
Filed:
August 9, 1995
Date of Patent:
March 16, 1999
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael Jerome Bienkowski, Vincent Edward Groppi, Jr.
Abstract: This invention comprises a scintillation proximity assay designed to assay for the presence of N-acetylgalactosaminyltransferase, also known as GalNAc-transferase. The assay is most conveniently carried out on 96-well microtiterplates. The assay is especially suitable for large volume screens for compounds affecting GalNAc-transferase activity.
Abstract: This invention describes the isolation and identification of a new protein, p56, useful for the identification of drugs that will selectively open or close K channels. The protein p56 has a molecular weight of about 56,000 daltons and the N-terminal peptide sequence is: Glu-Pro-Arg-Ala-Pro-Pro-Glu-Lys-Ile-Ala-Ile-Val-Gly-Ala-Gly-Ile.
Type:
Grant
Filed:
November 17, 1994
Date of Patent:
January 5, 1999
Assignee:
Pharmacia & Upjohn Company
Inventors:
Vincent E. Groppi, Jr., Martin R. Deibel, Jr., Mark L. Wolfe, Anthony W. Yem
Abstract: Provided are hybridomas for producing monoclonal antibodies against acetylated lysine residues of rbSt. The antibodies are specific to the presence of at least a single acetylated lysine in a protein and can differentiate between .alpha.-acetyl and .epsilon.-acetyl lysine as free amino acids.
Type:
Grant
Filed:
February 3, 1992
Date of Patent:
December 15, 1998
Assignee:
Pharmacia & Upjohn Company
Inventors:
Diane Marie Hamlin, Gustavus Adolphus Walker
Abstract: The present invention comprises human DNA compositions, including cDNA clones, with full sequences, called, KIRK-2 and KIRK-3, encoding proteins that confer potassium channel activity to membranes or recipient cell lines. The DNA compositions include structural genes coding for the potassium channel proteins, expression and replication plasmids or vectors containing the structural genes and host cells expressing those genes. Methods of screening compounds for potassium channel modulating activity are also described.
Abstract: This invention comprises novel compounds that inhibit the growth of helminths. The compounds have the structure of Formula I, below. ##STR1## Where the R groups are defined according to the specification and claims.
Type:
Grant
Filed:
September 5, 1996
Date of Patent:
July 7, 1998
Assignee:
Pharmacia & Upjohn Company
Inventors:
Byung H. Lee, Pil H. Lee, William W. McWhorter, Jr., Fred E. Dutton
Abstract: This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in FIG. BG.sub.4-1, where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, -(C.sub.1 -C.sub.8)alkyl, -(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.6 -C.sub.12 aryl), -(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, halogen, trifluoromethyl; where R.sup.2 is -(C.sub.1 -C.sub.8)alkyl, -(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.6 -C.sub.12 aryl), -(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.
Type:
Grant
Filed:
November 1, 1995
Date of Patent:
June 30, 1998
Assignee:
Pharmacia & Upjohn Company
Inventors:
William W. McWhorter, Thomas J. Fleck, Bruce A. Pearlman
Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
Type:
Grant
Filed:
May 20, 1994
Date of Patent:
April 15, 1997
Assignee:
The Upjohn Company
Inventors:
Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, Vera M. Wallach, legal representative
Abstract: This invention comprises novel compounds that are useful and effective as photoaffinity probes useful for the identification of the biochemical components that form K.sub.ATP channels in smooth muscle cells. The probes are described by the formula below, ##STR1## where R.sub.1 is H, C.sub.1-3 alkyl; R.sub.2 is H, C.sub.1-3 alkyl; orR.sub.1 and R.sub.2 may be joined together to form C.sub.3-6 cycloalkyl, or C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl;R.sub.3 is C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with 1-3 Halogens; or suitable salts thereof.
Type:
Grant
Filed:
June 10, 1994
Date of Patent:
June 11, 1996
Assignee:
The Upjohn Company
Inventors:
Robert C. Gadwood, Vincent E. Groppi, Jr.
Abstract: A quinolone compound of Formula (I) ##STR1## as defined herein having antibacteria properties, pharmaceutical compositions containing the quinoline compound and method for treating bacterial infections in animals including humans.
Type:
Grant
Filed:
July 20, 1993
Date of Patent:
January 31, 1995
Assignee:
The Upjohn Company
Inventors:
Ronald B. Gammill, Sharon N. Bisaha, Joseph M. Timko, Thomas M. Judge, Michael R. Barbachyn, Kyoung S. Kim
Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
Type:
Grant
Filed:
September 23, 1993
Date of Patent:
December 13, 1994
Assignee:
The Upjohn Company
Inventors:
Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
Abstract: The present invention relates to the use of taxol dependent cells, e.g. Tax 2-4 CHO cell line, as the basis of a screen for taxol or taxol-like compounds.
Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
Type:
Grant
Filed:
November 16, 1992
Date of Patent:
August 2, 1994
Assignee:
The Upjohn Company
Inventors:
Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.
Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
Type:
Grant
Filed:
November 6, 1992
Date of Patent:
December 28, 1993
Assignee:
The Upjohn Company
Inventors:
Gordon L. Bundy, Donald P. Wallach, deceased
Abstract: A quinolone compound of Formula (I) ##STR1## as defined herein having antibacteria properties, pharmaceutical compositions containing the quinoline compound and method for treating bacterial infections in animals including humans.
Type:
Grant
Filed:
June 3, 1991
Date of Patent:
November 16, 1993
Assignee:
The Upjohn Company
Inventors:
Ronald B. Gammill, Sharon N. Bisaha, Joseph M. Timko, Thomas M. Judge, Michael R. Barbachyn, Kyoung S. Kim
Abstract: The present invention provides an inactivated encephalomyocarditis virus (EMCV) vaccine produced from swine isolates which protects swine from diseases caused by EMCV. The vaccine is produced from swine isolates and protects against respiratory problems, myocardial and pulmonary inflammation and necrosis, and confers protection against reproductive disorders resulting from some strains of the virus.