Abstract: The invention provides a process for the optical resolution of a racemic mixture, or an optically enriched mixture, of trans-7-(hydroxymethyl)octa-hydro-2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(−) or L-(+)naproxen as a resolving agent.
Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a PDE IV inhibitor in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a PDE IV inhibitor and an anxiolytic agent or antidepressant.
Type:
Application
Filed:
March 12, 2003
Publication date:
December 25, 2003
Applicant:
Pfizer Inc.
Inventors:
Susan B. Sobolov-Jaynes, Christopher J. Schmidt
Abstract: This invention relates to methods of treating traumatic brain injury (TBI) or hypoxic or ischemic stroke, comprising administering to a patient in need of such treatment an NR2B subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist in combination with either: (a) a neutrophil inhibitory factor (NIF); (b) a sodium channel antagonist; (c) a nitric oxide synthase (NOS) inhibitor; (d) a glycine site antagonist; (e) a potassium channel opener; (f) an AMPA/kainate receptor antagonist; (g) a calcium channel antagonist; (h) a GABA-A receptor modulator (e.g., a GABA-A receptor agonist); or (i) an antiinflammatory agent.
Type:
Grant
Filed:
September 6, 2001
Date of Patent:
December 23, 2003
Assignee:
Pfizer Inc
Inventors:
Bertrand L. Chenard, Frank S. Menniti, Mario D. Saltarelli
Abstract: Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by adding one or more water-miscible co-solvents. In a preferred embodiment, the one or more co-solvents is propylene glycol.
Abstract: The present invention is directed to vaccine compositions that can be used to protect cats against feline immunodeficiency virus. More particularly, the present invention relates to polynucleotide molecules that can be used as vaccine components against feline immunodeficiency virus.
Abstract: There is provided a process for the production a compound of general formula I:
wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises the reaction of a compound of formula II,
wherein Rx is a group substitutable by an aminopyrazole, with a compound of general formula III
Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.
Type:
Grant
Filed:
June 12, 2002
Date of Patent:
December 23, 2003
Assignee:
Pfizer Inc
Inventors:
Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
Abstract: The present invention provides compounds of the formula:
wherein R1 is C3-6 cycloalkyl optionally substituted by one or more fluorine atoms, or C1-6 alkyl optionally substituted by one or more fluorine atoms, or C3-6 cycloalkylmethyl optionally ring-substituted by one or more fluorine atoms; and
R2 is phenyl optionally substituted by one or more fluorine atoms, to pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.
Type:
Grant
Filed:
May 25, 2001
Date of Patent:
December 23, 2003
Assignee:
Pfizer, Inc.
Inventors:
Manoussos Perros, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood
Abstract: This invention relates to methods of treating neurodegenerative diseases and inhibiting neurological damage, comprising administering to a patient in need of such treatment an N-NOS inhibitor in combination with an NMDA receptor antagonist.
Abstract: The present invention relates to polynucleotide molecules comprising nucleotide sequences encoding an aveC gene product, which polynucleotide molecules can be used to alter the ratio or amount of class 2:1 avermectins produced in fermentation cultures of S. avermitilis. The present invention further relates to vectors, host cells, and mutant strains of S. avermitilis in which the aveC gene has been inactivated, or mutated so as to change the ratio or amount of class 2:1 avermectins produced.
Type:
Application
Filed:
June 11, 2003
Publication date:
December 18, 2003
Applicant:
Pfizer Inc.
Inventors:
Kim J. Stutzman-Engwall, Yan Chen, Claes Gustafsson, Anke Krebber, Jeremy Minshull, Sun Ai Raillard
Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.
Type:
Grant
Filed:
March 28, 2001
Date of Patent:
December 16, 2003
Assignee:
Pfizer, Inc.
Inventors:
Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
Abstract: This invention relates to compounds of the formula 1
and to pharmaceutically acceptable salts and solvates thereof wherein X1, X2, R2, R15, R16 and R6 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.
Type:
Grant
Filed:
December 10, 1999
Date of Patent:
December 16, 2003
Assignee:
Pfizer Inc.
Inventors:
Wei-Guo Su, Takushi Kaneko, Yong-Jin Wu
Abstract: The present invention relates to novel benzotriazoles of the formula I
wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen;
R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;
R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;
s is an integer from 0-5;
to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Type:
Grant
Filed:
April 4, 2002
Date of Patent:
December 16, 2003
Assignee:
Pfizer Inc
Inventors:
Michael A. Letavic, Mark A. Dombroski, Kim F. McClure, Ellen R. Laird
Abstract: This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R1 through R6 are as defined in the specification
These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.
Abstract: A pharmaceutical composition comprises a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer and a lipophilic microphase-forming material. Alternatively, a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer is co-administered with a lipophilic microphase-forming material to an in vivo use environment.
Type:
Application
Filed:
January 31, 2003
Publication date:
December 11, 2003
Applicant:
Pfizer Inc.
Inventors:
Michael E. Perlman, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, Mark D. Rabenstein, Dan T. Smithey
Abstract: A composition comprising a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.
Type:
Application
Filed:
January 24, 2003
Publication date:
December 11, 2003
Applicant:
Pfizer Inc.
Inventors:
Alasdair Mark Naylor, Rachel Jane Russell, Stephen Derek Albert Street, Kim-Wah Tang, Pieter Hadewijn Van Der Graaf, Christopher Peter Wayman