Abstract: The present invention relates to crystalline polymorphic and amorphous form of 6-[2-(methylcarbamoyl)phenyl sulfanyl]-3-E-[2-(pyridin-2-yl)ethenyl]indazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one polymorphic form and to the therapeutic or prophylactic use of such polymorphic forms and compositions.
Type:
Grant
Filed:
March 25, 2008
Date of Patent:
July 29, 2014
Assignee:
Pfizer Inc.
Inventors:
Anthony Michael Campeta, Brian Patrick Chekal, Robert Alan Singer
Abstract: The present invention is directed to compounds of Formula (I), and to salts thereof, their synthesis, and their use as PI3-K? inhibitors and/or PI3-K?/mTOR dual inhibitors.
Type:
Grant
Filed:
September 18, 2009
Date of Patent:
July 29, 2014
Assignee:
Pfizer Inc.
Inventors:
Hengmiao Cheng, Ted William Johnson, Jacqui Elizabeth Hoffman, Lisa Chen Guo, Zhengyu Liu
Abstract: The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.
Type:
Application
Filed:
March 19, 2014
Publication date:
July 24, 2014
Applicant:
Pfizer Inc.
Inventors:
David James Dooley, Mark John Field, Richard Griffith Williams
Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
Type:
Application
Filed:
March 24, 2014
Publication date:
July 24, 2014
Applicant:
Pfizer Inc.
Inventors:
Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
Type:
Grant
Filed:
June 29, 2012
Date of Patent:
July 22, 2014
Assignees:
Agouron Pharmaceuticals, Inc., Pfizer Inc.
Inventors:
Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
Type:
Grant
Filed:
October 31, 2013
Date of Patent:
July 15, 2014
Assignee:
Pfizer Inc.
Inventors:
Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
Type:
Grant
Filed:
July 8, 2011
Date of Patent:
July 8, 2014
Assignees:
Pfizer Limited, Icagen Inc.
Inventors:
Alan Daniel Brown, Marcel John De Groot, Brian Edward Marron, David James Rawson, Thomas Ryckmans, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West
Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
Type:
Grant
Filed:
July 6, 2011
Date of Patent:
July 8, 2014
Assignee:
Pfizer Limited
Inventors:
Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
Type:
Application
Filed:
December 18, 2013
Publication date:
June 26, 2014
Applicant:
PFIZER INC.
Inventors:
Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
Type:
Application
Filed:
December 12, 2013
Publication date:
June 19, 2014
Applicant:
Pfizer Limited
Inventors:
Kiyoyuki Omoto, Robert McKenzie Owen, David Cameron Pryde, Christine Ann Louise Watson, Mifune Takeuchi
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:
Grant
Filed:
February 10, 2011
Date of Patent:
June 17, 2014
Assignee:
Pfizer Inc.
Inventors:
Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
Abstract: The present invention concerns dosages for the treatment of human patients susceptible to or diagnosed with a disorder characterized by marked elevations of low density lipoprotein particles in the plasma with a PCSK9 antagonist antibody alone or in combination with a statin.
Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Application
Filed:
December 10, 2013
Publication date:
June 12, 2014
Applicant:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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 a variety of chiral compounds.
Type:
Grant
Filed:
September 13, 2008
Date of Patent:
June 10, 2014
Assignees:
Codexis, Inc., Pfizer, Inc.
Inventors:
Jack Liang, Stephane J. Jenne, Emily Mundorff, Charlene Ching, John M. Gruber, Anke Krebber, Gjalt W. Huisman
Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
Type:
Grant
Filed:
March 23, 2012
Date of Patent:
June 10, 2014
Assignee:
Pfizer Inc.
Inventors:
Joseph Alan Abramite, Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.
Type:
Application
Filed:
December 2, 2013
Publication date:
June 5, 2014
Applicant:
Pfizer Inc.
Inventors:
James Thomas Anderson, Eugene Lvovich Piatnitski Chekler, Edmund L. Ellsworth, Bruce Kipp Erickson, Adam Matthew Gilbert, Anthony P. Ricketts, David P. Thompson, Rayomand Jal Unwalla, Patrick Robert Verhoest
Abstract: A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.
Type:
Application
Filed:
February 8, 2014
Publication date:
June 5, 2014
Applicant:
Pfizer Inc.
Inventors:
Antone John deBettencourt, III, Peter Robert Rose, Evgenyi Shalaev, George Joseph Quallich, Carl Bernard Ziegler
Abstract: The present disclosure provides isolated monoclonal antibodies, particularly human monoclonal antibodies, or antigen binding portions thereof, that specifically bind to integrin ?5?1 with high affinity. Nucleic acid molecules encoding the antibodies of the disclosure, expression vectors, host cells and methods for expressing the antibodies of the disclosure are also provided. Immunoconjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies or antigen binding portions thereof are also provided. The disclosure also provides methods for treating various cancers using the anti-?5?1 antibodies or antigen binding portions thereof described herein.
Type:
Application
Filed:
February 21, 2013
Publication date:
June 5, 2014
Applicants:
PFIZER INC., BRISTOL-MYERS SQUIBB COMPANY
Inventors:
STEVEN LEE BENDER, GERALD FRIES CASPERSON, DANA DAN HU-LOWE, XIN JIANG, GANG LI, MICHAEL AIDAN NORTH, JIANYING WANG, GRANT WICKMAN, PETER BRAMS, HAICHUN HUANG, BRIGITTE DEVAUX, HAIBIN CHEN, DAWN M. TANAMACHI, KRISTOPHER TOY, LAN YANG, TIM W. SPROUL, MARK YAMANAKA