Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Application
Filed:
December 13, 2017
Publication date:
June 21, 2018
Applicant:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, John M. Curto, Matthew S. Dowling, David Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Gajendra Ingle, Wenhua Jiao, Chris Limberakis, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.
Type:
Application
Filed:
January 23, 2018
Publication date:
June 21, 2018
Applicant:
PFIZER INC.
Inventors:
Tracy Chia-Chien KUO, Javier Fernando CHAPARRO RIGGERS, Wei CHEN, Amy Shaw-Ru CHEN, Edward Derrick PASCUA, Thomas John VAN BLARCOM, Leila Marie BOUSTANY, Weihsien HO, Yik Andy YEUNG, Pavel STROP, Arvind RAJPAL
Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death Ligand 1 receptor (PD-L1) and another therapeutic agent, and the use of the combination therapies for the treatment of cancer.
Type:
Application
Filed:
June 15, 2016
Publication date:
June 21, 2018
Applicants:
MERCK PATENT GMBH, PFIZER INC.
Inventors:
Glen Ian ANDREWS, Shihao CHEN, Alessandra DI PIETRO, David FONTANA, Zelanna GOLDBERG, Chia-Yang LIN, Hua LONG, Marcella MARTIGNONI, Dimitry Serge Antoine NUYTEN, Aron David THALL, Adrian WOOLFSON
Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 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:
January 30, 2018
Publication date:
June 14, 2018
Applicant:
PFIZER INC.
Inventors:
Mary Didiuk, Robert Lee Dow, David Andrew Griffith
Abstract: Bispecific heterodimeric diabody molecules and uses thereof in the treatment of cancer. The bispecific heterodimeric diabody molecules comprise two polypeptide chains that associate to form two epitope binding sites recognizing the P-cadherin tumor cell associated antigen and the CD3 T cell antigen.
Type:
Application
Filed:
December 13, 2017
Publication date:
June 7, 2018
Applicant:
Pfizer Inc.
Inventors:
Chad Michael May, Adam Reid Root, William A. Brady, Lioudmila Gennadievna Tchistiakova, Lidia Mosyak, Laird Bloom, Paul A. Moore, Leslie S. Johnson
Abstract: The present invention relates to the provision of novel immunogens comprising an antigenic PCSK9 peptide linked to an immunogenic carrier for the prevention, treatment or alleviation of PCSK9-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:
September 15, 2016
Date of Patent:
June 5, 2018
Assignee:
Pfizer Vaccines LLC
Inventors:
Brian Robert Champion, Jr., Leonard Gabriel Contillo, Jr., Michael Dale Eisenbraun, James Downey Fraser, Julie Jia Li Hawkins, James Richard Merson, Brian Gregory Pierce, Xiayang Qiu, Jakir Hussain Ullah, David Michael Wyatt
Abstract: Compounds, pharmaceutically acceptable salts thereof are disclosed wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Application
Filed:
May 16, 2016
Publication date:
May 31, 2018
Applicant:
Pfizer Inc.
Inventors:
Agustin Casimiro-Garcia, Jeffrey Scott Condon, Andrew Christopher Flick, Ariamala Gopalsamy, Steven J. Kirincich, John Paul Mathias, Joseph Walter Strobach, Jason Shaoyun Xiang, Li Huang Xing, Xiaolun Wang
Abstract: The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R9, X, m and n are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating kappa opioid (?-opioid) associated disorders including, e.g., a neurological disorder, or psychiatric disorder such as a neurocognitive disorder, substance abuse disorder, depressive disorder, anxiety disorder, trauma and stressor related disorder and feeding and eating disorder.
Type:
Application
Filed:
November 22, 2017
Publication date:
May 31, 2018
Applicant:
Pfizer Inc.
Inventors:
Natasha Mariam Kablaoui, Michael Eric Green, Justin Ian Montgomery, Michael Aaron Brodney, Patrick Robert Verhoest, Gregory Wayne Kauffman, Danica Antonia Rankic, Scot Richard Mente, Bruce Nelsen Rogers, Kapildev Kashmirilal Arora, Matthew Francis Dunn
Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
Type:
Application
Filed:
November 29, 2017
Publication date:
May 31, 2018
Applicant:
PFIZER INC.
Inventors:
Aaron Craig BURNS, Michael Raymond COLLINS, Samantha Elizabeth GREASLEY, Robert Louis Hoffman, Peter Qinhua HUANG, Robert Steven Kania, Pei-Pei KUNG, Maria Angelica LINTON, Lakshmi Sourirajan NARASIMHAN, Paul Francis RICHARDSON, Daniel Tyler RICHTER, Graham SMITH
Abstract: The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.
Type:
Application
Filed:
August 14, 2015
Publication date:
May 24, 2018
Applicants:
PFIZER INC., RINAT NEUROSCIENCE CORP.
Inventors:
Russell George DUSHIN, Pavel STROP, Magdalena Grazyna DORYWALSKA, Ludivine MOINE
Abstract: A three to six sided lip balm applicator of the present invention comprises a cap, a liner, and a base, having engagement assemblies for engaging the cap to the liner, the liner to the base, and a base from one lip balm applicator to an equivalent base from another lip balm applicator to form a lip balm container. The base comprises a partition with stabilizers which emerge from the partition and extend radially toward and overhang an aperture in the partition. The lip balm applicator may contain a domed lip balm, filled directly into the lip balm applicator or components thereof as a mold for manufacturing the domed lip balm, filled to a fill level approaching the partition top but not touching the partition top.
Type:
Grant
Filed:
September 26, 2016
Date of Patent:
May 22, 2018
Assignee:
Pfizer Inc.
Inventors:
Matthew Clifton Keller, David Dombrowski, David Charles Fuhrmeister, William H. Valls, Zachariah S. Simmering, Jonathon Keith Markey
Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.
Type:
Grant
Filed:
March 30, 2016
Date of Patent:
May 15, 2018
Assignee:
PFIZER INC.
Inventors:
Tracy Chia-Chien Kuo, Javier Fernando Chaparro Riggers, Wei Chen, Amy Shaw-Ru Chen, Edward Derrick Pascua, Thomas John Van Blarcom, Leila Marie Boustany, Weihsien Ho, Yik Andy Yeung, Pavel Strop, Arvind Rajpal
Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid and a therapeutic agent (1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea), or pharmaceutically acceptable salts thereof, and a polymer. Other aspects include methods of making and using such nanoparticles.
Type:
Application
Filed:
January 3, 2018
Publication date:
May 10, 2018
Applicant:
PFIZER INC.
Inventors:
Shubha Bagrodia, Jennifer Lafontaine, Zach Lovatt, Eyoung Shin, Young Ho Song, Greg Troiano, Hong Wang
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Application
Filed:
January 5, 2018
Publication date:
May 10, 2018
Applicant:
Pfizer Inc.
Inventors:
John David Trzupek, Katherine Lin Lee, Mark Edward Bunnage, Seungil Han, David Hepworth, Frank Eldridge Lovering, John Paul Mathias, Nikolaos Papaioannou, Betsy Susan Pierce, Joseph Walter Strohbach, Stephen Wayne Wright, Christoph Wolfgang Zapf, Lori Krim Gavrin, Arthur Lee, David Randolph Anderson, Kevin Joseph Curran, Christoph Martin Dehnhardt, Eddine Saiah, Joel Adam Goldberg, Xiaolun Wang, Horng-Chih Huang, Richard Vargas, Michael Dennis Lowe, Akshay Patny
Abstract: In accordance with the present invention, there are provided fully human monoclonal antibodies against human cytotoxic T-lymphocyte antigen 4 (CTLA-4). Nucleotide sequences encoding and amino acid sequences comprising heavy and light chain immunoglobulin molecules, particularly contiguous heavy and light chain sequences spanning the complementarity determining regions (CDRs), specifically from within FR1 and/or CDR1 through CDR3 and/or within FR4, are provided. Further provided are antibodies having similar binding properties and antibodies (or other antagonists) having similar functionality as antibodies disclosed herein.
Type:
Grant
Filed:
October 20, 2014
Date of Patent:
May 8, 2018
Assignees:
AMGEN FREMONT INC., PFIZER INC.
Inventors:
Douglas Charles Hanson, Mark Joseph Neveu, Eileen Elliott Mueller, Jeffrey Herbert Hanke, Steven Christopher Gilman, C. Geoffrey Davis, Jose Ramon Corvalan
Abstract: The present disclosure relates to RSV F protein mutants, nucleic acids or vectors encoding a RSV F protein mutant, compositions comprising a RSV F protein mutant or nucleic acid, and uses of the RSV F protein mutants, nucleic acids or vectors, and compositions.
Type:
Grant
Filed:
December 20, 2016
Date of Patent:
April 24, 2018
Assignee:
Pfizer Inc.
Inventors:
Ye Che, Philip Ralph Dormitzer, Alexey Vyacheslavovich Gribenko, Luke David Handke, Avvari Krishna Prasad, Xiayang Qiu, Mark Edward Ruppen, Xi Song, Kena Anne Swanson, Srinivas Kodali, Xin Xu, KariAnn Sweeney Efferen, Ping Cai, Kristin Rachael Tompkins, Lorna del Pilar Nunez
Abstract: The invention provides eTEC linked glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, immunogenic compositions comprising such glycoconjugates, and methods for the preparation and use of such glycoconjugates and immunogenic compositions.
Type:
Grant
Filed:
November 9, 2016
Date of Patent:
April 24, 2018
Assignee:
Pfizer Inc.
Inventors:
Jianxin Gu, Jin-hwan Kim, Avvari Krishna Prasad, Yu-ying Yang