Patents Assigned to Upjohn
  • Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
    Patent number: 6716870
    Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: April 6, 2004
    Assignees: Sugen, Inc., Pharmacia & Upjohn Company
    Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
  • Pyrrole substituted 2-indolinone protein kinase inhibitors
    Publication number: 20040063773
    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: Application
    Filed: April 14, 2003
    Publication date: April 1, 2004
    Applicant: SUGEN, Inc. & Pharmacia & Upjohn Co.
    Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Thomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
  • Methods of identifying compounds that bind to target species under isothermal denaturing conditions
    Patent number: 6713260
    Abstract: The present invention provides a method for identifying a test compound that binds to a target species. The method includes: incubating at least one test mixture under isothermal denaturing conditions, each test mixture comprising at least one test compound, and at least one target species, wherein the isothermal denaturing conditions are effective to cause at least a portion of the target species to denature to a measurable extent; detecting a denaturation signal of each target species in the presence of the at least one test compound by a change in the diffusion properties of the target molecule using fluorescence correlation spectroscopy; and comparing the denaturation signal of each target species in the presence of at least one test compound with a denaturation signal of the same target species in the absence of the at least one test compound under the same isothermal denaturing conditions.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: March 30, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Paul K. Tomich, Dennis E. Epps, Ferenc J. Kezdy, Charles K. Marschke, Ronald W. Sarver
  • Method of treating fibromyalgia and other somatoform disorders
    Publication number: 20040058925
    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: Application
    Filed: September 24, 2003
    Publication date: March 25, 2004
    Applicant: PHARMACIA & UPJOHN COMPANY
    Inventors: Erik H.F. Wong, Saeeduddin Ahmed, Robert Clyde Marshall, Robert McArthur, Duncan P. Taylor
  • Mannich base prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
    Patent number: 6710067
    Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: March 23, 2004
    Assignees: Sugen Incorporated, Pharmacia & UpJohn Company
    Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
  • Method of identifying agents that inhibit APP processing activity
    Patent number: 6706485
    Abstract: The present invention provides methods of identifying agents that inhibit the amyloid precursor protein (APP) processing activity of Asp2 polypeptide.
    Type: Grant
    Filed: April 12, 2000
    Date of Patent: March 16, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
  • Method of treating chronic pain
    Patent number: 6703389
    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: December 14, 2001
    Date of Patent: March 9, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson, Pasquale Cetera
  • Aqueous prolonged release formulation
    Patent number: 6699490
    Abstract: Prolonged parenteral release into the circulatory system of a cow of a bioactive bovine somatotropin at desirably effective levels can be achieved using novel compositions in which the bovine somatotropin is present in an aqueous liquid at a dose of at least about 150 mg and at a concentration of at least about 50 mg/ml. The aqueous bovine somatotropin formulation provides for the sustained release of bovine somatotropin into the circulatory system of the animal for greater than three (3) days.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: March 2, 2004
    Assignee: The Upjohn Co.
    Inventors: Michael John Hageman, Margaret Luise Possert
  • Alzheimer's disease secretase, APP substrates therefor, and uses therefor
    Patent number: 6699671
    Abstract: The present invention provides the enzyme and enzymatic procedures for cleaving the &bgr; 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: October 13, 1999
    Date of Patent: March 2, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
  • Double mutant alpha-7 nicotinic acetylcholine receptor
    Patent number: 6693172
    Abstract: The invention relates to a novel methods for measuring cellular ion channel transmission and methods and compositions useful in the identification of ligand gated ion channel agonists and modulators.
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: February 17, 2004
    Assignee: Pharmacia and Upjohn Company
    Inventors: Vincent E. Groppi, Jr., Mark L. Wolfe, Mitchell B. Berkenpas
  • 4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxamides as antiviral agents
    Patent number: 6693114
    Abstract: A compound of formula III: or a pharmaceutically acceptable salt thereof wherein, the variables are as in the specification is provided. The compounds are particularly effective in the treatment or prevention of herpes viruses.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: February 17, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Valerie A. Vaillancourt, Atli Thorarensen
  • Process and intermediates to prepare latanoprost
    Patent number: 6689901
    Abstract: The present invention is a novel intermediate, compound of the formula (VI) and salts thereof. In addition, the invention includes a process for the preparation of a 15(S)-prostaglandin intermediates compounds (IV) and (XVIII) which comprises (1) contacting a the corresponding enone with (−)-chlorodiisopinocampheylborane while maintaining the reaction mixture temperature in the range of from about −50° to about 0° and (2) contacting the reaction mixture of step (1) with a boron complexing agent.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: February 10, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventor: Kevin E. Henegar
  • Crystallization and structure determination of Staphylococcus aureus thymidylate kinase
    Patent number: 6689595
    Abstract: An unliganded form of Staphylococcus aureus thymidylate kinase (S. aureus TMK) has been crystallized, and the three dimensional x-ray crystal structure has been solved to 2.3 Å resolution. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing inhibitors of S. aureus TMK activity.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: February 10, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventor: Timothy E. Benson
  • Antimicrobial quinolone derivatives and use of the same to treat bacterial infections
    Patent number: 6689769
    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: November 29, 2001
    Date of Patent: February 10, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
  • Ligand binding assay and kit with a separation zone for disturbing analytes
    Publication number: 20040023412
    Abstract: The invention relates to method for determining an analyte by means of binding reactions, which method comprises: i) applying the sample to an application zone for sample (ASZ) on a flow matrix in which transport of components present in the sample can take place (transport flow), the flow matrix further exhibiting: a) optionally an application zone (AR*Z) for a binding reactant (Reactant*=R*) which is analytically detectable; b) a detection zone (DZ), which is located downstream of ASZ and exhibits an additional binding reactant (Capturer) firmly anchored to the matrix, and in which a complex (signal complex) containing the Capturer and the analyte and/or Reactant* is formed during the reaction, and ii) detecting the signal complex in the detection zone, the measured signal being used for determining the analyte.
    Type: Application
    Filed: August 5, 2003
    Publication date: February 5, 2004
    Applicant: Pharmacia & Upjohn Diagnostics AB.
    Inventors: Jan Carlsson, Maria Lonnberg
  • Inhibitors of &agr;4&bgr;1 mediated cell adhesion
    Patent number: 6685617
    Abstract: The present invention relates to compound of formula (I), that are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: February 3, 2004
    Assignees: Pharmacia & Upjohn Company, Tanabe Seiyaku Co., Ltd.
    Inventors: James Blinn, Robert Chrusciel, Jed Fisher, Steven Tanis, Edward Thomas, Thomas Lobl, Bradley Teegarden
  • Mutant presenilin 1 polypeptides
    Patent number: 6686449
    Abstract: The present invention provides mutant presenilin 1 and presenilin 2 polpeptides and polynucleotides encoding the polypeptides and methods for their production by recombinant and PCR techniques are disclosed. Methods for utilizing the mutant polypeptides in screens for inhibitors of activity are also disclosed.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: February 3, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Donald Bainbridge Carter, Alfredo Giuseppe Tomasselli
  • Pyridoquinoxaline antivirals
    Patent number: 6686356
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein R1 and R2 are as defined in the specification. The compounds are useful for the treatment of viral infections.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: February 3, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Joseph Walter Strohbach, Steven P. Tanis, Malcolm Wilson Moon
  • Method for discovering substances for inhibiting enzymes
    Publication number: 20040018581
    Abstract: This invention describes novel methods for the identification of compounds useful as inhibitors of enzymes. The methods involve obtaining a target gene-complemented microorganism which is dependent on the expression of the target gene for survival in test conditions. By measuring the viability of the complemented microorganism after exposure to a compound, compounds that inhibit growth in test conditions are identified. These compounds that inhibit growth are further tested in conditions where the expression of the target gene is not required for growth in order to identify compounds that specifically inhibit the target gene but do not effect the viability of the host.
    Type: Application
    Filed: July 24, 2002
    Publication date: January 29, 2004
    Applicant: Pharmacia and UpJohn Company
    Inventors: Timothy Geary, Margaret Favreau
  • Heterocyclic amines having central nervous system activity
    Patent number: RE38452
    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 pyrrolidine, 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.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: March 2, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventor: Arthur Glenn Romero