Abstract: Disclosed are compounds of formula I: and the pharmaceutically acceptable salts thereof wherein the variables RN, R1, R2, R3, RP and RC are defined herein. These compounds are 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:
October 4, 2002
Date of Patent:
July 17, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Jed F. Fisher, Jon S. Jacobs, Brian Sherer
Abstract: Disclosed herein are methods of treating an individual suffering from peripheral neuropathy. The methods generally include administration of a therapeutic amount of racemic reboxetine, or a pharmaceutically acceptable salt thereof, to the individual.
Type:
Grant
Filed:
February 7, 2006
Date of Patent:
July 10, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor
Abstract: The present invention relates to a novel cytochrome P450-like enzyme (Aspergillus ochraceus 11 alpha hydroxylase) and an oxidoreductase (Aspergillus ochraceus oxidoreductase) isolated from cDNA library generated from the mRNA of Aspergillus ochraceus spores. When the cDNA encoding the 11 alpha hydroxylase was co-expressed in Spodoptera frugiperda (Sf-9) insect cells with the cDNA encoding human oxidoreductase as an electron donor, it successfully catalyzed the conversion of the steroid substrate 4-androstene-3,17-dione (AD) to 11 alpha-hydroxy-AD as determined by HPLC analysis. The invention also relates to nucleic acid molecules associated with or derived from these cDNAs including complements, homologues and fragments thereof, and methods of using these nucleic acid molecules, to generate, for example, polypeptides and fragments thereof. The invention also relates to the generation of antibodies that recognizes the A.
Type:
Grant
Filed:
July 28, 2004
Date of Patent:
July 3, 2007
Assignee:
Pharmacia Corporation
Inventors:
Suzanne L. Bolten, Robert A. Clayton, Alan M. Easton, Leslie C. Engel, Dean M. Messing, John S. Ng, Beverly Reitz, Mark C. Walker, Ping T. Wang
Abstract: This patent application describes the treatment of Addictive disorders, Psychoactive Substance Use disorders, Intoxication disorders, Inhalation disorders, Alcohol addiction, Tobacco addiction and or Nicotine addiction; and Attention Deficit Hyperactivity Disorder (ADHD); comprising administering a therapeutically effective, nontoxic dose of Reboxetine and derivatives and or pharmaceutically acceptable salts thereof to a patient.
Type:
Application
Filed:
February 15, 2007
Publication date:
June 28, 2007
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Fred Hassan, John McCall, Duncan Taylor, Philip Von Voigtlander, Erik Ho Fong Wong
Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
Abstract: Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5 and R6 are as defined in the specification or a pharmaceutically acceptable salt or solvate thereof, compositions thereof, and methods of use thereof.
Type:
Application
Filed:
December 19, 2005
Publication date:
June 21, 2007
Applicant:
Pharmacia Italia S.p.A.
Inventors:
Ermes Vanotti, Barbara Forte, Katia Martina, Maria Menichincheri, Alessandra Cirla, Paolo Orsini
Abstract: Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Type:
Application
Filed:
December 16, 2005
Publication date:
June 21, 2007
Applicant:
Pharmacia Italia S.p.A.
Inventors:
Ermes Vanotti, Maria Menichincheri, Paolo Orsini, Alessandra Scolaro, Mario Varasi
Abstract: Methods for the production of recombinant peptides comprise fermenting cells to produce recombinant peptides. A metal salt is added to a concentrate of the fermented cells after the fermentation step, prior to peptide isolation, and the pH of the cell concentrate after the addition of the metal salt is less than or equal to 7, thereby reducing the amount of trifulsides formed in the production of the recombinant peptide, with the proviso that the production does not include conversion of formed trifulside peptide into native peptide form after the addition of the metal salt. In one embodiment, the recombinant peptide is recombinant growth hormone.
Type:
Grant
Filed:
July 5, 1999
Date of Patent:
June 19, 2007
Assignee:
Pharmacia AB
Inventors:
Barbro Hemmendorff, Andreas Castan, Anders Persson
Abstract: A process for preparing (S)-(?)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide (I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.
Type:
Grant
Filed:
February 28, 2005
Date of Patent:
June 19, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Sonja Suzanne MacKey, Michael E. Matison, Haifeng Wu, Michael Paul Goble, Moses W. McMillan, Vikram Gurudath Kalthod
Abstract: The invention relates to treatment of patients in need of increasing insulin sensitivity by administration of growth hormone or analogues thereof, preferably human growth hormone, in a low dose and the use of growth hormone or analogues thereof, preferably human growth hormone, for the manufacturing of a medicament useful for increasing insulin sensitivity in low dose therapy. The patient is preferably a normal subject, i.e. not growth hormone deficient patient and/or a non-obese patients. By low dose therapy is preferably meant less than 0.008 mg/kg/day, preferably 0.007 mg/kg/day or less, more preferably 0.005 mg/kg/day or less and most preferably 0.003 mg/kg/day or less. The therapy is preferably performed during short term treatment, preferably less than one month.
Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory drug of low water solubility, for example celecoxib, in an immediate-release fraction and a controlled-release, slow-release, programmed-release, timed-release, pulse-release, sustained-release or extended-release fraction. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.
Type:
Grant
Filed:
December 20, 2000
Date of Patent:
May 22, 2007
Assignee:
Pharmacia Corporation (of Pfizer, Inc.)
Inventors:
Subhash Desai, Sreekant R. Nadkarni, Randy J. Wald, Gary A. DeBrincat
Abstract: The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention.
Type:
Grant
Filed:
July 26, 2005
Date of Patent:
May 22, 2007
Assignee:
Pharmacia Corporation (of Pfizer, Inc.)
Inventors:
Michael J. Hageman, Xiaorong He, Tugrul T. Kararli, Lesley A. MacKin, Patricia J. Miyake, Brian R. Rohrs, Kevin J. Stefanski
Abstract: The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell proliferation or to disregulated protein kinase.
Type:
Application
Filed:
November 11, 2005
Publication date:
May 17, 2007
Applicant:
Pharmacia Italia S.p.A.
Inventors:
Ermes Vanotti, Francesco Angelucci, Alberto Bargiotti, Maria Brasca, Antonella Ermoli, Maria Menichincheri
Abstract: The present invention is substituted amines of formula (X) and of the formula (X?) useful in treating Alzheimer's disease and other similar diseases.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
May 8, 2007
Assignees:
Pharmacia & Upjohn, Elan Pharmaceuticals
Inventors:
James P. Beck, Lawrence Y. Fang, John N. Freskos, Andrea Gailunas, Roy Hom, Barbara Jagodzinska, Varghese John, Michel Maillard, Shon R. Pulley, Ruth E. TenBrink
Abstract: The invention includes selected novel optically active ?-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.
Abstract: The invention provides neuropeptide ligands, G protein-coupled receptors and methods of screening for modulators of receptor activity. Identified modulators, including neuropeptide ligand mimetics, are useful as biostatic and biocidal agents of varying scope, ranging from lethal activity restricted to particular invertebrate parasites to broad spectrum invertebrate parasiticides active on a wide range of invertebrates, including helminths and insects.
Type:
Grant
Filed:
August 28, 2003
Date of Patent:
April 24, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
David E. Lowery, Timothy G. Geary, Teresa M. Kubiak, Martha J. Larsen
Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens
Type:
Grant
Filed:
October 2, 2003
Date of Patent:
April 24, 2007
Assignee:
Pharmacia & Upjohn Company LLC
Inventors:
Michael Robert Barbachyn, Gordan L. Bundy, Paul Joseph Dobrowolski, Alexander Ross Hurd, Gary E. Martin, Dennis Joseph McNamara, John Raymond Palmer, Donna L. Romero, Arthur Glenn Romero, J. Craig Ruble, Debra Ann Sherry, Lisa Marie Thomasco, Peter Laurence Toogood
Abstract: The present invention is directed to novel substrates for Hu-Asp. More particularly, the invention provides peptide substrates and fusion polypeptide substrates comprising a ?-secretase cleavage site. Methods and compositions for making and using the peptides are disclosed.
Type:
Grant
Filed:
July 19, 2001
Date of Patent:
April 17, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Riqiang Yan, Alfredo G. Tomasselli, Mark E. Gurney, Thomas L. Emmons, Michael Jerome Bienkowski, Robert L. Heinrikson
Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
Type:
Grant
Filed:
January 10, 2005
Date of Patent:
March 27, 2007
Assignee:
Pharmacia Corporation
Inventors:
Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymbalov, Foe Siong Tjoeng
Abstract: The present invention relates to a process for purifying a hydrophobic or amphiphilic compound, by first mixing a starting material containing the hydrophobic or amphiphilic compound with a first polymeric material, water and at least one of a second polymeric material and a surfactant, wherein the first polymeric material and the second polymeric material and/or surfactant are immiscible in the resulting primary aqueous solution. The process further comprises maintaining the primary aqueous solution for a period of time sufficient for essentially separating the phases formed, and then removing the phase containing the main portion of the hydrophobic or amphiphilic compound and the second polymeric material and/or surfactant. The second polymeric material and/or surfactant are separated from the hydrophobic or amphiphilic compound, and subsequently recycled to the initial mixing step.
Type:
Grant
Filed:
June 8, 2004
Date of Patent:
March 20, 2007
Assignee:
Pharmacia & UpJohn AB
Inventors:
Hans Ageland, Lena Nyström, Josefine Persson, Folke Tjerneld