Abstract: This invention relates to the enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one, prodrugs thereof, and pharmaceutically acceptable salts and solvates of said compounds and said prodrugs, that are useful in the treatment of hyperproliferative diseases, such as cancers, in mammals. The invention also relates to processes for the production of enantiomerically pure or optically enriched (+)- or (−)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one enantiomers from a mixture containing two enantiomers using continuous chromatography.
Type:
Application
Filed:
April 14, 2004
Publication date:
September 30, 2004
Applicant:
Pfizer Inc.
Inventors:
R. Mark Guinn, Subramanian Sam Guhan, Karl K. Ng, Derek L. Tickner, Marcus Douglas Ewing, Clifford N. Meltz, Bryan Li, Kees Pouwer
Abstract: The invention provides new methods for treating certain disorders resulting from neurodegeneration and for treating depression which comprise administration of NR2B subunit selective NMDA antagonists. The disorders that can be treating by the invention include hearing loss, vision loss, neurodegeneration caused by epileptic seizures, neurotoxin poisoning, Restless Leg Syndrome, multi-system atrophy, non-vascular headache, and depression.
Type:
Application
Filed:
April 9, 2004
Publication date:
September 30, 2004
Applicants:
Pfizer, Inc., Pfizer Products, Inc.
Inventors:
Bertrand L. Chenard, Frank S. Menniti, Mario D. Saltarelli
Abstract: The invention is directed generally to the structure of prenyltransferases, particularly undecaprenyl pyrophosphate synthase, an enzyme important in bacterial cell wall synthesis. The invention relates to the crystal structure of undecaprenyl pyrophosphate synthase from Streptococcus pneumoniae and its interaction with cofactors and ligands. The invention also relates to the structure of ligand and cofactor binding sites of undecaprenyl pyrophosphate synthase.
Type:
Application
Filed:
March 31, 2004
Publication date:
September 30, 2004
Applicant:
Pfizer Inc
Inventors:
Kimberly F. Fennell, Mahmoud N. Mansour, Xiayang Qiu
Abstract: A long-acting antiparasitic formulation suitable for topical application including:
(a) 0.1-50% w/v an avermectin or milbemycin having activity against endo- and/or ectoparasites;
(b) 1-50% v/v a di(C2-4 glycol) mono(C1-4 alkyl) ether;
(c) an optional antioxidant; and
(d) an optional skin acceptable volatile solvent q.s. v/v.
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
September 28, 2004
Assignee:
Pfizer Inc.
Inventors:
Timothy Michael Lukas, Stephen Richard Wicks
Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.
Type:
Grant
Filed:
March 12, 2003
Date of Patent:
September 28, 2004
Assignee:
Pfizer Inc.
Inventors:
Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, William T. Gattrell, Joanna V. Geden, Peter J. Murray, Martin J. Procter, Robert J. Rowley, Jonathan G. Williams
Abstract: The use of a PDE5 inhibitor without substantial PDE2 inhibiting activity, or a pharmaceutically acceptable salt thereof in the preparation of a medicament for the treatment of Type 1 Diabetes. A method of treating Type 1 Diabetes in an individual suffering from Type 1 Diabetes, which method comprises administering to said individual an effective amount of a PDE5 inhibitor without substantial PDE2 inhibiting activity, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
March 12, 2004
Publication date:
September 23, 2004
Applicant:
Pfizer Inc
Inventors:
Gillian Munro Burgess, Earl Michael Gibbs, Christopher Peter Wayman
Abstract: A dosage form comprises (1) a solid amorphous dispersion comprising a cholesteryl ester transfer protein inhibitor and a neutral or neutralized acidic polymer and (2) an HMG-CoA reductase inhibitor. The dosage form provides improved chemical stability of the HMG-CoA reductase inhibitor.
Type:
Application
Filed:
December 18, 2003
Publication date:
September 23, 2004
Applicant:
Pfizer Inc
Inventors:
Dwayne T. Friesen, David K. Lyon, Douglas A. Lorenz, Rodney J. Ketner, Bruno C. Hancock, Timothy J. McDermott, Ravi M. Shanker
Abstract: Compounds of general formula (I):
wherein R1, R2, R3, R4, X, Y and A have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
Type:
Grant
Filed:
March 14, 2002
Date of Patent:
September 21, 2004
Assignee:
Pfizer Inc.
Inventors:
Charlotte Moira Norfor Allerton, Kevin Neil Dack, Mark Ian Kemp
Abstract: The present invention relates to an isolated target sequence. The target sequence is a splice variant of PDE5 called a PDE5a1, a component of which is presented as SEQ ID No 1. The identified target sequence of the present invention may be used to as a target to identify agents (such as modulators) useful in the prevention and/or treatment of a disease associated with scarring and/or fibrosis or to selectively identify smooth muscle cells and myofibroblasts and myoepithelial cells in samples of normal and diseased tissue from individuals.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
September 21, 2004
Assignee:
Pfizer Inc.
Inventors:
Dinah Parums, Stephen Charles Phillips, John Ridden
Abstract: The present invention is directed to the succinate salts of 5,7,13-triazatetracyclo[9.3.1.02,10.04,8]-pentadeca-2(10),3,5,8-tetraene
and pharmaceutical compositions thereof. The invention is also directed to a process for preparation of the succinate salts.
Abstract: An efficient synthesis of sulfonyl pyrazoles of formula I:
wherein the ring of the formula (R5)-A-(SOmR4), m, R1 through R9 are as defined in the specification, comprising reacting a compound of formula II:
wherein the ring of the formula (R5)-A-(SOmR4), m R1 through R9 are as defined above and wherein R10 is halo, (C1-C6)alkyl-SO3—, (C6-C10)aryl-SO3—, (C1-C6)alkyl-SO2—, or (C6-C10)aryl-SO2—; wherein each of said (C1-C6)alkyl component of said (C1-C6)alkyl-SO3— and (C1-C6)alkyl-SO2— radicals may optionally be substituted on any carbon atom by one to six fluoro substituents per (C1-C6)alkyl component; with a compound of formula R3—H, wherein R3 is as defined above, in the presence of a fluoride containing salt and in the presence of a solvent.
Type:
Grant
Filed:
November 1, 2002
Date of Patent:
September 21, 2004
Assignee:
Pfizer, Inc.
Inventors:
Andrei Shavnya, Subas M. Sayka, Martha L. Minich, Bryson Rast
Abstract: The invention relates to inhibitors of neutral endopeptidase enzyme (NEP), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of male and female sexual dysfunction, particularly female sexual dysfunction (FSD), especially wherein the FSD is female sexual arousal disorder (FSAD).
Abstract: Novel pyrazine compounds, including derivatives thereof, to intermediates for their preparation, 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, cancer and fibrotic diseases.
Abstract: The invention provides compounds of formula I,
R1—OP(O)(OH)2 I
wherein R1 represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceutically acceptable salt thereof.
The compounds of the invention are useful in the treatment of fungal infections, and have good aqueous solubility.
Type:
Grant
Filed:
January 9, 2003
Date of Patent:
September 14, 2004
Assignee:
Pfizer, Inc.
Inventors:
Stuart Green, Peter T. Stephenson, Charles W. Murtiashaw
Abstract: A material for packaging a nicotine product comprising a polymer based on dimethyl-2,6-naphthalene dicarboxylic or 2,6-naphthalene dicarboxylic acid monomers, such as polyethylene naphtalate (PEN) or polytrimethylene naphtalate (PTN), or a liquid crystal polymer (LPC). The material may be laminated to another polymer or to metal foil.
Type:
Grant
Filed:
October 17, 2001
Date of Patent:
September 14, 2004
Assignee:
Pfizer Health AB
Inventors:
Gustav Levander, Anders H. F. Karlsson, Ingemar Hildingsson