Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.
Type:
Application
Filed:
October 10, 2017
Publication date:
February 8, 2018
Applicant:
PFIZER INC.
Inventors:
MICHAEL AARON BRODNEY, JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, MICHAEL ERIC GREEN, JACLYN LOUISE HENDERSON, CHEWAH LEE, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, LEI ZHANG
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:
Grant
Filed:
June 26, 2015
Date of Patent:
February 6, 2018
Assignee:
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: 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:
Grant
Filed:
August 10, 2016
Date of Patent:
January 30, 2018
Assignee:
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: The present disclosure generally relates to a process for preparing therapeutic nanoparticles, where the process includes combining a therapeutic agent with an organic acid. The therapeutic nanoparticles may have, for example, improved drug loading and/or drug release properties.
Type:
Grant
Filed:
September 16, 2013
Date of Patent:
January 30, 2018
Assignee:
Pfizer Inc.
Inventors:
Maria Figueiredo, Erick Peeke, David Dewitt, Christina Van Geen Hoven, Greg Troiano, James Wright, Young-Ho Song, Hong Wang
Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
Type:
Grant
Filed:
June 24, 2016
Date of Patent:
January 23, 2018
Assignee:
Pfizer Inc.
Inventors:
Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
Type:
Grant
Filed:
March 17, 2016
Date of Patent:
January 23, 2018
Assignees:
Pfizer Inc, iTeos Therapeutics
Inventors:
Sacha Ninkovic, Stefano Crosignani, Indrawan James McAlpine, Michael Raymond Collins, Stephanie Anne Scales, Andreas Maderna, Martin Wythes
Abstract: The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.
Type:
Grant
Filed:
October 18, 2016
Date of Patent:
January 23, 2018
Assignee:
Pfizer Inc.
Inventors:
Greg Troiano, Young-ho Song, Stephen E. Zale, James Wright, Christina Van Geen Hoven
Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.
Type:
Grant
Filed:
May 23, 2016
Date of Patent:
January 23, 2018
Assignee:
Pfizer Inc.
Inventors:
Greg Troiano, Michael Figa, Abhimanyu Sabnis
Abstract: The present invention provides, in part, compounds of Formula (I) and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.
Type:
Grant
Filed:
April 13, 2015
Date of Patent:
January 16, 2018
Assignee:
Pfizer Inc.
Inventors:
David Lawrence Firman Gray, Lei Zhang, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Chakrapani Subramanyam
Abstract: Methods for the detection, enumeration and analysis of circulating tumor cells expressing insulin-like growth factor-1 receptors (IGF-1R) are disclosed. These methods are useful for cancer screening and staging, development of treatment regimens, and for monitoring for treatment responses, cancer recurrence or the like. Test kits that facilitate the detection, enumeration and analysis of such circulating tumor cells are also provided.
Type:
Application
Filed:
July 27, 2017
Publication date:
January 11, 2018
Applicants:
Janssen Diagnostics, LLC, Pfizer Inc.
Inventors:
Antonio GUALBERTO, Maria Luisa PACCAGNELLA, Carrie L. MELVIN, Madeline I. REPOLLET, David CHIANESE, Mark Carle CONNELLY, Leonardus Wendelinus Mathias Marie TERSTAPPEN
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:
April 28, 2015
Date of Patent:
January 9, 2018
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 provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
Type:
Application
Filed:
June 29, 2017
Publication date:
January 4, 2018
Applicant:
Pfizer Inc.
Inventors:
Lei Zhang, Christopher Ryan Butler, Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Laura Ann McAllister, Erik Alphie LaChapelle, Adam Matthew Gilbert
Abstract: An object of the present invention is to provide immunogenic compositions for protection against S. pneumoniae, in particular against S. pneumoniae serogroup 9, while limiting the number of conjugates. The present invention thereforerelates to new immunogenic compositions for use in pneumococcal vaccines and to vaccination of human subjects, in particular infants and elderly, against pneumoccocal infections using said immunogenic compositions.
Type:
Application
Filed:
January 5, 2016
Publication date:
January 4, 2018
Applicant:
Pfizer Inc.
Inventors:
David Cooper, Kathrin Ute Jansen, Michael William Pride
Abstract: The present invention provides antibodies and related molecules that bind to chemokine receptor 4 (CXCR4). The invention further provides antibody-drug conjugates comprising such antibodies, antibody encoding nucleic acids, and methods of obtaining such antibodies. The invention further relates to therapeutic methods for use of these antibodies and anti-CXCR4 antibody-drug conjugates for the treatment of a disorder associated with CXCR4 function or expression (e.g., cancer), such as colon, RCC, esophageal, gastric, head and neck, lung, ovarian, pancreatic cancer or hematological cancers.
Type:
Application
Filed:
May 31, 2017
Publication date:
January 4, 2018
Applicant:
PFIZER INC.
Inventors:
Shu-Hui LIU, Flavia Mercer PERNASETTI, Weihsien HO
Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 40 weight percent of a therapeutic agent and about 10 to about 90 weight percent a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa or the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa.
Type:
Application
Filed:
June 15, 2017
Publication date:
January 4, 2018
Applicant:
Pfizer Inc.
Inventors:
David Dewitt, Maria Conceicao Figueiredo, Hong Wang, Gregory Troiano, Young-Ho Song
Abstract: The present invention relates to the field of pharmaceutical formulations of antibodies. Specifically, the present invention relates to a stable liquid antibody formulation and its pharmaceutical preparation and use. This invention is exemplified by an aqueous formulation of an anti-vascular endothelial growth factor (VEGF) antibody.
Type:
Application
Filed:
January 20, 2016
Publication date:
January 4, 2018
Applicant:
Pfizer Inc.
Inventors:
Rebecca Lee Ingram, Sarah Elizabeth Weiser
Abstract: The present invention provides methoxy-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:
Application
Filed:
January 29, 2016
Publication date:
January 4, 2018
Applicant:
Pfizer Inc.
Inventors:
Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Goran Mattias Wennerstal, Li Xing, Edouard Zamaratski, Liying Zhang, Rayomand J. Unwalla
Abstract: The present invention provides, in part, compounds of Formula (I): and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.
Type:
Grant
Filed:
April 15, 2015
Date of Patent:
January 2, 2018
Assignee:
PFIZER INC.
Inventors:
David Lawrence Firman Gray, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, Scot Richard Mente, Chakrapani Subramanyam
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, 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:
August 16, 2017
Publication date:
December 28, 2017
Applicant:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill