Abstract: Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.
Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).
Type:
Grant
Filed:
July 26, 2012
Date of Patent:
December 4, 2012
Assignee:
Pfizer Inc.
Inventors:
Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
Type:
Application
Filed:
February 10, 2011
Publication date:
November 29, 2012
Applicant:
Pfizer Inc.
Inventors:
Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
Abstract: The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases. We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is 3- to 8-membered saturated heterocyclic group wherein one ring member is O; and R2 is phenyl or pyridinyl, each optionally substituted by C1-C6alkyl.
Type:
Application
Filed:
November 22, 2011
Publication date:
November 29, 2012
Applicant:
PFIZER LIMITED
Inventors:
Peter H. Jones, David Cameron Pryde, Thien Duc Tran
Abstract: A device for dispensing individual doses of powder from respective pockets of a disc-shaped carrier by outwardly rupturing a lidding foil by means of pressure on an opposite side surface, the device providing individual respective deaggregation flow paths for each pocket, split airstreams allowing improved entrainment of powder, a cam mechanism for outwardly rupturing the pockets, an indexing mechanism linked to the cam mechanism and a dose counter.
Type:
Application
Filed:
July 27, 2012
Publication date:
November 29, 2012
Applicant:
PFIZER LIMITED
Inventors:
Peter John Houzego, John Kelshaw Conway, Martin Douglas Pearl, Andrew Mark Bryant
Abstract: The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.
Type:
Grant
Filed:
May 18, 2009
Date of Patent:
November 27, 2012
Assignee:
Pfizer Inc.
Inventors:
Jeffrey W. Corbett, Richard Elliott, Kevin Freeman-Cook, David A. Griffith, Dennis P. Phillion
Abstract: The present invention relates to the provision of novel immunogens comprising an antigenic IgE peptide preferably linked to an immunogenic carrier for the prevention, treatment or alleviation of IgE-mediated disorders. The invention further relates to methods for production of these medicaments, immunogenic compositions and pharmaceutical compositing thereof and their use in medicine.
Type:
Application
Filed:
August 1, 2012
Publication date:
November 22, 2012
Applicant:
PFIZER VACCINES LLC
Inventors:
Alan Daniel Brown, Brian Robert Champion, Clare Christy, David Paul Gervais, Lyn Howard Jones, Anne Maria Kristina Kjerrstrom, David Cameron Pryde, Lee Richard Roberts, David Michael Wyatt
Abstract: Device for dispensing a plurality of unitary doses (2) of dry powder, comprising at least one support comprising conduits each defining a flow path for an airstream carrying one of the unitary dose (2), the support having first (26) and second (27) members secured to one another so that a first conduit portion (29) of the first member faces a second conduit portions (43) of the second member to define one of the conduits, and a first separation portion (30) of the first member faces a second separation portions (45) of the second member, the support comprising a plurality of barrier-forming elements (31, 46) each arranged between corresponding first (30) and second (45) separation portions to prevent dry powder from passing from one of the conduits to one of the adjacent conduits.
Abstract: The present invention is directed to the tosylate salt of trans-N-ethyl-3- fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.
Abstract: This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
Type:
Grant
Filed:
June 20, 2012
Date of Patent:
November 13, 2012
Assignee:
Pfizer Inc.
Inventors:
Sally Gut Ruggeri, Joel M Hawkins, Teresa M Makowski, Jennifer L Rutherford, Frank J Urban
Abstract: The present invention provides a FGF21 molecule covalently attached to the combining site of an antibody via a linker, wherein the linker is covalently attached to the side chain of a linking residue within FGF21. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.
Abstract: Methods and apparatus are provided that automatically determine whether or not eggs designated for removal from an egg carrier have been removed by an egg removal apparatus. Light is emitted along a path above and across an egg carrier as an egg picker moves to pick up an egg. The length of time that the light path is blocked when the egg picker is moved is measured and used to determine whether or not the egg has been removed from the carrier. Another apparatus and method is provided for detecting a malfunctioning egg picker. A detection device detects a number of eggs in the egg carrier. A control device monitors the egg picker and the detection device. The control device calculates the number of eggs in the egg carrier for determining when the number of eggs varies a predetermined amount from an egg count number for the egg carrier.
Abstract: The present invention provides novel cephalosporin derivatives of formula I, their analogues, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
Type:
Application
Filed:
April 30, 2012
Publication date:
November 8, 2012
Applicant:
PFIZER INC.
Inventors:
Brian A. Duclos, Edmund L. Ellsworth, Richard A. Ewin, Paul D. Johnson, Timothy A. Johnson, Graham M. Kyne, Susan M. K. Sheehan, Rajendran Vairagoundar
Abstract: The invention relates to a class of soft or semi-soft CpG immunostimulatory oligonucleotides that are useful for stimulating an immune response.
Type:
Grant
Filed:
October 4, 2006
Date of Patent:
November 6, 2012
Assignees:
Coley Pharmaceutical Group, Inc., Coley Pharmaceutical GmbH, Pfizer Inc.
Inventors:
Arthur M. Krieg, Ulrike Samulowitz, Jörg Vollmer, Eugen Uhlmann, Marion Jurk, Grayson B. Lipford, Robert Rankin
Abstract: The present invention is directed to a regio-and stereoselective bioconversion of selected aliphatic dinitriles into corresponding cyanocarboxylic acids. More particularly, the present invention provides methods for the conversion of 2-isobutyl-succinonitrile into (S)-3 cyano-5-methylhexanoic acid, which is a useful intermediate in the synthesis of (S)-3(aminomethyl)-5-methylhexanoic acid (pregabalin). Pregabalin can be used for treating certain cerebral diseases, for example, in the treatment and prevention of seizure disorders, pain, and psychotic disorders.
Type:
Grant
Filed:
April 20, 2010
Date of Patent:
November 6, 2012
Assignee:
Pfizer Inc.
Inventors:
Michael P. Burns, Justin K. Weaver, John Wing Wong
Abstract: The present disclosure provides engineered ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme. Also provided are polynucleotides encoding the engineered ketoreductase enzymes, host cells capable of expressing the engineered ketoreductase enzymes, and methods of using the engineered ketoreductase enzymes to synthesize chiral compounds.
Type:
Application
Filed:
June 15, 2012
Publication date:
November 1, 2012
Applicants:
PFIZER, INC., CODEXIS, INC.
Inventors:
Jack Liang, Stephane J. Jenne, Emily Mundorff, Rama Voladri, James Lalonde, Gjalt W. Huisman
Abstract: Methods of Treating Inflammatory Pain The invention relates to an anti-CGRP antibody for use in the prevention and/or treatment of inflammatory pain and/or symptoms of inflammatory pain, and to a method of treating and/or preventing inflammatory pain and/or symptoms of inflammatory pain using an anti-CGRP antibody.
Type:
Grant
Filed:
March 3, 2009
Date of Patent:
October 30, 2012
Assignee:
Pfizer Limited
Inventors:
Laura Corradini, Ian Machin, Kristian Todd Poulsen, David Louis Shelton, Joerg Zeller
Abstract: The present invention relates to the provision of novel immunogens comprising an antigenic IgE peptide preferably linked to an immunogenic carrier for the prevention, treatment or alleviation of IgE-mediated disorders. The invention further relates to methods for production of these medicaments, immunogenic compositions and pharmaceutical compositing thereof and their use in medicine.
Type:
Grant
Filed:
December 9, 2009
Date of Patent:
October 30, 2012
Assignee:
Pfizer Vaccines, LLC
Inventors:
Alan Daniel Brown, Brian Robert Champion, Clare Christy, David Paul Gervais, Lyn Howard Jones, Anne Maria Kristina Kjerrstrom, David Cameron Pryde, Lee Richard Roberts, David Michael Wyatt
Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
Type:
Application
Filed:
April 21, 2012
Publication date:
October 25, 2012
Applicant:
PFIZER INC.
Inventors:
Robert Lee Dow, David James Edmonds, David Andrew Griffith, James Alfred Southers, JR.