Patents Assigned to Upjohn
  • Arylsulphonyl substituted-tetrahydro-and hexahydro-carbazoles
    Publication number: 20040162332
    Abstract: The invention provides compounds of formula I for use in treating conditions in which 5-HT6 receptors are involved such as in anxiety, depression, schizophrenia, Alzheimer's disease, stress-related disease, panic, a phobia, obsessive compulsive disorder, obesity, post-traumatic stress syndrome, epilepsy, and other CNS disorders.
    Type: Application
    Filed: February 12, 2004
    Publication date: August 19, 2004
    Applicant: Pharmacia & Upjohn Company
    Inventor: Jian-Min Fu
  • Therapeutic 5-HT ligand compounds
    Publication number: 20040157831
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Applicant: Pharmacia & Upjohn Company
    Inventor: William W. McWhorter
  • Method for the preparation of oxazolidinones
    Patent number: 6774231
    Abstract: The present invention relates to a process for making a compound of structure 4 which comprises reacting a compound of structure 1 with vinyl sulfone in the presence of a Lewis-acid at a temperature in a range of from 40° C. to 170° C., wherein each R1 is independently H, fluoro, chloro or bromo.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: August 10, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Jiong Jack Chen, Cuong V. Lu
  • Method of treating or preventing peripheral neuropathy with a highly selective norepinephrine reuptake inhibitor
    Publication number: 20040147614
    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: January 16, 2004
    Publication date: July 29, 2004
    Applicant: PHARMACIA & UPJOHN COMPANY
    Inventors: Erik H.F. Wong, Saeeduddin Ahmed, Robert Clyde Marshall, Robert McArthur, Duncan P. Taylor
  • Novel component in the hedgehog signalling pathway
    Publication number: 20040146929
    Abstract: The present invention relates to a novel human patched-like gene (PTCH2), which for the first time has been cloned and sequenced. Several alternatively spliced mRNA forms of PTCH2 have been identified, including transcripts lacking segments thought to be involved in sonic hedgehog (SHH) binding and mRNAs with differentially defined 3′ terminal exons. Further, the invention also relates to the protein encoded by the present PTCH2 as well as to functional analogues and variants thereof.
    Type: Application
    Filed: March 4, 2004
    Publication date: July 29, 2004
    Applicant: Karolinska Innovations AB and Pharmacia & Upjohn Company
    Inventors: Peter G. Zaphiropoulos, Anne Birgitte Unden, Rune Toftgard, Fahimeh Rahnama, Robert E. Hollingsworth
  • Angiogenesis related molecules
    Publication number: 20040141978
    Abstract: The present invention provides the sequence of a protein capable of acting as an angiostatin receptor as well as the nucleic acid sequence thereof. The invention also relates to the use thereof in screening methods, wherein novel substances are created exhibiting the same advantageous anti-angiogenic properties as angiostatin.
    Type: Application
    Filed: November 25, 2003
    Publication date: July 22, 2004
    Applicant: PHARMACIA & UPJOHN AB
    Inventors: Lars Holmgren, Boris Troyanovsky
  • Methods of producing oxazolidinone compounds
    Publication number: 20040143131
    Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.
    Type: Application
    Filed: December 23, 2003
    Publication date: July 22, 2004
    Applicant: PHARMACIA & UPJOHN COMPANY
    Inventors: William R. Perrault, Robert C. Gadwood
  • Antimicrobial methods and materials
    Patent number: 6764823
    Abstract: The present invention provides methods of identifying antimicrobial agents that target genes essential for the survival of Staphylococcus bacteria, including antimicrobial agents that interfere with the expression of essential coding sequence products and antimicrobial agents that interfere with the function of essential coding sequence products.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: July 20, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Che-Shen C. Tomichi, Cheryl Quinn, Staffan Arvidson
  • Methods for creating a compound library
    Patent number: 6764858
    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.
    Type: Grant
    Filed: November 19, 2001
    Date of Patent: July 20, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventor: Brian J. Stockman
  • Tetracyclic azepinoindole compounds
    Publication number: 20040138202
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: December 23, 2003
    Publication date: July 15, 2004
    Applicant: Pharmacia and Upjohn Company
    Inventors: Jackson B. Hester, Bruce N. Rogers, Eric Jon Jacobsen, Michael D. Ennis, Brad A. Acker, Susan L. Vander Velde, Kristine E. Frank
  • Therapeutic compounds
    Patent number: 6762191
    Abstract: The present invention provides compounds of formula (I): wherein: R1, R2, R3 R4, R5, R6, X, - - - , m, and n have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts thereof. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I). The compounds are useful as 5-HT ligands.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: July 13, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: William W. McWhorter, Jr., Valentina Badescu
  • 1-(Pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
    Publication number: 20040127542
    Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-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: Application
    Filed: May 5, 2003
    Publication date: July 1, 2004
    Applicant: Pharmacia & Upjohn Co.
    Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao
  • Mannich base prodrugs of 3-(Pyrrol-2-yl-methylidene)-2-indolinone derivatives
    Publication number: 20040127544
    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: Application
    Filed: December 24, 2003
    Publication date: July 1, 2004
    Applicants: Sugen, Inc., Pharmacia & Upjohn Company
    Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
  • Chemical structure identification
    Patent number: 6757618
    Abstract: A method for generating a numeric or alpha-numeric identifier representative of a chemical structure having at least two atoms connected by a bond includes the step of assigning a numerical value to each atom and a numerical bond value to each bond. The method updates the numerical values for each atom based on the current values assigned to each atom and the numerical bond value. After the numerical values for each atom have been updated the method calculates a numeric or alpha-numeric identifier for the chemical structure.
    Type: Grant
    Filed: May 9, 2001
    Date of Patent: June 29, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mark A. Johnson, Yong-jin Xu
  • Alzheimer's disease secretase, APP substrates therefor, and uses therefor
    Patent number: 6753163
    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: February 28, 2001
    Date of Patent: June 22, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
  • Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
    Patent number: 6753316
    Abstract: Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1 and R2, which are the same or different, are selected from hydrogen, halogen, and C1-C4 alkyl; R3 is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and —C≡N; wherein R4, R5, R6, R7, R8, R10, R11, and R12 are, independently from each other, hydrogen or C1-C4 alkyl; and R9 is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R4, R5 and R6 is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: June 22, 2004
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Paolo Cozzi, Pier Giovanni Baraldi, Italo Beria, Marina Caldarelli, Laura Capolongo, Romeo Romagnoli
  • Substituted benzoxazines as integrin antagonists
    Patent number: 6750215
    Abstract: The present invention relates to a class of compounds represented by the formula (I) or a pharmaceutical acceptable salt, prodrug or ester thereof, pharmaceutical compositions comprising compounds of the formula (I), and methods of selectively inhibiting or antagonizing &agr;v&bgr;3 integrin.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: June 15, 2004
    Assignee: Pharmacia & Upjohn, S.p.A.
    Inventors: Paola Vianello, Tiziano Bandiera
  • Oxazalidinone compounds and methods of preparation and use thereof
    Patent number: 6743811
    Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: June 1, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
  • 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
    Publication number: 20040102510
    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: September 8, 2003
    Publication date: May 27, 2004
    Applicants: SUGEN, INC., PHARMACIA & UPJOHN COMPANY
    Inventors: Huiping Guan, Congxin Liang, Connie Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu Jin, Paul M. Herrinton, Michael A. Mauragis
  • Process to produce oxazolidinones
    Patent number: 6740754
    Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C*H(OH)—CH2—NH—CO—RN  (VIIIA) and processes for production of pharmacologically useful oxazolidinones.
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: May 25, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventor: Bruce Allen Pearlman