Abstract: Novel isothiazole compounds, including derivatives thereof, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, hyperproliferative disorders and fibrotic diseases.
Abstract: The present invention relates to attenuated forms of bovine viral diarrhea (BVD) viruses. In particular, the present invention relates to attenuated BVD viruses made by mutating the Npro protease gene and inserting a bovine ubiquitin coding sequence. The attenuated viruses of the present invention can be used to raise antibodies against BVDV. Immunogenic compositions and vaccine compositions, as well as therapeutic and diagnosis methods, are also provided by the present invention.
Abstract: A pharmaceutical kit for preparing an injectable depot formulation of an aryl-heterocyclic pharmaceutical compound, such as ziprasidone, and a method of preparing said depot formulation is disclosed.
Abstract: The invention provides methods for inhibiting oxidative degradation of pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient which methods comprise adding an oxidation-inhibiting amount of a ferrous ion source, preferably in the form of a pharmaceutical excipient, to the formulation.
The invention further provides pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient and an oxidation-inhibiting amount of a ferrous iron source, preferably in the form of a pharmaceutical excipient.
The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.
Abstract: Aqueous solubility of drugs including insoluble or poorly soluble drugs such as ziprasidone is improved using a functional polymer to form an ionic conjugate with said drug.
Type:
Application
Filed:
October 24, 2003
Publication date:
July 22, 2004
Applicant:
Pfizer Inc
Inventors:
Shalaby W. Shalaby, Jaymin C. Shah, Joel T. Corbett
Abstract: The present invention relates to novel crystalline forms of 3-isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine to pharmaceutical compositions containing such crystal forms and to methods of treatment. 3-Isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine is a potent inhibitor of MAP kinases, preferably p38 kinase (MAPK14/CSBP/RK kinase). 3-Isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine is useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Type:
Application
Filed:
August 27, 2003
Publication date:
July 22, 2004
Applicant:
Pfizer Inc
Inventors:
Ming Kang, Zheng Jane Li, Zhengong Bryan Li, Yong Tao
Abstract: The instant invention relates to the use of an alpha-2-delta ligand in the treatment of chronic obstructive pulmonary disease (COPD) and diseases associated with a diagnosis of COPD, and particularly to the treatment of chronic cough, which may be unrelated to COPD.
Type:
Application
Filed:
December 12, 2003
Publication date:
July 22, 2004
Applicant:
Pfizer Inc
Inventors:
Claude Philippe Bertrand, Maria Emilia Pereira Chicau Chovet, Pierangelo Geppetti, Charles Price Taylor, Andrew John Thorpe, David Juergen Wustrow
Abstract: The compounds of the formula
wherein R1, R2, R3, R4, R5 and R6 are as defined herein, are useful in the treatment of stress-related and other diseases. These compounds have corticotropin-releasing factor antagonist activity and as such are of use in the treatment of stress and anxiety related, and other disorders.
Abstract: The invention provides methods of protecting solid-state proteins from the effects of ionizing radiation which comprise combining the protein with a radiation-protecting amount of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde; radiation-protecting amounts of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde, and 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid; or radiation-protecting amounts of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde and isopropanol, prior to exposing the protein to ionizing radiation.
Type:
Grant
Filed:
March 12, 2001
Date of Patent:
July 20, 2004
Assignee:
Pfizer Inc.
Inventors:
Evgenyi Y. Shalaev, Renuka D. Reddy, Roger N. Kimball
Abstract: The present invention is directed to a novel strain of feline immunodeficiency virus, designated herein as FIV-141, and to attenuated forms of the virus produced by mutating specific regions of the viral genome. The virus and mutated forms of the virus may be used to induce the production of antibodies to FIV-141, and in vaccines designed to protect cats from FIV.
Abstract: Conventional spray-drying methods are improved by incorporation of a pressure nozzle and a diffuser plate to improve the flow of drying gas and a drying chamber extension to increase drying time, such improvements leading to the formation of homogeneous solid dispersions of drugs in concentration-enhancing polymers.
Type:
Grant
Filed:
January 28, 2003
Date of Patent:
July 20, 2004
Assignee:
Pfizer Inc.
Inventors:
Ronald A. Beyerinck, Heather L. M. Deibele, Dan E. Dobry, Roderick J. Ray, Dana M. Settell, Ken R. Spence
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
Type:
Grant
Filed:
May 23, 2002
Date of Patent:
July 20, 2004
Assignee:
Pfizer, Inc.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: Amino acid sequences and nucleotide sequences relating to PDE_XIV are described. In a preferred aspect, the amino acid sequences comprise the sequence presented as SEQ ID NO:1 or SEQ ID NO:3 or SEQ ID NO:5.
Abstract: The present invention provides a combination of (a) a histamine H1 receptor antagonist and (b) an antagonist that is at least 10-fold selective for the histamine H4 receptor as compared to the histamine H3 receptor; and an antagonist that is at least 10-fold selective for the histamine H4 receptor as compared to the histamine H3 receptor: and compositions and uses thereof.
Type:
Application
Filed:
December 16, 2003
Publication date:
July 15, 2004
Applicant:
Pfizer Inc
Inventors:
Stephen Jenkinson, Mark Anthony O'Reilly, Michael Andrew Trevethick
Abstract: An injectable depot formulation that is viscous, or becomes viscous in situ, comprising a solubilized aryl-heterocyclic pharmaceutical compound, such as ziprasidone, is provided.
Abstract: A process for preparing acyl derivatives as prodrugs of 5-(2-(4-(1,2 benzisothiazole-3-yl)-1-piperazinyl)ethyl-6-chloro-1,3-dihydro-2H-indol-2-one and pharmaceutically acceptable acid addition salts and methods of use as an antipsychotic.