Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.
Type:
Grant
Filed:
November 3, 2011
Date of Patent:
June 13, 2017
Assignees:
PFIZER INC., RINAT NEUROSCIENCE CORP.
Inventors:
Pavel Strop, Magdalena Grazyna Dorywalska, Arvind Rajpal, David Shelton, Shu-Hui Liu, Jaume Pons, Russell Dushin
Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.
Type:
Grant
Filed:
September 24, 2015
Date of Patent:
June 6, 2017
Assignee:
Pfizer Inc.
Inventors:
Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Göran Mattias Wennerstål, Li Xing, Edouard Zamaratski, Liying Zhang
Abstract: The present invention relates to a solid molecular dispersion of from 3:97 to 12:88 weight % ratio of fesoterodine hydrogen fumarate and a polymeric binder selected from the group consisting of an alkyl hydroxyalkylcellulose ether, a hydroxyalkylcellulose ether, an ester of either thereof, and a mixture of any two or more thereof.
Type:
Grant
Filed:
January 17, 2012
Date of Patent:
June 6, 2017
Assignee:
Pfizer Limited
Inventors:
Roland Bodmeier, Alan Francis Carmody, Mesut Ciper, Anne Therese Gustaaf De Paepe, John Mark Heimlich, Martin Korber, Mathias Walther, Neil Feeder
Abstract: This invention relates to compounds of general formula in which R1, R2, R6, U, V, W, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and salts, and to methods of using such compounds, salts and compositions.
Type:
Application
Filed:
February 6, 2017
Publication date:
June 1, 2017
Applicant:
Pfizer Inc.
Inventors:
Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCALPINE, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Application
Filed:
February 8, 2017
Publication date:
June 1, 2017
Applicant:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Gabriela Barreiro, Erik Alphie LaChapelle, Bruce Nelsen Rogers
Abstract: The present disclosure relates in part to methods of treating cancers having a mutation in a Ras gene in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a nanoparticle composition, wherein the nanoparticle composition comprises nanoparticles.
Abstract: A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C?O, —SO2—, etc.; A? is selected from the group consisting of a bond, C?O, etc.; Z is —(CH2)h— or a bond, etc.; R1 and R1? are independently selected from the group consisting of hydrogen, alkyl, etc.; R2 is selected from hydrogen, alkyl, etc.; R3 is selected from the group consisting of hydrogen, and amino; R4 is monocyclic or bicyclic, etc.; R5 is independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.
Type:
Grant
Filed:
August 19, 2015
Date of Patent:
May 30, 2017
Assignee:
Pfizer Inc.
Inventors:
Andrew Fensome, Ariamala Gopalsamy, Brian S. Gerstenberger, Ivan Viktorovich Efremov, Zhao-Kui Wan, Betsy Pierce, Jean-Baptiste Telliez, John I. Trujillo, Liying Zhang, Li Xing, Eddine Saiah
Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.
Type:
Application
Filed:
February 7, 2017
Publication date:
May 25, 2017
Applicant:
Pfizer Inc.
Inventors:
Thomas Allen Chappie, Nandini Chaturbhai Patel, Matthew Merrill Hayward, Christopher John Helal, Simone Sciabola, Erik Alphie LaChapelle, Joseph Michael Young, Patrick Robert Verhoest
Abstract: The present invention relates to compositions comprising probiotic and prebiotic components, mineral salts, lactoferrin, and possibly saccharomycetes, which perform correct, effective colonisation of the probiotic components administered, with enteric consequences which involve maintaining and/or restoring intestinal health and preventing the consequences of common dysbioses of the digestive tract caused by stress, incorrect dietary habits and antibiotic treatments. Said compositions also have a concomitant anti-inflammatory and immunomodulating action.
Abstract: Described herein are polymeric nanoparticles that include a therapeutic agent, and methods of making and using such therapeutic nanoparticles. In some embodiments, the contemplated nanoparticles may include an excipient.
Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
May 9, 2017
Assignee:
Pfizer Inc.
Inventors:
Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
Abstract: The present invention relates to a therapeutic method for the treatment of cancer that comprises the use of a combination of inotuzumab ozogamicin (CMC-544) and temsirolimus. The enhanced antitumor of the combination therapy is particularly useful for patient population that are recalcitrant to inotuzumab ozogamicin or temsirolimus therapy, relapse after treatment with inotuzumab ozogamicin or temsirolimus or where enhanced antitumor effect reduces toxicities associated with treatment using inotuzumab ozogamicin or temsirolimus.
Type:
Grant
Filed:
December 4, 2012
Date of Patent:
May 9, 2017
Assignees:
Pfizer Inc., Oncology Institute of Southern Switzerland
Inventors:
Andreas Bruederle, Padraig Moran, Anastasios Stathis
Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.
Type:
Application
Filed:
January 13, 2017
Publication date:
May 4, 2017
Applicant:
Pfizer Inc.
Inventors:
Maria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
Type:
Grant
Filed:
March 4, 2016
Date of Patent:
May 2, 2017
Assignee:
Pfizer Inc.
Inventors:
Joseph Francis Krzyzaniak, Jason Albert Leonard
Abstract: This invention relates to crystalline solvates of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benz- oxadiazacyclotetradecine-3-carbonitrile, useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to pharmaceutical compositions comprising such crystalline solvates, and to methods of using such solvates and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Type:
Grant
Filed:
June 17, 2014
Date of Patent:
May 2, 2017
Assignee:
Pfizer Inc.
Inventors:
Andrew James Jensen, Suman Luthra, Paul Francis Richardson
Abstract: Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.
Type:
Grant
Filed:
April 7, 2016
Date of Patent:
April 11, 2017
Assignee:
Pfizer Inc.
Inventors:
Spiros Liras, Vincent Mascitti, Benjamin Thuma